Patent ID: 6350735
Filing Date: 2002-02-26
Classification: A61P,C07H

Abstract:
A compound of the formula or a pharmaceutically acceptable salt or solvate thereof, whereinR1 is hydrogen or C1-C6 alkyl optionally substituted by 1 or 2 substituents each independently selected from phenyl and naphthyl, said phenyl and naphthyl being optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, halo or cyano; A is a bond or C1-C3 alkylene; R2 is (i) hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl or naphthyl, said C3-C7 cycloalkyl, phenyl or naphthyl being optionally substituted by C1-C6 alkyl, phenyl, C1-C6 alkoxy-(C1-C6)-alkyl, R3R3 N-(C1-C6)-alkyl, fluoro-(C1-C6)-alkyl, fluoro-(C1-C6)-alkoxy, C2-C5 alkanoyl, halo, â€”OR3, cyano, â€”COOR3, C3-C7 cycloalkyl, â€”S(O)mR4, â€”NR3R3, â€”SO2NR3R3, â€”CONR3R3, â€”NR3COR4 or â€”NR3SO2R4, with the proviso that R2 is not hydrogen when A is a bond, or (ii) when A is C2-C3 alkylene, â€”NR7R8, â€”OR3, â€”COOR3, â€”OCOR4, â€”SO2R4, â€”CN, â€”SO2NR3R3, â€”NR3COR4 or â€”CONR3R3, or (iii) a C-linked, 4 to 11 membered, mono or bicyclic heterocycle having either from 1 to 4 ring nitrogen atom(s) or 1 or 2 nitrogen and 1 oxygen or 1 sulphur ring atoms, optionally C-substituted by oxo, C1-C6 alkoxy-(C1-C6)-alkyl, R3R3N-(C1-C6)-alkyl, fluoro-(C1-C6)-alkyl, fluoro-(C1-C6)-alkoxy, fluoro-(C2-C5)-alkanoyl, halo, cyano, â€”OR5, R6, â€”COR5, â€”NR5R5, â€”COOR5 , â€”S(O)mR6, â€”SO2NR5R5, â€”CONR5R5, â€”NR5SO2R6 or â€”NR5COR6 and optionally N-substituted by C1-C6 alkoxy-(C1-C6)-alkyl, R3R3N-(C2-C6)-alkyl, fluoro-(C1-C6)-alkyl, fluoro-(C2-C5)-alkanoyl, R6, â€”COR5, â€”COOR5, â€”S(O)mR6, â€”SO2NR5R5 or â€”CONR5R5; R3 is H, C1-C6 alkyl, C3-C7 cycloalkyl or phenyl; R4 is C1-C6 alkyl, C3-C7 cycloalkyl or phenyl; R5 is H, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl, naphthyl or het; R6 is C1-C6 alkyl, C3-C7 cycloalkyl, phenyl, naphthyl or het; either, R7 and R8, taken together with the nitrogen atom to which they are attached represent azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, homopiperidinyl, homopiperazinyl or tetrahydroisoquinolinyl, each being optionally substituted on a ring carbon atom by C1-C6 alkyl, C3-C8 cycloalkyl, phenyl, C1-C6 alkoxy-(C1-C6)-alkyl, R3R3N-(C1-C6)-alkyl, fluoro-(C1-C6)-alkyl, â€”CONR3R3, â€”COOR3 or C2-C5 alkanoyl, and optionally substituted on a ring carbon atom not adjacent to a ring nitrogen atom by fluoro-(C1-C6)-alkoxy, halo, â€”OR3, cyano, S(O)mR4, â€”NR3R3, â€”SO2NR3R3, â€”NR3COR4 or â€”NR3SO2R4, and said piperazin-1-yl and homopiperazin-1-yl being optionally substituted on the ring nitrogen atom not attached to A by C1-C6 alkyl, phenyl, C1-C6 alkoxy-(C2-C6)-alkyl, R3R3N-(C2-C6)-alkyl, fluoro-(C1-C6)-alkyl, C2-C5 alkanoyl, â€”COOR4, C3-C8 cycloalkyl, â€”SO2R4, â€”SO2NR3R3 or â€”CONR3R3 , or, R7 is H, C1-C6 alkyl, C3-C8 cycloalkyl, phenyl or benzyl and R8 H, C1-C6 alkyl, C3-C8 cycloalkyl, phenyl, benzyl, fluoro-(C1-C6)-alkyl, â€”CONR3R3, â€”COOR4, C2-C5 alkanoyl or â€”SO2NR3R3; m is 0, 1 or 2; and â€œhetâ€ , used in the definitions of R5 and R6, means C-linked pyrrolyl, imidazolyl, triazolyl, thienyl, furyl, thiazolyl, oxazolyl, thiadiazolyl, oxadiazolyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzimidazolyl, quinazolinyl, phthalazinyl, benzoxazolyl or quinoxalinyl, each optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, cyano or halo.