Roche Palo Alto LLC

Steven Berthel

Zachary Kevin Sweeney

Yan Lou

Matthew C Lucas

Timothy D Owens

Fariborz Firooznia

Keshab Sarma

Joshua Paul Gergely Taygerly

Daniel Fishlock

Jun-Bae Hong

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

Mendham, NJ, United States of America

Steven Berthel