Roche Palo Alto LLC

F. Hoffmann-La Roche Ag

Jun-Bae Hong

Zachary Kevin Sweeney

Yan Lou

Matthew C Lucas

Fariborz Firooznia

Timothy D Owens

Keshab Sarma

Steven Joseph Berthel

Joshua Paul Gergely Taygerly

Daniel Fishlock

Steven Berthel

Thimothy D Owens

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 I-III: wherein, variables Q, R, X, X', Y, Y, Y, Y, Y, Y, m, and n 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 I-III and at least one carrier, diluent or excipient.

Inhibitors of Bruton's tyrosine kinase

Growing community of inventors

Ridgewood, NJ, United States of America

Jun-Bae Hong