C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 403/14 (2006.01) A61K 31/5513 (2006.01) A61K 31/553 (2006.01) A61P 29/00 (2006.01) C07D 413/14 (2006.01)
Patent
CA 2748414
This application discloses 5 -phenyl- 1H-pyridin-2-one, 6-phenyl-2H-pyridazin- 3-one, and 5-phenyl-1H- pyrazin-2-one derivatives according to generic Formula A wherein, variables Z* or Q1, Q2, Y3, Y4, Y5 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 containing compounds of Formula A and at least one carrier, diluent or excipient.
Cette invention porte sur des dérivés de 5-phényl-1H-pyridin-2-one, de 6-phényl-2H-pyridazine-3-one et de 5-phényl-1H-pyrazin-2-one répondant à la formule générale A dans laquelle les variables Z* ou Q1, Q2, Y3, Y4, Y5 et m sont définies comme dans la description, qui inhibent la Btk. Les composés de l'invention sont utiles pour moduler l'activité de la Btk et traiter des maladies associées à une activité excessive de la Btk. 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 contenant des composés de formule A et au moins un porteur, diluant ou excipient.
Dewdney Nolan James
Hawley Ronald Charles
Kondru Rama K.
Lai Yingjie
Lou Yan
Borden Ladner Gervais Llp
F. Hoffmann-La Roche Ag
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