Patent ID: 6500844
Filing Date: 2002-12-31
Classification: C07D

Abstract:
A compound of the formula I: wherein:X is selected from: â€”(CO)NR9â€”, â€”NR9(CO)â€”, â€”O(CO)NR9â€”, â€”NR9(CO)Oâ€”, and â€”NR9(CO)NR10â€”, where R9 is independently selected from: hydrogen, C1-10 alkyl, C3-8 cycloalkyl, C1-6 alkyl-C3-6 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, benzyl, phenyl, or naphthyl, which is unsubstituted or substituted with 1-3 substituents where the substituents are independently selected from: halo, hydroxy, C1-6 alkyl, C1-3 alkoxy, phenyl and trifluoromethyl, and where R10 is independently selected from: hydrogen, C1-6 alkyl, benzyl, or phenyl, 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, or where R9 and R10 may be joined together to form a 5-8 membered ring which may be unsubstituted or substituted with halo, C1-3 alkyl, and C1-3 alkoxy; Y is selected from: a single bond, â€”(CO)â€”, â€”(CO)Oâ€”, â€”SO2â€”, â€”SO2NR9â€”, â€”C1-10 alkyl-, â€”(CO)NR9â€”, and â€”(CS)NR9â€”; Z is selected from: a single bond, â€”NR9â€”, â€”Oâ€”, and â€”C1-10 alkyl-; R1 is selected from: phenyl, naphthyl, C1-10 alkyl, C3-6 cycloalkyl, C1-6 alkyl-C3-6 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, or C1-4 alkyl-phenyl, which is unsubstituted or substituted with 1-3 substituents where the substituents are independently selected from: halo, C1-3 alkyl, C1-3 alkoxy, trifluoromethoxy and trifluoromethyl, or when Z is â€”NR9â€”, then R9 and R1 may be joined together to form a 5-8 membered alkyl or heterocycle ring which may be unsubstituted or substituted with halo, C1-3 alkyl, and C1-3 alkoxy; R2 is selected from: (1) hydrogen, and (2) hydroxy, or R2 and Z may be joined together to form a double bond; R3 is selected from the group consisting of: phenyl and thienyl, which 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; 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) hydroxy, and (4) halo; R8 is selected from: C1-10 alkyl, C3-6 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, phenyl, C1-6 alkyl-phenyl, C1-6 alkyl-C3-6 cycloalkyl, C1-4 alkyl-O-phenyl, C1-4 alkyl-O-C1-4 alkyl-phenyl, which is unsubstituted or substituted with 1-7 of R12 where â€ƒR12 is independently selected from: (a) halo, (b) cyano, (c) hydroxy, (d) C1-6 alkyl, which is unsubstituted or substituted with 1-5 of R13 where R13 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 R13, (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, (v) â€”NR9S(O)2â€”NR9R10, (w) 1-naphthyl, and (x) 2-naphthyl; x is an integer selected from 0, 1 and 2, and y is an integer selected from 0, 1 and 2, with the proviso that the sum of x and y is 2; or a pharmaceutically acceptable salt thereof or an individual diastereomer thereof.