Patent ID: 6369084
Filing Date: 2002-04-09
Classification: A61P,C07D

Abstract:
A compound represented by formula A or a pharmaceutically acceptable salt, hydrate or ester thereof, wherein:y and z are independently 0-2, with the proviso that y+z=2; Ra is selected from the group consisting of: 1) heteroaryl, wherein heteroaryl is selected from the group consisting of: a) furyl, b) diazinyl, triazinyl or tetrazinyl, c) imidazolyl, d) isoxazolyl, e) isothiazolyl, f) oxadiazolyl, g) oxazolyl, h) pyrazolyl, i) pyrrolyl, j) thiadiazolyl, k) thiazoyl l) thienyl m) triazolyl and n) tetrazolyl, wherein heteroaryl is optionally substituted with one or more substituents independently selected from R11 or C1-4alkyl, 2) â€”COR6, 3) â€”NR7R8, 4) â€”SO2R9, 5) hydroxy, 6) C1-6alkoxy, optionally substituted with one or more substituents independently selected from R11, and 7) C1-6alkyl, C2-6alkenyl or C3-6cycloalkyl, optionally substituted with one or more substituents independently selected from R11, and further substituted with 1-3 substituents independently selected from the group consisting of: (a) â€”COR6 (b) â€”NR7R8, (c) â€”SO2R9, (d) hydroxy, (e) C1-6alkoxy or haloC1-6alkoxy, and (f) heteroaryl, with the proviso that Ra is positioned on the phenyl ring to which it is bonded in a 1,3 or 1,4 relationship relative to the thienyl group represented in formula A; each R1, R2, R3, R4 and R5 are independently selected from the group consisting of: 1) hydrogen, 2) halogen, 3) C1-6alkyl, 4) C1-6alkoxy, 5) C1-6alkylthio, 6) nitro, 7) carboxy and 8) CN, wherein items (3)-(5) above are optionally substituted with one or more substituents independently selected from R11; R6 is selected from the group consisting of hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy and NR7R8, wherein C1-6alkyl or C1-6alkoxy are optionally substituted with one or more substituents independently selected from R11; R7 and R8 are independently selected from the group consisting of: (1) hydrogen, (2) hydroxy, (3) SO2R9 (4) C1-6alkyl, (5) C1-6alkoxy, (6) phenyl, (7) naphthyl, (8) furyl, (9) thienyl and (10) pyridyl, wherein items (4)-(5) above are optionally substituted with one or more substituents independently selected from R11, and items (6)-(10) above are optionally substituted with one or more substituents independently selected from R11 or C1-4alkyl, R9 is selected from the group consisting of (1) hydroxy, (2) N(R10)2, (3) C1-6alkyl, optionally substituted with one or more substituents independently selected from R11, (4) phenyl, (5) naphthyl, (6) furyl, (7) thienyl and (8) pyridyl, wherein items (4)-(8) above are optionally substituted with one or more substituents independently selected from R11 or C1-4alkyl; R10 is hydrogen or C1-6alkyl; and R11 is the group consisting of halogen, hydroxy, C1-3alkoxy, nitro, N(R10)2 and pyridyl.