Patent ID: 6545023
Filing Date: 2003-04-08
Classification: A61K,A61P,C07D

Abstract:
A compound of the formula I: wherein:is selected from: â€”NR10â€”, â€”Oâ€”, â€”CH2Oâ€”, â€”CONR10â€”, â€”NR10COâ€”, â€”CO2â€”, â€”OCOâ€”, â€”CH2(NR10)COâ€”, â€”N(COR10)â€”, and â€”CH2N(COR10)â€”, and where R10 is independently selected from: hydrogen, C1-6 alkyl, benzyl, phenyl, and C1-6 alkyl-C3-6 cycloalkyl, â€ƒwhich is unsubstituted or substituted with 1-3 substituents where the substituents are independently selected from: halo, C1-3alkyl, C1-3alkoxy and trifluoromethyl; R1 is selected from: hydrogen, â€”C0-6alkyl-Yâ€”(C1-6alkyl)-, and â€”(C0-6alkyl)â€”Yâ€”(C0-6alkyl)â€”(C3-7cycloalkyl)â€”(C0-6alkyl), where Y is selected from: a single bond, â€”Oâ€”, â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, and â€”NR10â€”, and where the alkyl and the cycloalkyl are unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from: (a) halo, (b) hydroxy, (c) â€”Oâ€”C1-3alkyl, and (d) trifluoromethyl, (e) C1-3alkyl, (f) â€”Oâ€”C1-3alkyl, (g) â€”CO2R9, wherein R9 is independently selected from: hydrogen, C1-6 alkyl, C5-6 cycloalkyl, benzyl or phenyl, which is unsubstituted or substituted with 1-3 substituents where the substituents are independently selected from: halo, C1-3alkyl, C1-3alkoxy and trifluoromethyl, (h) â€”CN, (i) heterocycle, (j) â€”NR9R10, (k) â€”NR9COR10, (l) â€”NR9SO2R10, and (m) â€”CONR9R10; R2 is selected from: (C0-6alkyl)-phenyl and (C0-6alkyl)-heterocycle, 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€”C1-3alkyl, (d) trifluoromethyl, and (e) â€”C1-3alkyl, and where the phenyl and the heterocycle is unsubstituted or substituted with 1-5 substituents where the substituents are independently selected from: (a) halo, (b) trifluoromethyl, (c) trifluoromethoxy, (d) hydroxy, (e) C1-6alkyl, (f) C3-7cycloalkyl, (g) â€”Oâ€”C1-6alkyl, (h) â€”Oâ€”C3-7cycloalkyl, (i) â€”SCF3, (j) â€”Sâ€”C1-6alkyl, (k) â€”SO2â€”C1-6alkyl, (l) phenyl, (m) heterocycle, (n) â€”CO2R9, (o) â€”CN, (p) â€”NR9R10, (q) â€”NR9â€”SO2â€”R10, (r) â€”SO2â€”NR9R10, and (s) â€”CONR9R10; R3 is selected from: (C0-6alkyl)-phenyl, where the alkyl is unsubstituted or substituted with 1-5 substituents where the substituents are independently selected from: (a) halo, (b) hydroxy, (c) â€”Oâ€”C1-3alkyl, and (d) trifluoromethyl, and where the phenyl is unsubstituted or substituted with 1-5 substituents where the substituents are independently selected from: (a) halo, (b) trifluoromethyl, (c) hydroxy, (d) C1-3alkyl, (e) â€”Oâ€”C1-3alkyl, (f) â€”CO2R9, (g) â€”CN, (h) â€”NR9R10, and (i) â€”CONR9R10; R4 is selected from: a) hydrogen, b) hydroxy, c) C1-6alkyl, d) C1-6alkyl-hydroxy, e) â€”Oâ€”C1-3alkyl, f) â€”CO2R9, g) â€”CONR9R10, and h) â€”CN; or where R3 and R4 may be joined together to form a ring which is selected from: (a) 1H-indene, (b) 2,3-dihydro-1H-indene, (c) 2,3-dihydro-benzofuran, (d) 1,3-dihydro-isobenzofuran, (e) 2,3-dihydro-benzothiofuran, and (f) 1,3-dihydro-isobenzothiofuran, or where R3 and R5 or R4 and R6 may be joined together to form a ring which is phenyl, wherein the ring is unsubstituted or substituted with 1-7 substituents where the substituents are independently selected from: a) halo, b) trifluoromethyl, c) hydroxy, d) C1-3alkyl, e) â€”Oâ€”C1-3alkyl, f) â€”CO2R9, g) â€”CN, h) â€”NR9R10, and i) â€”CONR9R10; R5 and R6 are independently selected from: (a) hydrogen, (b) hydroxy, (c) C1-6alkyl, (d) C1-6alkyl-hydroxy, (e) â€”Oâ€”C1-3alkyl, (f) oxo, and (g) halo; and pharmaceutically acceptable salts thereof and individual diastereomers thereof.