2-substituted benzoyl-cycloalkyl-1-carboxylic acid derivatives

Details 2-substituted benzoyl-cycloalkyl-1-carboxylic acid derivatives 2-substituted benzoyl-cycloalkyl-1-carboxylic acid derivatives

C - Chemistry, Metallurgy

07

C

C07C 62/20 (2006.01) A61K 31/16 (2006.01) A61K 31/195 (2006.01) C07C 62/38 (2006.01) C07C 69/757 (2006.01) C07C 229/12 (2006.01) C07C 229/48 (2006.01) C07C 233/58 (2006.01) C07C 233/60 (2006.01) C07C 233/81 (2006.01) C07C 235/82 (2006.01) C07C 271/24 (2006.01) C07C 271/64 (2006.01) C07C 311/51 (2006.01)

Patent

CA 2283184

2-(substituted benzoyl)-cycloalkyl-1-carboxylic acids of formula (I) wherein E is a C1-C4 alkylene chain in which a carbon atom is optionally substituted; each of R and R1, being the same or different, is hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, phenyl, benzyl, C1-C6 alkyl, C1-C6 alkoxy, C1- C6 alkylthio, SOR4 or SO2R4; R2 is hydrogen or -N(R7R8) in which each of R7 and R8 is, independently, hydrogen, C1-C6 alkyl, benzyl, phenyl, hydroxy, C1- C6 alkoxy, benzyloxy or one of R7 and R8 is hydrogen and the other is COR9; R3 is hydroxy, C1-C6 alkoxy, phenoxy, benzyloxy or a group -N(R12R13); and pharmaceutically acceptable salts thereof, have kynurenine-3-hydroxylase enzyme inhibitor activity.

L'invention concerne des acides 2-(benzoyl substitué)-cycloalkyl-1-carboxyliques de formule (I), où E est une chaîne alcylène C¿1?-C¿4? dans laquelle un atome de carbone est éventuellement substitué; chacun des radicaux R ou R¿1?, qu'il soit identique ou différent, désigne hydrogène, halogène, hydroxy, trifluorométhyle, cyano, nitro, phényle, benzyle, alkyle C¿1?-C¿6?, alkoxy C¿1?-C¿6?, alcylthio C¿1?-C¿6?, SOR¿4? ou SO¿2?R¿4?; R¿2? désigne hydrogène ou -N(R¿7?R¿8?) où chacun des radicaux R¿7? ou R¿8? désigne indépendamment, hydrogène, alkyle C¿1?-C¿6? benzyle, phényle, hydroxy, alkoxy C¿1?-C¿6?, benzyloxy ou un de R¿7? ou de R¿8? désigne hydrogène, l'autre désignant COR¿9?; R¿3? désigne hydroxy, alkoxy C¿1?-C¿6?, phénoxy, benzyloxy ou un groupe -N(R¿12?R¿13?). L'invention concerne également leurs sels pharmaceutiquement acceptables. Ces dérivés et leurs sels ont une activité inhibitrice de l'enzyme cynurénine-3-hydroxylase.

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