Patent ID: 6506777
Filing Date: 2003-01-14
Classification: C07D

Abstract:
A compound of the formula I: wherein:X is â€”Yâ€”, â€”(C1-2 l alkyl)â€”Yâ€”(C1-6 alkyl)â€”, â€”(C1-6 alkyl)â€”, â€”(C1-2)â€”Yâ€”, or â€”Yâ€”(C1-6 alkyl)â€”, 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, where Y is selected from: â€”(CO)â€”, â€”(CO)Oâ€”, â€”O(CO)â€”, 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, C3-6 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, C1-3 alkyl, C1-3 alkoxy and trifluoromethyl, and where R10 is independently selected from: hydrogen, C1-6 alkyl, benzyl, or phenyl, which is unstibstituted 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 are joined together to form a 5-8 membered ring consisting of the â€”N(CO)Nâ€” functional group and a balance of carbon atoms, wherein the ring is be unsubstituted or substituted with halo, C1-3 alkyl, and C1-3 alkoxy; R1 is selected from: (1) â€”CO2H, (2) â€”NO2, (3) â€”tetrazolyl, (4) â€”hydroxyisoxazole, (5) â€”SO2NHCOâ€”R9 or â€”SO2NHCOâ€”(C1-3 alkyl)â€”R9, (6) â€”P(O)(OH)2; R2 is selected from: (1) hydrogen, and (2) hydroxy; 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; R4 and R5 are independently selected from: hydrogen, 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, and biphenyl, 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 are joined together to form a 3-8 membered saturated ring which is unsubstituted or substituted with 1-7 of R11, or where, if n is 1, R2 and R4 are 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, phenyl, naphthyl, and biphenyl, 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), 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, and (v) â€”NR9S(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; or a pharmaceutically acceptable salt thereof or an individual diastereomer thereof.