Patent ID: 6573267
Filing Date: 2003-06-03
Classification: A61P,C07D

Abstract:
A compound having Formula (I) and Formula (II): whereinA is a substituent selected from the group consisting of aryl and heteroaryl optionally substituted with one to two substituents selected from the group consisting of halogen, C1-8alkyl, C1-8alkoxy, tri(halogen)C1-8alkyl and tri(halogen)C1-8alkoxy; n is an integer from 1 to 5; R1 is C1-8alkyl optionally substituted with one to two substituents independently selected from the group consisting of hydroxy, C1-8alkoxy (optionally substituted with â€”SC1-8alkyl), C1-8acyl, carboxy, carbonyl (further substituted with C1-8alkyl, C1-8alkoxy, amino or â€”SC1-8alkyl), oxy (further substituted with carbonylC1-8alkyl, carbonylC1-8alkoxy or carbonylamino), amino (optionally further substituted with one or two substituents independently selected from C1-8alkyl, C1-8acyl, carbonylC1-8alkyl, carbonyfC1-8alkoxy, sulfinylC1-8alkyl or sulfonylC1-8alkyl), ureido (optionally further substituted with C1-8alkyl), thio (optionally further substituted with C1-8alkyl or amino), sulfinyl (optionally further substituted with C1-8alkyl or amino) and sulfonyl (optionally further substituted with C1-8alkyl or amino); R2 and R3 are substituents independently selected from the group consisting of hydrogen and C1-8alkyl; R4 and R5 are substituents independently selected from the group consisting of hydrogen, C1-8alkyl and arylC1-8alkyl; wherein aryl is optionally substituted with one to three substituents selected from the group consisting of C1-8alkyl, C1-8alkoxy, tri(halo)C1-8alkyl and tri(halo)C1-8alkoxy; or, in the alternative, R4 and R5 may be fused together with nitrogen to form a heterocyclic ring selected from the group consisting of: wherein x is an integer from 3 to 7 and Y is selected from the group consisting of N, S, S&boxH;O, SO2 and O; and R6 is a substituent selected from the group consisting of C1-8alkyl and hydroxyC1-8alkyl; and pharmaceutically acceptable acid addition salts thereof;with the proviso that,in the case of a compound wherein:n is an integer from 1 to 5; R1 is selected from the group consisting of hydrogen and C1-4alkyl; R2 and R3 are selected from the group consisting of hydrogen and C1-4alkyl; R4 and R5 are independently selected from the group consisting of hydrogen, C1-4alkyl, phenylC1-4alkyl and substituted phenylC1-4alkyl where the substituent is on phenyl and selected from the group consisting of methyl and methoxy; or in the alternative, are fused and together with the nitrogen form a heterocyclic ring selected from the group consisting of: 4-[bis(4-fluorophenyl)methylene]-piperidin-1-yl, 1,2,3,4-tetrahydro-6,7-dimethoxy-isoquinolin-2-yl, wherein Y is S or O and x is 3 to 7; and, R6 is selected from the group consisting of methyl and hydroxymethyl; then, A cannot be substituted or unsubstituted phenyl.