Patent ID: 6821984
Filing Date: 2004-11-23
Classification: A61P,C07D

Abstract:
A compound of Formula I or Formula II: wherein:R1 is â€”ORa, â€”NRaRb, â€”CRcRdRe, CO2Ra, or â€”C(O)NRaRb; R1 is hydrogen, halogen, cycloalkenyl or aryl, where each aryl is optionally substituted with one or more substituents independently selected from C1-6alkyl, C1-6alkoxy, C1-6alkylthio, C1-6alkylsulfonyl, halogen, haloalkyl, cyano, nitro, â€”C(O)NRaâ€²Rbâ€², and â€”NRaâ€²Rbâ€², where Raâ€² and Rbâ€² are each independently selected from the group consisting of hydrogen, C1-9alkyl, and C1-9alkylcarbonyl; R2 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylalkyl, C1-6alkylcarbonyl, C1-6alkylsulfonyl, aryl, or arylalkyl, wherein said aryl or arylalkyl is optionally substituted with one or more substituents independently selected from C1-6alkyl, haloalkyl, C1-6alkoxy, and halogen; R3 and R4 are each independently selected from hydrogen and C1-6alkyl; Ar is aryl optionally substituted with one or more substituents independently selected from the group consisting of C1-6alkyl, C1-6alkoxy, C1-6alkylthio, C1-6alkylsulfonyl, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, halogen, haloalkyl, cyano, nitro, and â€”NRaâ€³Rbâ€³, where Raâ€³ and Rbâ€³ are each independently selected from the group consisting of hydrogen, C1-9alkyl, and C1-9alkylcarbonyl; Ra and Rb are each independently selected from the group consisting of hydrogen, C1-9alkyl, hydroxyalkyl, C1-6alkoxyalkyl, C1-6alkylthioalkyl, carboxyalkyl, C1-6-alkoxycarbonyl, C1-6-alkoxyC1-3-alkylcarbonyl, acyl, C3-6cycloalkyl, C3-6cycloalkylalkyl, di-C3-6cycloalkylC1-3alkyl, C1-6heteroalkyl, aminoalkyl, aminocarbonylalkyl, cyanoalkyl, aryl, arylalkyl, phenylalkyl, diphenylalkyl, phenylsulfonyl optionally substituted as described for phenyl below, and C1-3alkyl substituted with both a C3-6cycloalkyl and a phenyl group, wherein each of said cycloalkyl, phenyl or aryl groups is optionally substituted with one or more substituents independently selected from the group consisting of C1-6alkyl, haloalkyl, C1-6alkoxy, amino, alkylamino, dialkylamino, hydroxyalkyl, cyano, acylamino, alkylsulfonyl, alkylsulfonyloxy, and halogen, and each of said amino groups is optionally monosubstituted or disubstituted with alkyl; Rc is hydrogen, hydroxy, C1-6alkoxy, or â€”NRaâ€²â€³Rbâ€²â€³; Rd and Re are each independently selected from the group consisting of hydrogen, C1-9alkyl, hydroxyalkyl, C1-6alkoxyalkyl, C1-6alkylthioalkyl, heteroalkyl, C3-6cycloalkyl, C3-6cycloalkylalkyl, di-C3-6cycloalkyl-C1-3alkyl, aryl, arylalkyl, phenylalkyl, diphenyl-C1-3alkyl, and C1-3alkyl substituted with both a C3-6cycloalkyl and a phenyl group, wherein each of said cycloalkyl, phenyl or aryl groups is optionally substituted with one or more substituents independently selected from the group consisting of C1-6alkyl, haloalkyl, C1-6alkoxy, amino, alkylamino, dialkylamino, and halogen; or Rc and Rd are taken together to form a divalent group selected from C1-6alkylidenyl, C1-6heteroalkylidenyl, C3-6cycloalkylidenyl, C3-6cycloalkyl-alkylidenyl, C3-6cycloalkylalkyl-alkylidenyl, C3-6C1-3alkylidenyl, aryl-C1-3alkyl-alkylidenyl, wherein each of said cycloalkyl or aryl groups is optionally substituted with one or more substituents independently selected from C1-6alkyl, haloalkyl, C1-6alkoxy, amino, alkylamino, dialkylamino, and halogen; or Rd and Re are taken together with the carbon to which they are attached to form a cycloalkyl; Raâ€²â€³ and Rbâ€²â€³ are each independently selected from the group consisting of hydrogen, C1-9alkyl, hydroxyalkyl, C1-6alkoxyalkyl, C1-6alkylthioalkyl, carboxyalkyl, C1-6-alkoxycarbonyl, C1-6-alkoxyC1-3-alkylcarbonyl, acyl, C3-6cycloalkyl, C3-6cycloalkylalkyl, di-C3-6cycloalkyl-C1-3alkyl, C1-6heteroalkyl, aminoalkyl, aminocarbonylalkyl, cyanoalkyl, aryl, arylalkyl, phenylalkyl, diphenyl-C1-3alkyl, and C1-3alkyl substituted with both a C3-6cycloalkyl and a phenyl group, wherein each of said cycloalkyl, phenyl or aryl groups is optionally substituted with one or more substituents independently selected from the group consisting of C1-6alkyl, haloalkyl, C1-6alkoxy, amino, alkylamino, dialkylamino, hydroxyalkyl, cyano, acylamino, alkylsulfonyl, alkylsulfonyloxy, and halogen, and each of said amino groups is optionally monosubstituted or disubstituted with alkyl; or, n is 1; a is a single bond; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof.