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1. WO2001077079 - PYRIDONES POLYCYCLIQUES 4-ARYL ET HETEROARYL SUBSTITUEES UTILES POUR L'INHIBITION SELECTIVE DE LA CASCADE DE COAGULATION

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

What we claim is:

1. A compound having the Formula (I):


or a pharmaceutically acceptable salt thereof, wherein;

B is formula (V):


wherein D 1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, no more than one of D 1, D2, J1, J2 and K1 is O,

no more than one of D 1, D2, J1, J2 and K1 is S, one of D 1, D2, J1, J2 and K1

must be a covalent bond when two of D 1, D2, J1, J2 and K1 are O and S, and

no more than four of D 1, D2, J1, J2 and K1 are N with the proviso that R32,

R33 , R34 , R35 , and R36 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R32 , R33 , R34 , R35 , and R36 are independently selected to be Qb;

R9 R10 R11 R12 R13 R16 R17 R18 R19 R32 R33, R34, R35 and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, trialkylphosphonium, dialkylsulfoniumalkyl, carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl, acylalkoxy, aryloylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfmylalkyl, halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,

cycloalkylsulfonylalkyl, heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, cycloalkenyloxy,

cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy,

halocycloalkenyloxyalkyl, hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl,

arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl,

heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl,

haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,

alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl, arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky,

alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl,

cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxy aralkyl, hydroxyalkyl, aminoalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano,

carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl ;

R32 and R33, R33 and R34, R34 and R35, and R35 and R36

substituent pairs are independently selected to form a spacer pair wherein a spacer pair is taken together to form a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 contiguous members, a partially saturated heterocyclyl ring having 5 through 8 contiguous members, a heteroaryl ring having 5 through 6 contiguous members, and an aryl with the proviso that no more than one of the group consisting of spacer pairs R32 and R33 , R33 and R34, R34

and R35, and R35 and R36 are used at the same time;

B is formula (VI):


wherein D3, D4, J3, a; nd J4 are indipendently selected from the group

consisting of C, N, O, and S, no more than one of D3, D4, J3, a ; nd J4 is O, no

more than one of D3, D4, J3, a ; nd J4 is S, and no more than three of D1 , D2 , J 1,

and J2 are N with the proviso that R32 , R33 , R34 , and R35 are each

independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

B is selected from the group consisting of C3-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl wherein each member of group B may be optionally substituted at any carbon up to and including 6

atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36,

B is selected from the group consisting of C3-C10 cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partially saturated heterocyclyl, wherein each ring carbon may be optionally substituted with R33, a ring carbon other than the ring carbon at the point of attachment of B to A may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbon and nitrogen atoms adjacent to the carbon atom at the point of attachment may be optionally substituted with R9 or R13 , a ring carbon or nitrogen atom adjacent to the R9 position and two atoms from the point of attachment may be substituted with

R10, a ring carbon or nitrogen atom adjacent to the R13 position and two atoms

from the point of attachment may be substituted with R 12, a ring carbon or

nitrogen atom three atoms from the point of attachment and adjacent to the R10

position may be substituted with R1 1, a ring carbon or nitrogen atom three

atoms from the point of attachment and adjacent to the R12 position may be

substituted with R33, and a ring carbon or nitrogen atom four atoms from the

point of attachment and adjacent to the R 11 and R33 positions may be

substituted with R34;

R9 and R10 , R10 and R1 1 , R1 1 and R12 , and R12 and R13 spacer pairs are independently selected to form a spacer pair wherein a spacer pair is taken together to form a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 contiguous members, a partially saturated heterocyclyl ring having 5 through 8 contiguous members, a heteroaryl ring having 5 through 6 contiguous members, and an aryl with the proviso that no more than one of the group

consisting of spacer pairs R9 and R10, R10 and R 11, R11 and R12, and R12

and R 13 is used at the same time;

A is selected from the group consisting of single covalent bond,

(W7)rr-(CH(R15))pa and (CH(R15))pa-(W7)rr wherein rr is an integer

selected from 0 through 1, pa is an integer selected from 0 through 6, and W7

is selected from the group consisting of O, S, C(O), C(S), C(O)S, C(S)O,

C(O)N(R7), C(S)N(R7), (R7)NC(O), (R7)NC(S), S(O), S(O)2, S(O)2N(R7),

(R7)NS(O)2, Se(O), Se(O)2, Se(O)2N(R7), (R7)NSe(O)2, P(O)(R8),

N(R7)P(O)(R8), P(O)(R8)N(R7), C(NR7)N(R7), (R7)NC(NR7), and N(R7);

R7 and R8 are independently selected from the group consisting of hydrido, hydroxy, alkyl, alkenyl, aryl, aralkyl, aryloxy, alkoxy, alkenyloxy, alkylthio, alkylamino, arylthio, arylamino, acyl, aroyl, heteroaroyl, aralkoxyalkyl, heteroaralkoxyalkyl, , aryloxyalkyl, alkoxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, aralkoxyalkyl, heteroaralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, heteroaryl, heteroaryloxy, heteroarylamino, heteroaralkyl, heteroaralkyloxy, heteroaralkylamino, and heteroaryloxyalkyl;

R14, R15, R37R R38, R39, R40, R41 and R42 are independently selected from the group consisting of hydrido, hydroxy, halo, cyano, aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl, aminoalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, sulfhydryl, acylamido, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkylalkoxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkoxythioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, saturated heterocyclyl, partially saturated

heterocyclyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl,

heteroaralkylthioalkyl, monocarboalkoxyalkyl, dicarboalkoxyalkyl,

monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, alkylsulfinyl, alkylsulfonyl, haloalkylsulfmyl, haloalkylsulfonyl, arylsulfinyl,

arylsulfinylalkyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfinyl,

aralkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl,

aralkylsulfonylalkyl, carboxy, carboxyalkyl, carboalkoxy, carboxamide, carboxamidoalkyl, carboaralkoxy, trialkylsilyl, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl, and

diaralkoxyphosphonoalkyl ;

R14 and R14, when bonded to different carbons, are taken together to form a group selected from the group consisting of covalent bond, alkylene, haloalkylene, and a linear moiety spacer selected to form a ring selected from the group consisting of cycloalkyl ring having from 5 through 8 contiguous members, cycloalkenyl ring having from 5 through 8 contiguous members, and a heterocyclyl having from 5 through 8 contiguous members;

R14 and R15, when bonded to different carbons, are taken together to form a group selected from the group consisting of covalent bond, alkylene, haloalkylene, and a linear moiety spacer selected to form a ring selected from the group consisting of a cycloalkyl ring having from 5 through 8 contiguous members, a cycloalkenyl ring having from 5 through 8 contiguous members, and a heterocyclyl having from 5 through 8 contiguous members;

R15 and R 15, when bonded to different carbons, are taken together to form a group selected from the group consisting of covalent bond, alkylene, haloalkylene, and a linear moiety spacer selected to form a ring selected from the group consisting of cycloalkyl ring having from 5 through 8 contiguous members, cycloalkenyl ring having from 5 through 8 contiguous members, and a heterocyclyl having from 5 through 8 contiguous members;

R14 and R15, when bonded to the same carbon, are taken together to form a group selected from a group consisting of oxo, thiono, alkylene, haloalkylene, and a linear moiety spacer selected to form a ring selected from the group consisting of cycloalkyl ring having from 5 through 8 contiguous

members, cycloalkenyl ring having from 5 through 8 contiguous members, and a heterocyclyl having from 5 through 8 contiguous members;

Ψ is selected from the group consisting of NR5 , O, C(O), C(S), S,

S(O), S(0)2, ON(R5), P(O)(R8), and CR39 R40 ;

R5 is selected from the group consisting of hydrido, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxy, alkoxy, alkenyloxy, alkylthio, arylthio, aralkoxyalkyl, heteroaralkoxyalkyl, aryloxyalkyl, alkoxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, aralkoxyalkyl, heteroaralkoxyalkyl,

alkylsulfinylalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl,

cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl, halocycloalkenyloxyalkyl, heteroaryl, heteroarylalkyl, monocarboalkoxyalkyl, monocarboalkoxy, dicarboalkoxyalkyl,

monocarboxamido, monocyanoalkyl, dicyanoalkyl, carboalkoxycyanoalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, and dialkoxyphosphonoalkyl;

R1 is selected from the group consisting of hydrido, alkyl, alkenyl, haloalkyl, and alkoxyalkyl;

X0 and R2 are independently selected from the group consisting of Z0 -Q, hydrido, alkyl, alkenyl, and halo;

X0 and R2 are independently selected from the group consisting of amidino, guanidino, dialkylsulfonium, trialkylphosphonium,

dialkylsulfoniumalkyl, heteroarylamino, amino, nitro, alkylamino, arylamino, aralkylamino, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl,

heteroaralkanoyl, haloalkanoyl, hydroxyhaloalkyl, cyano, and phosphono;

X0 and R1 are taken together to form a spacer pair wherein the spacer pair forms a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members with the proviso that no more than one of the group consisting of spacer pair X0 and R1

and spacer pair R 2 and R1 is used at the same time;

R2 and R1 are taken together to form a spacer pair wherein the spacer pair forms a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members with the proviso that no more than one of the group consisting of spacer pair X and R and spacer pair R 2 and R1 are used at the same time;

X0 and R5 are taken together to form a spacer pair wherein the spacer pair forms a linear spacer moiety having from 2 through 5 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members;

X0 and R39 are taken together to form a spacer pair wherein the spacer pair forms a linear spacer moiety having from 2 through 5 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members;

X0 and R40 are taken together to form a spacer pair wherein the spacer pair forms a linear spacer moiety having from 2 through 5 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members;

X0 is selected to form a linear moiety having from 2 through 5 contiguous atoms linked to the points of bonding of both R39 and R40 to form a heterocyclyl ring having from 5 through 8 contiguous members;

R2 and R4a, R2 and R4b, R2 and R14, and R2 and R 15 spacer pairs are independently selected to form spacer pairs wherein a spacer pair is taken together to form a linear moiety having from 2 through 5 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members with the proviso that no more than one of the group of spacer pairs consisting of R2 and

R4a, R2 and R4b, R2 and R14, and R2 and R15 is u1 sed at the same time;

R2 is independently selected to form a linear moiety having from 2 through 5 contiguous atoms linked to the points of bonding of both R4a and R4b to form a heterocyclyl ring having from 5 through 8 contiguous members;

Z0 is selected from the group consisting of covalent single bond, (CR41 R42)q wherein q is an integer selected from 1 through 6, (CH(R41))g- W0 -(CH(R42 ))p wherein g and p are integers independently selected from 0 through 3 and W is selected from the group consisting of O, S, C(O), C(S),

C(O)O, C(S)0, C(O)S, C(S)S, C(O)N(R41), (R41)NC(O), C(S)N(R41 ),

(R41)NC(S), OC(O)N(R41), (R41)NC(O)O, SC(S)N(R41), (R41)NC(S)S, SC(O)N(R41), (R41 )NC(O)S, OC(S)N(R 41), (R41)NC(S)O,

N(R42)C(O)N(R41), (R41)NC(O)N(R42), N(R42)C(S)N(R41),

(R41)NC(S)N(R42), S(O), S(O)2, S(O)2N(R41), N(R41)S(O)2, Se, Se(O),

Se(O)2, Se(O)2N(R41), N(R41)Se(O)2, P(O)(R8), N(R7)P(O)(R8),

P(O)(R8)N(R7), N(R41), ON(R41), and SiR28 R29 , and (CH(R41))e-W2 -(CH(R42))h wherein e and h are integers independently selected from 0 through 2 and W2 is selected from the group consisting of CR41 =CR42 , CR41 R42 =C; vinylidene), and ethynylidene (C≡C; 1,2-ethynyl), with the provisos that R41 and R42 are selected from other than halo and cyano when directly bonded to N and Z0 is directly bonded to the pyridone ring;

Q is formula (II):


wherein D 1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, no more than one of D 1, D2, J1, J2 and K1 is O,

no more than one of D 1, D2, J1, J2 and K1 is S, one of D 1, D2, J1, J2 and K1

must be a covalent bond when two of D 1, D2, J1, J2 and K1 are O and S, and

no more than four of D 1, D2, J1, J2 and K1 are N, with the proviso that R9 ,

R10 , R11 , R12 , and R13 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

Q is formula (III):


wherein D3, D4, J3, and J4 are independently selected from the group

consisting of C, N, O, and S, no more than one of D3, D4, J3, and J4 is O, no

more than one of D3, D4, J3, and J4 is S, and no more than three of D 1 , D2 , J1 , and J2 are N with the proviso that R9 ,R10 , R1 1 , andR 12 are each

independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

Q is selected from the group consisting of alkyl, alkoxy, alkylamino, alkylthio, haloalkylthio, alkenyl, alkynyl, saturated heterocyclyl, partially saturated heterocyclyl, acyl, aroyl, heteroaroyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, cycloalkylalkenyl, haloalkyl, haloalkoxy, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl,

haloalkenyloxyalkyl, halocycloalkoxyalkyl, and halocycloalkenyloxyalkyi;

K is (CR4a R4b )n wherein n is an integer selected from 1 through 4;

R4a and R4b are independently selected from the group consisting of halo, hydrido, hydroxy, cyano, hydroxyalkyl, alkyl, alkenyl, aryl, aralkyl, aralkoxyalkyl, aryloxyalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, aralkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, haloalkenyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, cyanoalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfmyl, arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfonylalkyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl, and aralkylsulfonylalkyl;

R4a and R4b, when bonded to the same carbon, are taken together to form a group selected from the group consisting of oxo, thiono, and a linear spacer moiety having from 2 through 7 contiguous atoms connected to form a ring selected from the group consisting of a cycloalkyl ring having 3 through 8 contiguous members, a cycloalkenyl ring having 5 through 8 contiguous members, and a heterocyclyl ring having 5 through 8 contiguous members;

E0 is E1 , when K is (CR4a R4b )n, wherein E is selected from the group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O, C(S)O, C(O)S,

C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S), OC(O)N(R7),

(R7)NC(O)O, SC(S)N(R7), (R7)NC(S)S, SC(O)N(R7), (R7)NC(O)S,

OC(S)N(R7), (R7)NC(S)O, N(R8)C(O)N(R7), (R7)NC(O)N(R8),

N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2, S(O)2N(R7), N(R7)S(O)2,

S(O)2N(R7)C(O), C(O)N(R7)S(O)2, Se, Se(O), Se(O)2, Se(0)2N(R7),

N(R7)Se(O)2, P(O)(R8), N(R7)P(O)(R8), P(O)(R8)N(R7), N(R7), ON(R7),

SiR28 R29 , CR4a =CR4b , ethynylidene (G≡C; 1,2-ethynyl), and C=CR4a R4b ;

K is (CH(R14 ))j-T wherein j is selected from a integer from 0 through

3 and T is selected from the group consisting of single covalent bond, O, S, and

N(R7 ) with the proviso that (CH(R14 ))j is bonded to the pyridone ring;

E0 is E2 , when K is (CH(R14 ))j-T, wherein E is selected from the group consisting of a covalent single bond, C(O), C(S), C(O)0, C(S)O, C(O)S, C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S), (R7)NC(O)O,

(R7)NC(S)S, (R7)NC(O)S, (R7)NC(S)O, N(R8)C(O)N(R7),

(R7)NC(O)N(R8), N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2,

S(O)2N(R7), N(R7)S(O)2, S(O)2N(H)C(O), C(O)N(H)S(O)2, Se(O),

Se(0)2, Se(O)2N(R7), N(R7)Se(O)2, P(O)(R8), N(R7)P(O)(R8),

P(O)(R8)N(R7), and N(R7);

K is G-(CH(R15))k wherein k is selected from an integer from 1

through 3 and G is selected from the group consisting of O, S, and N(R7 ) with

the proviso that R15 is other than hydroxy, cyano, halo, amino, alkylamino, dialkylamino, and sulfhydryl when k is 1;

E0 is E3 , when K is G-(CH(R15 ))k, wherein E is selected from the group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O, C(S)O, C(0)S, C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S),

OC(0)N(R7), (R7)NC(O)O, SC(S)N(R7), (R7)NC(S)S, SC(O)N(R7),

(R7)NC(O)S, OC(S)N(R7), (R7)NC(S)O, N(R8)C(O)N(R7),

(R7)NC(O)N(R8), N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2,

S(O)2N(R7), N(R7)S(O)2, Se, Se(O), Se(O)2, Se(O)2N(R7), N(R7)Se(O)2,

P(O)(R8), N(R7)P(O)(R8), P(O)(R8)N(R7), N(R7), ON(R7), SiR^R29,

CR4a =CR4b , ethynylidene (C≡C; 1,2-ethynyl), and C=CR4a R4b ;

Y0 is formula (IV):


wherein D5, D6, J5, and J6 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K2 is independently selected from the group

consisting of C, and N , no more than one of D5, D6, J5, and J6 is O, no more

than one of D5, D6, J5, and J6 is S, one of D5, D6, J5, and J6 must be a

covalent bond when two of D5, D6, J5, and J6 are O and S, no more than three

of D5, D6, J5, and J6 are N when K2 is N+ , and no more than four of D5, D6,

J5, and J6 are N when K2 is carbon with the provisos that R16, R17, R18, and

R19 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R16 and R17 are independently taken together to form a linear moiety spacer having from 3 through 6 contiguous atoms connected to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 through 8 contiguous members, a partially saturated heterocyclyl ring having from 5 through 8 contiguous members, a heteroaryl having from 5 through 6 contiguous members, and an aryl;

R18 and R 19 are independently taken together to form a linear moiety spacer having from 3 through 6 contiguous atoms connected to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 through 8 contiguous members, a partially saturated heterocyclyl ring having from 5 through 8 contiguous members, a heteroaryl having from 5 through 6 contiguous members, and an aryl;

Qb is selected from the group consisting of NR20 R21 ,+ NR20 R21 R22 , oxy, alkyl, alkylaminoalkyl, aminoalkyl, dialkylsulfoniumalkyl, and acylamino wherein R20 , R21 , and R22 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl with the provisos that no more than one of R20,

R21, and R22 is hydroxy, alkoxy, alkylamino, ammo, and dialkylamino and that

R20, R21, andR must be other than be hydroxy, alkoxy, alkylamino, ammo,

and dialkylamino when K2 is N+;

R20 and R21, R20 and R22, and R21 and R22 pairs are independently selected to form a spacer pair wherein a spacer pair is taken together to form a linear moiety having from 4 through 7 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having 5 through 8 contiguous members with the proviso that no more than one of the group consisting of spacer pairs R20 and R21, R20 and R22, andR21 and R22

is used at the same time;

Qb is selected from the group consisting of N(R26 )SO2N(R23 )(R24 ),

N(R26)C(O)OR5, N(R26)C(O)SR5, N(R26)C(S)OR5 and N(R26)C(S)SR5

with the proviso that no more than one of R23, R24, andR26 are hydroxy, alkoxy, alkylamino, amino, or dialkylamino when two of the group consisting of R23 , R24 , and R26 are bonded to the same atom;

Qb is selected from the group consisting of dialkylsulfonium,

trialkylphosphonium, C(NR25 )NR23 R24 , N(R26 )C(NR25 )N(R23 )(R24 ),

N(R26)C(O)N(R23)(R24), N(R26)C(S)N(R23)(R24), C(NR25)OR5,

C(O)N(R26)C(NR25)N(R23)(R24), C(S)N(R26)C(NR25)N(R23)(R24),

N(R26)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)SO2N(R23)(R24),

C(NR25 )SR5, C(O)NR23 R24, and C(O)NR23 R24 with the provisos that no

more than one of R23 , R24, and R26 is hydroxy, alkoxy, alkylamino, amino, or

dialkylamino when two of the group consisting of R23 , R24, and R26 are

bonded to the same atom and that said Qb group is bonded directly to a carbon atom;

R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl;

R23 and R24 are taken together to form a linear spacer moiety having from 4 through 7 contiguous atoms connecting the points of bonding to form a heterocyclyl ring having 5 through 8 contiguous members;

R23 and R25, R24 and R25, R25 and R26, R2 4 and R26 , and R23

and R26 pairs are independently selected to form a spacer pair wherein a spacer pair is taken together from the points of bonding of selected spacer pair members to form the group L-U-V wherein L, U, and V are independently selected from the group of 1,2-disubstituted radicals consisting of a cycloalkyl radical, a cycloalkenyl radical wherein cycloalkyl and cycloalkenyl radicals are substituted with one or more groups selected from R30 and R3 1, an aryl radical, an heteroaryl radical, a saturated heterocyclic radical and a partially saturated heterocyclic radical wherein said 1,2-substitutents are independently selected from C=O, C=S, C(R28 )R32 ,

S(O), S(O)2, OP(OR31)R30, P(O)R30, P(S)R30 and Si(R28)R29;

R23 and R25, R24 and R25, R25 and R26, R24 and R26, and R23 and R26

pairs are independently selected to form a spacer pair wherein a spacer pair is taken together from the points of bonding of selected spacer pair members to form the group L-U-V wherein L, U, and V are independently selected from the group of radicals consisting of 1,2-disubstituted alkylene radicals and 1,2-disubstituted alkenylene radical wherein said 1,2-substitutents are independently selected from

C=O, C=S, C(R28)R29, S(O), S(O)2, OP(OR31)R30, P(O)R30, P(S)R30, and Si(R28 )R29 and said alkylene and alkenylene radical are substituted with one or more R30 or R31 substituents;

R23 and R25, R24 and R25, R25. and R26, R24 and R26, and R23 and R26

pairs are independently selected to form a spacer pair wherein a spacer pair is taken together from the points of bonding of selected spacer pair members to form the group L-U-V wherein L, U, and V are independently selected from the group consisting of O, S, C(O), C(S), C(JH)2 S(O), SO2, OP(OR31)R30, P(O)R30,

P(S)R30 , C(R30 )R31, C=C(R30 )R31, (O)2POP(O)2, R30 (O)POP(O)R30,

Si(R29)R28) Si(R29)R28Si(R29)R28, Si(R29)R28OSi(R29)R28,

(R28)R29COC(R28)R29, (R28)R29CSC(R28)R29, C(O)C(R3°)=C(R31), C(S)C(R30)=C(R31), S(O)C(R30)=c(R31), 0O2C(R30)=C(R31),

PR30C(R30)=C(R31), P(O)R30C(R30)=C(R31), P(S)R30C(R30)=C(R31),

DC(R3°)(R31)D, OP(OR31)R30, P(O)R30, P(S)R30, Si(R28)R29 and N(R30), and a covalent bond with the proviso that no more than any two of L, U and V are simultaneously covalent bonds and the heterocyclyl comprised of by L, U, and V has from 5 through 10 contiguous member;

D is selected from the group consisting of oxygen, C=O, C=S, and S(O)m wherein m is an integer selected from 0 through 2;

JH is independently selected from the group consisting of OR27 , SR27 and

N(R20)R21;

R 27 is selected from the group consisting of hydrido, alkyl, alkenyl, alkynyl, aralkyl, aryloxyalkyl, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkylthioalkyl, alkoxyalkyl, heteroaryloxyalkyl,

alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl, haloalkenyloxyalkyl,

halocycloalkoxyalkyl, halocycloalkenyloxyalkyi, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, arylsulfinylalkyl, arylsulfonylalkyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl,

heteroarylsulfonylalkyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl and

aralkylsulfonylalkyl;

R28 and R29 are independently selected from the group consisting of hydrido, hydroxyalkyl, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, acyl, aroyl, aralkanoyl, heteroaroyl, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkylthioalkyl, alkoxyalkyl, heteroaryloxyalkyl,

alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl, haloalkenyloxyalkyl,

halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyi, perhaloaryl, perhaloaralkyl, perhaloaryloxyalkyl, heteroaryl, heteroarylalkyl, heteroarylthioalkyl, heteroaralkylthioalkyl, cyanoalkyl, dicyanoalkyl, carboxamidoalkyl,

dicarboxamidoalkyl, cyanocarboalkoxyalkyl, carboalkoxyalkyl, dicarboalkoxyalkyl, cyanocycloalkyl, dicyanocycloalkyl, carboxamidocycloalkyl,

dicarboxamidocycloalkyl, carboalkoxycyanocycloalkyl, carboalkoxycycloalkyl, dicarboalkoxy cycloalkyl, formylalkyl, acylalkyl, arylsulfinylalkyl, arylsulfonylalkyl, aralkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsufonylalkyl,

heteroarylsulfonylalkyl, heteroarylsulfinylalkyl, aralkylsulfinylalkyl,

aralkylsulfonylalkyl, carboxy, dialkoxyphosphono, diaralkoxyphosphono, dialkoxyphosphonoalkyl and diaralkoxyphosphonoalkyl;

R28 and R29 are taken together to form a linear moiety spacer having from

2 through 7 contiguous atoms and forming a ring selected from the group consisting of a cycloalkyl ring having from 3 through 8 contiguous members, a cycloalkenyl ring having from 3 through 8 contiguous members, and a heterocyclyl ring having from 3 through 8 contiguous members;

R30 and R31 are independently selected from hydrido, hydroxy, thiol, aryloxy, amino, alkylamino, dialkylamino, hydroxyalkyl, heteroaryloxyalkyl, alkoxy, alkylthio, arylthio, alkyl, alkenyl, alkynyl, aryl, aralkyl, aryloxyalkyl, aralkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aralkylthioalkyl, heteroaralkoxythioalkyl, alkoxyalkyl, heteroaryloxyalkyl, alkenyloxyalkyl, alkylthioalkyl, arylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, haloaralkylsulfmylalkyl, aralkylsulfonylalkyl, cyanoalkyl, dicyanoalkyl, carboxamidoalkyl, dicarboxamidoalkyl, cyanocarboalkoxyalkyl, carboalkoxyalkyl, dicarboalkoxyalkyl, cyanocycloalkyl, dicyanocycloalkyl, carboxamidocycloalkyl, dicarboxamidocycloalkyl, carboalkoxycyanocycloalkyl, carboalkoxycycloalkyl, dicarboalkoxycycloalkyl, formylalkyl, acylalkyl,

dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, phosphonoalkyl,

dialkoxyphosphonoalkoxy, diaralkoxyphosphonoalkoxy, phosphonoalkoxy, dialkoxyphosphonoalkylamino, diaralkoxyphosphonoalkylamino,

phosphonoalkylamino, dialkoxyphosphonoalkyl, diaralkoxyphosphonoalkyl, sulfonyl alkyl, alkoxysulfonylalkyl, aralkoxysulfonylalkyl, alkoxysulfonylalkoxy, aralkoxysulfonylalkoxy, sulfonylalkoxy, alkoxysulfonylalkylamino,

aralkoxysulfonylalkylamino, and sulfonylalkylamino;

R30 and R3 1 are taken to form a linear moiety spacer group having from 2 through 7 contiguous atoms to form a ring selected from the group consisting of a cycloalkyl ring having from 3 through 8 contiguous members, a cycloalkenyl ring having from 3 through 8 contiguous members, and a heterocyclyl ring having from 3 through 8 contiguous members;

Qs is selected from the group consisting of a single covalent bond,

(CR37 R38 )b-(W0 )az wherein az is an integer selected from 0 through 1 , b is an

integer selected from 1 through 4, and W is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R14),

(R14)NC(O), C(S)N(R14), (R14 )NC(S), OC(O)N(R14 ), SC(S)N(R14 ),

SC(0)N(R 14), OC(S)N(R 14), N(R15)C(O)N(R14), (R14)NC(0)N(R15), N(R15)C(S)N(R14), (R 14)NC(S)N(R15), S(O), S(O)2, S(0)2N(R 14),

N(R14)S(O)2, Se, Se(O), Se(O)2, Se(O)2N(R17), N(R14)Se(O)2, P(O)(R8),

N(R7 )P(0)(R8), P(O)(R8)N(R7), N(R14), ON(R14), and SiR28 R29 ,

(CH(R14))C-W1 -(CH(R 15)) d wherein c and d are integers independently selected from 1 through 4, and W is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R14), (R14)NC(O),

C(S)N(R14),(R14)NC(S), OC(O)N(R14),(R14)NC(O)O, SC(S)N(R14),

(R14)NC(S)S, SC(O)N(R14), (R14)NC(O)S, OC(S)N(R14), (R14)NC(S)O, N(R15)C(O)N(R14),(R14)NC(O)N(R15),N(R15)C(S)N(R14),

(R14)NC(S)N(R15), S(O), S(O)2, S(O)2N(R14), N(RM)S(O)2, Se, Se(O), Se(O)2, Se(0)2N(R14),N(R14)Se(O)2, P(O)(R8), N(R7)P(O)(R8),

P(O)(R8)N(R7),N(R14),ON(R14), SiR28R29,and(CH(R14))e-W2-(CH(R15 )) h wherein e and h are integers independently selected from 0 through 2 and W2 is selected from the group consisting of CR4a =CR4b , ethynylidene (C≤≡C; 1,2-ethynyl), and C=CR4a R4b with the provisos that R14 and R 15 are selected from other than halo and cyano when directly bonded to

N and that (CR37R38)b, (CH(R14))C, (CH(R14))e and are bonded to E0;

Y0 is Qb -Qss wherein Qss is selected from the group consisting of

(CR37 R38 )f wherein f is an integer selected from 1 through 6, (CH(R14 ))c-

W1 -(CH(R15)) d wherein c and d are integers independently selected from 1

through 4, and W is selected from the group consisting of W is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S

C(O)N(R14), (R14)NC(O), C(S)N(R14), (R14)NC(S), OC(O)N(R14),

(R14)NC(O)O, SC(S)N(R14), (R14)NC(S)S, SC(O)N(R14), (R14)NC(O)S,

OC(S)N(R14), (R14)NC(S)O, N(R 15)C(O)N(R 14), (R 14 )NC(O)N(R15),

N(R15)C(S)N(R14), (R14)NC(S)N(R15), S(O), S(O)2, S(O)2N(R14),

N(R14)S(O)2, Se, Se(O), Se(O)2, Se(O)2N(R14), N(R14)Se(O)2, P(O)(R8),

N(R7)P(O)(R8), P(O)(R8)N(R7), N(R14), ON(R14), SiR28 R29 , and

(CH(R14))e-W2 -(CH(R15))n wh)rein e and h are integers independently

selected from 0 through 2 and W2 is selected from the group consisting of

CR4a =CR4b , ethynylidene (C=C; 1,2-ethynyl), and C=CR4a R4b with the

provisos that R14 and R15 are selected from other than halo and cyano when

directly bonded to N and that (CR37 R38 )f, (CH(R15))c, and (CH(R15))e are bonded to E ;

Y0 is Qb -Qsss wherein Qsss is (CH(R38 ))r-W3 , r is an integer selected

from 1 through 3, and W3 is selected from the group consisting of 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1 -cyclobutyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 13-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 13-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, lβ-piperazinyl, 1,4-piperazinyl, 23-ρiperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 13-piperidinyl, 1,4-piperidinyl, 23-piperidinyl, 2,4-ρiperidinyl, 2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-ρyrrolidinyl, 2,4-ρyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl, 2H-2,5-ρyranyl, 4H-23-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-ρyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the proviso that (CH(R38))r

is bonded to E0 and Qb is bonded to lowest numbered substituent position of

eachW ;

Y0 is Qb -Qsssr wherein Qsssr is (CH(R38))r-W4 , r is an integer

selected from 1 through 3, and W4 is selected from the group consisting of 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 1,3-ρiperazinyl, 1,4-piperazinyl, 2,3-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 1,4-piρeridinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-ρyrrolidinyl, 2,4-pyπolidinyl, 2,5-pyπolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl, 2H-2,Spyranyl, 4H-23~ρyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrαfuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the provisos that (CH(R38))r

is bonded to E0 and Qb is bonded to highest number substituent position of

each W4 ;

Y0 is Qb -Qssss wherein Qssss is (CH(R38))r-W5, r is an integer

selected from 1 through 3, and W is selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindoIyl, 3,4-indazolyl, 3,5-indazoIyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyI, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinohnyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinoUnyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinohnyl, 1,4-isoquinolinyl, 1,5-isoquinoUnyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Q is bonded to lowest number substituent position of each

W5 and that (CH(R38))r is bonded to E0;

Y0 is Qb -Qssssr wherein Qssssr is (CH(R38))r-W6, r is an integer

selected from 1 through 3, and W is selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,Sbenzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-

benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,Squinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,Squinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinoUnyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Q is bonded to highest number substituent position of each

W6 and that (CH(R38 ))r is bonded to E0;

R37 and R37 , when bonded to different carbons, are taken together to form a linear moiety spacer having from 1 through 7 contiguous atoms to form a ring selected from the group consisting of a cycloalkyl ring having from 3 through 8 contiguous members, a cycloalkenyl ring having from 3 through 8 contiguous members, and a heterocyclyl ring having from 3 through 8 contiguous members;

R37 and R38 , when bonded to different carbons, are taken together to form a linear moiety spacer having from 1 through 7 contiguous atoms to form a ring selected from the group consisting of a cycloalkyl ring having from 3 through 8 contiguous members, a cycloalkenyl ring having from 3 through 8 contiguous members, and a heterocyclyl ring having from 3 through 8 contiguous members;

R38 and R38 , when bonded to different carbons, are taken together to form a linear moiety spacer having from 1 through 7 contiguous atoms to form a ring selected from the group consisting of a cycloalkyl ring having from 3 through 8 contiguous members, a cycloalkenyl ring having from 3 through 8 contiguous members, and a heterocyclyl ring having from 3 through 8 contiguous members;

R37 and R38 , when bonded to the same carbon, are taken together to form a group selected from a group consisting of oxo, thiono, alkylene, haloalkylene, and a linear moiety spacer having from 2 through 7 contiguous atoms to form a ring selected from the group consisting of a cycloalkyl ring having from 3 through 8 contiguous members, a cycloalkenyl ring having from 3 through 8 contiguous members, and a heterocyclyl ring having from 3 through 8 contiguous members;

R3 9 and R40 , when bonded to the same carbon, are taken together to

form a group selected from a group consisting of oxo, thiono, R5 -N, alkylene, haloalkylene, and a linear moiety spacer having from 2 through 7 contiguous atoms to form a ring selected from the group consisting of a cycloalkyl ring having from 3 through 8 contiguous members, a cycloalkenyl ring having from 3 through 8 contiguous members, and a heterocyclyl ring having from 3 through 8 contiguous members.

2. The compound as recited in Claim 1 or a pharmaceutically acceptable salt thereof, wherein;

B is formula (V):


wherein D1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, no more than one of D1, D2, J1, J2 and K1 is O,

no more than one of D1, D2, J1, J2 and K1 is S, one of D1, D2, J1, J2 and K1

must be a covalentbond when two of D1, D2, J1, J2 and K1 are O and S, and

no more than four of D1, D2, J1, J2 and K1 are N with the proviso that R32 ,

R33 , R34 , R35 , and R36 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R32 , R33 , R34 , R35 , and R36 are independently selected to be Qb ;

R9, R1 0, R1 1, R12, R13, R16, R17, R1 8, R19, R32, R33, R34, R35, and

R36 are independently selected from the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, trialkylphosphonium, dialkylsulfoniumalkyl, carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl, acylalkoxy, aryloylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,

cycloalkylsulfonylalkyl, heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, cycloalkenyloxy,

cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy,

halocycloalkenyloxyalkyi, hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl,

arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl,

heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl,

haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,

alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl, arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky,

alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl,

cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, aminoalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl;

R32 and R33 , R33 and R34 , R34 and R35 , and R35 and R36 pairs are independently selected to form a spacer pair wherein a spacer pair is taken together to form a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 contiguous members, a partially saturated heterocyclyl ring having 5 through 8- contiguous members, a heteroaryl ring having 5 through 6 contiguous members, and an aryl with the proviso that no more than one of the group

consisting of spacer pairs R32 and R33 , R33 and R34 , R34 and R35 , and R35

and R36 is used at the same time;

B is selected from the group consisting of C3-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl wherein each member of group B may be optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36,'

B is selected from the group consisting of C3-C10 cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partially saturated heterocyclyl, wherein each ring carbon may be optionally substituted with R33, a ring carbon other than the ring carbon at the point of attachment of B to A may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbon and nitrogen atoms adjacent to the carbon atom at the point of attachment may be optionally substituted with R9 or R13, a ring carbon or nitrogen atom adjacent to the R9 position and two atoms from the point of attachment may be substituted with

R10, a ring carbon or nitrogen atom adjacent to the R13, position and two atoms

from the point of attachment may be substituted with R12, a ring carbon or

nitrogen atom three atoms from the point of attachment and adjacent to the R10

position may be substituted with R 11 , a ring carbon or nitrogen atom three

atoms from the point of attachment and adjacent to the R12 position may be

substituted with R33, and a ring carbon or nitrogen atom four atoms from the

point of attachment and adjacent to the R11 and R33 positions may be

substituted with R34;

R9 and R 10, R10 and R1 1, R11 and R12 , and R 12 and R13 pa1irs are independently selected to form a spacer pair wherein a spacer pair is taken together to form a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a ring selected from the group consisting of a cycloalkenyl ring having 5 through 8 contiguous members, a partially saturated heterocyclyl ring having 5 through 8 contiguous members, a heteroaryl ring having 5 through 6 contiguous members, and an aryl with the proviso that no more than one of the group consisting of spacer pairs R9 and R10 , R10 and R1 1 , R11 and R12 , and R12

and R13 is used at the same time;

A is selected from the group consisting of single covalent bond, (W7)rr-(CH(R15))pa and (CH(R15))pa-(W7)rr wherein rr is an integer

selected from 0 through 1, pa is an integer selected from 0 through 6, and W7

is selected from the group consisting of O, S, C(O), C(S), C(O)S, C(S)O,

C(O)N(R7), C(S)N(R7), (R7)NC(O), (R7)NC(S), S(O), S(O)2, S(O)2N(R7),

(R7)NS(O)2, P(O)(R8), N(R7)P(O)(R8), P(0)(R8)N(R7), C(NR7)N(R7),

(R7)NC(NR7), and N(R7);

R7 and R8 are independently selected from the group consisting of hydrido, hydroxy, alkyl, acyl, aroyl, heteroaroyl, and alkoxyalkyl;

R14 , R15 , R37 , and R38 are independently selected from the group consisting of hydrido, hydroxy, halo, cyano, hydroxyalkyl, alkoxy, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxyalkyi, carboxy, carboxyalkyl, carboalkoxy, carboxamide, and carboxamidoalkyl;

Ψ is selected from the group consisting of NR , O, C(O), C(S), S,

S(O), S(O)2, ON(R5 ), P(O)(R8 ), and CR39 R40 ;

R5 is selected from the group consisting of hydrido, alkyl, alkoxy, alkoxyalkyl, haloalkyl, acyl, aroyl, and heteroaroyl;

R39 and R40 are independently selected from the group consisting of hydrido, hydroxy, halo, cyano, hydroxyalkyl, acyl, aroyl, heteroaroyl, acylamido, alkoxy, alkyl, alkoxyalkyl, haloalkyl, haloalkoxy, haloalkoxyalkyl, alkylsulfonyl, haloalkylsulfonyl, carboxy, carboxyalkyl, carboalkoxy, carboxamide, and carboxamidoalkyl;

R 1 is selected from the group consisting of hydrido, alkyl, alkenyl, haloalkyl, and alkoxyalkyl;

X0 and R2 are independently selected from the group consisting of Z0 - Q, hydrido, alkyl, alkenyl, and halo;

A0 and R2 are independently selected from the group consisting of amidino, guanidino, dialkylsulfonium, trialkylphosphonium,

dialkylsulfoniumalkyl, heteroarylamino, amino, nitro, alkylamino, arylamino, aralkylamino, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl,

heteroaralkanoyl, haloalkanoyl, hydroxyhaloalkyl, cyano, and phosphono;

X0 and R1 are taken together to form a spacer pair wherein the spacer pair forms a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members with the proviso that no more than one of the group consisting of spacer pair X0 and R1

and spacer pair R 2 and R1 is used at the same time;

R 2 and R1 are taken together to form a spacer pair wherein the spacer pair forms a linear moiety having from 3 through 6 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having from 5 through 8 contiguous members with the proviso that no more than one of the group consisting of spacer pair X0 and R1

and spacer pair R 2 and R1 is used at the same time;

Z0 is selected from the group consisting of covalent single bond,

(CR41 R42 )q wherein q is an integer selected from 1 through 6, (CH(R41 ))„-

W0 -(CH(R42 ))p wherein g and p are integers independently selected from 0

through 3 and W0 is selected from the group consisting of O, S, C(O), C(S),

C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R41), (R41)NC(O), C(S)N(R41),

(R41)NC(S), OC(O)N(R41), (R41)NC(0)O, SC(S)N(R41), (R41)NC(S)S,

SC(O)N(R41), (R41)NC(O)S, OC(S)N(R41), (R41)NC(S)O,

N(R42)C(O)N(R41), (R41 )NC(O)N(R42), N(R42)C(S)N(R41),

(R41)NC(S)N(R42), S(O), S(O)2, S(O)2N(R41), N(R41)S(O)2, P(O)(R8),

N(R7)P(O)(R8), P(O)(R8)N(R7), N(R41), ON(R41), and (CH(R41))e- W2-

(CH(R42))h wherein e and h are integers independently selected from 0

through 2 and W2 is selected from the group consisting of CR41 =CR42 ,

CR41 R42 =C; vinylidene), and ethynylidene (G≡C; 1,2-ethynyl), with the

provisos that R41 and R42 are selected from other than halo and cyano when directly bonded to N and Z0 is directly bonded to the pyridone ring;

R41 and R42 are independently selected from the group consisting of hydrido, hydroxy, halo, cyano, aryloxy, hydroxyalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, alkoxy, alkyl, aryl, aralkyl, aryloxyalkyl,

aralkoxyalkylalkoxy, alkoxyalkyl, heteroaryloxyalkyl, cycloalkyl,

cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl,

halocycloalkenyloxyalkyi, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaralkyl, heteroarylthioalkyl,

heteroaralkylthioalkyl, alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl, arylsulfonylalkyl, aralkylsulfonyl, cycloalkylsulfonyl, cycloalkylsufonylalkyl, heteroarylsulfonylalkyl, heteroarylsuafonyl, and aralkylsulfonylalkyl;

Q is formula (II):


wherein D1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, no more than one of D1, D2, J1, J2 and K1 is O,

no more than one of D1, D2, J1, J2 and K1 is S, one of D1, D2, J1, J2 and K1

mustbe a covalentbond when two of D1, D2, J1, J2 and K1 are O and S, and

no more than four of D1, D2, J1, J2 and K1 are N, with the proviso that R9 ,

R 10, R1 1, R12, and R13 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

Q is formula (III):


wherein D3, D4, J3, and J4 are independently selected from the group

consisting of C, N, O, and S, no more than one of D3, D4, J3, and J4 is O, no

more than one of D3, D4, J3, and J4 is S, and no more than three of D 1, D2, J1, and J2 are N with the proviso that R9 , R10 , R11 , and R12 are each

independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

Q is selected from the group consisting of alkyl, alkoxy, alkylamino, alkylthio, haloalkylthio, alkenyl, alkynyl, saturated heterocyclyl, partially saturated heterocyclyl, acyl, aroyl, heteroaroyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, cycloalkylalkenyl, haloalkyl, haloalkoxy, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl,

haloalkenyloxyalkyl, halocycloalkoxyalkyl, and halocycloalkenyloxyalkyi;

K is (CR4a R4b )n wherein n is an integer selected from 1 through 2;

R4a and R4b are independently selected from the group consisting of halo, hydrido, hydroxy, cyano, hydroxyalkyl, alkyl, alkenyl, alkoxyalkyl, haloalkyl, haloalkenyl, and cyanoalkyl;

R4a and R4b , when bonded to the same carbon, are taken together to form a group selected from the group consisting of oxo, and a linear spacer moiety having from 2 through 7 contiguous atoms connected to form a ring selected from the group consisting of a cycloalkyl ring having 3 through 8 contiguous members, a cycloalkenyl ring having 5 through 8 contiguous members, and a heterocyclyl ring having 5 through 8 contiguous members;

E0 is E1 , when K is (CR4a R4b )n, wherein E is selected from the group consisting of a covalent single bond, O, S, C(O), C(S), C(O)0, C(S)O, C(O)S,

C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S), OC(O)N(R7),

(R7)NC(O)O, SC(S)N(R7), (R7)NC(S)S, SC(O)N(R7), (R7)NC(O)S,

OC(S)N(R7), (R7)NC(S)O, N(R8)C(O)N(R7), (R7)NC(O)N(R8),

N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2, S(O)2N(R7), N(R7)S(O)2,

S(O)2N(R7)C(O), C(O)N(R7)S(O)2, P(O)(R8), N(R7)P(O)(R8),

P(O)(R8)N(R7), N(R7), ON(R7), CR4a=CR4b, ethynylidene (C≡C; 1,2-

ethynyl), and C=CR4aR4b;

K is (CH(R14))j-T wherein j is selected from a integer from 0 through

2 and T is selected from the group consisting of single covalent bond, O, S, and N(R7 ) with the proviso that (CH(R14 ))j is bonded to the pyridone ring;

E0 is E2 , when K is (CH(R 14 ))j-T, wherein E is selected from the group consisting of a covalent single bond, C(O), C(S), C(O)O, C(S)O, C(0)S, C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S), (R7)NC(O)O,

(R7)NC(S)S, (R7)NC(O)S, (R7)NC(S)O, N(R8)C(O)N(R7),

(R7)NC(O)N(R8), N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2,

S(O)2N(R7), N(R7)S(O)2, S(O)2N(H)C(O), C(O)N(H)S(O)2, P(O)(R8),

N(R7)P(O)(R8), P(O)(R8)N(R7), and N(R7);

K is G-(CH(R15)) k wherein k is selected from an integer from 1

through 2 and G is selected from the group consisting of O, S, and N(R7 ) with

the proviso that R15 is other than hydroxy, cyano, halo, amino, alkylamino, dialkylamino, and sulfhydryl when k is 1;

E0 is E3 , when K is G-(CH(R15 ))k , wherein E3 is selected from the group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O, C(S)0,

C(O)S, C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S),

OC(O)N(R7), (R7)NC(O)O, SC(S)N(R7), (R7)NC(S)S, SC(O)N(R7),

(R7)NC(O)S, OC(S)N(R7), (R7)NC(S)O, N(R8)C(O)N(R7),

(R7)NC(O)N(R8), N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2,

S(O)2N(R7), N(R7)S(O)2, P(O)(R8), N(R7)P(O)(R8), P(O)(R8)N(R7),

N(R7 ), ON(R7 ), CR4a =CR4b , ethynylidene (C≡C; 1,2-ethynyl), and

C=CR4a R4b ;

Y0 is formula (IV):


wherein D5, D6, J5, and J6 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K2 is independently selected from the group

consisting of C, and N+, no more than one of D5, D6, J5, and J6 is O, no more

than one of D5, D6, J5, and J6 is S, one of D5, D6, J5, and J6 must be a

covalent bond when two of D5, D6, J5, and J6 are O and S, no more than three

of D5, D6, J5, and J6 are N when K2 is N+ , and no more than four of D5 , D6 ,

J5 , and J6 are N when K2 is carbon with the provisos that R16 , R17 , R18 , and

R19 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R16 and R17 are taken together to form a linear moiety spacer having from 3 through 6 contiguous atoms connected to form a ring selected from the group consisting of a cycloalkenyl ring having from 5 through 8 contiguous members, a partially saturated heterocyclyl ring having from 5 through 8 contiguous members, a heteroaryl having from 5 through 6 contiguous members, and an aryl;

Qb is selected from the group consisting of NR20 R21 ,+ NR20 R21 R22 , oxy, alkyl, alkylaminoalkyl, aminoalkyl, dialkylsulfoniumalkyl, and acylamino wherein R20 , R21 , and R22 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl with the provisos that no more than one of R20 ,

R21 , and R22 is hydroxy, alkoxy, alkylamino, ammo, and dialkylamino and that

R20 , R21 , and R22 must be other than be hydroxy, alkoxy, alkylamino, amino,

and dialkylamino when K2 is N+ ;

R20 and R21 , R20 and R22 , and R21 and R22 pairs are independently selected to form a spacer pair wherein a spacer pair is taken together to form a linear moiety having from 4 through 7 contiguous atoms connecting the points of bonding of said spacer pair members to form a heterocyclyl ring having 5 through 8 contiguous members with the proviso that no more than one of the group consisting of spacer pairs R20 and R21 , R20 and R22 , and R21 and R22 is used at the same time;

Qb is selected from the group consisting of N(R26 )SO2N(R23 )(R24 ),

N(R26)C(O)OR5, N(R26)C(O)SR5, N(R26)C(S)OR5 and N(R26)C(S)SR5

with the proviso that no more than one of R23 , R24 , and R26 is hydroxy, alkoxy, alkylamino, amino, or dialkylamino when two of the group consisting of R23 , R24 , and R26 are bonded to the same atom;

Q is selected from the group consisting of dialkylsulfonium,

trialkylphosphonium, C(NR25 )NR 23 R24 , N(R26 )C(NR25 )N(R23 )(R24 ),

N(R26)C(O)N(R23)(R24), N(R26)C(S)N(R23)(R24), C(NR25)OR5,

C(O)N(R26 )C(NR25 )N(R23 )(R24 ), C(S)N(R26 )C(NR25 )N(R23 )(R24 ),

N(R26)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)SO2N(R23)(R24),

C(NR25 )SR5 , C(O)NR23 R24 , and C(O)NR23 R24 with the provisos that no

more than one of R23 , R24 , and R26 is hydroxy, alkoxy, alkylamino, ammo, or

dialkylamino when two of the group consisting of R23 , R24 , and R26 are

bonded to the same atom and that said Qb group is bonded directly to a carbon atom;

R23 , R24 , R25 , and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl;

R23 and R24 are taken together to form a linear spacer moiety having from

4 through 7 contiguous atoms connecting the points of bonding to form a heterocyclyl ring having 5 through 8 contiguous members;

Qs is selected from the group consisting of a single covalent bond,

(CR37 R38 ) b-(W0 )az wherein az is an integer selected from 0 through 1 , b is an integer selected from 1 through 4, and W is selected from the group consisting ofO, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R14),

(R14)NC(O), C(S)N(R14),(R14)NC(S), OC(O)N(R14), SC(S)N(R14), SC(O)N(R14),OC(S)N(R14),N(R15)C(O)N(R14),(R14)NC(O)N(R15),

N(R15)C(S)N(R14),(R14)NC(S)N(R15), S(O), S(O)2, S(O)2N(R14),

N(R14)S(O)2,P(O)(R8),N(R7)P(O)(R8),P(O)(R8)N(R7),N(R14),

ON(R 14 ), (CH(R14 ))C-W1 -(CH(R15 ))d wherein c and d are integers

1

independently selected from 1 through 4, and W is selected from the group

consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R14),

(R14)NC(O), C(S)N(R14),(R14)NC(S), OC(O)N(R14),(R14)NC(O)O,

SC(S)N(R14),(R14)NC(S)S,SC(O)N(R14),(R14)NC(O)S,OC(S)N(R14),

(R14)NC(S)O, N(R15)C(O)N(R14), (R14)NC(O)N(R15),

N(R15)C(S)N(R14),(R14)NC(S)N(R15), S(O), S(O)2, S(O)2N(R14), N(R14)S(O)2,P(O)(R8),N(R7)P(O)(R8),P(O)(R8)N(R7),N(R14),

ON(R14 ), and (CH(R14 ))e-W2 -(CH(R15 ))h wherein e and h are integers

independently selected from 0 through 2 and W^ is selected from the group

consisting of CR4a =CR4b , ethynylidene (C≡C; 1,2-ethynyl), and C=CR4a R4b

with the provisos that R14 and R15 are selected from other than halo and cyano

when directly bonded to N and that (CR37 R38 )b, (CH(R14 ))c, (CH(R14 ))e and are bonded to E0 ;

Y0 is Qb -Qss wherein Qss is selected from the group consisting of

(CR37 R38 )f wherein f is an integer selected from 1 through 6, (CH(R 14 ))c-

W 1 -(CH(R 15 )) d wherein c and d are integers independently selected from 1

through 4, and W is selected from the group consisting of W 1 is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,

C(O)N(R14), (R14)NC(O), C(S)N(R14), (R14)NC(S), OC(O)N(R14),

(R14 )NC(O)O, SC(S)N(R14 ), (R14 )NC(S)S, SC(O)N(R14 ), (R14 )NC(O)S,

OC(S)N(R14), (R14)NC(S)O, N(R15)C(O)N(R14), (R14)NC(O)N(R15),

N(R15)C(S)N(R14), (R14)NC(S)N(R15), S(O), S(O)2, S(O)2N(RM),

N(R 14 )S(O)2, P(O)(R8 ), N(R7 )P(O)(R8 ), P(O)(R8 )N(R7 ), N(R14 ),

ON(R14 ), and (CH(R14 ))e-W2 -(CH(R15 ))h wherein e and h are integers

independently selected from 0 through 2 and W2 is selected from the group

consisting of CR4a =CR4b , ethynylidene (CsC; 1,2-ethynyl), and C=CR4a R4b

with the provisos that R14 and R15 are selected from other than halo and cyano

when directly bonded to N and that (CR37 R38 )f, (CH(R 15 ))c , and

(CH(R15))e are bonded to E0

Y0 is Qb -Qsss , wherein Qsss is (CH(R38 ))r-W3 , r is an integer selected

from 1 through 3, and W 3 is selected from the group consisting of 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 13-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 23-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3 ,4-morpholinyl,3,5-morpholinyl, 1,2-piperazinyl, 13-piperazinyl, 1,4-piperazinyl, 23-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-ρiperidinyl, 13-piperidinyl, 1,4-piperidinyl, 23-piρeridinyl, 2,4-piperidinyl, 2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl, 13-pyrrolidinyl, 23-ρyrrolidinyl, 2,4-pyπolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl, 2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-23-yl, 23-tetrahydrαfuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 23-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the proviso that (CH(R38 ))r

is bonded to E0 and Qb is bonded to lowest numbered substituent position of

each W3 ;

Y0 is Qb -Qsssr , wherein Qsssr is (CH(R38 ))r-W4 , r is an integer

selected from 1 through 3, and W is selected from the group consisting of 1 ,2-cyclobutyl, 1,2-cyclohexyl, 13-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 13-piperazinyl, 1,4-ρiperazinyl, 2,3-piperazinyl, 2,5-piperazinyl, 2,6-piρerazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 1,4-piperidinyl, 23-ρiperidinyl, 2,4-piperidinyl, 2,5-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-ρyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-2,3-pyranyl, 2H-2,4-pyranyl, 2H-2,5-pyranyl, 4H-2,3-pyranyl, 4H-2,4-ρyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the provisos that (CH(R38 ))r

is bonded to E0 and Qb is bonded to highest number substituent position of

4

each W ;

Y0 is Qb -Qssss , wherein Qssss is (CH(R38 ))r-W5 , r is an integer

selected from 1 through 3, and W5 is selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 13-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinoUnyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-

isoquinoUnyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Q is bonded to lowest number substituent position of each

W and that (CH(R38 ))r is bonded to E0;

Y0 is Qb -Qssssr , wherein Qssssr is (CH(R38 ))r-W 6 , r is an integer

selected from 1 through 3, and W is selected from the group consisting of 1,4-indenyl, 1 ,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3 ,4-indenyl, 3 ,5-indenyl, 3 ,6-indenyl, 3 ,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2r5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinoUnyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyI, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Q is bonded to highest number substituent position of each

W6 and that (CH(R38 ))r is bonded to E0.

3. The compound as recited in Claim 1 or a pharmaceutically acceptable salt thereof, wherein;

B is formula (V):


wherein D1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, no more than one of D1, D2, J1, J2 and K1 is O,

no more than one of D1, D2, J1, J2 and K1 is S, one of D1, D2, J1, J2 and K1

must be a covalent bond when two of D1, D2, J1, J2 and K1 are O and S, and

no more than four of D1, D2, J1, J2 and K1 are N;

R32 , R33 , R34 , R35 , and R36 are independently selected to be Qb ;

R9,R10,R11,R12,R13 ,R16,R17,R18,R19,R32,R33,R34,R35,and

R36 are independently selected from the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, trialkylphosphonium, dialkylsulfoniumalkyl, carboxy, heteroaralkylthio, heteroaralkoxy, cycloalkylamino, acylalkyl, acylalkoxy, aryloylalkoxy, heterocyclyloxy, aralkylaryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, perhaloaralkyl, aralkylsulfonyl, aralkylsulfonylalkyl, aralkylsulfinyl, aralkylsulfinylalkyl, halocycloalkyl, halocycloalkenyl, cycloalkylsulfinyl, cycloalkylsulfinylalkyl, cycloalkylsulfonyl,

cycloalkylsulfonylalkyl, heteroarylamino, N-heteroarylamino-N-alkylamino, heteroarylaminoalkyl, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, heteroaralkoxy, cycloalkoxy, cycloalkenyloxy,

cycloalkoxyalkyl, cycloalkylalkoxy, cycloalkenyloxyalkyl, cycloalkylenedioxy, halocycloalkoxy, halocycloalkoxyalkyl, halocycloalkenyloxy,

halocycloalkenyloxyalkyi, hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, arylamino, aralkylamino, arylthio, arylthioalkyl, heteroaralkoxyalkyl, alkylsulfinyl, alkylsulfinylalkyl,

arylsulfinylalkyl, arylsulfonylalkyl, heteroarylsulfinylalkyl,

heteroarylsulfonylalkyl, alkylsulfonyl, alkylsulfonylalkyl,

haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido,

alkylaminosulfonyl, amidosulfonyl, monoalkyl amidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl, arylsulfonamido, diarylamidosulfonyl, monoalkyl monoaryl amidosulfonyl, arylsulfinyl, arylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, heterocyclylsulfonyl, heterocyclylthio, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl, heteroaralkanoyl, haloalkanoyl, alkyl, alkenyl, alkynyl, alkenyloxy, alkenyloxyalky,

alkylenedioxy, haloalkylenedioxy, cycloalkyl, cycloalkylalkanoyl,

cycloalkenyl, lower cycloalkylalkyl, lower cycloalkenylalkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyaralkyl, hydroxyalkyl, aminoalkyl, hydoxyheteroaralkyl, haloalkoxyalkyl, aryl, aralkyl, aryloxy, aralkoxy, aryloxyalkyl, saturated heterocyclyl, partially saturated heterocyclyl, heteroaryl, heteroaryloxy, heteroaryloxyalkyl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido, alkylamidocarbonylamido, arylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboaralkoxy, carboxamido, carboxamidoalkyl, cyano, carbohaloalkoxy, phosphono, phosphonoalkyl, diaralkoxyphosphono, and diaralkoxyphosphonoalkyl ;

B is selected from the group consisting of C3-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl wherein each member of group B may be optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33 , R34, R35, and R35;

B is selected from the group consisting of C3-C10 cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partially saturated heterocyclyl, wherein each ring carbon may be optionally substituted with R33, a ring carbon other than the ring carbon at the point of attachment of B to A may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbon and nitrogen atoms adjacent to the carbon atom at the point of attachment may be optionally substituted with R9 or R13, a ring carbon or nitrogen atom adjacent to the R9 position and two atoms from the point of attachment may be substituted with

R10, a ring carbon or nitrogen atom adjacent to the R 13 position and two atoms

from the point of attachment may be substituted with R12, a ring carbon or

nitrogen atom three atoms from the point of attachment and adjacent to the R10

position may be substituted with R11, a ring carbon or nitrogen atom three

atoms from the point of attachment and adjacent to the R12 position may be

substituted with R33, and a ring carbon or nitrogen atom four atoms from the

point of attachment and adjacent to the R 11 and R33 positions may be

substituted with R34;

A is selected from the group consisting of single covalent bond, (W7)rr-(CH(R15))pa and (CH(R15))pa-(W7)rr wherein rr is an integer

selected from 0 through 1, pa is an integer selected from 0 through 6, and W7 is selected from the group consisting of O, S, C(O), C(S), C(O)S, C(S)O,

C(O)N(R7), C(S)N(R7), (R7)NC(O), (R7)NC(S), S(O), S(O)2, S(O)2N(R7),

(R7)NS(O)2, C(NR7)N(R7), (R7)NC(NR7), and N(R7);

R7 and R8 are independently selected from the group consisting of hydrido, hydroxy, alkyl, and alkoxyalkyl;

R14 , R15 , R37 , and R38 are independently selected from the group consisting of hydrido, hydroxy, halo, alkyl, alkoxyalkyl, haloalkyl, haloalkoxy, and haloalkoxyalkyl;

Ψ is selected from the group consisting of NR5 , O, C(O), C(S), S,

S(O), S(O)2, and CR39 R40 ;

R5 is selected from the group consisting of hydrido, alkyl, and alkoxy;

R39 and R40 are independently selected from the group consisting of hydrido, hydroxy, halo, hydroxyalkyl, alkyl, alkoxyalkyl, haloalkyl, haloalkoxy, and haloalkoxyalkyl;

R 1 is selected from the group consisting of hydrido, alkyl, alkenyl, haloalkyl, and alkoxyalkyl;

X0 and R2 are independently selected from the group consisting of Z0 -Q, hydrido, alkyl, alkenyl, and halo;

X0 and R2 are independently selected from the group consisting of amidino, guanidino, dialkylsulfonium, trialkylphosphonium,

dialkylsulfoniumalkyl, heteroarylamino, amino, nitro, alkylamino, arylamino, aralkylamino, alkanoyl, alkenoyl, aroyl, heteroaroyl, aralkanoyl,

heteroaralkanoyl, haloalkanoyl, hydroxyhaloalkyl, cyano, and phosphono;

Z0 is selected from the group consisting of covalent single bond, (CR41 R42 )q wherein q is an integer selected from 1 through 2, (CH(R41 ))g-

W0-(CH(R42))p wherein g and p are integers independently selected from 0 through 2 and W is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R41), (R41)NC(O), C(S)N(R41),

(R41 )NC(S), OC(O)N(R41), (R41)NC(O)O, SC(S)N(R41), (R41)NC(S)S,

SC(O)N(R41 ), (R41 )NC(O)S, OC(S)N(R41 ), (R41 )NC(S)O,

N(R42 )C(O)N(R41 ), (R41)NC(O)N(R42), N(R42)C(S)N(R41),

(R41)NC(S)N(R42 ), S(O), S(O)2, S(O)2N(R41 ), N(R41 )S(O)2, N(R41 ),

ON(R41), and (CH(R41))e-W2-(CH(R42))h wherein e and h are integers

independently selected from 0 through 2 and W2 is selected from the group

consisting of CR41 =CR42 , CR41R42 =C; vinylidene), and ethynylidene (C≡C;

1,2-ethynyl), with the provisos thatR41 and R42 are selected from other than halo and cyano when directly bonded to N and Z0 is directly bonded to the pyridone ring;

R41 and R42 are independently selected from the group consisting of hydrido, hydroxy, halo, cyano, aryloxy, hydroxyalkyl, acyl, aroyl, heteroaroyl, heteroaryloxyalkyl, alkoxy, alkyl, aryl, aralkyl, aryloxyalkyl,

aralkoxyalkylalkoxy, alkoxyalkyl, heteroaryloxyalkyl, cycloalkyl,

cycloalkylalkyl, cycloalkylalkenyl, cycloalkenyl, cycloalkenylalkyl, haloalkyl, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxy, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxy, halocycloalkoxyalkyl,

halocycloalkenyloxyalkyi, saturated heterocyclyl, partially saturated

heterocyclyl, heteroaryl, and heteroaralkyl;

Q is formula (II):


wherein D1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covaien, bond, no more than one of D1, D2, J1, J2 and K1 is O,

no more than one of D1, D2, J1, J2 and K1 is S, one of D1, D2, J1, J2 and K1

mustbe a covalentbond when two of D1, D2, J1, J2 and K1 are O and S, and

no more than four of D1, D2, J1, J2 and K1 are N, with the proviso that R9 , R10 , R11 , R12 , and R13 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

Q is selected from the group consisting of alkyl, alkoxy, alkylamino, alkylthio, haloalkylthio, saturated heterocyclyl, alkyl, partially saturated heterocyclyl, acyl, aroyl, heteroaroyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, cycloalkylalkenyl, haloalkyl, haloalkoxy, haloalkenyl, halocycloalkyl, halocycloalkenyl, haloalkoxyalkyl, haloalkenyloxyalkyl, halocycloalkoxyalkyl, and halocycloalkenyloxyalkyi;

K is (CR4a R4b )n wherein n is the integer 1;

R4a and R4b are independently selected from the group consisting of halo, hydrido, hydroxy, hydroxyalkyl, alkyl, alkoxyalkyl, and haloalkyl;

E0 is E 1 , when K is (CR4a R4b )n, wherein E1 is selected from the group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S), OC(O)N(R7),

(R7)NC(O)O, SC(S)N(R7), (R7)NC(S)S, SC(O)N(R7), (R7)NC(O)S,

OC(S)N(R7), (R7)NC(S)O, N(R8)C(O)N(R7), (R7)NC(O)N(R8),

N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(0), S(O)2, S(O)2N(R7), N(R7)S(O)2,

S(O)2N(R7 )C(O), C(O)N(R7 )S(O)2, N(R7 ), ON(R7 ), CR4a =CR4b,

ethynylidene (C≡C; 1,2-ethynyl), and C=CR4aR4b;

K is (CH(R14 ))j-T wherein j is selected from a integer from 0 through

1 and T is selected from the group consisting of single covalent bond, O, S, and

N(R7 ) with the proviso that (CH(R14 )): is bonded to the pyridone ring;

E0 is E2 , when K is (CH(R14 ))j-T, wherein E is selected from the group consisting of a covalent single bond, C(O), C(S), C(0)O, C(S)O, C(O)S,

C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S), (R7)NC(O)O,

(R7)NC(S)S, (R7)NC(O)S, (R7)NC(S)O, N(R8)C(O)N(R7),

(R7)NC(0)N(R8), N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2,

S(O)2N(R7), N(R7)S(O)2, S(O)2N(H)C(O), C(O)N(H)S(O)2, and N(R7);

K is G-(CH(R 15 )) k wherein k is the integer 1 and G is selected from

the group consisting of O, S, and N(R7 );

E0 is E3 , when K is G-(CH(R 15 )) k, wherein E3 is selected from the group consisting of a covalent single bond, O, S, C(O), C(S), C(O)O, C(S)O,

C(O)S, C(S)S, C(O)N(R7), (R7)NC(O), C(S)N(R7), (R7)NC(S),

OC(O)N(R7), (R7)NC(O)O, SC(S)N(R7), (R7)NC(S)S, SC(O)N(R7),

(R7)NC(0)S, OC(S)N(R7), (R7)NC(S)O, N(R8)C(O)N(R7),

(R7)NC(0)N(R8), N(R8)C(S)N(R7), (R7)NC(S)N(R8), S(O), S(O)2,

S(O)2N(R7 ), N(R7 )S(O)2, N(R7 ), ON(R7 ), CR4a =CR4b , ethynylidene (C≡C;

1,2-ethynyl), and C=CR4a R4b ;

Y0 is formula (IV):


wherein D , D , J , and J are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more

2

than one is a covalent bond, K is independently selected from the group consisting of C and N , no more than one of D5, D6, J5, and J6 is O, no more

than one of D5, D6, J5, and J6 is S, one of D5, D6, J5, and J6 must be a

covalent bond when two of D5, D6, J5, and J6 are O and S, no more than three

of D5, D6, J5, and J6 are N when K2 is N+ , and no more than four of D5 , D6 ,

J5 , and J6 are N when K2 is carbon with the provisos that R16, R17, R18, and

R19 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

Qb is selected from the group consisting of NR20 R21,+ NR20 R21 R22, oxy, alkyl, alkylaminoalkyl, aminoalkyl, dialkylsulfoniumalkyl, and acylamino wherein R20 , R21 , and R22 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl with the provisos that no more than one of R20,

R21 , and R22 is hydroxy, alkoxy, alkylamino, amino, or dialkylamino and that

R20 , R21 , and R22 must be other than be hydroxy, alkoxy, alkylamino, ammo,

and dialkylamino when K2 is N+ ;

Qb is selected from the group consisting of N(R26)SO2N(R23)(R24),

N(R26)C(O)OR5 , N(R26)C(O)SR5 , N(R26)C(S)OR5 and N(R26)C(S)SR5

with the proviso that no more than one of R23 , R24 , and R26 is hydroxy, alkoxy, alkylamino, amino, or dialkylamino when two of the group consisting of R23, R24, and R26 are bonded to the same atom;

Qb is selected brom the group consisting of dialkylsulfonium,

trialkylphosphonium, C(NR25)NR23R24, N(R26)C(NR25)N(R23)(R24),

N(R26)C(O)N(R23)(R24), N(R26)C(S)N(R23)(R24), C(NR25)OR5,

C(0)N(R26)C(NR25)N(R23)(R24), C(S)N(R26)C(NR2:5)N(R23)(R24),

N(R26)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)SO2N(R23)(R24),

C(NR25 )SR5, C(O)NR23 R24 , and C(O)NR23 R24 with the provisos that no

more than one of R23 , R24 , and R26 is hydroxy, alkoxy, alkylamino, amino, or

dialkylamino when two of the group consisting of R23, R24, and R26 are

bonded to the same atom and that said Qb group is bonded directly to a carbon atom;

R23, R24, R25, and R, 26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl;

Qs is selected from the group consisting of a single covalent bond,

(CR37 R38 )b,-(W0 )az wherein az is an integer selected from 0 through 1 , b is an integer selected from 1 through 2, and W is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S, C(O)N(R14),

(R14)NC(O), C(S)N(R14), (R14)NC(S), OC(O)N(R14), SC(S)N(R 14),

SC(O)N(R 14), OC(S)N(R14), N(R15)C(O)N(R 14), (R14)NC(O)N(R 15),

N(R 15)C(S)N(R 14), (R 14)NC(S)N(R 15), S(O), S(O)2, S(O)2N(R 14),

N(R14)S(O)2, N(R14), ON(R14), (CH(R14))c-W1-(CH(R15))d wherein c

and d are integers independently selected from 1 through 2, and W is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,

C(O)N(R14),(R14)NC(O), C(S)N(R14),(R14)NC(S), OC(O)N(R14),

(R14)NC(O)O, SC(S)N(R14),(R14)NC(S)S, SC(O)N(R14),(R14)NC(O)S,

OC(S)N(R14),(R14)NC(S)O,N(R15)C(O)N(R14),(R14)NC(O)N(R15),

N(R15)C(S)N(R14),(R14)NC(S)N(R15), S(O), S(O)2, S(0)2N(R14),

N(R14)S(O)2,N(R14),ON(R14),and(CH(R14))e-W2^CH(R15))hwherein e and h are integers independently selected from 0 through 2 and W^^ is

selected from the group consisting of CR4a =CR4b , ethynylidene (C≡C; 1,2-

ethynyl), and C=CR4a R4b with the provisos that R14 and R15 are selected from other than halo and cyano when directly bonded to N and that

(CR37 R38)b, (CH(R14))c, and (CH(R 14))e are bonded to E0;

Y0 is Qb -Qss wherein Qss is selected from the group consisting of (CR37 R38)f wherein f is an integer selected from 1 through 4, (CH(R14))c- W 1 -(CH(R15 ))j wherein c and d are integers independently selected from 1

through 2, and W1 is selected from the group consisting of W1 is selected from the group consisting of O, S, C(O), C(S), C(O)O, C(S)O, C(O)S, C(S)S,

C(O)N(R 14), (R 14)NC(O), C(S)N(R14), (R14)NC(S), OC(O)N(R14),

(R14)NC(O)O, SC(S)N(R14), (R14)NC(S)S, SC(O)N(R14), (R14)NC(O)S,

OC(S)N(R14), (R14)NC(S)O, N(R15)C(O)N(R14), (R14)NC(O)N(R15),

N(R 15)C(S)N(R 14), (R14)NC(S)N(R15), S(O), S(O)2, S(O)2N(R14),

N(R14)S(O)2, N(R14), ON(R14), and (CH(R14))e-W2-(CH(R15))h wherein e and h are integers independently selected from 0 through 2 and W2 is

selected from the group consisting of CR4a =CR4b , ethynylidene (C≡C; 1,2-

ethynyl), and C=CR4a R4b with the provisos that R14 and R14 are selected from other than halo when directly bonded to N and that (CR37 R38)f ,

(CH(R15))C, and (CH(R15))e are bonded to E°;

Y0 is Qb -Qsss wherein Qsss is (CH(R38))r-W3, r is an integer selected

from 1 through 2, and W3 is selected from the group consisting of 1,1-cyclopropyl, 1,2-cyclopropyl, 1,1-cyclobutyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 13-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 23-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl, 23-piperazinyl, 2,5-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 13-piperidinyl, 1,4-piperidinyl, 23-ρiρeridinyl, 2,4-piperidinyl, 2,Spiperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 3,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-23-pyranyl, 2H-2,4-ρyranyl, 2H-2,5-ρyranyl, 4H-2,3-pyranyl, 4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-pyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 2,3-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the proviso that (CH(R38))r

is bonded to E0 and Qb is bonded to lowest numbered substituent position of

each W3;

Y0 is Qb -Qsssr wherein Qsssr is (CH(R38))r- W4 , r is an integer

selected from 1 through 2, and W4 is selected from the group consisting of 1,2-cyclobutyl, 1 ,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,5-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 1,4-piperazinyl, 2,3-piperazinyl, 2,Spiperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 13-piperidinyl, 1,4-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,5-piperidinyl, 2,6-piperidinyl, 3,4-piρeridinyl, 3 ,5-piperidinyl, 3,6-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-ρyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2H-23-pyranyl, 2H-2,4-ρyranyl, 2H-2,5-ρyranyl, 4H-2,3-pyranyl,

4H-2,4-pyranyl, 4H-2,5-pyranyl, 2H-pyran-2-one-3,4-yl, 2H-ρyran-2-one-4,5-yl, 4H-pyran-4-one-2,3-yl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, 3,4-tetrahydrofuranyl, 23-tetrahydropyranyl, 2,4-tetrahydropyranyl, 2,5-tetrahydropyranyl, 2,6-tetrahydropyranyl, 3,4-tetrahydropyranyl, and 3,5-tetrahydropyranyl with the provisos that (CH(R38))r

is bonded to E0 and Qb is bonded to highest number substituent position of

each W4 ;

Y0 is Qb -Qssss wherein Qssss is (CH(R38 ))r-W5 , r is an integer

selected from 1 through 2, and W5 is selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinohnyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,S isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,Sisoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinoUnyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnoϊinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Qb is bonded to lowest number substituent position of each

W5 and that (CH(R38)). is bonded to E0

Y0 is Qb -Qssssr wherein Qssssr is (CH(R38))r-W6, r is an integer

selected from 1 through 2, and W is selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyI, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,Snaphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyI, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,S quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinoUnyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Q is bonded to highest number substituent position of each

W6 and that (CH(R38 ))r is bonded tdo E0.

4. The compound as recited in Claim 3 or a pharmaceutically acceptable salt thereof, wherein;

B is formula (V):


wherein D1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, no more than one of D1, D2, J1, J2 and K1 is O,

no more than one of D1, D2, J1, J2 and K1 is S, one of D1, D2, J1, J2 and K1

mustbe a covalentbond whentwo of D1, D2, J1, J2 and K1 are O and S, and

no more than four of D1, D2, J1, J2 and K1 are N;

R32, R33, R34, R35, and R36 are independently selected to be Qb ;

R9, R10, R11, R12, R 12, R32, R33, R34, R35, and R36 are

independently selected from the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, carboxy, haloalkylthio, alkanoyloxy, alkoxy, alkoxyalkyl, haloalkoxylalkyl, hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylthioalkyl, alkylsulfinyl, alkylsulfinylalkyl, alkylsulfonyl, alkylsulfonylalkyl, haloalkylsulfmylalkyl, haloalkylsulfonylalkyl, alkylsulfonamido, alkylaminosulfonyl, amidosulfonyl, monoalkyl

amidosulfonyl, dialkyl amidosulfonyl, monoarylamidosulfonyl, alkanoyl, alkenoyl, haloalkanoyl, alkyl, alkenyl, alkenyloxy, alkenyloxyalky, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboxyalkyl, carboalkoxy, alkoxycarboxamido,

alkylamidocarbonylamido, carboalkoxyalkyl, carboalkoxyalkenyl, carboxamido, carboxamidoalkyl, and cyano;

B is selected from the group consisting of C3-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl wherein each member of group B may be optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36;

B is selected from the group consisting of C3-C10 cycloalkyl, CSC10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partially saturated heterocyclyl, wherein each ring carbon may be optionally substituted with R33, a ring carbon other than the ring carbon at the point of attachment of B to A may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbon and nitrogen atoms adjacent to the carbon atom at the point of attachment may be optionally substituted with R9 or R13 , a ring carbon or nitrogen atom adjacent to the R9 position and two atoms from the point of attachment may be substituted with

R10, a ring carbon or nitrogen atom adjacent to the R13 position and two atoms

from the point of attachment may be substituted with R12, a ring carbon or

nitrogen atom three atoms from the point of attachment and adjacent to the R10

position may be substituted with R 11 , a ring carbon or nitrogen atom three

atoms from the point of attachment and adjacent to the R12 position may be

substituted with R33, and a ring carbon or nitrogen atom four atoms from the

point of attachment and adjacent to the R11 and R33 positions may be

substituted with R34;

A is selected from the group consisting of single covalent bond,

(W7 )rr-(CH(R15))pa and (CH(R15))pa-(W7)rr wherein rr is an integer

7 selected from 0 through 1, pa is an integer selected from 0 through 6, and W is selected from the group consisting of O, S, C(O), C(S), C(O)S, C(S)O,

C(O)N(R7), C(S)N(R7), (R7)NC(O), (R7)NC(S), S(O), S(O)2, S(O)2N(R7),

(R7)NS(O)2, C(NR7)N(R7), (R7)NC(NR7), and N(R7) with the proviso that no more than one of the group consisting of rr and pa is 0 at the same time;

R7 and R8 are independently selected from the group consisting of hydrido, hydroxy, alkyl, and alkoxyalkyl;

R15 is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;

Ψ is NH;

X0 is hydrido;

R 1 is selected from the group consisting of hydrido, alkyl, and haloalkyl;

R 2 is selected from the group consisting of Z0 -Q, hydrido, alkyl, alkenyl, and halo;

Z0 is a covalent single bond;

Q is formula (II):


wherein D1, D2, J1, J2 and K1 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, no more than one of D1, D2, J1, J2 and K1 is O,

no more than one of D1, D2, J1, J2 and K1 is S, one of D1, D2, J1, J2 and K1

mustbe a covalentbond when two of D1, D2, J1, J2 and K1 are O and S, and

no more than four of D1, D2, J1, J2 and K1 are N, with the proviso that R9 , R10, R1 1, R12, and R13 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

K is CR4a R4b ;

R4a and R4b are independently selected from the group consisting of halo, hydrido, hydroxy, alkyl, and haloalkyl;

E0 is E1 , when K is CR4a R4b , wherein E1 is selected from the group consisting of a covalent single bond, (O)N(H), (H)NC(O), C(S)N()),

(H)NC(S), S(O)2N(H), N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

K is (CH(R14))j-T wherein j is selected from an integer from 0 through

1 and T is selected from the group consisting of single covalent bond and

N(R7) with the proviso that (CH(R 14))j is bonded to the pyridone ring;

R14 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

E0 is E2 , when K is (CH(R 14))j-T, wherein E is selected from the

group consisting of C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S), S(O)2N(H),

N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

Y0 is formula (IV):


wherein D5, D6, J5, and J6 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K2 is independently selected from the group

consisting of C and N+ , no more than one of D5, D6, J5, and J6 is O, no more

than one of D5, D6, J5, and J6 is S, one of D5, D6, J5, and J6 must be a

covalent bond when two of D5, D6, J5, and J6 are O and S, no more than three

of D5, D6, J5, and J6 are N when K2 is N+, and no more than four of D5, D6,

J5, and J6 are N whenK2 is carbon with the provisos that R16, R17, R18, and

R19 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of nitrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R 16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, carboxy, haloalkylthio, alkoxy, hydroxy, amino, thio, nitro, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, alkenoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyalkyl, aminoalkyl,

haloalkoxyalkyl, carboalkoxy, carboalkoxyalkyl, and cyano;

Qb is selected from the group consisting of NR20 R21 ,+ NR20 R21 R22, oxy, alkyl, alkylaminoalkyl, aminoalkyl, dialkylsulfoniumalkyl, and acylamino wherein R20, R21, and R22 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl with the provisos that no more than one of R20,

R21, and R22 is hydroxy, alkoxy, alkylamino, amino, or dialkylamino and that

R20, R21, and R22 must be other than be hydroxy, alkoxy, alkylamino, amino,

or dialkylamino when K2 is N+;

Qb is N(R26)SO2N(R23)(R24) with the proviso that no more than one

of R23, R24, and R26 is hydroxy, alkoxy, alkylamino, ammo, or dialkylamino

when two of the group consisting of R23, R24, and R26 are bonded to the same atom;

R23 , R24 , R25 , and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl;

Q is selected from the group consisting of dialkylsulfonium,

trialkylphosphonium, C(NR25)NR23 R24 , N(R26)C(NR25)N(R23 )(R24),

N(R26)C(O)N(R23)(R24), N(R26)C(S)N(R23)(R24),

C(O)N(R26)C(NR25)N(R23)(R24), C(S)N(R26)C(NR25)N(R23)(R24),

N(R26)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)SO2N(R23)(R24),

C(O)NR23 R24 , and C(O)NR23 R24 with the provisos that no more than one of

R23, R24 , and R26 is hydroxy, alkoxy, alkylamino, ammo, or dialkylamino when

two of the group consisting of R23, R24, and R26 are bonded to the same atom and

that said Qb group is bonded directly to a carbon atom;

Qs is selected from the group consisting of a single covalent bond and

(CR37 R38 )b-(W0 )az wherein az is an integer selected from 0 through 1, b is an integer selected from 1 through 2, and W is selected from the group consisting of O, S, C(O), S(O)2, N(R14 ), and ON(R 14 ) with the proviso that R 14 is

selected from other than halo when directly bonded to N and that (CR37 R38)b is bonded io E0;

R37 and R38 are independently selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

Y0 is Qb -Qssss wherein Qssss is (CH(R38))r-W5, r is an integer

selected from 1 through 2, and W5 is selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyI, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinohnyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinoUnyl, 3,4-cinnoUnyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Q is bonded to lowest number substituent position of each

W5 and that (CH(R38))r is bonded to E0;

Y0 is Qb -Qssssr wherein Qssssr is (CH(R3 ))r- WW, r is an integer

selected from 1 through 2, and W is selected from the group consisting of 1 ,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5- indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyI, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinoIinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,Scinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl with the proviso that Q is bonded to highest number substituent position of each

W6 and that (CH(R38 ))r is bonded to E0.

5. The compound as recited in Claim 4 having the Formula I-S:


or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyπolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 1,2,4-triazol-3-yl, 1,2,4~triazol-5-yI, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 13,4-oxadiazol-3-yl, 1,3,4-oxadiazol-5-yl, 3-isothiazolyl, 5-isothiazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, 1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl, 1,2,4-triazin-6-yl, and 1,23-triazin-4-yl, wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R32, the other carbon adjacent

to the carbon at the point of attachment may be substituted by R36, a carbon

adjacent to R32 and two atoms from the carbon at the point of attachment may

be substituted by R33, a carbon adjacent to R36 and two atoms from the carbon

at the point of attachment may be substituted by R35, and any carbon adjacent

to both R33 and R35 may be substituted by R34 ;

R32, R33, R34, R35, and R36 ar3 independently selected from the group consisting of hydrido, amidino, guanidino, dimethylsulfonium, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, thio, nitro, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio,

isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, 2,2,2-trifϊuoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl, methoxycarbonyl,

ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Qb;

B is selected from the group consisting of 1-propenyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, 2-butynyl, sec-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 1-methyl-2-butenyl, 1-methyl-3-butenyl, 1-methyl-2-butynyl, 3-pentyl, 1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 1-propyl-2-proρenyl, 1-ethyl-2-butynyl, 1-heptyl, 2-heptenyl, 3-heρtenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-5-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl, 1-butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 1-octyl, 2-octenyl, 3-octenyl, 4-octenyl, 5-octenyl, 6-octenyl, 7-octenyl, 2-octynyl, 3-octynyl, 4-octynyl, 5-octynyl, 6-octynyl, 2-octyl, 1-methyl-2-heptenyl, 1-methyl-3-heptenyl, 1-methyl-4-heptenyl, 1-methyl-5-heptenyl, 1-methyl-6-heptenyl, 1-methyl-2-heptynyl, 1-methyl-3-heptynyl, 1-methyl-4-heptenyl, 1-methyl-5-heptenyl, 1-methyl-6-heptenyl, 1-methyl-2-heptenyl, 1-methyl-3-heptynyl, 1-methyl-4-heptynyl, 1-methyl-5-heptynyl, 3-octyl, 1-ethyl-2-hexenyl, 1-ethyl-3-hexenyl, 1-ethyl-4-hexenyl, 1-ethyl-2-hexynyl, 1-ethyl-3-hexynyl, 1-ethyl-4-hexynyl, 1-ethyl-5-hexenyl, 1-pentyl-2-propenyl, 4-octyl, 1-propyl-2-pentenyl, 1-propyl-3-pentenyl, 1-propyl-4-pentenyl, 1-butyl-2-butenyl, 1-propyl-2-ρentynyl, 1-ρropyl-3-ρentynyl, 1-butyl-2-butynyl, 1-butyl-3-butenyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein each member of group B may be optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33 , R34, R35, and R36;

B is selected from the group consisting of cyclopropyl, cyclobutyl, oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, thiaetan-2-yl, thiaetan-3-yl, cyclopentyl, cycIopent-2-enyl, cyclopent-3-enyl, cyclohexyl, 4-methylcyclohexyl, 4-chloro-3-ethylphenoxycyclohexyl, 3-trifluoromethoxyphenoxycyclohexyl, 3-trifluoromethylcyclohexyl, 4-

trifluoromethylcyclohexyl, 3,Sbis-trifluoromethylcyclohexyl, adamantyl, 3-trifluoromethyladamantyl, norbomyl, 3-trifluoromethylnorbornyl, norbomenyl, 7-oxabicyclo[2.2.1]heptan-2-yl, bicyclo[3.1.0]hexan-6-yl, cyclohex-2-enyl, cyclohex-3-enyl, cycloheptyl, cyclohept-2-enyl, cyclohept-3-enyl, cyclooctyl, cyclooct-2-enyl, cyclooct-3-enyϊ, cyclooct-4-enyl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 2H-2-pyranyl, 2H-3-pyranyl, 2H-4-pyranyl, 4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 2H-pyran-2-one-3-yl, 2H-pyran-2-one-4-yl, 2H-pyran-2-one-5-yl, 4H-pyran-4-one-2-yl, 4H-pyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein each ring carbon may be optionally substituted with

R33, a ring carbon and nitrogen atoms adjacent to the carbon atom at the point

of attachment may be optionally substituted with R9 or R13, a ring carbon or

nitrogen atom adjacent to the R9 position and two atoms from the point of

attachment may be substituted with R10, and a ring carbon or nitrogen atom

adjacent to the R13 position and two atoms from the point of attachment may

be substituted with R12;

R9 , R10 , R1 1 , R12 , and R13 are independently selected from the group consisting of amidino, guanidino, dimethylsulfonium, methylethylsulfonium, carboxy, methoxy, ethoxy, isopropoxy, propoxy, butoxy, hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-dimethylamino, N-methylamino, N-ethylamino, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl, butanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, 2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl , carboxymethyl, 2-carboxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

A is selected from the group consisting of single covalent bond, O, C(O), CH2, CH3CH, CF3CH, CH3CC(O), CF3CC(O), C(O)CCH3,

C(O)CCF3, CH2C(O), (O)CCH2, CH2CH2, CH2CH2CH2, CH3CCH2,

CF3CCH2, CH3CC(O)CH2, CF3CC(O)CH2, CH2C(O)CCH3,

CH2C(O)CCF3, CH2CH2C(O), and CH2(O)CCH2;

R1 is selected from the group consisting of hydndo, methyl, ethyl, propyl, butyl, 2,2,2-trifluoroethyl, and 2,2,333-pentafluoropropyl;

R 2 is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl,

2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 1,2,4-triazol-3-yl, 1,2,4-triazol-Syl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 1,3,4-oxadiazol-3-yl, 1,3,4-oxadiazol-5-yl, 3-isothiazolyl, 5-isothiazolyl, 2-oxazoIyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, 1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl, 1,2,4-triazin-6-yl, and 1,2,3-triazin-4-yl, wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R9, the other carbon adjacent

to the carbon at the point of attachment may be substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment may be

substituted by R10 , a carbon adjacent to R13 and two atoms from the carbon at

the point of attachment may be substituted by R 12, and any carbon adjacent to

both R10 and R 12 may be substituted by R1 1;

K is CR4a R4b wherein R4a and R4b are independently selected from the group consisting of chloro, fluoro, and hydrido;

E0 is E1 , when K is CR4a R4b, wherein E is selected from the group

consisting of a covalent single bond, C(O)N(H), (H)NC(O), S(O)2N(H),

N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

K is selected from the group consisting of N(H) and CH2N(H);

E0 is E2 , when K is N(H) and CH2N(H), wherein E2 is selected from the group consisting of C(O)N(H), (H)NC(O), S(O)2N(H), N(H)S(O)2,

S(O)2N(H)C(O), and C(O)N(H)S(O)2;

Y0 is selected from the group of formulas consisting of:


R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, dimethylsuϊfonium, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, thio, nitro, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio,

isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifiuoroethyl, 2,2,333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, 2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl, carboxymethyl, methoxycarbonyl,

ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

Qb is selected, when bonded to a carbon, from the group consisting of

NR20 R21, + NR20 R21 R22, dimethylsulfonium, methylethylsulfonium,

diethylsulfonium, trimethylphosphonium, C(NR25)NR23 R24,

N(R26)C(NR25)N(R23)(R24), C(O)N(R26)C(NR25)N(R23)(R24),

N(R26)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)SO2N(R23)(R24),

C(O)NR23 R24, and C(O)NR23 R24 with the provisos that no more than one of

R20, R21 , and R22 is hydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or amino and that no more than one of

R23, R24, and R26 is hydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or amino when two of the group consisting of R23 , R24 , and R26 are bonded to the same atom and that said Qb

group is bonded directly to a carbon atom;

R20, R21 , R22, R23, R24, R25, andR26 are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, hydroxy, methoxy, ethoxy, isopropoxy, propoxy, 2-aminoethyl, 2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino, N-(2-hydroxyethyl)-N-(2-aminoethyl)amino, N-methylamino, N-ethylamino, N,N-dimethylamino, N,N-diethylamino, and N,N,N-trimethylamino;

Qb is selected, when bonded to a nitrogen, from the group consisting of oxy, methyl, ethyl, 2-aminoethyl, 2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylammo)ethyl, N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino, amino, hydroxylamino, N-methoxyamino, N-methylamino, N,N-dimethylamino, and N,N,N-trimethylamino;

Qs is selected from the group consisting of a single covalent bond, CH2,

CH3CH, CF2, CF3CH, CH2O, CH3C(H)O, CF3C(H)O, CH2S, CH3C(H)S,

CF3C(H)S, CH2C(O), CH3C(H)C(O), CF3C(H)C(O), and CF2C(O) with the proviso that Qs is bonded to E0 through a carbon atom.

6. The compound as recited in Claim 1 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of aryl and heteroaryl wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R32, the ,ther carbon adjacent to the carbon at the point of attachment may be substituted by R36, a carbon adjacent to R32 and two atoms from the carbon at

the point of attachment may be substituted by R33 , a carbon adjacent to R36

and two atoms from the carbon at the point of attachment may be substituted by

R35 , and any carbon adjacent to both R33 and R35 may be substituted by R34 ;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, carboalkoxy, carboxamido, cyano, and

Qb;

B is selected from the group consisting of C3-C8 alkyl, C3-C8 alkenyl, C3-C8 haloalkyl, and C3-C8 haloalkenyl wherein each member of group B may be optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of

R32, R33, R34, R35, and R36;

B is selected from the group consisting of C3-C10 cycloalkyl, C5-C10 cycloalkenyl, C4-C9 saturated heterocyclyl, and C4-C9 partially saturated heterocyclyl, wherein each ring carbon may be optionally substituted with R33, a ring carbon other than the ring carbon at the point of attachment of B to A may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbon and nitrogen atoms adjacent to the carbon atom at the point of attachment may be optionally substituted with R9 or R13, a ring carbon or nitrogen atom adjacent to the R9 position and two atoms from the point of attachment may be substituted with

R10, a ring carbon or nitrogen atom adjacent to the R13 position and two atoms

from the point of attachment may be substituted with R12, a ring carbon or

nitrogen atom three atoms from the point of attachment and adjacent to the R10 position may be substituted with R 11, a ring carbon or nitrogen atom three

atoms from the point of attachment and adjacent to the R12 position may be

substituted with R33, and a ring carbon or nitrogen atom four atoms from the

point of attachment and adjacent to the R11 and R33 positions may be

substituted with R34;

R9 , R10 , R11 , R12 , and R 13 are independently selected irom the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, thio, nitro, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, carboalkoxy, carboxamido, and cyano;

A is selected from the group consisting of single covalent bond,

(W7)rr-(CH(R15))pa and (CH(R15))pa-(W7)rr wherein rr is an integer

selected from 0 through 1, pa is an integer selected from 0 through 6, and W7

is selected from the group consisting of O, S, and C(O) with the proviso that no more than one of the group consisting of rr and pa is the integer 0 at the same time;

R 15 is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;

Ψ is NH;

X0 is hydrido;

R1 is selected from the group consisting of hydrido, alkyl, and haloalkyl;

R2 is Q, wherein Q is selected from the group consisting of aryl and heteroaryl wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R9 , the other carbon adjacent to the carbon at the point of

attachment may be substituted by R13, a carbon adjacent to R9 and two atoms

from the carbon at the point of attachment may be substituted by R10, a carbon

adjacent to R13 and two atoms from the carbon at the point of attachment may

be substituted by R12, and any carbon adjacent to both R 10 and R12 may be

substituted by R11;

K is CR4a R4b wherein R4a and R4b are independently selected from the group consisting of halo and hydrido;

E0 is E 1 , when K is CR4a R4b , wherein E1 is selected from the group

consisting of a covalent single bond, C(0)N(H), (H)NC(O), S(O)2N(H),

N(H)S(0)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

K is (CH(R14 ))j-T wherein j is selected from an integer from 0 through

1 and T is selected from the group consisting of single covalent bond and

N(R7) with the proviso that (CH(R14))j is bonded to the pyridone ring;

R7 is selected from the group consisting of hydrido, hydroxy, alkyl, and alkoxyalkyl;

R14 is selected from the group consisting of hydrido and halo;

E0 is E2 , when K is (CH(R 14))j-T, wherein E is selected from the

group consisting of C(O)N(H), (H)NC(O), S(O)2N(H), N(H)S(O)2,

S(O)2N(H)C(O), and C(O)N(H)S(O)2;

Y0 is formula (IV):


wherein D5, D6, J5, and J6 are independently selected from the group consisting of C, N, O, S and a covalent bond with the provisos that no more than one is a covalent bond, K2 is independently selected from the group

consisting of C and N , no more than one of D5, D6, J5, and J6 is O, no more

than one of D5, D6, J5, and J6 is S, one of D5, D6, J5, and J6 must be a

covalent bond when two of D5, D6, J5, and J6 are O and S, no more than three

of D5, D6, J5, and J6 are N when K2 is N+ , and no more than four of D5 , D6 ,

J5 , and J6 are N when K2 is carbon with the provisos that R16 , R14 , R18 , and

R19 are each independently selected to maintain the tetravalent nature of carbon, trivalent nature of mtrogen, the divalent nature of sulfur, and the divalent nature of oxygen;

R16, R 17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, dialkylsulfonium, carboxy, haloalkylthio, alkoxy, hydroxy, amino, thio, nitro, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, alkenoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyalkyl, aminoalkyl,

haloalkoxyalkyl, carboalkoxy, carboalkoxyalkyl, and cyano;

Qb is selected from the group consisting of NR20 R21 ,+ NR20 R21 R22 , oxy, alkyl, alkylaminoalkyl, aminoalkyl, dialkylsulfoniumalkyl, and acylamino wherein R20 , R21 , and R22 are independently selected from the group

consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl with the provisos that no more than one of R20,

R21, and R22 is hydroxy, alkoxy, alkylamino, ammo, or dialkylamino and that

R20 , R21 , and R22 must be other than be hydroxy, alkoxy, alkylamino, amino,

or dialkylamino when K2 is N+ ;

Qb is selected from the group consisting of dialkylsulfonium,

trialkylphosphonium, C(NR25)NR23R24, N(R26)C(NR25)N(R23)(R24),

C(O)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)C(NR25)N(R23)(R24),

N(R26 )N(R26 )SO2N(R23 )(R24 ), C(O)NR23 R24 , and C(O)NR23 R24 with

the provisos that no more than one of R23 , R24 , and R26 is hydroxy, alkoxy,

alkylamino, amino, or dialkylamino when two of the group consisting of R23 ,

R24 , and R26 are bonded to the same atom and that said Qb group is bonded directly to a carbon atom;

R23 , R24 , R25 , and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, alkoxy, alkylamino, dialkylamino, aminoalkyl, and hydroxyalkyl;

Qs is selected from the group consisting of a single covalent bond and

(CR37 R38 )b-(W0)az wherein az is an integer selected from 0 through 1, b is the integer 1, and W is selected from the group consisting of O, S, and C(O) with the proviso that (CR37 R38 )b is bonded to E ;

R37 and R38 are independently selected from the group consisting of hydrido, halo, alkyl, and haloalkyl.

7. The compound as recited in Claim 6 having the Formula I-MPS:


or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-ρyrazinyl, 2-pyrimidinyl, 4-ρyrimidinyl, 5-ρyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R32 , the other carbon adjacent to

the carbon at the point of attachment may be substituted by R36 , a carbon

adjacent to R32 and two atoms from the carbon at the point of attachment may

be substituted by R33, a carbon adjacent to R36 and two atoms from the carbon

at the point of attachment may be substituted by R35, and any carbon adjacent

to both R33 and R35 may be substituted by R34;

R32, R33, R34, R35, and R36 a3e independently selected from the group consisting of hydrido, amidino, guanidino, dimethylsulfonium, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, thio, nitro, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio,

trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, NJSf-dimethylamidosulfonyl, acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, 2,2,2-trifluoro-1- trifluoromethyl- 1 -hydroxyethyl, carboxymethyl, methoxycarbonyl,

ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Qb ;

B is selected from the group consisting of 1-propenyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, sec-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentyl, 1-methyl-2-butenyl, 1-methyl-3-butenyl, 3-pentyl, 1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl, 3-methylbutyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, 2,2-difluoropropyl, 2-trifluoromethyl-333-trifluoropropyl, 1,1,1,2,2,2-hexafluoropropyl, 3,3,3-trifluoroprop-1-yl, and 3,33-trifluoroprop-2-yl, wherein each member of group B may be optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36;

B is selected from the group consisting of cyclopropyl, cyclobutyl, oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, thiaetan-2-yl, thiaetan-3-yl, wherein each ring carbon may be optionally substituted with R33, a ring carbon and nitrogen atoms adjacent to the carbon atom at the point of attachment may be optionally substituted with R9 or R13, a ring carbon or

nitrogen atom adjacent to the R9 position and two atoms from the point of

attachment may be substituted with R10, and a ring carbon or nitrogen atom

adjacent to the R13 position and two atoms from the point of attachment may

be substituted with R12;

R9 , R10 , R11 , R12 , and R13 are independently selected from the group consisting of amidino, guanidino, dimethylsulfonium, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro- 1-hydroxyethyl, 2,2,2-trifluoro- 1- trifluoromethyl-1-hydroxyethyl, carboxymethyl, methoxycarbonyl,

ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

A is selected from the group consisting of single covalent bond, O, C(O), CH2, CH3CH, CF3CH, CH3CC(O), CF3CC(O), CC(O)CCH3,

C(O)CCF3, CH2C(O), and (O)CCH2;

R1 is selected from the group consisting of hydrido, methyl, ethyl, and 2,2,2-trifluoroethyl;

R2 is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-ρyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R9 , the other carbon adjacent to

the carbon at the point of attachment may be substituted by R 13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment may be

substituted by R 10 , a carbon adjacent to R13 and two atoms from the carbon at

the point of attachment may be substituted by R12 , and any carbon adjacent to

both R10 and R12 may be substituted by R1 1;

K is CR4a R4b wherein R4a and R4b are independently selected from the group consisting of chloro, fluoro, and hydrido;

E0 is E1 , when K is CR4a R4b, wherein E1 is selected from the group

consisting of a covalent single bond, C(O)N(H), (H)NC(O), S(O)2N(H),

N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

K is selected from the group consisting of N(H) and CH2N(H);

E0 is E2 , when K is selected from the group consisting of N(H) and CH2N(H), wherein E2 is selected from the group consisting of C(O)N(H),

(H)NC(O), S(O)2N(H), N(H)S(O)2, S(0)2N(H)C(O), and C(O)N(H)S(O)2;

Y is selected from the group of formulas consisting of:

R 16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, methoxy, ethoxy, isopropoxy, methylthio, ethylthio, trifluoromethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl, methoxycarbonyl, ethoxycarbonyl, and cyano;

Qb is selected, when bonded to a carbon, from the group consisting of

NR20 R21,+ NR20 R21 R22, dimethylsulfonium, methylethylsulfonium,

diethylsulfonium, trimethylphosphonium, C(NR25 )NR23 R24 ,

N(R26)C(NR25)N(R23)(R24), C(O)N(R26)C(NR25)N(R23)(R24),

N(R26)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)SO2N(R23)(R24),

C(O)NR23 R24, and C(O)NR23 R24 with the provisos that no more than one of

R20, R21, and R22 is hydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or amino and that no more than one of

R23, R24, a, nd R26 is hydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or amino when two of the group

consisting of R23, R24, and R26 are bonded to the same atom and that said Qb

group is bonded directly to a carbon atom;

R20, R21, R22, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, methyl, ethyl, hydroxy, methoxy, ethoxy, 2-aminoethyl, 2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino, N-(2-hydroxyethyl)-N-(2-aminoethyl)amino, N-methylamino, N,N-dimethylamino, and N,N,N-trimethylamino;

Qb is selected, when bonded to a nitrogen, from the group consisting of oxy, methyl, ethyl, 2-aminoethyl, 2-(N-methylamino)ethyl, 2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino, N,N-bis-(2-hy droxy ethyl)amino, amino, hydroxylamino, N-methoxyamino, N-methylamino, N JS[-dimethylamino, and N,N,N-trimethylamino;

Qs is selected from the group consisting of a single covalent bond, CH2, CH3CH, CF2, CF3CH, CH2O, CH3C(H)O, CF3C(H)O, CH2S, CH3C(H)S,

CF3C(H)S, CH2C(O), CH3C(H)C(O), CF3C(H)C(O), and CF2C(O) with the proviso that Qs is bonded to E0 through a carbon atom.

8. The compound as recited in Claim 7 having the Formula I-EMPS:


or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, and 4-pyridyl, wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R32, the other carbon adjacent to the carbon at the point of

attachment may be substituted by R36, a carbon adjacent to R32 and two atoms

from the carbon at the point of attachment may be substituted by R33 , a carbon

adjacent to R36 and two atoms from the carbon at the point of attachment may

be substituted by R35, and any carbon adjacent to both R33 and R35 may be

substituted by R34;

R32 , R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, methoxy, ethoxy, hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2333-pentafluoropropyl, fluoro, chloro, bromo, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, 2,2,2-trifluoro-1-trifluoromethyl-1-hydroxyethyl,

methoxycarbonyl, ethoxycarbonyl, cyano, and Qb ;

B is selected from the group consisting of propyl, isopropyl, butyl, sec-butyl, isobutyl, 1-pentyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-difluoropropyl, 2-trifluoromethyl-3,33-trifluoropropyl, 1,1,1,2,2,2-hexafluoropropyl, 333-trifluoroprop-1-yl, and 3,33-trifluoroprop-2-yl, wherein each member of group B may be optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36;

B is selected from the group consisting of cyclopropyl, cyclobutyl, oxetan-2-yl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, thiaetan-2-yl, thiaetan-3-yl, wherein each ring carbon may be optionally substituted with R33, a ring carbon and nitrogen atoms adjacent to the carbon atom at the point of attachment may be optionally substituted with R9 or R13, a ring carbon or

nitrogen atom adjacent to the R9 position and two atoms from the point of

attachment may be substituted with R10, and a ring carbon or nitrogen atom

adjacent to the R13 position and two atoms from the point of attachment may

be substituted with R12;

R9 , R10, R1 1, R12, and R13 are independently selected from the group consisting of amidino, guanidino, carboxy, methoxy, ethoxy, hydroxy, amino, methoxyamino, ethoxyamino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-N-methylamino, dimethylamino, N-ethylamino, acetyl, propanoyl, trifluoroacetyl, pentafluoropropanoyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy methyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

A is selected from the group consisting of single covalent bond, O,

C(O), CH2, CH2C(O), and (O)CCH2;

R1 is selected from the group consisting of hydrido and methyl;

R2 is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-ρyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-tiiazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment may be substituted by R9 , the other carbon adjacent to

the carbon at the point of attachment may be substituted by R 13 , a ca,rbon

adjacent to R9 and two atoms from the carbon at the point of attachment may be

substituted by R10 , a carbon adjacent to R13 and two atoms from the carbon at

the point of attachment may be substituted by R12 , and any carbon adjacent to

both R10 and R12 may be substituted by R 11;

K is CR4a R4b wherein R4a and R4b are independently selected from the group consisting of chloro, fluoro, and hydrido;

E0 is E1 , when K is CR4a R4b , wherein E1 is selected from the group consisting of a covalent single bond, C(O)N(H), (H)NC(O), S(O)2N(H), N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

K is selected from the group consisting of N(H) and CH2N(H);

E0 is E2 , when K is selected from the group consisting of N(H) and CH2N(H), wherein E2 is selected from the group consisting of C(O)N(H),

(H)NC(O), S(O)2N(H), N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2; i is selected from the group of formulas consisting of:


R 16, R17, R 18, and R 19 are independently selected from the group consisting of hydrido, methoxy, ethoxy, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, bromo, acetyl, trifluoroacetyl, methoxycarbonyl, ethoxycarbonyl, and cyano;

Qb is selected from the group consisting of NR20 R21 ,+ NR20 R21 R22, dimethylsulfonium, methylethylsulfonium, dietiiylsulfonium,

trimethylphosphonium, C(NR25 )NR23 R24 , N(R26 )C(NR25 )N(R23 )(R24 ),

C(O)N(R26)C(NR25)N(R23)(R24), N(R26)N(R26)C(NR25)N(R23)(R24),

N(R26 )N(R26 )SO2N(R23 )(R24 ), C(O)NR23 R24 , and C(O)NR23 R24 with

the provisos that no more than one of R20 , R21 , and R22 is hydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino, and N,N,N-trimethylamino, or ammo and that no more than one of R23, R24, and R26 is 2ydroxy, methoxy, ethoxy, N-methylamino, N,N-dimethylamino, N,N,N-trimethylamino, or amino

when two of the group consisting of R23, R24, and R26 are bonded to the same atom;

R20, R21, R22, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, methyl, ethyl, hydroxy, methoxy, ethoxy, 2-aminoethyl, 2-(N-methylammo)ethyl, 2-(N,N-dimethylamino)ethyl, 2-(N,N,N-trimethylamino)ethyl, N-(2-hydroxyethyl)amino, N,N-bis-(2-hydroxyethyl)amino, N-(2-hydroxyethyl)-N-(2-aminoethyl)amino, N-methylamino, N,N-dimethylamino, and N,N,N-trimethylamino;

Qs is selected from the group consisting of a single covalent bond, CH2, CH3CH, CF2, CF3CH, CH2O, CH3C(H)O, CF3C(H)0, CH2C(O),

CH3C(H)C(O), CF3C(H)C(O), and CF2C(O) with the proviso that Qs is bonded to E through a carbon atom.

9. A composition for inhibiting thrombotic conditions in blood comprising a compound of any one of Claims 1 through 8 and a pharmaceutically acceptable carrier.

10. A method for inhibiting thrombotic conditions in blood comprising adding to blood a therapeutically effective amount of a composition of Claim 9.

11. A method for inhibiting formation of blood platelet aggregates in blood comprising adding to blood a therapeutically effective amount of a composition of Claim 9.

12. A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a composition of Claim 9.

13. A method for treating or preventing venuous thromboembolism and

pulmonary embolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of Claim 9.

14. A method for treating or preventing deep vein thrombosis in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of Claim 9.

15. A method for treating or preventing cardiogenic thromboembolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of Claim 9.

16. A method for treating or preventing thromboembolic stroke in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of Claim 9.

17. A method for treating or preventing thrombosis associated with cancer and cancer chemotherapy in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of Claim 9.

18. A method for treating or preventing unstable angina in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of Claim 9.

19. A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a compound of any one of Claims 1 through 8 with a therapeutically effective amount of fibrinogen receptor antagonist.

20. The use of a compound of any one of Claims 1 through 8, or a

pharmaceutically acceptable salt thereof, in the manufacture of medicament for inhibiting thrombus formation, treating thrombus formation, or preventing thrombus formation in a mammal.

21. A compound of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is phenyl or a heteroaryl of 5 or 6 ring members, wherein a nitrogen with a removable hydrogen or a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, a nitrogen with a removable hydrogen or a carbon at the other position

adjacent to the point of attachment is optionally substituted by R36, a nitrogen

with a removable hydrogen or a carbon adjacent to R32 and two atoms from the

point of attachment is optionally substituted by R33, a nitrogen with a

removable hydrogen or a carbon adjacent to R36 and two atoms from the point

of attachment is optionally substituted by R35, and a nitrogen with a removable

hydrogen or a carbon adjacent to both R33 and R35 is optionally substituted by

R34

R9 , R10 , R1 1 , R12 , R13 , R32 , R33 , R34 , R35 , and R363re

independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy ,heterocyclyloxy, heterocyclylalkoxy, alkoxyalkyl,

haloalkoxylalkyl, hydroxy, amino, alkoxyamino, nitro, alkylamino,

N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino,

heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio,

alkylthioalkyl, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl,

cycloalkylsulfonyl, heteroarylsulfonyl, alkylsulfonylalkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboxyalkyl, carboalkoxy, carboxy, carboxamido, carboxamidoalkyl, and cyano;

R32, R33, R34, R35, and R36 are independently optionally Qb;

B is optionally selected from the group consisting of hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36;

B is optionally a C3-C12 cycloalkyl or C4-C9 saturated heterocyclyl, wherein each ring carbon is optionally substituted with R33 , a ring carbon other than the ring carbon at the point of attachment of B to A is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbons and a nitrogen adjacent to the carbon atom at the point of attachment are optionally substituted with R9 or R13, a ring

carbon or nitrogen atom adjacent to the R9 position and two atoms from the

point of attachment is optionally substituted with R10, a ring carbon or nitrogen

adjacent to the R13 position and two atoms from the point of attachment is

optionally substituted with R12, a ring carbon or nitrogen three atoms from the

point of attachment and adjacent to the R10 position is optionally substituted

with R11 , a ring carbon or nitrogen three atoms from the point of attachment

and adjacent to the R12 position is optionally substituted with R33, and a ring carbon or nitrogen four atoms from the point of attachment and adjacent to the

R11 and R33 positions is optionally substituted with R34 ;

A is selected from the group consisting of a bond,

(W?)rr-(CH(R15))pa, and (CH(R15))pa-(W7)rr wherein rr is 0 or 1, pa is an

integer selected from 0 through 6, and W7 is selected from the group

consisting of O, S, C(O), (R7)NC(O), (R7)NC(S), and N(R7) with the proviso that no more than one of the group consisting of rr and pa is 0 at the same time;

R7 is selected from the group consisting of hydrido, hydroxy, and alkyl;

R15 is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;

Ψ is NH or NOH;

X0 is selected from the group consisting of hydrido, alkyl, alkenyl, cyano, halo, haloalkyl, haloalkoxy, haloalkylthio, amino, aminoalkyl, alkylamino, amidino, hydroxy, hydroxyamino, alkoxy, hydroxyalkyl, alkoxyamino, thiol, and alkylthio;

R1 is selected from the group consisting of hydrido, alkyl, alkenyl, haloalkyl, amino, aminoalkyl, alkylamino, hydroxy, and hydroxyalkyl;

X0 and R 1 or R1 and R2 is optionally bonded together to form a partially saturated C5-C8 heterocyclyl ring, wherein said heterocyclyl ring is optionally substituted with one or more of the group consisting of R9, R10,

R11, R12, and R13 ;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, (CR41 R42 )q

wherein q is an integer selected from 1 through 3, and (CH(R41 ))p-W -

(CH(R42 ))p wherein g and p are integers independently selected from 0

through 3 and W0 is selected from the group consisting of O, S, C(O), S(O),

N(R41), and ON(R4 1);

Z0 is optionally (CH(R41))e-W22-(CH(R42))h wherein e and h are

independently 0 or 1 and W22 is selected from the group consisting of

CR41 =CR42, 1,2-cyclopropyl, 1,2-cyclobutyl, 1 ,2-cyclohexyl, 13-cyclohexyl,

1,2-cyclopentyl, 13-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl,

2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl,

13-piperazinyl, 2,3-piperazinyl, 2,6-ρiperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyπolidinyl, 2,3-pyπolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl,

3,4-pyrrolidinyl, 23-tetrahydrofuranyl, 2,4-tetrahydrofuranyl,

2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z0 is directly bonded to the 4-pyridone ring and W22 is optionally substituted with one or more

substituents selected from the group consisting of R9, R 10, R11, R12, and R13;

R41 and R42 are independently selected from the group consisting of amidino, hydroxyamino, hydrido, hydroxy, amino, and alkyl;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a nitrogen with a removable hydrogen or a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , a nitrogen with a removable hydrogen or a carbon at the other position

adjacent to the point of attachment is optionally substituted by R13, a nitrogen

with a removable hydrogen or a carbon adjacent to R9 and two atoms from the

point of attachment is optionally substituted by R 10, a nitrogen with a

removable hydrogen or a carbon adjacent to R13 and two atoms from the point

of attachment is optionally substituted by R12, and a nitrogen with a removable hydrogen or a carbon adjacent to both R 10 and R12 is optionally substituted by

R 11;

Q is optionally hydrido with the proviso that Z0 is selected from other than a bond;

K is CR4a R4b;

R4a and R4b are independently selected from the group consisting of halo, hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;

E0, with the proviso that K is CR4a R4b, is E1 wherein E1 is selected from the group consisting of a covalent single bond, C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S), S(O)2N(H), N(H)S(O)2, S(O)2N(H)C(O), and

C(O)N(H)S(O)2;

K is optionally (CH(R14 ))j-T wherein j is 0 or 1 and T is a bond or

N(R7) with the proviso that (CH(R14))j is bonded to the phenyl ring;

R 14 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

E0 , with the proviso that K is (CH(R14))j-T, is E2 wherein E2 is selected from the group consisting of C(O)N(H), (H)NC(O), C(S)N(H),

(H)NC(S), S(O)2N(H), N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

Y is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs, a carbon two or three

contiguous atoms from the point of attachment of Qs to said phenyl or said

heteroaryl to said phenyl or said heteroaryl is substituted by Qb , a carbon

adjacent to the point of attachment of Qs is optionally substituted by R17, another carbon adjacent to the point of attachment of Qs is optionally

substituted by R18 , a carbon adjacent to Qb is optionally substituted by R16 ,

and another carbon adjacent to Qb is optionally substituted by R19 ;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, nitro, alkoxyamino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboalkoxy, and cyano;

R16 or R19 is optionally selected from the group consisting of

NR20 R21 ,N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23 R24 , with the

proviso that R16 , R19 , and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21 , aminoalkyl,

hydrido, N(R26)CCNR25)N(R23)(R24), and C(NR25)NR23 R24 , with the

proviso that no more than one of R20 and R21 is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time, with the further proviso that no more than one of R23 and R24 is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time;

R20, R21, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, aminoalkyl, amino, dialkylamino, alkylamino, and hydroxyalkyl;

Q is selected from the group consisting of a bond, (CR37 R38)b

wherein b is an integer selected from 1 through 4, and (CH(R14))c- W1 -

(CH(R15))d wherein c and d are integers independently selected from 1

through 3 and W1 is selected from the group consisting of C(O)N(R14),

(R14)NC(O), S(O), S(O)2, S(O)2N(R14), N(R14)S(O)2, and N(R14), with the

proviso that R14 is selected from other than halo when directly bonded to N,

and with the additional proviso that (CR37 R38) b and (CH(R14))c are bonded to E0

R37 and R38 are independently selected from the group consisting of hydrido, alkyl, and haloalkyl;

R38 is optionally aroyl or heteroaroyl, wherein R38 is optionally substituted with one or more substituents selected from the group consisting of R16 , R17 , R18 , and R19 ;

Y0 is optionally Y AT wherein YAT is Qb -Qs ;

Y0 is optionally Qb-QSS wherein QSS is (CH(R14))e-W2-(CH(R15))h,

wherein e and h are independently 1 or 2 and W2 is CR4a =CR4b , with the

proviso that (CH(R 14))e is bonded to E0 ;

Y0 is optionally Qb-QSSSS or Qb-Qssssr wherein QSSSS is (CH(R38))r-

W5 , Qssssr is (CH(R38))r- W6, r is 1 or 2, W5 and W6 are independently selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl,

3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl,

2,7-imidazo(1 ,2-a)pyridinyl, 3 ,4-imidazo(1 ,2-a)pyridinyl,

3 ,5-imidazo( 1 ,2-a)pyridinyl, 3 ,6-imidazo( 1 ,2-a)pyridinyl ,

3,7-imidazo(1,2-a)pyridinyl, 2,4-indolyl, 2,5-indoIyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 13-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3 ,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl,

2,4-naphthyl , 2,5-naphthyl , 2,6-naphthyl , 2,7-naphthyl, 2,8-naphthyl ,

2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinotinyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl, and each carbon and hyrido containing nitrogen member of the ring of the W5

and of the ring of the W6, other than the points of attachment of W5 and W6,

is optionally substituted with one or more of the group consisting of R9 , R10,

R11 , and R12 , with the proviso that Qb is bonded to lowest number substituent

position of each W5 , with the further proviso that Qb is bonded to highest

number substituent position of each W6, and with the additional proviso that

(CH(R38))r is bonded to E0.

22. Compound of Claim 21 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R36, a carbon

adjacent to R32 and two atoms from the carbon at the point of attachment is

optionally substituted by R33, a carbon adjacent to R36 and two atoms from the

carbon at the point of attachment is optionally substituted by R35, and any

carbon adjacent to both R33 and R35 is optionally substituted by R34;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, hydroxy, amino,

alkoxyamino, haloalkanoyl, nitro, alkylamino, alkylthio, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxamido, cyano, and

Qb;

B is optionally selected from the group consisting of hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32 , R33, R34, R35, and R36;

B is optionally a C3-C12 cycloalkyl or a C4-C9 saturated heterocyclyl, wherein each ring carbon is optionally substituted with R33 , a ring carbon other than the ring carbon at the point of attachment of B to A is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbons and a nitrogen adjacent to the carbon atom at the point of attachment are optionally substituted with R9 or R13, a ,ing

carbon or nitrogen atom adjacent to the R9 position and two atoms from the

point of attachment is optionally substituted with R10 , a ring carbon or nitrogen

atom adjacent to the R13 position and two atoms from the point of attachment

is optionally substituted with R12 , a ring carbon or nitrogen atom three atoms

from the point of attachment and adjacent to the R10 position is optionally

substituted with R1 1, a ring carbon or nitrogen atom three atoms from the

point of attachment and adjacent to the R12 position is optionally substituted

with R33, and a ring carbon or nitrogen atom four atoms from the point of

attachment and adjacent to the R1 1 and R33 positions is optionally substituted

with R34 ;

R9 , R10 , R1 1 , R 12 , and R13 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, alkoxyamino, alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy, haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,

heteroaralkoxy jheterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl,

cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, and cyano;

A is bond or (CH(R15 ))pa-(W7 )rr wherein rr is 0 or 1, pa is an integer

selected from 0 through 3, and W7 is selected from the group consisting of O,

S, C(O), (R7)NC(O), (R7)NC(S), and N(R7), with the proviso that W? is bonded to the N(H) on the 4-pyridone ring;

R7 is selected from the group consisting of hydrido, hydroxy and alkyl;

R15 is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;

X0 is selected from the group consisting of hydrido, alkyl, cyano, halo, haloalkyl, haloalkoxy, amino, aminoalkyl, alkylamino, amidino, hydroxy, hydroxyamino, alkoxy, hydroxyalkyl, alkoxyamino, thiol, and alkylthio;

R1 is selected from the group consisting of hydrido, alkyl, haloalkyl, amino, aminoalkyl, alkylamino, hydroxy, and hydroxyalkyl;

X0 and R 1 or R1 and R2 is optionally bonded together to form a partially saturated C5-C8 heterocyclyl ring, wherein said heterocyclyl ring is optionally substituted with one or more of the group consisting of R9 , R 10,

R1 1, R12, and R13;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, (CR41 R42)q

wherein q is 1 or 2, and (CH(R41 ))g-W0 -(CH(R42 ))p wherein g and p are integers independently selected from 0 through 3 and W is selected from the group consisting of O, S, C(O), S(O), N(R41), and ON(R41);

Z0 is optionally (CH(R41))e-W2 -(CH(R42))h wherein e and h are

independently 0 or 1 and W22 is selected from the group consisting of

CR41 =CR42, 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 13-cyclohexyl,

1,2-cyclopentyl, 13-cycloρentyl, 23-morpholinyl, 2,4-morpholinyl,

2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl,

13-ρiρerazinyl, 2,3-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 13-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl,

1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrrlidinyl,

2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z is directly bonded to the 4-pyridone ring and W22 is optionally substituted with one or more

substituents selected from the group consisting of R9, R10, R11, R12, and R13;

R41 and R42 are independently selected from the group consisting of hydrido, hydroxy, alkyl, and amino;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10, a carbon adjacent to R13 and two atoms from the

carbon at the point of attache, is optionally substituted by R12 and any

carbon adjacent to both R10 and R12 is optionally substituted by R11 ;

Q is optionally hydrido with the proviso that Z0 is other than a bond; K is CR4a R4b;

R4a and R4b are independently selected from the group consisting of hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;

E0, with the proviso that K is CR4a R4b, is E 1 wherein E is selected from the group consisting of a covalent single bond, C(O)N(H), (H)NC(O), S(O)2N(H), and N(H)S(O)2;

K is optionally (CH(R14))j-T wherein j is 0 or 1 and T is a bond or

N(R7) with the proviso that (CH(R14))j is bonded to the phenyl ring;

R14 is hydrido or halo;

E0 , with the proviso that K is (CH(R14 ));-T, is E2 wherein E2 is selected from the group consisting of C(O)N(H), (H)NC(O), C(S)N(H),

(H)NC(S), S(O)2N(H), N(H)S(O)2, S(O)2N(H)C(O), and C(O)N(H)S(O)2;

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs, a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is

substituted by Qb , a carbon adjacent to the point of attachment of Qs is

optionally substituted by R 17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R18 , a carbon adjacent to Qb is

optionally substituted by R 16 , and another carbon adjacent to Qb is optionally

substituted by R19;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, alkylsulfinyl,

alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R16 or R19 is optionally selected from the group consisting of

NR20 R21 ,N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23 R24, with the

proviso that R 16 , R19 , and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21, hydrido,

N(R26)C(NR25)N(R23 )(R24), and C(NR25)NR23 R24, with the proviso that no

more than one of R20 and R21 is sel2cted from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time, with the further proviso that no more than one of R23 and R24 is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time;

R20, R21, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, amino, alkylamino and dialkylamino;

Q is selected from the group consisting of a bond, (CR37R38)j,

wherein b is an integer selected from 1 through 4, and (CH(R14))C-W1-

(CH(R15))j wherein c and d are integers independently selected from 1

through 3 and W1 is selected from the group consisting of C(O)N(R 14),

(R14)NC(O), S(O), S(O)2, S(O)2N(R14), N(R14)S(O)2, and N(R14), with the

proviso that R14 is selected from other than halo when directly bonded to N,

and with the additional proviso that (CR 37 R38)b, and (CR37 R38)b, and

(CH(R14))C are bonded to E0;

R37 and R38 are independently selected from the group consisting of hydrido, alkyl, and haloalkyl;

R38 is optionally aroyl or heteroaroyl, wherein R38 is optionally substituted with one or more substituents selected from the group consisting of

R16 , R17 ,R18 , andR19 ;

Y0 is optionally YAT wherein YAT is Qb -Qs ;

T0 is optionally Qb -Qss wherein Qss is (CH(R14))e-W2 -(CH(R 15))h,

wherein e and h are independently 1 or 2 and W2 is CR4a =CR4b with the

proviso that (CH(R14))e is bonded to E0.

20. Compound of Claim 22 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36 ;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q ;

A is (CH(R15 ))pa-W7 wherein pa is an integer selected from 0 through

3 and W7 is selected from the group consisting of O, S, and N(R7 ) wherein R7

is hydrido or alkyl;

R15 is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl ;

X0 is selected from the group consisting of hydrido, amino, alkyl, cyano, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;

R1 is selected from the group consisting of hydrido, alkyl, haloalkyl, amino, aminoalkyl, alkylamino, hydroxy, and hydroxyalkyl ;

R2 is Z0-Q;

Z0 is a bond or (CR41 R42 )q wherein q isl or 2;

R41 and R42 are independently selected from the group consisting of hydrido, hydroxy, and amino;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carb,n adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10 , a carbon adjacent to R13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R12 is optionally substituted by R1 1, with the proviso that Q is other than a phenyl when Z0 is a bond;

R9 , R10 , R11 , R12 , and R13 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, alkoxyamino, alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy, haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,

heteroaralkoxy ,heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl,

cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, and cyano;

K is CHR4a wherein R4a is selected from the group consisting of hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;

E0 is selected from the group consisting of a bond, C(O)N(H),

(H)NC(O), (R7)NS(O)2, and S(O)2N(R7);

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs , a carbon two or three

contiguous atoms from the point of attachment of Qs to the phenyl or

heteroaryl ring is substituted by Qb, a carbon adjacent to the point of

attachment of Qs is optionally substituted by R17, another carbon adjacent to

the point of attachment of Qs is optionally substituted by R18 , a carbon

adjacent to Qb is optionally substituted by R 16 , and another carbon adjacent to

Qb is optionally substituted by R19;

R16, R17, R18, and R 19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R 16 or R19 is optionally selected from the group consisting of

NR20 R21 ,N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23R24, with the

proviso that R16, R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21 , hydrido,

N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23 R24, with the proviso that no

more than one of R20 and R21 is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time and with the further proviso that no more than one of R23 and R24 is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time;

R20, R21, R23 , R24, R25, and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, amino, alkylamino and dialkylamino;

Qs is selected from the group consisting of a bond, (CR37 R38)b wherein b is an integer selected from 1 through 3, and

(CH(R14))C-W1 -(CH(R15)) d wherein c and d are independently 1 or 2 and

W1 is selected from the group consisting of C(O)N(R14), (R14)NC(O), S(O),

S(O)2, S(O)2N(R14), N(R14)S(O)2, and N(R14), with the prov1so that R14 is

selected from other than halo when directly bonded to N and with the further proviso that (CR37 R38)b, and (CH(R14))c are bonded to E0 ;

R14 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

R37 and R38 are independently selected from the group consisting of hydrido, alkyl, and haloalkyl;

R38 is optionally aroyl and heteroaroyl;

Y0 is optionally Qb-QSS wherein QSS is (CH(R14))e-W2-(CH(R15))h,

wherein e and h are integers independently selected from 1 through 2 and w2

is CR4a =CH with the proviso that (CH(R 14))e is bonded to E .

24. Compound of Claim 23 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, trialkylsilyl, C2-C4 alkyl, C3-C5 alkylenyl, C3-C4 alkenyl, C3-C4 alkynyl, and C2-C4 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 3 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, and R34;

R32, R33, and R34 are 3ndependently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, and cyano;

A is (CH(R 15))pa-N(R7) wherein pa is an integer selected from 0

through 2 and R7 is hydrido or alkyl;

R 15 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

X00 is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;

R 1 is selected from the group consisting of hydrido, alkyl, haloalkyl, amino, aminoalkyl, hydroxy, and hydroxyalkyl;

R2 is Z0-Q;

Z0 is a bond or CH2;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13 , a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10 , a carbon adjacent to R 13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R 12 is optionally substituted by R11 ;

R9 , R1 1 , and R13 are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy,

heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino,

heterocyclylamino, heterocyclylalkylamino, alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl,

carboxamido, halo, haloalkyl, and cyano;

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs , a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is

substituted by Qb , a carbon adjacent to the point of attachment of Qs is

optionally substituted by R17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R 18 , a carbon adjacent to Qb is

optionally substituted by R16, and another carbon adjacent to Qb is optionally

substituted by R 19;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, allcylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R16 or R19 is optionally selected from the group consisting of

NR20R21, N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23R24 with the

proviso that R 16 , R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21, hydrido,

C(NR25)NR23R24, and N(R26)C(NR25)N(R23)(R24), with the proviso that

no more than one of R20 and R21 is hydroxy at the same time and with the

further proviso that no more than one of R23 and R24 is hydroxy at the same time;

R20, R21, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, alkyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2, and CH2CH2.

25. Compound of Claim 24 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, -CH2CH2CH2-, -CH2CH2CH2CH2-, butyl,

2-butenyl, 3-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl,

2-methylpropenyl, 2,2,2-trifluoroethyl, 3 ,33-trifluoropropyl, and

2,2-difluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 3 atoms from the point of attachment of B to

A with one or more of the group consisting of R32, R33, and R34;

R32, R33, and R34 are i3dependently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,

amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,

2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,

amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

A is selected from the group consisting of a bond, NH, and N(CH3);

X0 is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, n-butyl, 2,2,2-trifluoroethyl, 3,33-trifluoropropyl, 2,2333-pentafluoropropyl, 2-aminoethyl, 3-aminopropyl, 2-hydroxyethyl, 3-hydroxypropyl, and 2,3-dihydroxypropyl;

R2 is Z0-Q;

Z0 is a bond or CH2;

Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl,

3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazm-2-yl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the carbon at the point

of attachment is optionally substituted by R13 , a carbon adjacent to R9 and two atoms from the carbon at the point of attachment is optionally substituted by

R10 , a carbon adjacent to R13 and two atoms from the carbon at the point of

attachment is optionally substituted by R12, and any carbon adjacent to both

R10 and R12 is optionally substituted by R1 1;

R9 , R1 1, and R 13 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,

2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl,

N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl,

2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl,

ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,

N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl,

N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl , N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(l-phenylethyl)amidocarbonyl, N-(1-methyl- l-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl,

N-(2-chlorobenzyl)amidosulfonyl, N-isopropylamidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy,

4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy, 3-bromobenzyloxy, 4-bromobenzyloxy,

4-bromobenzylamino, 5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethylphenoxy,

4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino,

3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl,

4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy, 3,5-difluorophenoxy,

3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 23-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy, 3,5-dimethylphenoxy,

3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy, 3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy,

2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-Strifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,

4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,

1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy,

3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy,

2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl,

3 ,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy,

3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy,

4-trifluoromethylthiobenzyloxy, 2,3,4-trifluorophenoxy,

2,3 ,5-trifluorophenoxy, 3-ρentafluoroethylphenoxy ,

3-(l,1,2,2-tetrafluoroethoxy)phenoxy, and 3-trifluoromethylthiophenoxy; x is selected from the group consisting of:

1-Qb.4-Qs-2-R16-3-R17-5-R18-6-R19benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine, 2-Qb-5-Qs-3-R16-6-R18pyrazine,

3-Qb-6-Qs-2-R18-5-R18-4-R19pyridazine,

2-Qb-5-Qs-4-R17-6-R18pyrimidine, 5-Qb-2-Qs-4-R16-6-R19pyrimidine,

3-Q -5-Qs-4-R16-2-R thiophene, 2-Qb -5-Qs-3-R16-4-RR7 thiophene,

3-Qb-5-Qs-4-R16-2-R19furan, 2-Qb-5-Qs-3-R16-4-R17furan,

3-Qb-5-Qs-4-R16-2-R19pyrrole, 2-Qb-5-Qs-3-R16-4-R17pyrrole,

4-Qb-2-Qs-5-R 19 imidazole, 2-Qb-4-Qs-5-R17 imidazole,

3-Qb-5-Qs-4-R16 isoxazole, 5-Qb-3-Qs-4-R16 isoxazole,

2-Qb-5-Qs-4-R16 pyrazole, 4-Qb-2-Qs-5-R19 thiazole, and

2-Qb-5-Qs-4-R17 thiazole;

R16, R17, R 18, and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,

aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2333-pentafluoropropyl,

trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy , fluoro, chloro, bromo,

hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;

R 16 or R 19 is optionally selected from the group consisting of

NR20R2R, N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23R24, with the

proviso that R16, R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21 , hydndo,

C(NR25)NR23R24 and N(R26)C(NR25)N(R23)(R24), with the proviso that

no more than one of R20, R21, R23, and R24 can be hydroxy, when any two

of the group consisting of R20, R21, R23 , and R24 are bonded to the same

atom and with the further proviso that said Qb group is bonded directly to a carbon atom;

R20, R21, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2, and CH2CH2.

26. Compound of Claim 24 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

A is selected from the group consisting of CH2N(CH3),

CH2N(CH2CH3), CH2CH2N(CH3), and CH2CH2N(CH2CH3);

X0 is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, n-butyl, 2,2,2-trifluoroethyl, 3,33-trifluoropropyl, 2,2,333-pentafluoropropyl, 2-aminoethyl, 3-aminopropyl, 2-hydroxyethyl, 3-hydroxypropyl, and 2,3-dihydroxypropyl;

R2 is Z0-Q;

Z0 is a bond or CH2;

Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl,

3-pyridazinyl, 4-pyridazinyl, and 13,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the carbon at the point

of attachment is optionally substituted by R 13, a carbon adjacent to R9 and two atoms from the carbon at the point of attachment is optionally substituted by

R 10, a carbon adjacent to R13 and two atoms from the carbon at the point of

attachment is optionally substituted by R12, and any carbon adjacent to both

R10 and R12 is optionally substituted by R11 ;

R9, R1 1, and R13 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,

2,2333-pentafϊuoropropyl, trifluoromethoxy, 1,1,2,2-tetiafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

R 10 and R 12 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,

methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl,

N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hyd-oxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,

amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,

N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethyIbenzyl)amidocarbonyl,

N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,

N-isopropylamidocarbonyl, N-cyclobutylamidocarbonyl,

N-cyclopentylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,

3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,

5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl,

4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy,

4-chlorobenzyl sulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy,

2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy,

3 ,5-difluorophenoxy, 3 ,5-difluorobenzyloxy , 4-difluoromethoxybenzyloxy , 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy,

3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,

3,5-dimethylbenzyloxy, 4-ethoxyphenoxy , 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy,

2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-5-trifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,

4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,

1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy,

3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy,

2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl,

3 ,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy ,

3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy,

4-trifluoromethylthiobenzyloxy, 2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and

3-trifluoromethylthiophenoxy;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine, 2-Qb-5-Qs-3-R16-6-R18pyrazine,

3-Qb -6-Qs-2-R 18-5-R 18-4-R 19 pyridazme,

2-Qb-5-Qs-4-R17-6-R18 pyrimidine, 5-Qb-2-Qs-4-R 16-6-R19 pyrimidine,

3-Qb-5-Qs-4-R 16-2-R 19 thiophene, 2-Qb-5-QSs-3-R16-4-R17 thiophene,

3-Qb-5-Qs-4-R16-2-R19furan, 2-Qb-5-Qs-3-R16-4-R17furan,

3-QB-5-Qs-4-R 16-2-R19 pyrrole, 2-Qb-5-Qs-3-R16-4-R17 pyrrole,

4-Qb-2-Qs-5-R19 imidazole, 2-Qb-4-Qs-5-R 17 imidazole,

3-Qb-5-Qs-4-R16 isoxazole, 5-Qb -3-Qs-4-R16 isoxazole,

2-Qb-5-Qs-4-R16 pyrazole, 4-Qb-2-Qb-5-R19 thiazole, and

2-Qb-5-Qs-4-R 17 thiazole;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,333-pentafluoropropyl, trifluoromethoxy,

1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl,

1 -hydroxyethyl, 2-hydroxyethyl, and cyano;

Qb is selected from the group consisting of NR20R21,

C(NR25)NR23R24, and N(R26)C(NR25)N(R23)(R24 ), with the proviso that

no more than one of R20, R21, R23, and R24 can be hydroxy, when any two

of the group consisting of R20, R21, R23 , and R24 are bonded to the same

atom, and with the further proviso that said Qb groub is bonded directly to a carbon atom;

R20 , R21 , R23 , R24 , R25 , and R26 are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2, and CH2CH2.

27. Compound of Claim 26 or a pharmaceutically acceptable salt thereof, wherein;

A is selected from the group consisting of CH2N(CH3),

CH2N(CH2CH3), CH2CH2N(CH3), and CH2CH2N(CH2CH3);

X0 is selected from the group consisting of hydrido, hydroxy,1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, ammo, methyl, ethyl, 2,2,2-trifluoroethyl, 333-trifluoropropyl, 2-aminoethyl, and 2-hy droxy ethyl;

R2 is Z0-Q;

Z0 is a bond or CH2;

Q is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-S(2-phenylethyl)phenyl,

3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl, 3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-S(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(l-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-propylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-S(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-S(N-cyclopentylamidocarbonyl)phenyl,

3-amino-S(N-cyclohexylamidocarbonyl)phenyl,

Samino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl,

5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl,

3-amino-2-methylphenyl, Samino-2-methylthiophenyl, 3-aminophenyl, 3-carboxyphenyi, 3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl,

3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,

3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trϋluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,

3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19benzene,

2-Qb-5-Qs-6-R 17-4-R18-3-R19 pyridine,

3-Qb-6-Qs-2-R 16-5-R 18-4-R19 pyridine,

3-Qb-5-Qs-4-R 16-2-R 19. thiophene, and 2-Qb-5-Qs-3-R16-4-R17 thiophene;

R16 and R19 are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R17 and R18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is C(NR25)NR23R24;

R23 , R24 , and R25 are independently selected from the group consisting of hydrido and methyl;

Qs is CH2.

28. A compound as recited in Claim 27 or a pharmaceutically acceptable salt thereof where said compound is selected from the group consisting of:

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-aminophenyl]-5-[N,N-dimethylhydrazino]-4-pyridonyl]]acetømide;

2-[3-[N-[[4-aminoiminomethylphenyl jmethyl]-2-[3-aminophenyl]-5-[N-ethyl-N-methylhydrazino]-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aimnoiminomethylphnnyl jmethyl]-2-[3-aminophenyl ]-5-[N,N-dimethylhydrazino]-N-methyl-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aιmnoiminomethylphenyl]methyl]-2-[3-aminophenyl]-5-[N-ethyl-N-methylhydrazino]-N-methyl-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3,5-diaminophenyl]- 5-[N,N-dimethylhydrazino]-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3,5-diaminophenyl]-5- [N-ethyl-N-methylhydrazmo]-4-pyridonyl]]acetømide ;

2-[3-[N-[[4-aminoiπύnomethylphenyl]methylJ-2-[3,5-diaminophenyl]-5-[N,N-dimethylhydrazino]-N-methyl-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aιmnoiminomethylphenyl]methyl]-2-[3,5-diaminophenyl]-5-pSf-ethyl-N-methylhydrazino]-N-methyl-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-carboxyphenyl]-S[N,N-dimethylhydrazino]-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-carboxyphenyl]-5-[N-ethyl-N-methylhydrazino]-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-carboxyphenyl]-5-[N,N-dimethylhydrazino]-N-methyl-4-pyridonyl]]acetømide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-S

carboxyphenyl]- 5-[N-ethyl-N-methylhydrazino]-N-methyl-4-ρyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-(N-benzylamidocarbonyOphenyl]- 5-[N,N- dimethylhydrazino]-4-ρyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-(N-benzylamidocarbonyl)phenyl]-5-[N-ethyl-N-methylhydrazino]-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-(N-benzylamidocarbonyl)phenyl]-5-[N,N-dimethylhydrazino]-N-methyl-4-pyridonyl]]acetamide;

2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2[3-amino-5-(N-benzylamidocarbonyl)phenyl]-5-[N-ethyl-N-methylhydrazino]-N-methyl-4-pyridonyl]]acetamide.

29. Compound of Claim 22 of the formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R36, a carbon

adjacent to R32 and two atoms from the carbon at the point of attachment is

optionally substituted by R33 , a carbon adjacent to R36 and two atoms from the

carbon at the point of attachment is optionally substituted by R35, and any

carbon adjacent to both R33 and R35 is optionally substituted by R34 ;

R32, R33 , R34, R35, and R36 ar3e independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Qb ;

A is a bond or (CH(R15))pa-(W7 )rr wherein rr is 0 or 1, pa is an

integer selected from 0 through 3, and W7 is (R7 )NC(O) or N(R7 );

R7 is selected from the group consisting of hydrido, hydroxy and alkyl;

R 15 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

X0 is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;

R 1 is independently selected from the group consisting of hydrido, hydroxy, amino, hydroxyalkyl, alkyl, aminoalkyl, and haloalkyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, CH2CH2, W -(CH(R42))p wherein p is 0 or 1 and W is selected from the group consisting

of O, S, and N(R41);

R41 and R42 are independently hydrido or alkyl;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10 , a carbon adjacent to R13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12 , and any

carbon adjacent to both R10 and R12 is optionally substituted by R11 ;

R9 , R1 1 , and R13 are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,

heteroaralkoxy .heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, arallcylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino,

alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl,

cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl,

cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo, haloalkyl, and cyano;

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs, a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is

substituted by Qb , a carbon adjacent to the point of attachment of Qs is

optionally substituted by R17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R18, a carbon adjacent to Qb is

optionally substituted by R16, and another carbon adjacent to Qb is optionally

substituted by R19;

R16, R 17, R 18, and R19 are 1ndependently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R16 or R 19 is optionally NR20 R21 or C(NR25 )NR23R24, with the

proviso that R16, R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21, hydrido, and

C(NR25)NR23 R24 , with the proviso that no more than one of R20 and R21 is

hydroxy at the same time and with the further proviso that no more than one of R23

and R24 is hydroxy at the same time;

R20, R21, R23, R24, and R25 are independently selected from the group consisting of hydrido, alkyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2, and

CH2CH2.

30. Compound of Claim 29 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl,

4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl,

3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, the other carbon adjacent to the carbon at the

point of attachment is optionally substituted by R36, a carbon adjacent to R32

and two atoms from the carbon at the point of attachment is optionally

substituted by R33, a carbon adjacent to R36 and two atoms from the carbon at the point of attachment is optionally substituted by R35, and any carbon

adjacent to both R33 and R35 is optionally substituted by R34;

R32 , R33 , R34 , R35 , and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl,

N,N-dimethylamidosulfonyl, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,

amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Q ;

A is selected from the group consisting of a bond, NH, N(CH3),

N(OH), CH2, CH3CH, CF3CH, NHC(O), N(CH3)C(O), C(O)NH,

C(O)N(CH3), CH2CH2, CH2CH2CH2, CH3CHCH2, and CF3CHCH2;

X0 is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hy droxy ethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, n-butyl, 2,2,2-trifluoroethyl, 333-trifluoropropyl, 2,2333-pentafluoropropyl, 2-aminoethyl, 3-aminopropyl, 2-hy droxy ethyl, 3-hydroxypropyl, and 2,3-dihydroxypropyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, CH2CH2, O, S, NH, N(CH3), OCH2, SCH2, N(H)CH2, and N(CH3)CH2;

Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl,

3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9, the other carbon adjacent to the carbon at the point

of attachment is optionally substituted by R13, a carbon adjacent to R9 and two atoms from the carbon at the point of attachment is optionally substituted by R10, a carbon adjacent to R13 and two atoms from the carbon at the point of

attachment is optionally substituted by R12, and any carbon adjacent to both

R10 and R12 is optionally substituted by R1 1;

R9, R1 1, and R13 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino,

N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,

2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,

2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl,

N,N-di

R 10 and R12 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,

methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl,

N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,

amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,

N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(l-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,

N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,

N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,

3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,

Sbromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl,

4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy,

2,4-difluorobenzyloxy , 3,4-difluorobenzyloxy , 2,5-difluorobenzyloxy ,

3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy,

,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,

3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy , 4-fluorobenzyloxy,

2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-Strifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy , 3-isopropylphenoxy, 4-isopropylphenoxy,

4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,

1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy,

3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy,

2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbeήzyl,

3 ,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy,

3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy,

4-trifluoromethylthiobenzyloxy, 23,4-trifluorophenoxy, 2,3,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and

3-trifluoromethylthiophenoxy;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R 17-5-R18-6-R19 benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19 pyridine,

3-Qb-6-Qs-2-R 16-5-R18-4-R19 pyridine, 2-Qb-5-Qs-3-R16-6-R18 pyrazine,

3-Qb-6-Qs-2-R18-5-R18-4-R 19 pyridazine,

2-Qb -5-Qs-4-R17-6-R18 pyrimidine, 5-Qb-2-Qs-4-R16-6-R19 pyrimidine,

3-Qb-5-Qs-4-R16-2-R19 thiophene, 2-Qb-5-Qs-3-R16-4-R17 thiophene,

3-Qb-5-Qs-4-R16-2-R19 furan, 2-Qb-5-Qs-3-R16-4-R17 furan,

3-Qb-5-Qs-4-R19-2-R19 pyrrole, 2-Qb-5-Qs-3-R 16-4-R17 pyrrole,

4-Qb-2-Qs-5-R 19 imidazole, 2-Qb-4-Qs-5-R 17 imidazole,

3-Qb-5-Qs-4-R 16 isoxazole, 5-Qb-3-Qs-4-R 16 isoxazole,

2-Qb-5-Qs-4-R16 pyrazole, 4-Qb-2-Qs-5-R 19 thiazole, and

2-Qb-5-Qs-4-R17 thiazole;

R16, R 17, R18, and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,333-pentafluoropropyl,

trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,

hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;

R16 or R19 is optionally C(NR25)NR23R24 with the proviso that R16,

R 19, and Qb are not simultaneously hydrido;

Qb is C(NR25)NR23 R24 or hydrido, with the proviso that no more than

one of R23 and R24 is hydroxy at the same time;

R23 , R24 , and R25 are independently selected from the group consisting of hydrido, methyl, ethyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2 and CH2CH2.

31. Compound of Claim 30 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of 2-aminophenyl,

3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl,

3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl,

3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl,

3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl,

3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoromethylphenyl, 2-imidazoyl, 2-pyridyl, 3-pyridyl,

5-chloro-3-trifluoromethyl-2-pyridyl, 4-pyridyl, 2-thienyl, 3-thienyl, and

3-trifluoromethyl-2-pyridyl;

A is selected from the group consisting of CH2, CH3CH, CF3CH,

NHC(O), CH2CH2, and CH2CH2CH2;

X0 isi selected from the group consisting of hydrido, hydroxy,

1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, 2,2,2-trifluoroethyl, 3,33-trifluoropropyl, 2,2,3,33-pentafluoropropyl, 2-aminoethyl, and 2-hydroxy ethyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, O, S, NH,

N(CH3), OCH2, and SCH2;

Q is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl,

3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl, 3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(l-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-S(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-propylamidocarbonyl)phenyl,

3-amino-S(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-S(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-antinophenyl, 3-amino-S(4-trifluoromethylbenzylamino)phenyl,

3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,

3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3 -fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,

3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,

3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,

2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,

3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19 benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine,

3-Qb-6-Qs-2-R16-5-R 18-4-R19 pyridine,

3-Qb-5-Qs-4-R16-2-R19 thiophene, and 2-Qb-5-Qs-3-R16-4-R17 thiophene;

R 16 and R19 are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R16 or R19 is optionally C(NR25)NR23R24 with the proviso that R16 ,

R 19, and Qb are not simultaneously hydrido;

R17 and R 18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is C(NR25)NR23R24 or hydrido;

R23, R24 , and R25 are independently hydrido or methyl;

Qs is CH2.

2. Compound of Claim 29 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R36, a carbon

adjacent to R32 and two atoms from the carbon at the point of attachment is

optionally substituted by R33 , a carbon adjacent to R36 and two atoms from the

carbon at the point of attachment is optionally substituted by R35, and any

carbon adjacent to both R33 and R35. is optionally substituted by R34;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Qb ;

A is a bond or (CH(R15 ))pa-(W7 )rr wherein rr is 0 or 1 , pa is an

integer selected from 0 through 3, and W7 is N(R7 );

R7 is hydndo or alkyl;

R15 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

X0 is selected from the group consisting of hydrido, alkyl, halo, haloalkyl, aminoalkyl, and hydroxyalkyl;

R1 is selected from the group consisting of hydrido, alkyl,

hydroxyalkyl, and haloalkyl;

R2 is Z0-Q;

Z0 is a bond;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10 , a carbon adjacent to R13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R12 is optionally substituted by R1 1 ;

R9 , R11 ,and R13 are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;

R10 and R 12 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy, amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido, carboxyalkyl, and cyano;

x is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs, a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is substituted by Qb , a carbon adjacent to the point of attachment of Qs is

optionally substituted by R17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R18, a carbon adjacent to Qb is

optionally substituted by R16, and another carbon adjacent to Qb is optionally

substituted by R 19;

R16 , R17 , R18 , and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R16 or R 19 is optionally NR20 R21 or C(NR25 )NR23 R24 , with the

proviso that R16 , R19 , and Qb are not simultaneously hydrido;

Q4 is selected from the group consisting of NR20 R21 , hydrido, and

C(NR25)NR23R24;

R20, R21, R23, R24, and R25 are independently hydrido or alkyl;

Qs is CH2.

33. Compound of Claim 32 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl,

2-furyl, 3-furyl, 2-pyπolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, and 5-isoxazolyl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R36, a carbon

adjacent to R32 and two atoms from the carbon at the point of attachment is optionally substituted by R33 , a carbon adjacent to R36 and two atoms from the

carbon at the point of attachment is optionally substituted by R35 , and any

carbon adjacent to both R33 and R35 is optionally substituted by R34 ;

R32, R33, R34 , R35, and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Qb;

A is selected from the group consisting of a bond, NH, N(CH3), CH2,

CH3CH, and CH2CH2;

X0 is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl,

2-hydroxyethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, propyl, 2,2,2-trifluoroethyl, 3,33-trifluoropropyl, 2,2333-pentafluoropropyl, and 2-hy droxy ethyl;

R2 is selected from the group consisting of phenyl, 2-thienyl, 2-furyl,

2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to the 4-pyridone ring is optionally substituted by R9, the other carbon adjacent to the carbon at the point of attachment is optionally substituted by R13, a carbon adjacent to R9 and two atoms from the carbon at

the point of attachment is optionally substituted by R10, a carbon adjacent to

R13 and two atoms from the carbon at the point of attachment is optionally substituted by R12, and any carbon adjacent to both R10 and R 12 is optionally

substituted by R1 1 ;

R9 , R1 1 , and R13 are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl,

N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl,

N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,

N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-( l-phenylethyl)amidocarbonyl, N-(1-methyl- l-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,

N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,

N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxy ethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine, 2-Qb-5-Qs-3-R16-4-R17thiophene,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine, 3-Qb-5-Qs-4-R16-2-R19thiophene,

3-Qb -5-Qs-4-R16-2-R19 furan, 2-Qb-5-Qs-3-R16-4-R 17 furan,

3-Qb-5-Qs-4-R16-2-R19 pyrrole, 2-Qb-5-Qs-3-R 16-4-R17 pyrrole,

4-Qb-2-Qs-5-R19 thiazole, and 2-Qb-5-Qs-4-R17 thiazole;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,

dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;

Qb is NR20 R21 or C(NR25)NR23R24;

R20 , R21 , R23 , R24 , and R25 are independently selected from the group consisting of hydrido, methyl, and ethyl;

Qs is CH2.

34. Compound of Claim 33 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of 2-aminophenyl,

3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl,

3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl,

3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl,

3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoromethylphenyl, 2-imidazoyl, 2-pyridyl, 3-pyridyl,

5-chloro-3-trifluoromethyl-2-pyridyl, 4-pyridyl, 2-thienyl, 3-thienyl, and 3-trifluoromethyl-2-pyridyl;

A is CH2 or CH2CH2;

X0 is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, and 2,2,2-trifluoroethyl;

R2 is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,

3-amino-5-(N-benzylamidocarbonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-S(N-(1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-S(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-S(N-propylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-S(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-S(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,

3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,

3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,

3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,

3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl,

2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl,

3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,

3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, Samino-2-thienyl, 5-amino-3-thienyl,

3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R 19 benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine,

3-Qb-5-Qs-4-R16-2-R 19 thiophene, and 2-Qb-5-Qs-3-R 16-4-R17 thiophene;

R16 and R19 are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R17 and R18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is C(NR25)NR23 R24 ;

R23, R24, and R25 are independently hydrido or methyl;

Qs is CH2.

35. Compound of Claim 34 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of 3-aminophenyl,

3-amidinophenyl, 4-amidinophenyl, 3-chlorophenyl, 4-chlorophenyl,

3,4-dichlorophenyl, 2-fluorophenyl, 4-methylphenyl, phenyl, 2-imidazoyl, 3-pyridyl, 4-ρyridyl, and 3-trifluoromethyl-2-pyridyl;

A is CH2 or CH2CH2;

X0 is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, and 2,2,2-trifluoroethyl;

R2 is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-S(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-propylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,

3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,

3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,

3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of 5-amidino-2-thienylmethyl,

4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amdinobenzyl.

36. Compound of Claim 29 where said compound is selected from the group of the Formula:


or a pharmaceutically acceptable salt thereof, wherein B, A, R1 , R2 , X0, and Y0 are selected to form a compound selected from the group consisting of;

R2 is 3-aminophenyl, B is phenyl, A is CH2,Y0 is 4-amidinobenzyl, and

R1 is methyl;

R2 is 3-aminophenyl, B is 3-chlorophenyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is phenyl, A is CH2, Y0 is 4-amidinobenzyl, and

R 1 is hydrido;

R2 is 3-aminophenyl, B is 2-imidazoyl, A is CH2CH2CH2, Y0 is 4-amidinobenzyl, and R is methyl;

R2 is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A is CH2CH2,

Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH2CH2,Y0 is 4-amidinobenzyl, and R1 is methyl;

2

R is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is 3-chlorophenyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)- phenyl, B is

3-chlorophenyl, A is CH2CH2,Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 3,5-diamιnophenyl, B is 3-chlorophenyl, A is CH2CH2,Y00 is 4-amidinobenzyl, and R 1 is methyl;

R 2 is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH2CH2,Y0 is

4-amidinobenzyl, and R1 is methyl;

R2 is 3-amidocarbonyl-Saminophenyl, B is 3-chlorophenyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R 1 is hydrido;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is 3-chlorophenyl, A is CH2CH2,Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)- phenyl, B is

3-chlorophenyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R 1 is hydrido;

R2 is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH2CH2,Y0 is 4-amidinobenzyl, and R1 is hydrido; and

R2 is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH2CH2,Y0 is

4-amidinobenzyl, and R1 is hydrido.

37. Compound of Claim 22 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32,

R33 , R34, R35, and R36 ;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Qb;

A is a bond or (CH(R 15))pa-(W7)rr wherein rr is 0 or 1, pa is an

integer selected from 0 through 3, and W7 is (R7 )NC(O) or N(R7);

R7 is selected from the group consisting of hydrido, hydroxy and alkyl;

R15 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

X0 is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;

R 1 is independently selected from the group consisting of hydrido, hydroxy, amino, hydroxyalkyl, alkyl, aminoalkyl, and haloalkyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, CH2CH2, W - (CH(R42))p wherein p is 0 or 1 and W0 is selected from the group consisting

of O, S, and N(R41);

R41 and R42 are independently hydrido or alkyl;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10, a carbon adjacent to R13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R12 is optionally substituted by R1 1;

R9, R1 1, and R13 are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio,

alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guamdino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,

heteroaralkoxy ,heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino,

alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl,

cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl,

cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo, haloalkyl, and cyano;

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs, a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is

substituted by Qb , a carbon adjacent to the point of attachment of Qs is

optionally substituted by R17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R18, a carbon adjacent to Qb is

optionally substituted by R16, and another carbon adjacent to Qb is optionally

substituted by R19;

R 16, R17, R18, and R19 are 1ndependently selected from the group consisting of hydrido, amidino, guamdino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R16 or R 19 is optionally selected from the group consisting of

NR20 R21 , N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23 R24 , with the

proviso that R 16, R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21 , hydrido,

C(NR25)NR23R24, and N(R26)C(NR25)N(R23)(R24), with the proviso that

no more than one of R20 and R21 is hydroxy at the same time and with the

further proviso that no more than one of R23 and R24 is hydroxy at the same time;

R20, R21, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, alkyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2, and

CH2CH2-

38. Compound of Claim 37 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, ethyl, 2-propynyl, 2-propenyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 1-methyl-2-butenyl,

1-methyl-3-butenyl, 1-methyl-2-butynyl, 3-pentyl, 1-ethyl-2-propenyl,

2-methylbutyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl,

1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl,

1-ethyl-3-butenyl, 1-propyl-2-propenyl, 1-ethyl-2-butynyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl, 3-heptynyl,

4-heptynyl, 5-heptynyl, 2-heρtyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl-4-h-xenyl, 1-methyl-5-hexenyl, 1-methyl-2-hexynyl,

1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl, 1-butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 333-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to

A with one or more of the group consisting of R32 , R33 , R34 , R35 , and R36 ;

R32 , R33 , R34 , R35 , and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, 2,2333-pentafluoropropyl, trifluoromethoxy,

1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl,

N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hy droxy ethyl, 2,2,2-trifluoro-1-hydroxyethyl,

methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,

N,N-dimethylamidocarbonyl, cyano, and Qb ;

A is selected from the group consisting of bond, NH, N(CH3), N(OH),

CH2, CH3CH, CF3CH, NHC(O), N(CH3)C(O), C(O)NH, C(O)N(CH3),

CH2CH2, CH2CH2CH2, CH3CHCH2, and CF3CHCH2;

X0 is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy , fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, n-butyl, 2,2,2-trifluoroethyl, 333-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl, 2-aminoethyl, 3-aminopropyl, 2-hydroxyethyl, 3-hydroxypropyl, and 23-dihydroxypropyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, CH2CH2, O,

S, NH, N(CH3), OCH2, SCH2, N(H)CH2, and N(CH3)CH2;

Q is selected from the group consisting of phenyl, 2-thienyl,

3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl,

5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 13,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent

to the carbon at the point of attachment is optionally substituted by R13, a

carbon adjacent to R9 and two atoms from the carbon at the point of attachment

is optionally substituted by R10, a carbon adjacent to R13 and two atoms from

the carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R12 is optionally substituted by R1 1;

R9, R1 1, and R13 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,

2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyythyl,

2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl,

N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, amidino, guamdino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,

methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl,

1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl,

N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl,

2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl,

N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl,

N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(l-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl , N-benzylamidosulf onyl , N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl,

N-isopropylamidocarbonyl, N-propylamidocarbonyl ,

N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,

N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,

3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,

5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethyIphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,Sdifluorobenzyloxy, 3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,Sdifluorophenoxy,

3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,

3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy,

2-fluoro-3 -trifluoromethylbenzyloxy , 3-fluoro-5-trifluoromethylbenzyloxy , 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy,

2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,

4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino,

1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl , 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy , 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy,

3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy,

2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl,

3 ,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy ,

3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy,

4-trifluoromethylthiobenzyloxy , 2,3 ,4-trifluorophenoxy , 23 ,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(l,1,2,2-tetrafluoroethoxy)phenoxy, and

3-trifluoromethylthiophenoxy;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19benzene,

2-Qb -5-Qs -6-R17 -4-R18 -3-R19 pyridme,

3-Qb-6-Qs-2-R16-5-R 18-4-R19 pyridine, 2-Qb-5-Qs-3-R16-6-R18 pyrazine,

3-Qb-6-Qs-2-R18-5-R18-4-R19 pyridazine,

2-Qb-5-Qs-4-R17-6-R18 pyrimidine, 5-Qb-2-Qs-4-R16-6-R19 pyrimidine,

3-Qb-5-Qs-4-R16-2-R19 thiophene, 2-Qb-5-Qs-3-R16-4-R17 thiophene,

3-Qb-5-Qs-4-R 16-2-R19 furan, 2-Qb-5-Qs-3-R 16-4-R17 furan,

3-Qb-5-Qs-4-R16-2-R19 pyrrole, 2-Qb-5-Qs-3-R16-4-R17 pyrrole,

4-Qb-2-Qs-5-R19 imidazole, 2-Qb-4-Qs-5-R17 imidazole,

3-Qb-5-Qs-4-R16 isoxazole, 5-Qb-3-Qss-4-R 16 isoxazole,

2-Qb-5-Qs-4-R16 pyrazole, 4-Qb-2-Qs-5-R19 thiazole, and

2-Qb-5-Qs-4-R17 thiazole;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino,

guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,

aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino,

N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio,

methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,333-pentafluoropropyl,

trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,

hydroxymethyl, 1-hydroxyethyl, 2-hy droxy ethyl, and cyano;

R16 or R19 is optionally selected from the group consisting of NR20 R21,

C(NR25)NR23R24, and N(R26)C(NR25)N(R23)(R24), with the proviso that R16,

R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21, hydrido,

C(NR25))R23R24, and N(R26)C(NR25)N(R23)(R24), with the proviso that no

more than one of R20 and R21 is hydroxy at the same time and with the further

proviso that no more than one of R23 and R24 is hydroxy at the same time;

R20, R21, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, and hydroxy;

Q is selected from the group consisting of a bond, CH2, and CH2CH2.

39. Compound of Claim 38 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl,

tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl,

6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl,

1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl,

2-dimethylaminoproρyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hy droxy ethyl,

2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl,

3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl,

3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;

A is selected from the group consisting of a bond, CH2, NHC(O),

CH2CH2, CH2CH2CH2, and CH3CHCH2;

X0 is selected from the group consisting of hydrido, hydroxy, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, 2,2,2-trifluoroethyl, 333-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl, 2-aminoethyl, and 2-hydroxyethyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, O, S, NH,

N(CH3), OCH2, and SCH2;

Q is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-S(2-phenylethyl)phenyl,

3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenyIethylamino)phenyl,

3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-S(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-ρropylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,

3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, 3-amino-S(4-tiifluoromethylbenzylamino)phenyl,

3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,

3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2-hy droxy phenyl, 3-hydroxyphenyl,

3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,

3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyI, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,

2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,

3-bromo-2-tbienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

x is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19benzene,

2-Qb -5-Qs -6-R17 -4-R18 -3-R19 pyridine,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine,

3-Qb -5-Qs -4-R16 -2-R19 thiophene, and 2-Qb -5-Qs -3-R16 -4-R17 thiophene;

R16 and R19 are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R16 or R19 is optionally C(NR25 )NR23 R24 with the proviso that R ,

R19, and Qb are not simultaneously hydrido;

R17 and R18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is C(NR25)NR23R24 or hydrido;

R23, R24, and R25 are independently hydrido or methyl;

Qs is i CH2.

40. Compound of Claim 37 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32,

R33 , R34, R35, and R36;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q ;

A is a bond or (CH(R15))pa-(W7)rr wherein rr is 0 or 1, pa is an

integer selected from 0 through 3, and W7 is N(R7);

R7 is hydrido or alkyl;

R15 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

X0 is selected from the group consisting of hydrido, alkyl, halo, haloalkyl, aminoalkyl, and hydroxyalkyl;

R1 is selected from the group consisting of hydrido, alkyl,

hydroxyalkyl, and haloalkyl;

1014

R2 is Z0-Q;

Z0 is a bond;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10, a carbon adjacent to R13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R12 is optionally substituted by R1 1;

R9, R1 1, and R13 are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guamdino, alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy,

alkoxyamino, hydroxy, amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido, carboxyalkyl, and cyano;

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs, a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is

substituted by Qb , a carbon adjacent to the point of attachment of Qs is

optionally substituted by R17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R18, a carbon adjacent to Q is optionally substituted by R16 , and another carbon adjacent to Qb is optionally

substituted by R19 ;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R16 or R19 is optionally selected from the group consisting of

NR20 R21, N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23 R24 , with the

proviso that R16, R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21, hydrido,

N(R26 )C(NR25 )N(R23 )(R24 ), and C(NR25 )NR23 R24 ;

R20, R21, R23, R24, R25, andR26 are independently hydrido or alkyl;

Qs is CH2.

41. Compound of Claim 40 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 2-methyl-2-butenyl,

3-methylbutyl, 3-methyl-2-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl,

1-methyl-3-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl^4-hexenyl, 1-methyl-2-hexynyl,

1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl,

1-ethyl-3-pentenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl,

4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 3,33-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Qb ;

A is selected from the group consisting of a bond, NH, N(CH3), CH2,

CH3CH, and CH2CH2;

A is optionally selected from the group consisting of CH2N(CH3),

CH2N(CH2CH3), CH2CH2N(CH3), and CH2CH2N(CH2CH3) with the proviso that B is hydrido;

X0 is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl,

2-hy droxy ethyl , chloro, and fluoro;

R 1 is selected from the group consisting of hydrido, methyl, ethyl, propyl, 2,2,2-trifluoroethyl, 333-trifluoropropyl, 2,2333-pentøfluoropropyl, and 2-hy droxy ethyl;

R2 is selected from the group consisting of phenyl, 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-ρyridyl, and 3-pyridyl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to the 4-pyridone ring is optionally substituted by R9, the other carbon adjacent to the carbon at the point of attachment is optionally substituted by R13, a carbon adjacent to R9 and two atoms from the carbon at the point of attachment is optionally substituted by R10, a carbon adjacent to

R13 and two atoms from the carbon at the point of attachment is optionally

substituted by R12 , and any carbon adjacent to both R10 and R12 is optionally

substituted by R1 1 ;

R9 , R1 1 , and R13 are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl,

N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl,

N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,

N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,

N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,

N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R 16-3-R17-5-R18-6-R19 benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine, 2-Qb-5-Qs-3-R16-4-R17thiophene,

-Qb-6-Qs-2-R16-5-R18-4-R19pyridine, 3-Qb-5-Qs-4-R16-2-R19thiophene,

-Qb-5-Qs-4-R16-2-R19furan, 2-Qb-5-Qs-3-R16-4-R17furan,

3-Qb -5-Qs-4-R 16 -2-R19 pyrrole, 2-Qb -5-Qs-3-R16 -4-R17 pyrrole,

4-Qb -2-Qs -5-R19 thiazole, and 2-Qb -5-Qs -4-R17 thiazole;

R16 , R17 , R18 , and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,

dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;

Qb is selected from the group consisting of NR20 R21,

C(NR25 )NR23 R24 , and N(R26 )C(NR25 )N(R23 )(R24 );

R20 , R21 , R23 , R24 , R25 , and R26 are independently selected from the group consisting of hydrido, methyl, and ethyl;

Qs is CH2.

42. Compound of Claim 41 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-ρentyl, 3-hydroxypropyl,

1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;

A is selected from the group consisting of a bond, CH2, CH3CH, and

CH2CH2;

X0 is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, and 2,2,2-trifluoroethyl;

R2 is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,

3-amino-5-(N-benzylamidocarbonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl ,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-S(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-ρropylamidocarbonyl)phenyl,

3-amino-S(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,

3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl ,

3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,

3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,

3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of:

1-Qb -4-Qs-2-R16 -3-R 17 -5-R 18 -6-R19 benzene,

2-Qb -5-Qs -6-R 17 -4-R 18 -3-R19 pyridine,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine,

3-Qb -5-Qs -4-R 16 -2-R19 thiophene, and 2-Qb -5-Qs -3-R16 -4-R17 thiophene;

R16 and R19 are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R17 and R18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is C(NR25 )NR23 R24 ;

R23 , R24 , and R25 are independently hydrido or methyl;

Qs is CH2.

43. Compound of Claim 42 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl,

1-methoxy-2-ρropyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl,

3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;

A is selected from the group consisting of a bond, CH2, CH3CH, and

CH2CH2;

X0 is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, and

2,2,2-trifluoroethyl;

R2 is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-propylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,

3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,

3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,

3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,

3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of 5-amidino-2-thienylmethyl,

4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amidinobenzyl.

44. Compound of Claim 37 where said compound is selected from the group of the Formula:


or a pharmaceutically acceptable salt thereof, wherein B, A, R1 , R2 , X0, and Y0 are selected to form a compound selected from the group consisting of;

R2 is 3-aminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is (S)-2-butyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 5-amino-2-fluorophenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 2-methyl-3-aminophenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is ethyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is ethyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-proρenyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 3-aminophenyl, B is isopropyl, A is a bond, Y0 is 4-amidmo-2-fluorobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is isopropyl, A is a bond, Y0 is 4-amidιnobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-butyl, A is a bond, Y0 is 4-amidinobenzyl, and

R is methyl;

R2 is 3-aminophenyl, B is (R)-2-butyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-propynyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 3-aminophenyl, B is 3-pentyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-aminophenyl, B is hydrido, A is CH2, Y0 is 4-amidinobenzyl, and

R1 is methyl;

R2 is 3-aminophenyl, B is ethyl, A is CH2, Y0 is 4-amidinobenzyl, and R is methyl;

R 2 is 3-aminophenyl, B is 2-methypropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-propyl, A is CH3CH, Y0 is 4-amιdmobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is propyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R 2 is 3-aminophenyl, B is 6-amidocarbonylhexyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is tert-butyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-aminophenyl, B is tert-butyl, A is a bond, Y0 is 4-amidmobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 3-hydroxypropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-methylpropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is butyl, A is a bond, Y0 is 4-amidinobenzyl, and

R 1 is methyl;

R 2 is 3-aminophenyl, B is 1-methoxy-2-propyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-methoxyethyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-propyl, A is a bond, Y0 is 5-amidino-2-thienylmethyl, and R1 is methyl;

R2 is 5-amino-2-methylthiophenyl, B is 2-propyl, A is a bond, Y0 is 4-amidinobenzyl, and R is methyl;

R 2 is 3-amino-Scarboxyphenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-Scarbomethoxyphenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is ethyl;

R2 is 3-amino-5-carboxamidophenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-benzyl-N-methylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(l-phenylethyl)amidocarbonyl)phenyl, B is isopropyl,

A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-phenyl-2-propyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-(2,4-dichlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(4-bromobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl , and R1 is methyl ;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl, B is isopropyl,

A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(3-trifluoromethylbenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-isobutylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-cyclobutylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-cycloρentylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-cycloheptylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(3-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-(2-(4-methoxyphenyl)ethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(3-phenylpropyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2,2-diphenylethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-(2-naphthylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-(1,23,4-tetrahydronaphth-2-ylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-propyl, A is a bond, Y0 is 4-amidino-3-fluorobenzyl, and R1 is hydrido;

R 2 is 3-carboxyphenyl, B is 2-proρyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-ammophenyl, B is 2-propyl, A is a bond, Y0 is 4-amιdino-3-fluorobenzyl, and R 1 is methyl;

R2 is 3 ,5-diaminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3,5-diaminophenyl, B is (S)-2-butyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R 2 is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3 ,5-diaminophenyl, B is isopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzylbenzyl, and R1 is methyl;

R 2 is 3,5-diaminophenyl, B is ethyl, A is a bond, Y0 is 4-amidinobenzyl, and

R1 is methyl;

R2 is 3,5-diaminophenyl, B is ethyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-carboxyphenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y0 is

4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-carboxyphenyl, B is (S)-2-butyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzylbenzyl, and R1 is methyl;

R2 is 3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-Scarboxyphenyl, B is ethyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 2,2,2-trifluoroethyl,

A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is (S)-2-butyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyI)phenyI, B is isopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzylbenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is a bond,

Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is a bond,

Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl; and

R2 is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y0 is 4-amidinobenzylbenzyl, and R1 is hydrido.

45. Compound of Claim 22 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is a C3-C7 cycloalkyl or a C4-C6 saturated heterocyclyl, wherein each ring carbon is optionally substituted with R33 , a ring carbon other than the ring carbon at the point of attachment of B to A is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbons and a nitrogen adjacent to the carbon atom at the point of attachment are optionally substituted with R9 or R13 , a ring carbon or

mtrogen adjacent to the R9 position and two atoms from the point of attachment

is optionally substituted with R10 , a ring carbon or nitrogen adjacent to the R 13

position and two atoms from the point of attachment is optionally substituted with R12, a ring carbon or nitrogen three atoms from the point of attachment

and adjacent to the R10 position is optionally substituted with R 1 1, a ring carbon or nitrogen three atoms from the point of attachment and adjacent to the

R12 position is optionally substituted with R33, and a ring carbon or nitrogen

four atoms from the point of attachment and adjacent to the R1 1 and R33

positions is optionally substituted with R34;

R9, R11 , and R13 are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;

R 10 and R12 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,

heteroaralkoxy ,heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino,

alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl,

cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl,

cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo, haloalkyl, and cyano;

R33 and R34 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy,

carboxamido, and cyano;

R33 is optionally Qb;

A is a bond or (CH(R15))pa-(W7)rr wherein rr is 0 or 1 , pa is an

integer selected from 0 through 3, and W7 is (R7)NC(O) or N(R7);

R7 is selected from the group consisting of hydrido, hydroxy and alkyl;

R15 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

X is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;

R1 is independently selected from the group consisting of hydrido, hydroxy, amino, hydroxyalkyl, alkyl, aminoalkyl, and haloalkyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, CH2CH2,

W0 -(CH(R42 ))p wherein p is 0 or 1 and W0 is selected from the group

consisting of O, S, and N(R41);

R41 and R42 are independently hydrido or alkyl;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R 13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10, a carbon adjacent to R13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R 12 is optionally substituted by R1 1;

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs , a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is

substituted by Qb , a carbon adjacent to the point of attachment of Qs is

optionally substituted by R 17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R18 , a carbon adjacent to Qb is optionally substituted by R16, and another carbon adjacent to Qb is optionally

substituted by R19;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guamdino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R 16 or R19 is optionally NR20 R21 or and C(NR25 )NR23 R24 , with the

proviso that R16, R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21 , hydrido, and

C(NR25 )NR23 R24 , with the proviso that no more than one of R20 and R21 is

hydroxy at the same time and with the further proviso that no more than one of R23

and R24 is hydroxy at the same time;

R20, R21, R23, R24, and R25 are independently selected from the group consisting of hydrido, alkyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2, and

CH2CH2.

46. Co4pound of Claim 45 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of cyclopropyl, cyclobutyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, thiaetan-3-yl, cyclopentyl, cyclohexyl, norbornyl, 7-oxabicyclo[2.2.1]heptan-2-yl,

bicyclo[3.1.0]hexan-6-yl, cycloheptyl, 2-morpholmyl, 3-morpholinyl,

4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl,

3-ρiρeridinyl, 4-piρeridinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-ρyrrolidinyl,

2-dioxanyl, 4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 4H-pyran-4~one-2-yl, 4H-ρyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl,

2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl,

2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein each ring carbon is optionally substituted with R33 , ring carbons and a mtrogen adjacent to the

carbon atom at the point of attachment are optionally substituted with R9 or

R13, a ring carbon or nitrogen adjacent to the R9 position and two atoms from

the point of attachment is optionally substituted with R10, and a ring carbon or

nitiogen adjacent to the R13 position and two atoms from the point of

attachment is optionally substituted with R12;

R9, R1 1, and R 13 are independently selected from the group consisting of hydrido, amidino, guamdino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,

2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, amidino, guamdino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl,

N,N-dimethylamidosulfonyl, hydroxymethyl, 1 -hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,

amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,

N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,

N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,

N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy,

3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino,

5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy,

2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy,

3 ,5-difluorophenoxy, 3 ,5-difluorobenzyloxy, 4-difluoromethoxybenzyIoxy , 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy,

3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy,

3 ,5-dimethylbenzyloxy, 4-ethoxyphenoxy , 4-ethylbenzyloxy , 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy,

2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-5-trifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy,

4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4~isopropyl-3-methylphenoxy, phenylamino,

1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy,

3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy,

2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl,

3 ,5-bis-trifluoromethylbenzyloxy , 4-trifluoromethylphenoxy,

3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy,

4-trifluoromethylthiobenzyloxy, 23,4-trifluorophenoxy, 2,3,Strifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and

3-trifluoromethylthiophenoxy;

R33 is selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropooy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio,

trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl,

2,2333-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl,

N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxy ethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl,

amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Qb;

A is selected from the group consisting of a bond, NH, N(CH3),

N(OH), CH2, CH3CH, CF3CH, NHC(O), N(CH3)C(O), C(O)NH,

C(O)N(CH3), CH2CH2, CH2CH2CH2, CH3CHCH2, and CF3CHCH2;

X0 is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, n-butyl, 2,2,2-trifluoroethyl, 3,33-trifluoropropyl, 2,2333-pentafluoropropyl, 2-aminoethyl, 3-aminopropyl, 2-hydroxyethyl, 3- hydroxypropyl, and 23-dihydroxyρropyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, CH2CH2, O,

S, NH, N(CH3), OCH2, SCH2, N(H)CH2, and N(CH3)CH2;

Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl,

3-pyridazinyl, 4-pyridazinyl, and 13,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z is optionally substituted by R9, the other carbon adjacent to the carbon at the point

of attachment is optionally substituted by R 13, a carbon adjacent to R9 and two atoms from the carbon at the point of attachment is optionally substituted by R10 , a carbon adjacent to R13 and two atoms from the carbon at the point of

attachment is optionally substituted by R12, and any carbon adjacent to both

R10 and R12 is optionally substituted by R1 1;

Y is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19 benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine,

3-Qb-6-Qs-2-R16-5-R18-4-R19 pyridine, 2-Qb-5-Qs-3-R16-6-R 18 pyrazine,

3-Qb-6-Qs-2-R18-5-R18-4-R19pyridazine,

2-Qb-5-Qs-4-R17-6-R 18 pyrimidine, 5-Qb-2-Qs-4-R16-6-R19 pyrimidine,

3-Qb-5-Qs-4-R16-2-R19 thiophene, 2-Qb-5-Qs-3-R16-4-R17 thiophene,

3-Qb-5-Qs-4-R16-2-R19 furan, 2-Qb-5-Qs-3-R16-4-R17 furan,

3-Qb-5-Qs-4-R16-2-R19pyrrole, 2-Qb-5-Qs-3-R16-4-R17pyrrole,

4-Qb -2-Qs -5-R19 imidazole, 2-Qb -4-Qs -5-R17 imidazole,

3-Qb -5-Qs -4-R16 isoxazole, 5-Qb -3-Qs -4-R16 isoxazole,

2-Qb -5-Qs -4-R16 pyrazole, 4-Qb -2-Qs -5-R19 thiazole, and

2-Qb -5-Qs -4-R17 thiazole;

R16 , R 17 , R18 , and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino,

aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio,

methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2333-pentafluoropropyl,

trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo,

hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;

R16 or R19 is optionally C(NR25 )NR23 R24 with the proviso that R16 ,

R19 , and Qb are not simultaneously hydrido;

Qb is C(NR25 )NR23 R24 or hydrido, with the proviso that no more than

one of R23 and R24 is hydroxy at the same time;

R23 , R24 , and R25 are independently selected from the group consisting of hydrido, methyl, ethyl, and hydroxy;

Qs is selected from the group consisting of a bond, CH2 and CH2CH2.

47. Compound of Claim 46 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, 1-pyrrolidinyl, 1-piperidinyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl,

azetidin-3-yl, 7-oxabicyclo[2.2.1jheptan-2-yl, bicyclo[3.1.0]hexan-6-yl,

2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piρerazinyl,

1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl,

2-pyrrolidinyl, 3-ρyrrolidinyl, 2-dioxanyl, 4H-2-pyranyl, 4H-3-pyranyl,

4H-4-pyranyl, 4H-pyran-4-one-2-yl, 4H-pyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl,

4-tetrahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl;

A is selected from the group consisting of a bond, CH2, NHC(O),

CH2CH2, and CH2CH2CH2;

X0 is selected from the group consisting of hydrido, hydroxy, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, 2,2,2-trifluoroethyl, 3,33-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl, 2-aminoethyl, and 2-hy droxy ethyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, CH2, O, S, NH,

N(CH3), OCH2, and SCH2;

Q is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl,

3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl,

3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl ,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-S(N-propylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, Samino-2-fluorophenyl,

3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, 3-amino-S(4-trifluoromethylbenzylamino)phenyl,

3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,

3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,

3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,

3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,

2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,

3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of:

1-Qb-4-Qs-2-R16-3-R17-5-R18-6-R19benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine,

3-Qb-5-Qs-4-R16-2-R19thiophene, and 2-Qb-5-Qs-3-R16-4-R17thiophene;

R16 and R19 are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R16 or R19 is optionally C(NR25 )NR23 R24 with the proviso that R ,

R19, and Qb are not simultaneously hydrido;

R17 and R18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is C(NR25)NR23R24 or hydrido;

R23, R24, and R25 are independently hydrido or methyl;

Qs is CH2.

8. Compound of Claim 45 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is a C3-C7 cycloalkyl or a C4-C6 saturated heterocyclyl, wherein each ring carbon is optionally substituted with R33, a ring carbon other than the ring carbon at the point of attachment of B to A is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbons and a nitrogen adjacent to the carbon atom at the point of attachment are optionally substituted with R9 or R13, a ring carbon or

nitrogen adjacent to the R9 position and two atoms from the point of attachment

is optionally substituted with R10, a ring carbon or nitrogen adjacent to the R13

position and two atoms from the point of attachment is optionally substituted with R12, a ring carbon or nitrogen three atoms from the point of attachment

and adjacent to the R10 position is optionally substituted with R1 1, a ring carbon or nitrogen three atoms from the point of attachment and adjacent to the

R12 position is optionally substituted with R33, and a ring carbon or nitrogen

four atoms from the point of attachment and adjacent to the R1 1 and R33

positions is optionally substituted with R34 ;

R9, R1 1, and R131 are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy, amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido, carboxyalkyl, and cyano;

R33 and R34 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, and cyano;

R33 is optionally Qb ;

A is a bond or (CH(R15 ))pa-( W7 )rr wherein rr is 0 or 1 , pa is an

integer selected from 0 through 3, and W7 is N(R7 );

R7 is hydrido or alkyl;

R 15 is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;

X0 is selected from the group consisting of hydrido, alkyl, halo, haloalkyl, aminoalkyl, and hydroxyalkyl;

R 1 is selected from the group consisting of hydrido, alkyl,

hydroxyalkyl, and haloalkyl;

R2 is Z0-Q;

Z0 is a bond;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9 , the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10, a carbon adjacent to R13 and two atoms from the carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R 10 and R12 is optionally substituted by R1 1 ;

Y0 is phenyl or a heteroaryl of 5 or 6 ring members, wherein one carbon of said phenyl or said heteroaryl is substituted by Qs, a carbon two or three

atoms from the point of attachment of Qs to said phenyl or said heteroaryl is

substituted by Qb, a carbon adjacent to the point of attachment of Qs is

optionally substituted by R17, another carbon adjacent to the point of

attachment of Qs is optionally substituted by R18 , a carbon adjacent to Qb is

optionally substituted by R16, and another carbon adjacent to Qb is optionally

19

substituted by R ;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R16 or R19 is optionally NR20 R21 or C(NR25)NR23 R24, with the

proviso that R 16, R19, and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21, hydrido, and

C(NR25 )NR23 R24 ;

R20 , R21 , R23 , R24 , and R25 are independently hydrido or alkyl;

Qs is CH2i

49. Compound of Claim 48 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, bicyclo[3.1.0]hexan-6-yl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 2-tetiahydrofuranyl,

3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl,

4-tetiahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein each ring carbon is optionally substituted with R33 , ring carbons and a nitrogen adjacent to the carbon atom at the point of attachment are optionally substituted with R9 or R13 , a ring carbon or nitrogen adjacent to the R9 position and two

atoms from the point of attachment are optionally substituted with R10, and a

ring carbon or nitrogen atom adjacent to the R13 position and two atoms from

the point of attachment is optionally substituted with R12 ;

R9, R 11, and R13 are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl,

N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;

R1 0 and R12 are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl,

N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,

N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1--henylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,

N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,

N-cyclohexylamidocarbonyl, guamdino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hy droxy ethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;

R33 is selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, carboxy, amino,

N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, cyano, and Qb ;

A is selected from the group consisting of a bond, NH, N(CH3), CH2,

CH3CH, CH2CH2, and CH2CH2CH2;

X0 is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl,

2-hy droxy ethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, propyl, 2,2,2-trifluoroethyl, 333-trifluoropropyl, 2,2,333-pentafluoropropyl, and 2-hydroxy ethyl;

R2 is selected from the group consisting of phenyl, 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to the 4-pyridone ring is optionally substituted by R9 , the other carbon adjacent to the carbon at the point of attachment is optionally substituted by R13, a carbon adjacent to R9 and two atoms from the carbon at

the point of attachment is optionally substituted by R10, a carbon adjacent to

R13 and two atoms from the carbon at the point of attachment is optionally

substituted by R12, and any carbon adjacent to both R10 and R12 is optionally

substituted by R1 1;

x is selected from the group consisting of:

1-Qb -4-Qs -2-R16 -3-R17 -5-R 18 -6-R19 benzene,

2-Qb-5-Qs-6-R17-4-R18-3-R19pyridine, 2-Qb-5-Qs-3-R16-4-R17thiophene,

3-Qb-6-Qs-2-R16-5-R18-4-R19pyridine, 3-Qb-5-Qs-4-R16-2-R19thiophene,

3-Qb-5-Qs-4-R16-2-R19furan, 2-Qb-5-Qs-3-R16-4-R17furan,

3-Qb -5-Qs-4-R16 -2-R 19 pyrrole, 2-Qb -5-Qs-3-R16 -4-R17 pyrrole,

4-Qb -2-Qs -5-R19 thiazole, and 2-Qb -5-Qs -4-R17 thiazole;

R 16, R17, R18, and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino,

dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;

Qb is NR20 R21 or C(NR25 )NR23 R24;

R20, R21 , R23, R24, and R25 are independently selected from the group consisting of hydrido, methyl, and ethyl;

Qs is CH2.

50. Compound of Claim 49 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, 1-pyrrolidinyl and 1-piρeridinyl;

A is selected from the group consisting of a bond, CH2, CH2CH2 and

CH2CH2CH2;

X0 is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, and 2,2,2-trifluoroethyl;

R2 is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,

3-amino-5-(N-benzylamidocarbonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl ,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-propylamidocarbonyl)phenyl ,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,

3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,

3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,

3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl,

2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,

3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, Samino-3-thienyl,

3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of:

1-Qb -4-Qs -2-R16 -3-R17 -5-R18 -6-R 19 benzene,

2-Qb-5-QS-6-R17-4-R18-3-R19pyridine,

3-Qb-6-QS-2-R16-5-R18-4-R19pyridine,

3-Qb -5-Qs -4-R16 -2-R 19 thiophene, and 2-Qb -5-Qs -3-R 16 -4-R 17 thiophene;

R 16 and R19 are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R17 and R18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is C(NR25 )NR23 R24 ;

R23 , R24 , and R25 are independently hydrido or methyl;

Qs is CH2.

51. Compound of Claim 50 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, and 1-piperidinyl;

A is selected from the group consisting of a bond, CH2, CH2CH2 and

CH2CH2CH2;

X0 is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, chloro, and fluoro;

R1 is selected from the group consisting of hydrido, methyl, ethyl, and 2,2,2-trifluoroethyl;

R2 is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(l-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3 -amino-5-(N-propylamidocarbonyl)phenyl ,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyI,

3-amino-5-(N-cycloρentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,

3-carboxy-5-aminophenyl, 3-chlorophenyl, 3 ,Sdiaminophenyl,

3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,

3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,

3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl;

Y0 is selected from the group consisting of 5-amidino-2-thienylmethyl, 4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amdinobenzyl.

52. Compound of Claim 45 where said compound is selected from the group of the Formula:


or a pharmaceutically acceptable salt thereof, wherein B, A, R , R , X°, and Y are selected to form a compound selected from the group consisting of;

R 2 is 3-aminophenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R 7 is 3-aminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R 7 is 3-aminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 7 is 3-aminophenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R 7 is 3-aminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-3-fluorobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is cyclopentyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 5-amino-2-thienyl, B is cyclobutyl, A is a bond, Y0 is 4- amidinobenzyl, and R 1 is methyl;

R2 is 3-ammophenyl, B is cyclopropyl, A is CH2, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 2-(2R)-bicyclo[2.2.1]-heptyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is cyclopentyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is cyclohexyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-aminophenyl, B is oxalan-2-yl, A is CH2, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-ammophenyl, B is 1-piperidinyl, A is CH2CH2, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-aminophenyl, B is 1-pyrrolidinyl, A is CH2CH2CH2, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond, Y0

is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-amino-Scarboxyphenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3,Sdiaminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R 2 is 2-amino-6-carboxy-4-pyridyl, B is cyclobutyl, A is a bond, Y0 is

4-amidinobenzyl, and R1 is hydrido;

R 2 is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond, Y0

is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amιno-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3, 5-diaminophenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is hydrido;

R 2 is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-3-fluorobenzyl, and R1 is methyl;

R2 is 3,5-diaminophenyl, B is cyclopentyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R 2 is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R 2 is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R 1 is methyl;

R2 is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-3-fluorobenzyl, and R1 is methyl;

R 2 is 3-carboxy-5-aminophenyl, B is cyclopentyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-3-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopentyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amιdosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-3-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopentyl, A is a bond, Y0 is 4-amidinobenzyl, and R 1 is methyl;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclopropyl, A is a bond, Y0 is 4-amidino-2-fluorobenzyl, and R1 is methyl;

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is hydrido;

R2 is 3-antino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y0 is 4-amidino-3-fluorobenzyl, and R1 is methyl; and

R2 is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl,

B is cyclopentyl, A is a bond, Y0 is 4-amidinobenzyl, and R1 is methyl.

53. Compound of Claim 22 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R36, a carbon adjacent to R32 and two atoms from the carbon at the point of attachment is

optionally substituted by R33, a carbon adjacent to R36 and two atoms from the

carbon at the point of attachment is optionally substituted by R35, and any

carbon adjacent to both R33 and R35 is optionally substituted by R34 ;

R32, R33, R34, R35, and R36 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, hydroxy, amino,

alkoxyamino, haloalkanoyl, nitro, alkylamino, alkylthio, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyalkyl, alkylamino, carboalkoxy, carboxy, carboxamido, cyano, and Q ;

B is optionally selected from the group consisting of hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36;

B is optionally a C3-C12 cycloalkyl or a C4-C9 saturated heterocyclyl, wherein each ring carbon is optionally substituted with R33 , a ring carbon other than the ring carbon at the point of attachment of B to A is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, ring carbons and a nitrogen adjacent to the carbon atom at the point of attachment are optionally substituted with R9 or R 13, a ring

carbon or nitrogen adjacent to the R9 position and two atoms from the point of

attachment is optionally substituted with R10, a ring carbon or nitrogen adjacent

to the R13 position and two atoms from the point of attachment is optionally

substituted with R12, a ring c,rbon or nitrogen three atoms from the point of attachment and adjacent to the R10 position is optionally substituted with R1 1 , a ring carbon or nitrogen three atoms from the point of attachment and adjacent to the R12 position is optionally substituted with R33, and a ring carbon or

nitrogen four atoms from the point of attachment and adjacent to the R1 1 and

R33 positions is optionally substituted with R34 ;

R9, R10, R1 1, R12, and R13 are independently selected from the group consisting of hydrido, acetamido, haloacetamido, alkoxyamino, alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy, haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy,

heteroaralkoxy ,heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl,

cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy,

hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy,

carboxyalkyl, carboxamido, and cyano;

A is a bond or (CH(R15 ))pa-(W7 )rr wherein rr is 0 or 1, pa is an

integer selected from 0 through 3, and W7 is selected from the group

consisting of O, S, C(O), (R7)NC(O), (R7)NC(S), and N(R7);

R7 is selected from the group consisting of hydrido, hydroxy and alkyl;

R15 is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;

X0 is selected from the group consisting of hydrido, amino, alkyl, cyano, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;

R1 is selected from the group consisting of hydrido, alkyl, haloalkyl, amino, aminoalkyl, alkylamino, hydroxy, and hydroxyalkyl;

R2 is Z0-Q;

Z0 is selected from the group consisting of a bond, (CR41 R42 )q

wherein q is 1 or 2, and (CH(R41))g-W0 -(CH(R42))p wherein g and p are integers independently selected from 0 through 3 and W is selected from the group consisting of O, S, C(O), S(O), N(R41), and ON(R41);

Z0 is optionally (CH(R41))e-W22-(CH(R42))h wherein e and h are

independently 0 or 1 and w22 is selected from the group consisting of

CR41 =CR42 , 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 13-cyclohexyl,

1,2-cyclopentyl, 13-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl,

2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl,

13-piperazinyl, 23-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl,

1 ,2-pyrrolidinyl, 1 ,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl,

2,5-pyrrolidinyl, 3,4-pyπolidinyl, 2,3-tetiahydrofuranyl, 2,4-tetrahydrofuranyl,

2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z is directly bonded to the 4-pyridone ring and W22 is optionally substituted with one or more

substituents selected from the group consisting of R9 , R 10 , R1 1 , R12 , and R13;

R41 and R42 are independently selected from the group consisting of hydrido, hydroxy, alkyl, and amino;

Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z0 is optionally substituted by R9, the other carbon adjacent to the

carbon at the point of attachment is optionally substituted by R13, a carbon

adjacent to R9 and two atoms from the carbon at the point of attachment is

optionally substituted by R10, a carbon adjacent to R13 and two atoms from the

carbon at the point of attachment is optionally substituted by R12, and any

carbon adjacent to both R10 and R12 is optionally substituted by R1 1, with the proviso that Q is other than a phenyl when Z0 is a bond;

Q is optionally hydrido with the proviso that Z0 is selected from other than a bond;

K is CHR4a wherein R4a is selected from the group consisting of hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;

E is selected from the group consisting of a bond, C(O)N(H), (H)NC(O), (R7)NS(O)2, and S(O)2N(R7);

YAT is Qb -Qs ;

Q is (CR37 R38)b wherein b is an integer selected from 1 through 4,

R37 is selected from the group consisting of hydrido, alkyl, and haloalkyl, and

R38 is selected from the group consisting of hydrido, alkyl, haloalkyl, aroyl, and heteroaroyl with the proviso that there is at least one aroyl or heteroaroyl substituent, with the further proviso that no more than one aroyl or heteroaroyl is bonded to (CR37 R38)b at the same time, with the still further proviso that said aroyl and said heteroaroyl are optionally substituted with one or more substituents selected from the group consisting of R16, R 17, R18, and R19, with another further proviso that said aroyl and said heteroaroyl are bonded to the CR37 R38 that is directly bonded to E0 , with still another further proviso

that no more than one alkyl or one haloalkyl is bonded to a CR37 R38 at the same time, and with the additional proviso that said alkyl and haloalkyl are bonded to a carbon other than the one bonding said aroyl or said heteroaroyl;

R16, R17, R18, and R19 are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;

R 16 or R19 is optionally selected from the group consisting of

NR20R21, N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23R24 with the

proviso that R16 , R19 , and Qb are not simultaneously hydrido;

Qb is selected from the group consisting of NR20 R21 , hydrido,

N(R26)C(NR25)N(R23)(R24), and C(NR25)NR23 R24 , with the proviso that

no more than one of R20 and R21 is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time and with the further proviso that no more than one of R23 and R24 is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time;

R20, R21, R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, alkyl, hydroxy, amino, alkylamino and dialkylamino.

54. Compound of Claim 53 of the Formula:


or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl,

3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, and 5-isoxazolyl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to A is optionally substituted by R32, the other carbon adjacent

to the carbon at the point of attachment is optionally substituted by R36 , a

carbon adjacent to R32 and two atoms from the carbon at the point of

attachment is optionally substituted by R33 , a carbon adjacent to R36 and two atoms from the carbon at the point of attachment is optionally substituted by R35, and any carbon adjacent to both R33 and R35 is optionally substituted by

R34

R32, R33 , R34, R35, and R36 are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Qb ; b

B is optionally selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl,

3-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 3-ρentyl, 2-methylbutyl,

2-methyl-2-butenyl, 3-methylbutyl, 3-methyl-2-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-heχyl,

1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-2-pentynyl,

1-methyl-3-ρentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-heptyl, 2-heρtenyl,

3-heptenyl, 4-heptenyl, 5-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heρtyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl,

1-methyl-4-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl,

1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl,

1-ethyl-2-pentynyl, 1-ethyI-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl,

5,5,6,6,6-pentafluorohexyl, and 333-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R32, R33, R34, R35, and R36;

B is optionally selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, oxalan-2-yl,

2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, bicyclo[3.1.0]hexan-6-yl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyπolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, and

3-tetrahydrothienyl, wherein each ring carbon is optionally substituted with R33 , ring carbons and a nitrogen adjacent to the carbon atom at the point of

attachment are optionally substituted with R9 or R 13, a ring carbon or nitrogen

adjacent to the R9 position and two atoms from the point of attachment is

optionally substituted with R10, and a ring carbon or nitrogen adjacent to the

R13 position and two atoms from the point of attachment is optionally

substituted with R12 ;

R9 , R1 1 , and R13 are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl,

N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;

R10 and R12 are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl,

N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl,

N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(l-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl,

N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl,

N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl,

N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl,

2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;

A is selected from the group consisting of a bond, NH, N(CH3), CH2,

CH3CH, CH2CH2, and CH2CH2CH2;

X0 is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy , fluoro, chloro, and bromo;

R 1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, propyl, n-butyl, 2,2,2-trifluoroethyl, 333-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl, 2-aminoethyl, 3-aminopropyl, 2-hydroxyethyl, 3-hydroxypropyl, and 2,3-dihydroxypropyl;

R2 is selected from the group consisting of phenyl, 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to the 4-pyridone ring is optionally substituted by R9, the other carbon adjacent to the carbon at the point of attachment is optionally substituted by R13, a carbon adjacent to R9 and two atoms from the carbon at

the point of attachment is optionally substituted by R10, a carbon adjacent to

R 13 and two atoms from the carbon at the point of attachment is optionally

substituted by R12 , and any carbon adjacent to both R10 and R12 is optionally

substituted by R1 1;

YAT is Qb-QS;

Q is selected from the group consisting of:

C[R37(benzoyI)(CR37R38)b],

C[R37 (2-pyridylcarbonyl)(CR37 R38 )b],

C[R37(3-pyridylcarbonyl)(CR37R38)b],

C[R37(4-pyridylcarbonyl)(CR37R38)b],

C[R37 (2-thienylcarbonyl)(CR37 R38 )b],

C[R37(3-thienylcarbonyl)(CR37R38)b],

C[R37(2-thiazolylcarbonyl)(CR37R38)b],

C[R37 (4-thiazolylcarbonyl)(CR37 R38 )b], and

C[R37 (5-thiazolylcarbonyl)( (CR37 R38 )b], wherein b is an integer selected

from 1 through 3, R37 and R38 are independently selected from the group consisting of hydrido, alkyl, and haloalkyl, with the proviso that said benzoyl and the heteroaroyls are optionally substituted with one or more substituents selected from the group consisting of R16, R 17, R18, and R19 with the proviso

that R17 and R18 are optionally substituted at a carbon selected from other than the meta and para carbons relative to the carbonyl of the benzoyl or heteroaroyl, with the further proviso that said benzoyl or said heteroaroyl are bonded to the carbon directly bonded to amide nitiogen of the l-(amidocarbonymethylene)

group, and with the still further proviso that is no more than one alkyl or one haloalkyl is bonded to a CR37 R38 at the same time;

R 16, R17, R18, and R19 are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;

Qb is C(NR25)NR23R24 or N(R26)C(NR25)N(R23)(R24);

R23, R24, R25, and R26 are independently selected from the group consisting of hydrido, methyl, and ethyl.

55. Compound of Claim 54 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of 2-aminophenyl,

3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl,

3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl,

3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-teifluoromethylphenyl, 2-imidazoyl, 2-pyridyl, 3-pyridyl,

5-chloro-3-trifluoromethyl-2-ρyridyl, 4-pyri4yl, 2-thienyl, 3-thienyl, and 3-trifluoromethyl-2-pyridyl ;

B is optionally selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-ρentyl, 3-pentyl, 2-methylbutyl,

2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-ρentyl,

3-hydroxyproρyl, 1-methoxy-2-proρyl, 2-methoxy ethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxyproρyl, 4-hydroxybutyl, 6-cyanohexyl,

2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;

B is optionally selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, 1-pyπolidinyl and 1-piperidinyl;

A is selected from the group consisting of a bond, CH2, CH3CH,

CH2CH2, and CH2CH2CH2;

X0 is selected from the group consisting of hydrido, hydroxy,l-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;

R1 is selected from the group consisting of hydrido, hydroxy, amino, methyl, ethyl, 2,2,2-trifluoroethyl, 3,33-trifluoropropyl, 2-aminoethyl, and

2-hydroxyethyl;

R2 is selected from the group consisting of

3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,

3-amino-S(N-benzylamidocarbonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-S(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl ,

3-anιino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-S(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-propylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cycloρentylamidocarbonyl)phenyl,

3-amino-S(N-cyclohexylamidocarbonyl)phenyl,

5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl,

Samino-3-methoxycarbonylphenyl, 3-amidinophenyl,

3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl,

3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3 -carboxy-5-hy droxy phenyl, 3-carboxymethyl-5-aminophenyl, 3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, ,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,

3-methanesulfonylaminophenyl, 2-methoxy phenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,

2-trifluoromethylphenyl, 5-amino-2-thienyl, Samino-3-thienyl,

3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;

YAT is Qb-QS;

Q is selected from the group consisting of:

[CH(benzoyl)](CH2)b, [CH(2-pyridylcarbonyl)](CH2)b,

[CH(3-pyridylcarbony!)j(CH2)b, [CH(4-pyridylcarbonyl)j(CH2)b,

[CH(2-thienylcarbonyl)](CH2)b,[CH(3-thienylcarbonyl)](CH2)b,

[CH(2-thiazolylcarbonyl)](CH2)b, [CH(4-thiazolylcarbonyl)](CH2)b,

and [CH(5-thiazolylcarbonyl)](CH2)b, wherein b is an integer selected from 1 through 3, with the proviso that said benzoyl and said heteroaroyls are optionally substituted with one or more substituents selected from the group consisting of R16, R 17, R18, and R19 with the proviso that R 17 and R 18 are optionally substituted at a carbon selected from other than the meta and para carbons relative to the carbonyl of the benzoyl or the heteroaroyl, and that said benzoyl or said heteroaroyl are bonded to the carbon directly bonded to amide nitiogen of the l-(amidocarbonymethylene) group;

R16 and R191re independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;

R17 and R 18 are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;

Qb is N(R26)C(NR25)N(R23)(R24);

R23, R24, R25, and R26 are independently hydrido or methyl.

56. Compound of Claim 55 or a pharmaceutically acceptable salt thereof, wherein;

B is selected from the group consisting of 3-aminophenyl,

3-amidinophenyl, 4-amidinophenyl, 3-chlorophenyl, 4-chlorophenyl,

3 ,4-dichlorophenyl, 2-fluorophenyl, 4-methylphenyl, phenyl, 2-imidazoyl, 3-pyridyl, 4-pyridyl, and 3-trifluoromethyl-2-pyridyl;

B is optionally selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl,

(S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl,

2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4~methyl-2-pentyl,

3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxy ethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hy droxy ethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl,

2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;

B is optionally selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, and 1-piρeridinyl;

A is selected from the group consisting of a bond, CH2, CH2CH2 and

CH2CH2CH2;

X0 is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl,

2-hydroxyethyl, chloro, and fluoro;

R 11 is selected from the group consisting of hydrido, methyl, ethyl,

2,2,2-trifluoroethyl, 333-trifluoropropyl, and 2-hydroxy ethyl;

3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,

3-amino-S(N-(3-fluorobenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,

3-amino-5-(N-benzylamidosulfonyl)phenyl,

3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,

3-amino-5-(N-ethylamidocarbonyl)phenyl,

3-amino-5-(N-isopropylamidocarbonyl)phenyl,

3-amino-5-(N-ρropylamidocarbonyl)phenyl,

3-amino-5-(N-isobutylamidocarbonyl)phenyl,

3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,

3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,

3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,

3-amino-5-(N-cyclohexylarnidocarbonyl)phenyl, 3-aminophenyl,

3-carboxy-Saminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,

3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,

3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl;

YAT is selected from the group consisting of 5-guani dino- 1 -oxo- 1 -(2-thiazolyl)-2-pentyl, Sguanidino-1-oxo-1-(4-thiazolyl)-2-pentyl, 5-guanidino-1-oxo-1-(5-thiazolyl)-2-pentyl, 5- guanidino- 1 -oxo- l-(4-amino-2-thiazolyl)-2-pentyl, and 5- guanidino- 1 -oxo- 1 -phenyl-2-ρentyl .

57. A compound as recited in Claim 53 where said compound is selected from the group of the Formula:


or a pharmaceutically acceptable salt thereof, wherein B, A, R 1, R2 , X0, and YAT are selected to form a compound selected from the group consisting of;

R2 is 3-aminophenyl, B is phenyl, A is CH2CH2, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is hydrido, and X° is hydrido;

R2 is 3,5-diaminophenyl, B is phenyl, A is CH2CH2, YAT is 5- guanidino- 1-oxo-1-(2-thiazolyl)-2-pentyl, R is hydrido, and X° is hydrido;

R2 is 3-carboxy-5-aminophenyl, B is phenyl, A is CH2CH2,YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R 1 is hydrido, and X0 is hydrido;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is phenyl, A is

CH2CH2, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R 1 is hydrido, and

X0 is hydrido;

R2 is 3,Sdiaminophenyl, B is isopropyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is hydrido, and X0 is hydrido;

R2 is 3-carboxy-Saminophenyl, B is isopropyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-ρentyl, R1 is hydrido, and X0 is hydrido;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is hydrido, and

X0 is hydrido;

R2 is 3,Sdiaminophenyl, B is cyclobutyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-ρentyl, R1 is hydrido, and X0 is hydrido;

R2 is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is hydrido, and X0 is hydrido;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is hydrido, and X0 is hydrido;

R2 is 3-aminophenyl, B is phenyl, A is CH2CH2, YAT is 5-guanidino- 1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and X0 is hydrido;

R2 is 3,5-diaminophenyl, B is phenyl, A is CH2CH2, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and X0 is hydrido;

R2 is 3-carboxy-5-aminophenyl, B is phenyl, A is CH2CH2, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and X0 is hydrido; .

R2 is 3-amino-5-(N-benzylamidocarbonyI)phenyl, B is phenyl, A is CH2CH2,YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and X0 is hydrido;

R2 is 3,5-diaminophenyl, B is isopropyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R is methyl, and X° is hydrido;

R2 is 3-carboxy-5-aminophenyl, B is isopropyl, A is single bond, YAT is 5-guanidino- l-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and X0 is hydrido;

R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and

X0 is hydrido;

R2 is 3,5-diaminophenyl, B is cyclobutyl, A is single bond, Y is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and X0 is hydrido;

R2 is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R1 is methyl, and X0 is hydrido; and R2 is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is single bond, YAT is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, R 1 is methyl, and X0 is hydrido.

58. A composition for inhibiting thrombotic conditions in blood comprising a compound of Claim 21 and a pharmaceutically acceptable carrier.

59. A method for inhibiting thrombotic conditions in blood comprising adding to blood a therapeutically effective amount of a composition of Claim 58.

60. A method for inhibiting formation of blood platelet aggregates in blood comprising adding to blood a therapeutically effective amount of a composition of Claim 58.

61. A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a composition of Claim 58.

62. A method for treating or preventing venuous thromboembolism and

pulmonary embolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of Claim 58.

63. A method for treating or preventing deep vein thrombosis in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of Claim 58.

64. A method for treating or preventing cardiogenic thromboembolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of Claim 58.

65. A method for treating or preventing thromboembolic stroke in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of Claim 58.

66. A method for treating or preventing thrombosis associated with cancer and cancer chemotherapy in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of Claim 58.

67. A method for treating or preventing unstable angina in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of Claim 58.

68. A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a compound of Claim 21 with a therapeutically effective amount of fibrinogen receptor antagonist.

69. The use of a compound of Claim 21, or a pharmaceutically acceptable salt thereof, in the manufacture of medicament for inhibiting thrombus formation, treating thrombus formation, or preventing thrombus formation in a mammal.