Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Lucja Orzechowski

Steven Joseph Berthel

Yan Lou

Francisco Javier Lopez-Tapia

Fariborz Firooznia

Timothy D Owens

Peter Michael Wovkulich

Robert Francis Kester

Roland Joseph Billedeau

Christine E Brotherton-Pleiss

Buelent Kocer

Saul Jaime-Figueroa

Stephen Deems Gabriel

Jenny Tan

Xiaochun Han

Ramona Hilgenkamp

This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y, 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 and at least one carrier, diluent or excipient.

Inhibitors of bruton's tyrosine kinase

The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.

Isoindolinone derivatives

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Kinnelon, NJ, United States of America

Lucja Orzechowski