Pyridylisoxazole derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 413/04 (2006.01) A61K 31/4439 (2006.01) A61P 1/04 (2006.01) A61P 1/16 (2006.01) A61P 3/10 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 11/00 (2006.01) A61P 11/02 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 15/06 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 19/06 (2006.01) A61P 19/08 (2006.01) A61P 19/10 (2006.01) A61P 25/28 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) A61P 31/04 (2006.01) A61P 31/06 (2006.01) A61P 31/18 (2006.01) A61P 35/00

Patent

CA 2656159

An isoxazole derivative represented by the formula (1) or a pharmaceutically acceptable salt thereof, which has excellent inhibitory activity on p38MAP kinase, has reduced adverse side-effects, and is useful for the treatment of a disease such as rheumatoid arthritis and ulcerative colitis. (1) wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group, an amino group or the like; R3 represents a substituted or unsubstituted aryl or heteroaryl group; R4 represents a hydrogen atom or a lower alkyl group; R5 represents a substituted or unsubstitutedphenyl or furyl group; and Y represents -CH2-, -CO-, -O-, -NH- or the like.

La présente invention concerne un dérivé d'isoxazole de formule (1) dans laquelle: R<SUP>1 </SUP>et R<SUP>2</SUP>, indépendamment représentent un atome d'hydrogène, un groupe alkyle inférieur, un groupe amino ou analogue; R<SUP>3</SUP> représente un aryle ou hétéroaryle substitué ou non; R<SUP>4</SUP> représente un atome d'hydrogène ou un groupe alkyle inférieur; R<SUP>5</SUP> représente un groupe phényle ou furyle substitué ou non; et Y représente -CH<SUB>2</SUB>-, -CO-, -O-, -NH- ou analogue; ou un sel pharmaceutiquement acceptable de celui-ci, présentant une excellente activité d'inhibition de la MAP kinase p38, des effets secondaires réduits, et utile pour le traitement d'une maladie telle que la polyarthrite rhumatoïde et la rectocolite hémorragique.

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