Patent ID: 6432981
Filing Date: 2002-08-13
Classification: C07D

Abstract:
A compound of the formula I: wherein:X is selected from: â€”(C0-6 alkyl)â€”Yâ€”(C0-6 alkyl)â€”, â€”(C0-6 alkyl)-C3-8 cycloalkyl-(C0-6 alkyl)â€”, C2-10 alkenyl, and C2-10 alkynyl, â€ƒwhere 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, â€ƒand where Y is selected from: a single bond, â€”Oâ€”, â€”SO2â€”, â€”NR10â€”, â€”NR10â€”SO2â€”, â€”SO2â€”NR10â€”, â€”Sâ€”, and â€”SOâ€”, â€ƒand where R10 is independently selected from: hydrogen, C1-6 alkyl, 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; R1 is selected from: (1) â€”CO2H, (2) â€”NO2, (3) â€”tetrazolyl, (4) â€”hydroxyisoxazole, (5) â€”SO2NHCOâ€”(C0-3 alkyl)â€”R9, and (6) â€”P(O)(OH)2; â€ƒwhere R9 is independently selected from: hydrogen, C1-10 alkyl, C3-6 cycloalkyl, C1-6 alkyl-C3-6 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, benzyl or phenyl, which is unsubstituted or substituted with 1-3 substituents where the substituents are independently selected from: halo, C13 alkyl, C13 alkoxy and trifluoromethyl, R2 is selected from: (1) hydrogen, and (2) hydroxy; R3 is selected from the group consisting of: â€ƒphenyl and heterocycle, 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; R4 and R5 are independently selected from: â€ƒhydrogen, hydroxy, fluoro, C1-10 alkyl, C3-8 cycloalkyl, C2-10 alkenyl, C2-10 alkynyl, phenyl, â€”(C1-6 alkyl)-phenyl, â€”(C1-6 alkyl)â€”C3-8 cycloalkyl, naphthyl, biphenyl, and heterocycle, which is unsubstituted or substituted with 1-7 of R11 where R11 is independently selected from: (a) halo, (b) trifluoromethyl, (c) hydroxy, (d) C1-3 alkyl, (e) â€”Oâ€”C1-3 alkyl, (f) â€”CO2R9, and (g) â€”CONR9R10, or where R4 and R5 may be joined together to form a 3-8 membered saturated ring which may be unsubstituted or substituted with 1-7 of R11, or where, if n is 1, R2 and R4 may be joined together to form a double bond; 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: hydrogen, C3-8 cycloalkyl, phenyl, naphthyl, biphenyl, and heterocycle, which is unsubstituted or substituted with 1-7 of R12 where R12 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), 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€”CBF2, (h) â€”CH2F, (i) â€”NO2, (j) C0-6 alkyl-phenyl or C0-6 alkyl-heterocycle, which is unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from: (i) halo, (ii) hydroxy, (iii) C1-6 alkyl, (iv) â€”Oâ€”C-6 alkyl, (v) â€”CF3, (vi) â€”OCF3, (vii) â€”NO2, (viii) â€”CN, (ix) â€”SO2â€”C1-6 alkyl, (x) â€”CO2R9, (xi) â€”NR9R10, (xii) â€”CONR9R10, (xiii) â€”SO2â€”NR9R10, and (xiv) â€”NR9â€”SO2â€”R10; (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€”NR9 S(O)2â€”NR9R10; n is an integer selected from 1, 2, 3 and 4; 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; and pharmaceutically acceptable salts thereof and individual diastereomers thereof.