Novel phenylpyrazinones as kinase inhibitors

Details Novel phenylpyrazinones as kinase inhibitors Novel phenylpyrazinones as kinase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 403/10 (2006.01) A61K 31/4725 (2006.01) A61P 37/00 (2006.01) C07D 401/14 (2006.01) C07D 403/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2728683

The present invention provides 5 -phenyl- 1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2', Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

La présente invention porte sur des dérivés de 5-phényl-1H-pyrazin-2-one selon les formules génériques I-V : dans lesquelles les variables Q, R, Y1, Y2, Y2', Y3, Y4, n et m sont définies comme décrit dans la description, qui inhibent Btk. Les composés de la présente invention sont utiles pour moduler l'activité de Btk et traiter des maladies associées à une activité de Btk excessive. Les composés sont en outre utiles pour traiter des maladies inflammatoires et auto-immunes associées à une prolifération aberrante des lymphocytes B, telles que la polyarthrite rhumatoïde. L'invention porte également sur des compositions renfermant des composés représentés par les formules I-V et au moins un véhicule, diluant ou excipient.

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