3-(2-hydroxy-phenyl)-1h-pyrazole-4-carboxylic acid amide...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/14 (2006.01) A61K 31/415 (2006.01) A61K 31/4155 (2006.01) A61K 31/4439 (2006.01) A61K 31/496 (2006.01) A61K 31/5377 (2006.01) A61K 31/63 (2006.01) A61P 35/00 (2006.01) C07D 401/12 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/06 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2508574

Compounds of formula (IA) or (IB) or salts, N-oxides, hydrates or solvates thereof are Inhibitors of HSP90, and useful in the treatment of, for example, cancer: formula (IA), formula (IB) wherein Ar is an aryl or heteroaryl radical which is linked via a ring carbon, and which is substituted by a hydroxy group on a carbon in the 2-position, and which is otherwise either unsubstituted or optionally substituted; R1 is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and R3 is a carboxamide group.

L'invention concerne des composés représentés par les formules (IA) ou (IB) ou des sels, des N-oxydes, des hydrates ou des solvates de ceux-ci, lesquels composés sont des inhibiteurs de HSP90, et sont utilisés dans le traitement du cancer, par exemple: formule (IA), formule (IB), dans ces formules, Ar représente un radical aryle ou hétéroaryle lequel est lié par l'intermédiaire d'un carbone cyclique à la position 2, et lequel est, soit non substitué, soit éventuellement substitué; R¿1? représente l'hydrogène ou alkyle C¿1?-C¿6? éventuellement substitué; R¿2? représente l'hydrogène, cycloalkyle éventuellement substitué, cycloalcényle, alkyle C¿1?-C¿6?, alcényle C¿1?-C¿6?, ou alkynyl C¿1?-C¿6?; ou un groupe carboxyle, carboxamide ou ester carboxamide; et R¿3? représente un groupe carboxamide.

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