Patent Number: 8,822,457

Title: Inhibitors of bruton's tyrosine kinase

Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: ##STR00001## wherein, variables R, X, Y.sup.1, Y.sup.2, Y.sup.2', Y.sup.3, Y.sup.4, 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-IV and at least one carrier, diluent or excipient.

Inventors: Dewdney; Nolan James (Repluse, HK), Kondru; Rama K. (Morris Plans, NJ), Loe; Bradley E. (Santa Cruz, CA), Lou; Yan (Glen Ridge, NJ), McIntosh; Joel (Pacifica, CA), Owens; Timothy D. (Jersey City, NJ), Soth; Michael (Glen Rock, NJ)

Assignee: Roche Palo Alto LLC

International Classification: C07D 417/14 (20060101)

Expiration Date: 9/02/12018