Novel substituted pyridin-2-ones and pyridazin-3-ones

C - Chemistry – Metallurgy – 07 – D

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C07D 413/14 (2006.01) A61K 31/501 (2006.01) A61P 9/02 (2006.01) C07D 401/10 (2006.01) C07D 401/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2728016

This invention dis-closes 5 -phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic For-mulae I-IV: wherein variables R, X, Y1, Y2, Y2', Y3, Y4, n and m are de-fined as described herein, which in-hibit Btk. The compounds disclosed herein are useful to modulate the ac-tivity of Btk and treat diseases associ-ated 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 composi-tions comprising compounds of For-mulae I-IV and at least one carrier, diluent or excipient.

Cette invention concerne des dérivés de 5-phényle-1H-pyridine-2-one et de 6-phényle-2H-pyridazine-3-one selon les formules générales I à IV, les variables R, X, Y1, Y2, Y2', Y3, Y4, n et m étant définies comme décrit ici, qui inhibent Btk. Les composés décrits ici sont utilisés pour moduler lactivité de Btk et pour traiter les maladies associées avec une activité Btk excessive. Les composés sont également utilisés pour traiter les maladies inflammatoires et auto-immunes associées avec la prolifération aberrante des lymphocytes B, comme la polyarthrite rhumatoïde. Linvention concerne également des compositions comprenant les composés de formules I à IV et au moins un vecteur, diluant ou excipient.

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