Wyeth

Wyeth Holdings Corporation

Pharmaengine, Inc.

Yanong Daniel Wang

Diane H Boschelli

Dan Maarten Berger

Allan Wissner

Biqi Wu

Hwei-Ru Tsou

Nan Zhang

Dennis William Powell

Fei Ye

Ayako Yamashita

Frenel Fils DeMorin

Elsebe Geraldine Overbeek-Klumpers

Frank Boschelli

Xiong Cai

Changgeng Qian

Derek Cecil Cole

Russell Dushin

Lawrence Nathan Tumey

Magda Asselin

Amarnauth Shastrie Prashad

Gary Harold Birnberg

Diane Marie Joseph-McCarthy

Chuan S Niu

Joan Chen

Steve Lawrence Johnson

Diane Harris Boschelli

Diane Marie Joseph-Mccarthy

Diane Marie Joseph-Mcarthy

The present invention provides compounds of formula (I) which are potent inhibitors of Chk1 and have the structural formula below: wherein R, R, R, R, and Rare as defined herein. Pharmaceutical compositions comprising the compounds, uses thereof and their preparation process are also provided.

3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (Chk1) inhibitors, and their preparations and applications

The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R, R, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

Substituted 3-cyanopyridines as protein kinase inhibitors

There is herein provided a process for Zr-mediated hydroboration of alkynes which offers (E)-vinylboronic esters in high yield with stereoselectivity and regioselectivity.

Stereoselective synthesis of (E)-vinylboronic esters via a Zr mediated hydroboration of alkynes

This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.

Method for the regioselective preparation of substituted benzo[g]quinoline-3-carbonitriles and benzo[g]quinazolines

There is provided a process for the preparation of 7-substituted-3-quinolinecarbonitriles and intermediates useful in a process to prepare 7-substituted-3-quinolinecarbonitriles and pharmaceutically acceptable salts is described. Where 7-fluoro-4-oxo-1,4-dihydro-3-quinolinecarbonitrile is converted in three steps to 7-substituted-3-quinolinecarbonitriles which inhibit the action of certain protein kinases and are useful in the treatment of cancer.

Process for the preparation of 7-substituted-3 quinolinecarbonitriles

3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors

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Warren, NJ, United States of America

Yanong Daniel Wang