Merck + Co., Inc.

Locus Pharmaceuticals, Inc.

Speedel Experimenta Ag

Zenon D Konteatis

Rui Liang

Joseph Leslie Duffy

Frank Peter Hollinger

Kristofer K Moffett

Younghee Lee

Jennifer Lee Ludington

Elizabeth Louise Campbell

Peter Herold

Bruce D Dorsey

Robert Mah

Stefan Stutz

Enrique Luis Michelotti

Vincenzo Tschinke

Bin Liu

Kevin Tyler Chapman

James R Tata

Aleksandar Stojanovic

Christiane Marti

Dirk Behnke

Michael Siegfried Quirmbach

Stjepan Jelakovic

Rupa S Shetty

Martin S Springer

Duyan Nguyen

Eric Bruce Springman

Brian Anthony Kirk

Kevin J Moriarty

Salvatore J Siciliano

Ted Tsutomis Fujimoto

Wenchun Chao

Kristofer Moffett

A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has a Btk inhibitory activity, and is useful as a method for preventing and/or treating a rheumatoid arthritis, an autoimmune disease, a B cell lymphoma of cancer, and the like.

Pyrrolotriazine compounds

The present invention is directed to a compound having the formula wherein R, R, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.

Urea inhibitors of MAP kinases

Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent. 

Substituted piperidines

The present invention addresses substituted thiophene derivatives, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.

Substituted bicylic thiophene derivatives, compositions containing such compounds and methods of use

The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.

Cyanothiophene derivatives, compositions containing such compounds and methods of use

The invention is an assay, including a series of peptides, which allow screening for inhibitors of C5a binding targeted to the subsite on the C5a receptor occupied by the C-terminus of C5a. These peptides allow compound testing efforts to be targeted to this same subsite so that C5a agonists and antagonists can be identified. These peptides have much greater affinity (Ki&lt;10 nM) than does the natural C-terminus of C5a (Ki=300 .mu.M) and have been labeled to allow for detection of molecules which inhibit binding of these peptides at this receptor subsite. The invention is useful to develop agonists, partial agonists, and antagonists of C5a, and the invention includes compounds identified according to the method of this invention and methods of their use.

Assay to identify human C5a antagonists and agonists

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Chatham Twp, NJ, United States of America

Zenon D Konteatis