Roche Palo Alto LLC

Syntex (u.s.a.) Inc.

F. Hoffmann-la Roche Ag

Bradley E Loe

Yan Lou

Timothy D Owens

Michael Soth

Rama K Kondru

Joel McIntosh

Nolan James Dewdney

Robert Stephen Wilhelm

Zachary Kevin Sweeney

David Michael Goldstein

Francisco Javier Lopez-Tapia

Ralph New Harris, Iii

David Bruce Repke

Russell Stephen Stabler

Leyi Gong

Christine E Brotherton-Pleiss

Wylie Solang Palmer

Humberto Bartolome Arzeno

David Mark Rotstein

Keith Adrian Murray Walker

Michael G Martin

Tania M Silva

Joshua Paul Gergely Taygerly

Joshua Kennedy-Smith

Bruce H Devens

Robert Alvarez

Yun-chou Tan

Lubov Konstantinovna Filonova

Pankaj D Rege

Yun-Chou Tan

Erin M O'Brien

Lubov Filonova

Tania Silva

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R, R, and Rare as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

[1,2,4]triazolo[3,4-C][1,4]oxazines as P2X7 modulators

This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y, Y, Y, Y, Y, 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.

Inhibitors of bruton's tyrosine kinase

Inhibitors of JNK

This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y, Y, Y, Y, 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 containing compounds of Formulae I-III and at least one carrier, diluent or excipient.

Benzo or pyridopyridazinones and pyridazinthiones of the formula ##STR1## wherein: X and Y are nitrogen or carbon, provided that at least one is carbon, and Z is oxygen or sulfur;

Benzopyridazinone and pyridopyridazinone compounds

The disclosed 8-aryl-1,6-naphthyridin-5-ones, compounds of Formula I, ##STR1## wherein: R.sub.1 is hydrogen, alkyl, lower alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkyl lower alkyl, heterocycloalkyl lower alkyl, aralkyl or heteroaralkyl; and

8-phenyl-1,6-naphthyridin-5-ones

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Santa Cruz, CA, United States of America

Bradley E Loe