Patent ID: 6545002
Filing Date: 2003-04-08
Classification: A61P,C07D

Abstract:
A compound of formula I: wherein R, and R1 are independently hydrogen, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)alkoxy, (C3-C8)cycloalkyl, (C4-C16)cycloalkylalkyl, heterocycle, (C6-C10)aryl, (C7-C18)aralkyl or heteroaryl; X is (C1-C8)alkylene, (C2-C8)alkenylene, (C2-C8)alkynylene, wherein one of the carbon atoms in the alkylene, alkenylene or alkynylene groups is optionally replaced with a group having the formula â€”Oâ€”, â€”N(R4)C(O)â€”, â€”OC(O)â€”, â€”Sâ€”, â€”S(O)â€” or â€”SO2â€”, R2 is hydrogen, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)alkoxy, (C3-C8)cycloalkyl, (C4-C16)cycloalkylalkyl, (C6-C10)aryl, (C7-C18)aralkyl, heterocycle or heteroaryl; wherein R2 is optionally substituted with one or more substituents selected from the group consisting of â€”OH, â€”SH, â€”NH2, â€”NHR7, â€”CN, â€”COOH and â€”SO3H, wherein R4, and R7 are independently hydrogen, (C1-C8)alkyl, (C2-C8)alkenyl, (C3-C8)cycloalkyl, (C6-C10)aryl, (C7-C18)aralkyl or halo(C1-C6)alkyl; and wherein R8 is hydrogen, (C3-C8)cycloalkyl, (C4-C16)cycloalkylalkyl, (C7-C18)aralkyl, heterocycle or heteroaryl, each optionally substituted with one or more substituents, wherein the substituents independently are oxo, (C1-C8)alkyl, halo(C1-C6)alkyl, (C2-C8)alkenyl, (C6-C10)aryl, (C7-C18)aralkyl, heteroaryl, halo, â€”OR15, â€”CN, â€”NO2, â€”CO2R15, â€”OC(O)R16, â€”C(O)R16, â€”NR13R14, â€”N(R23)C(O)R24, â€”C(O)NR17R18, â€”SR19, â€”SO2R20 or â€”SO3H; or R8 is (C6-C10)aryl, substituted with one or more substituents independently selected from the group consisting of (C1-C8)alkyl, halo(C1-C6)alkyl, (C2-C8)alkenyl, (C7-C18)aralkyl, heteroaryl, â€”OR15, â€”CN, â€”NO2, â€”CO2R15, â€”OC(O)R16, â€”C(O)R16, â€”NR13R14, â€”N(R23)C(O)R24, â€”C(O)NR17R18, â€”SR19, â€”SO2R20 and â€”SO3H; and wherein R9 is (C3-C8)cycloalkyl, (C4-C16)cycloalkylalkyl, heterocycle or heteroaryl, each optionally substituted with one or more substituents, wherein the substituents independently are oxo, (C1-C8)alkyl, halo(C1-C6)alkyl, (C2-C8)alkenyl, (C6-C10)aryl, (C7-C18)aralkyl, heteroaryl, â€”OR15, halo, â€”CN, â€”NO2, CO2R15, â€”OC(O)R16, â€”C(O)R16, â€”NR13R14, â€”N(R23)C(O)R24, â€”C(O)NR17R18, â€”SR19, â€”SO2R20 or â€”SO3H; or R9 is (C6-C10)aryl, substituted with one or more substituents independently selected from the group consisting of (C1-C8)alkyl, halo(C1-C6)alkyl, (C2-C8)alkenyl, (C7-C18)aralkyl, heteroaryl, â€”OR15, â€”CN, â€”NO2, O2R15, â€”OC(O)R16, â€”C(O)R16, â€”NR13R14, â€”N(R23)C(O)R24, â€”C(O)NR17R18, â€”SR19, and â€”SO2R20, and wherein R13, R14, R15, R16, R17, R18, R19, R20, R23 and R24 are independently hydrogen (C1-8)alkyl, (C2-C8)alkenyl, (C3-C8)cycloalkyl, (C6-C8)aryl, (C7-C18)aralkyl or halo(C1-C6)alkyl; provided that when R and R8 are both H, and R1 and R2 are both alkyl, R9 is not methylphenyl or hydroxyphenyl; or a pharmaceutically acceptable salt thereof.