Wyeth

American Cyanamid Company

Wyeth Holdings Corporation

Other

Osi Pharmaceuticals, Inc.

Dan Maarten Berger

Allan Wissner

Hwei-Ru Tsou

Nan Zhang

Minu D Dutia

Dennis William Powell

Biqi Wu

Diane H Boschelli

Rolf Paul

Dennis W Powell

William A Hallett

Fei Ye

Yanong Daniel Wang

Frenel Fils DeMorin

Middleton B Floyd, Jr

Philip Frost

Philip R Hamann

Ayako Yamashita

Elsebe Geraldine Overbeek-Klumpers

Frank Boschelli

Andrew Philip Crew

Jing Wang

Hanqing Dong

Mark E Salvati

Bijoy Panicker

An-Hu Li

Mark Joseph Mulvihill

Middleton Brawner Floyd

Xin Chen

Arno G Steinig

Kam W Siu

Qinghua Weng

Gary Harold Birnberg

Philip Ross Hamann

Andrew Kleinberg

James G Tarrant

Keith Hornberger

Ramesh C Gupta

Lifu Ma

Steve Lawrence Johnson

Rajaram Sangem

Mark Ernest Salvati

Compounds of Formula 1, as shown below and defined herein: 

7-aminofuropyridine derivatives

This invention provides compounds of formula I having the structure wherein G, G, R, R, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.

Substituted 3-cyanoquinolines

This invention provides a compound of Formula 1 where Ar, X, R, R, R, and Rare defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.

3-Quinolinecarbonitrile protein kinase inhibitors

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

This invention provides compounds of formula 1, having the structure which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.

Tricyclic protein kinase inhibitors

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

This invention provides compounds of formula I having the structure

Compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are herein described, A is a straight or branched (C.sub.2 -C.sub.12)alkyl or a phenyl moiety and B is a moiety of the formula: ##STR2## The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.

MDR reversal agents

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New City, NY, United States of America

Dan Maarten Berger