Hoffmann-la Roche Inc.

Roche Palo Alto LLC

F. Hoffmann-la Roche Ag

Daniel Fishlock

Zachary Kevin Sweeney

Yan Lou

Matthew C Lucas

Timothy D Owens

Fariborz Firooznia

Hans Iding

Charles Alois Dvorak

Keshab Sarma

Jean-Michel Adam

Steven Joseph Berthel

Shaoning Wang

Christophe Pfleger

Eric Roy Humphreys

Justin Philip Vitale

Joshua Paul Gergely Taygerly

Xianqing Shi

Pankaj D Rege

Marian Zajac

Steven Berthel

Jun-Bae Hong

Eric R Humphreys

Thimothy D Owens

The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates  The compounds of formula I and the corresponding hydrates are pharmaceutically active substances.

(3,4-dichloro-phenyl)-((S)-3-propyl-pyrrolidin-3-yl)-methanone hydrochloride and manufacturing processes

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

Verona, NJ, United States of America

Daniel Fishlock