Patent ID: 6511998
Filing Date: 2003-01-28
Classification: A61P,C07D

Abstract:
A compound of the formula (I): whereinR1 is selected from the group consisting of C2-C8 alkyl, aryl, substituted aryl, arC1-C8 alkyl, substituted arC1-C8 alkyl, heteroaryl, substituted heteroaryl, C3-C8 cycloalkyl, heteroC3-C8cycloalkyl, fluorinated C1-C8 alkyl, cyanoC1-C8alkyl and hydroxyC1-C8alkyl; wherein the aryl, aralkyl or heteroaryl group is substituted with one or more substituents independently selected from halogen, C1-C8 alkyl, C1-C8 alkoxy, fluorinated C1-C8 alkyl, fluorinated C1-C8 alkoxy, nitro, amino, amido, Nâ€”C1-C8alkylamido, N,N-di(C1-C8alkyl)amido, C1-C8 alkylsulfonyl, sulfonamido, Nâ€”C1-C8alkylsulfonamido, N,N-di(C1-C8alky)sulfonamido, C1-C8alkylsulfonylamino, or C1-C8alkylcarbonylamino; R2 is selected from the group consisting of di(C1-C6 alkyl)amino-C1-C6 alkyl, unsubstituted or substituted heteroarylC1-C6 alkyl, unsubstituted or substituted heterocycloalkylC1-C6 alkyl, unsubstituted or substituted aryl, unsubstituted or substituted arC1-C6 alkyl, and unsubstituted or substituted C3-C8 cycloalkylC1-C6 alkyl where the substituent is arylsulfonamidoC1-C6 alkyl; wherein (a) the substituents on the aryl group are one or more substituents independently selected from the group consisting of halogen, nitro, amino, substituted amino where the substituents on the amino are one or two of C1-C6 alkyl or phenyl; fluorinated C1-C6 alkyl, fluorinated C1-C6 alkoxy, C1-C6 alkyl, substituted C1-C6 alkyl where the substituent on the alkyl is Nâ€”(C1-C6 alkyl)â€”Nâ€”(C3-C8 cycloalkyl)amino; C1-C8 alkoxy, arC1-C8 alkyl, arC1-C8 alkoxy, arylcarbonyl, phenyl, aminophenyl, C1-C6 alkylthio, substituted arylsulfonamido where the substituent on the arylsulfonamido is C1-C6 alkyl or C1-C6 alkoxy; heteroaryl, substituted heteroaryl where the substituent on the heteroaryl is C1-C6 alkyl, heterocycloalkyl and oxo; (b) the substituents on the aralkyl group are one or more substituents independently selected from halogen or fluorinated C1-C4 alkyl; (c) the substituents on the heterocycloalkyl group are one or more substituents independently selected from C1-C6 alkyl or arC1-C8 alkyl; (d) the substituents on the heteroaryl group are one or more substituents independently selected from oxo, C1-C6 alkyl or halogen; R3 is selected from the group consisting of hydrogen, halogen, C1-C8 ALKYL, arC1-C8 alkyl, heteroarylC1-C8 alkyl, C1-C8 alkoxy, fluorinated C1-C8 alkyl, fluorinated C1-C8 alkoxy, aminoC1-C8 alkyl and C1-C8 alkylaminoC1-C8 alkyl; R4 is selected from the group consisting of halogen, C1-C8 alkyl, arC1-C8 ALKYL, heteroarylC1-C8 alkyl, fluorinated C1-C8 alkyl, aminoC1-C8 alkyl and C1-C8 alkylaminoC1-C8 alkyl; R5 is selected from the group consisting of hydrogen and C1-C8 alkyl; provided that when R1 is phenyl or benzyl, and R3 is hydrogen, and R4 is methyl, and R5 is hydrogen, then R2 is selected from di(C1-C6 alkyl)aminoC1-C6 alkyl, unsubstituted or substituted heteroarylC1-C6 alkyl, unsubstituted or substituted heterocycloalkylC1-C6 alkyl, substituted arC1-C6 alkyl, unsubstituted or substituted C3-C8 cycloalkylC1-C6 alkyl where the substituent is arylsulfonamidoC1-C6 alkyl, and substituted aryl wherein the substituents on the aryl group are one or more substituents independently selected from the group consisting of halogen, nitro, amino, substituted amino where the substituents on the amino are one or two of C1-C6 alkyl or phenyl; fluorinated C1-C6 alkyl, fluorinated C1-C6 alkoxy, C1-C6 alkyl (provided that R2 is not di(C1-C4 alkyl)phenyl), substituted C1-C6 alkyl where the substituent on the alkyl is Nâ€”(C1-C6 alkyl)â€”Nâ€”(C3-C8 cycloalkyl)amino; C1-C8 alkoxy, arC1-C8 alkyl, arC1-C8 alkoxy, phenyl, aminophenyl, C1-C6 alkylthio, substituted arylsulfonamido where the substituent on the arylsulfonamido is C1-C6 alkyl or C1-C6 alkoxy; heteroaryl, substituted heteroaryl where the substituent on the heteroaryl is C1-C6 alkyl; heterocycloalkyl and oxo; and pharmaceutically acceptable salts thereof.