Di and trifluoro-triazolo-pyridines anti-inflammatory compounds

Details Di and trifluoro-triazolo-pyridines anti-inflammatory compounds Di and trifluoro-triazolo-pyridines anti-inflammatory compounds

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61P 9/10 (2006.01) A61P 19/00 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2494754

The present invention relates to novel triazolo-pyridines of the formula (I) wherein R1 is fluoro; s is an integer from two to three; R2 is (C3- C6)cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (Cl-C4)alkyl, hydroxy, (Cl- C6)alkoxy and (C1-C6)alkyl-(C=O)-0-; or R2 is (Cl-C6)alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy and (C1-C6)alkyl- (C=O)-0-; with the proviso that said compound of formula (I) cannot be 6-~4- (2,4-Difluoro-phenyl)-oxazol-5-yl~-3-isopropyl-~1,2,4~triazolo~4,3-a~pyridine; or 6-~4-(3,4-Difluoro-phenyl)-oxazol-5-yl~-3-isopropyl-~1,2,4~triazolo~4,3- a~pyridine; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

La présente invention concerne de nouvelles triazolo-pyridines représentées par la formule (I). Dans cette formule, R?1¿ est fluoro. "s" est un entier valant 2 ou 3. R?2¿ est (C¿3?-C¿6?) cycloalkyle éventuellement substitué par 1 ou 2 groupes fonctionnels choisis indépendamment dans le groupe des halo, (C¿l?-C¿4?) alkyle, hydroxy, (C¿l?-C¿6?) alcoxy et (C¿1?-C¿6?) alkyle-(C=O)-0-. R?2¿ est (C¿l?-C¿6?) alkyle éventuellement substitué par 1 ou 2 groupes fonctionnels choisis dans le groupe des halo, (C¿1?-C¿6?) alkyle, hydroxy, (C¿1?-C¿6?) alcoxy et (C¿1?-C¿6?) alkyle-(C=O)-0-. Toutefois, le composé de la formule (I) ne doit être, ni 6-Ý4-(2,4-difluoro-phényl)-oxazol-5-yl¨-3-isopropyl-Ý1,2,4¨triazoloÝ4,3-a¨pyridine, ni 6-Ý4-(3,4-difluoro-phényl)-oxazol-5-yl¨-3-isopropyl-Ý1,2,4¨triazoloÝ4,3-a¨pyridine. L'invention concerne également des intermédiaires servant à leur élaboration, des compositions pharmaceutiques les contenant, et leur utilisation médicale. Les composés de la présente invention sont de puissants inhibiteurs des kinases MAP, de préférence de la kinase p38. Ces composés se prêtent au traitement de l'inflammation, de l'ostéoarthrite, de l'arthrite rhumatoïde, du cancer, de la reperfusion, de l'ichémie en cas d'accident cérébrovasculaire ou de crise cardiaque, d'affections auto-immunes et d'autres troubles.

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