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1. (WO1998050346) ACETAMIDE AND UREA DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF CNS DISORDERS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/050346 International Application No.: PCT/EP1998/002263
Publication Date: 12.11.1998 International Filing Date: 14.04.1998
Chapter 2 Demand Filed: 14.11.1998
IPC:
C07C 233/29 (2006.01) ,C07C 271/58 (2006.01) ,C07C 275/34 (2006.01) ,C07C 275/36 (2006.01) ,C07C 275/40 (2006.01) ,C07C 323/44 (2006.01) ,C07D 209/08 (2006.01) ,C07D 213/40 (2006.01) ,C07D 213/56 (2006.01) ,C07D 401/06 (2006.01) ,C07D 401/12 (2006.01) ,C07D 401/14 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
233
Carboxylic acid amides
01
having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
16
having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
24
with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
29
having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
271
Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06
Esters of carbamic acids
40
having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
58
with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
32
being further substituted by singly-bound oxygen atoms
34
having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
32
being further substituted by singly-bound oxygen atoms
34
having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
36
with at least one of the oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. N-aryloxyphenylureas
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
40
being further substituted by nitrogen atoms not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
23
containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
39
at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
43
Y being a hetero atom
44
X or Y being nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
08
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero 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
36
Radicals substituted by singly-bound nitrogen atoms
40
Acylated substituent nitrogen atom
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
54
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
56
Amides
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
06
linked by a carbon chain containing only aliphatic carbon atoms
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
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
14
containing three or more hetero rings
Applicants:
SMITHKLINE BEECHAM PLC [GB/GB]; New Horizons Court Brentford Middlesex TW8 9EP, GB (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW)
GASTER, Laramie, Mary [GB/GB]; GB (UsOnly)
WYMAN, Paul, Adrian [GB/GB]; GB (UsOnly)
Inventors:
GASTER, Laramie, Mary; GB
WYMAN, Paul, Adrian; GB
Agent:
WATERS, David, Martin; SmithKline Beecham plc Corporate Intellectual Property Two New Horizons Court, Brentford Middlesex TW8 9EP, GB
Priority Data:
9707874.518.04.1997GB
9801632.226.01.1998GB
Title (EN) ACETAMIDE AND UREA DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF CNS DISORDERS
(FR) DERIVES D'ACETAMIDE ET D'UREE, PROCEDE DE PREPARATION ET UTILISATION DE CES DERIVES DANS LE TRAITEMENT DES TROUBLES DU SYSTEME NERVEUX CENTRAL
Abstract:
(EN) Compounds of formula (I), processes for their preparation and their use as CNS agents are disclosed, in which Ra is a group of formula (i), in which P1 is phenyl, bicyclic aryl, a 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, or a bicyclic heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur; or Ra is a group of formula (ii); L is a group of formula -Y-C(=V)-DG-, in which Y is -NH-, NR5 where R5 is C1-6alkyl, or Y is -CH2- or -O-; V is oxygen or sulphur; D is nitrogen, carbon or a CH group, G is hydrogen or C1-6alkyl providing that D is nitrogen or a CH group, or G together with Rb1 forms a group W where W is (CR16R17)t where t is 2, 3 or 4 and R16 and R17 are independently hydrogen or C1-6alkyl or W is (CR16R17)u-J where u is 0, 1, 2 or 3 and J is oxygen, sulphur, CR16=CR17, CR16=N, =CR16O, =CR16S or =CR16-NR17; B is CH2, oxygen, S(O)p where p is 0, 1 or 2, NR6 where R6 is hydrogen or C1-6alkyl or B is CR7=CR8 where R7 and R8 are independently hydrogen or C1-6alkyl; Rc and Rd are independently hydrogen or C1-6alkyl; Ry is a 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, or Ry is a group of formula -NReRf in which Re and Rf are independently hydrogen, C1-6alkyl or aralkyl; Rb1 and Rb2 are independently hydrogen, halogen, hydroxy, C1-6alkyl, trifluoromethyl, C1-6alkoxy or aryl, or Rb1 together with G forms a group W as defined above; and n is 0, 1, 2, 3 or 4.
(FR) Composés ayant la formule (I), leurs procédés de préparation et leur utilisation en tant qu'agents CNS, formule dans laquelle Ra est un groupe ayant la formule (i) dans laquelle P1 représente phényle, aryle bicyclique, un anneau hétérocyclique de 5 à 7 membres et contenant de 1 à 3 hétéroatomes sélectionnés parmi oxygène, azote et soufre, ou un anneau hétérocyclique bicyclique contenant de 1 à 3 hétéroatomes sélectionnés parmi oxygène, azote et soufre; ou Ra est un groupe de formule (ii); L est un groupe de formule -Y-C(=V)-DG-, dans laquelle Y représente -NH-, NR5 où R5 représente C1-6 alkyle, ou Y représente -CH2-, ou -O-; V représente oxygène ou soufre; B représente azote, carbone ou un groupe CH, G représente hydrogène ou C1-6 alkyle à condition que D soit azote ou un groupe CH, ou G forme avec Rb1 un groupe W qui est (CR16R17)t, t valant 2, 3 ou 4 et R16 et R17 représente indépendamment hydrogène ou C1-6 alkyle ou W représente (CR16R17)u-J où u vaut 0, 1, 2 ou 3 et J représente oxygène, soufre, CR16=CR17, CR16=N, =CR16O, =CR16S ou =CR16-NR17; B représente CH2, oxygène, S(O)p où p vaut 0, 1 ou 2, NR6 où R6 est hydrogène ou C1-6 alkyle ou B est CR7=CR8 où R7 et R8 sont indépendamment hydrogène ou C1-6 alkyle; Rc et Rd représentent indépendamment hydrogène ou C1-6 alkyle; Ry est un anneau hétérocyclique ayant de 5 à 7 membres et contenant de 1 à 3 hétéroatomes sélectionnés parmi oxygène, azote et soufre, ou Ry est un groupe ayant la formule NReRf dans laquelle Re et Rf représentent indépendamment hydrogène, C1-6 alkyle ou aralkyle; Rb1 et Rb2 représentent indépendamment hydrogène, halogène, hydroxy, C1-6 alkyle, trifluorométhyle, C1-6 alcoxy ou aryle, ou Rb1 forment ensemble avec G un groupe W tel que défini ci-dessus; et n représente 0, 1, 2, 3 ou 4.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, 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:
AU1998075267