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1. (WO1997016433) PROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/016433 International Application No.: PCT/US1996/018000
Publication Date: 09.05.1997 International Filing Date: 30.10.1996
Chapter 2 Demand Filed: 22.05.1997
IPC:
C07C 243/34 (2006.01) ,C07C 311/16 (2006.01) ,C07C 311/29 (2006.01) ,C07D 213/30 (2006.01) ,C07D 215/36 (2006.01) ,C07D 241/24 (2006.01) ,C07D 249/10 (2006.01) ,C07D 271/10 (2006.01) ,C07D 277/56 (2006.01) ,C07D 285/12 (2006.01) ,C07D 285/125 (2006.01) ,C07D 295/155 (2006.01) ,C07D 295/215 (2006.01) ,C07D 307/91 (2006.01) ,C07D 333/34 (2006.01) ,C07D 333/76 (2006.01) ,C07D 401/12 (2006.01) ,C07D 405/12 (2006.01) ,C07D 417/12 (2006.01) ,C12N 9/64 (2006.01) ,C12Q 1/37 (2006.01) ,G01N 33/573 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
243
Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
24
Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
26
with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
34
to carbon atoms of a carbon skeleton further substituted by nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15
Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
16
having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
22
Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
29
having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24
with substituted hydrocarbon radicals attached to ring carbon atoms
28
Radicals substituted by singly-bound oxygen or sulfur atoms
30
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
36
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02
not condensed with other rings
10
having three double bonds between ring members or between ring members and non-ring members
14
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
08
1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
10
1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
12
1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
12
1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
125
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04
with substituted hydrocarbon radicals attached to ring nitrogen atoms
14
substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
155
with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16
acylated on ring nitrogen atoms
20
by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
215
Radicals derived from nitrogen analogues of carbonic acid
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77
ortho- or peri-condensed with carbocyclic rings or ring systems
91
Dibenzofurans; Hydrogenated dibenzofurans
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
04
not substituted on the ring sulfur atom
26
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
30
Hetero atoms other than halogen
34
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
50
condensed with carbocyclic rings or ring systems
76
Dibenzothiophenes
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
9
Enzymes, e.g. ligases (6.); Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating, or purifying enzymes
14
Hydrolases (3.)
48
acting on peptide bonds, e.g. thromboplastin, leucine aminopeptidase (3.4)
50
Proteinases
64
derived from animal tissue, e.g. rennin
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
Q
MEASURING OR TESTING PROCESSES INVOLVING ENZYMES OR MICRO-ORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1
Measuring or testing processes involving enzymes or micro-organisms; Compositions therefor; Processes of preparing such compositions
34
involving hydrolase
37
involving peptidase or proteinase
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53
Immunoassay; Biospecific binding assay; Materials therefor
573
for enzymes or isoenzymes
Applicants:
SMITHKLINE BEECHAM CORPORATION [US/US]; Corporate Intellectual Property, UW2220 709 Swedeland Road P.O. Box 1539 King of Prussia, PA 19406-0939, US (AllExceptUS)
CARR, Thomas, Joseph [US/US]; US (UsOnly)
DESJARLAIS, Renee, Louise [US/US]; US (UsOnly)
GALLAGHER, Timothy, Francis [US/US]; US (UsOnly)
HALBERT, Stacie, Marie [US/US]; US (UsOnly)
OH, Hye-Ja [US/US]; US (UsOnly)
THOMPSON, Scott, Kevin [US/US]; US (UsOnly)
VEBER, Daniel, Frank [US/US]; US (UsOnly)
YAMASHITA, Dennis, Shinji [US/US]; US (UsOnly)
YEN, Jack, Hwekwo [US/US]; US (UsOnly)
Inventors:
CARR, Thomas, Joseph; US
DESJARLAIS, Renee, Louise; US
GALLAGHER, Timothy, Francis; US
HALBERT, Stacie, Marie; US
OH, Hye-Ja; US
THOMPSON, Scott, Kevin; US
VEBER, Daniel, Frank; US
YAMASHITA, Dennis, Shinji; US
YEN, Jack, Hwekwo; US
Agent:
STERCHO, Yuriy, P. ; SmithKline Beecham Corporation Corporate Intellectual Property, UW2220 709 Swedeland Road P.O. Box 1539 King of Prussia, PA 19406-0939, US
Priority Data:
60/007,47322.11.1995US
60/008,10830.10.1995US
60/008,99221.12.1995US
60/013,74720.03.1996US
60/013,74820.03.1996US
60/013,76420.03.1996US
60/017,45517.05.1996US
60/017,89217.05.1996US
60/022,04722.07.1996US
60/023,49407.08.1996US
Title (EN) PROTEASE INHIBITORS
(FR) INHIBITEURS DE PROTEASES
Abstract:
(EN) The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
(FR) La présente invention concerne des composés inhibiteurs de protéases, y compris de la cathepsine K, et des compositions pharmaceutiques à base de ces composés. L'invention concerne également des thérapies contre des affections telles que l'excès de déperdition osseuse, la dégénérescence des cartilages ou de la matrice osseuse, y compris l'ostéoporose, contre les affections gingivales, y compris la gingivite et la parondite, contre l'arthrite et plus spécifiquement l'ostéoarthrite et la polyarthrite rhumatoïde, contre la maladie osseuse de Paget, contre l'hypercalcémie provoquée par une tumeur maligne et contre les maladies métaboliques de l'os. La thérapie consiste à inhiber l'excès de déperdition osseuse et la dégénérescence des cartilages ou de la matrice osseuse en administrant à un patient qui nécessite un tel traitement un composé selon la présente invention.
Designated States: AL, AM, AU, BB, BG, BR, CA, CN, CZ, EE, GE, HU, IL, IS, JP, KG, KP, KR, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, SG, SI, SK, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
CZPV1998-1327NO19981938NO20006716NO20006717NO20006718SK56798
TR1998/00767MXPA/a/1998/003548APAP/P/1998/001222SG52008VN4074IL137739
IL137737IL137738EP0934291JP2000500742CN1207095CA2236111
EA199800353KR1019990067184NZ324101AU1997011180