Patent ID: 6525032
Filing Date: 2003-02-25
Classification: A61P,C07D,C07H

Abstract:
A compound of the formula: or a pharmaceutically acceptable salt or solvate thereof,wherein R1 is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl, each optionally substituted by 1 or 2 substituents each independently selected from hydroxyl, fluorenyl, 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-C6 alkylene; R2 is (i) hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl or naphthyl, said C3-C7 cycloalkyl, phenyl and naphthyl being optionally substituted by C1-C6 alkyl, phenyl, C1-C6 alkoxy-(C1-C6)-alkyl, amino-(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-C6 alkylene, â€”NR3R3, â€”OR3, â€”COOR3, â€”OCOR4, â€”SO2R4, â€”CN, â€”SO2NR3R4, â€”NR3SO2R4, â€”NR3SO2R4 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, amino-(C1-C6)-alkyl, fluoro-(C1-C6)-alkyl, fluoro-(C1-C6)-alkoxy, fluoro-(C2-C5)-alkanoyl, halo, cyano, âˆ’OR5,R6, â€”COR5, â€”NR5R5, â€”COOR5, â€”S(O)mR6, â€”SO2N5R5R5, â€”CONR5R5, â€”NR5SO2R6 or â€”NR5COR6 and optionally N-substituted by C1-C6 alkoxy-(C1-C6)-alkyl, amino-(C2-C6)-alkyl, fluoro-(C1-C6)-alkyl, fluoro-(C2-C5)-alkanoyl, R6, â€”COR5, â€”COOR6, â€”SO2R6, â€”SO2NR5R5 or â€”CONR5R5, or (iv) when A is C2-C6 alkylene, N-linked azetidinyl, pyrrolidinyl, morpholinyl, tetrahydroisoquinolinyl, piperidinyl or piperazinyl, each being optionally C-substituted by C1-C6 alkyl, phenyl, C1-C6 alkoxy-(C1-C6)-alkyl, amino-(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 and said piperazinyl being optionally N-substituted by C1-C6 alkyl, phenyl, C1-C6 alkoxy-(C1-C6)-alkyl, amino-(C2-C6)-alkyl, fluoro-(C1-C6)-alkyl, C2-C5 alkanoyl, â€”COOR4, C3-C7 cycloalkyl, â€”SO2R4, â€”SO2NR3R3 or â€”CONR3R3; each R3 is independently selected from H, C1-C6 alkyl, phenyl or pyridinyl; R4 is C1-C6 alkyl 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; m is 0, 1 or 2; R7 is hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl, naphthyl, azetidin-3-yl, pyrrolidin-3-yl, piperidin-3-yl, piperidin-4-yl or het, said azetidin-3-yl, pyrrolidin-3-yl, piperidin-3-yl and piperidin-4-yl being optionally substituted by C1-C6 alkyl; R8 is H or C1-C6 alkyl; and â€œhetâ€ , used in the definitions of R5, R6 and R7, 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 being optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, cyano or halo.