Patent ID: 6399619
Filing Date: 2002-06-04
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula I: wherein:R2 is wherein R7 is selected from: (1) hydrogen, (2) C1-6 alkyl, which is unsubstituted or substituted with 1-4 substituents where the substituents are independently selected from: hydroxy, cyano, and halo, (3) cyano, (4) hydroxy, and (5) halo, wherein X is â€”(C0-6 alkyl)-Yâ€”(C0-6 alkyl)-, where the alkyl is unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from: (a) halo, (b) hydroxy, (c) â€”Oâ€”C1-3 alkyl, and (d) trifluoromethyl, and where Y is selected from: â€”(CO)â€”, â€”(CO)Oâ€”, â€”O(CO)â€”, â€”(CO)NR10â€”, â€”NR10(CO)â€”, â€”O(CO)NR10â€”, â€”NR10(CO)Oâ€”, and â€”NR10(CO)NR9â€”, and where R10 is independently selected from: hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, benzyl, phenyl, and C1-6 alkyl-C3-6 cycloalkyl, which is unsubstituted or substituted with 1-3 substituents where the substituents are independently selected from: halo, C1-3 alkyl, C1-3 alkoxy and trifluoromethyl, and wherein R8 is selected from: phenyl, naphthyl, biphenyl, and heterocycle, which is unsubstituted or substituted with 1-7 of R11 where R11 is independently selected from: (a) halo, (b) cyano, (c) hydroxy, (d) C1-6 alkyl, which is unsubstituted or substituted with 1-5 of R12 where R12 is independently selected from: halo, cyano, hydroxy, C1-6 alkoxy, â€”CO2H, â€”CO2(C1-6 alkyl), phenyl, trifluoromethyl, and â€”NR9R10, (e) â€”Oâ€”C1-6 alkyl, which is unsubstituted or substituted with 1-5 of R12, (f) â€”CF3, (g) â€”CHF2, (h) â€”CH2F, (i) â€”NO2, (j) phenyl, (k) â€”CO2R9, (l) tetrazolyl, (m) â€”NR9R10, (n) â€”NR9â€”COR10, (o) â€”NR9â€”CO2R10, (p) â€”COâ€”NR9R10, (q) â€”OCOâ€”NR9R10, (r) â€”NR9COâ€”NR9R10, (s) â€”S(O)mâ€”R9, wherein m is an integer selected from 0, 1 and 2, (t) â€”S(O)2â€”NR9R10, (u) â€”NR9S(O)2â€”R10, and (v) â€”NR9S(O)2â€”NR9R10; R3 is selected from the group consisting of: phenyl and thienyl, which is unsubstituted or substituted with 1-5 substituents where the substituents are independently selected from: (a) halo, (b) trifluoromethyl, (c) hydroxy, (d) C1-3 alkyl, (e) â€”Oâ€”C1-3 alkyl, (f) â€”CO2R9, (g) â€”NR9R10, and (h) â€”CONR9R10; R4 is selected from: C1-10 alkyl, C3-8 cycloalkyl, â€”(C1-3 alkyl)-C3-8 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, phenyl, â€”(C1-6 alkyl)-phenyl, naphthyl, biphenyl, heterocycle, hydrogen, cyclohexenyl, dihydronaphthyl, tetrahydronaphthyl, and octahydronaphthyl, which is unsubstituted or substituted with 1-7 of R11 where R11 is independently as defined above; R5 is selected from: hydrogen or C1-6 alkyl, wherein the alkyl is unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from: (a) halo, (b) trifluoromethyl, (c) hydroxy, (d) C1-3 alkyl, (e) â€”Oâ€”C1-3 alkyl, (f) â€”CO2R9, (g) â€”NR9R10, and (h) â€”CONR9R10, or where R4 and R5 may be joined together to form a C3-8 cycloalkyl ring which may be unsubstituted or substituted with 1-7 of R11; and pharmaceutically acceptable salts thereof and individual diastereomers thereof.