Warner-Lambert Company

Wyeth

Wyeth Holdings Corporation

American Cyanamid Company

Diane H Boschelli

David T Connor

James Bernard Kramer

Biqi Wu

Nan Zhang

Allan Wissner

Paul C Unangst

Dan Maarten Berger

Hwei-Ru Tsou

James Marino Hamby

Dennis William Powell

Fei Ye

Yanong Daniel Wang

Frenel Fils DeMorin

Jagadish C Sircar

Annette Marian Doherty

Milton L Hoefle

Vijaykumar M Baragi

Sonya Shah Khatana

Richard Raymond Renkiewicz

Daniel L Flynn

William Alexander Denny

Catherine R Kostlan

Annette M Doherty

Sylvester R Klutchko

Brian Desmond Palmer

Minu D Dutia

Clifton J Blankley

Ayako Yamashita

Robert Lee Panek

Elsebe Geraldine Overbeek-Klumpers

Frank Boschelli

Haris Durutlic

Ana Carolina Barrios Sosa

Clifford D Wright

Derek Cecil Cole

John F Poletto

Russell Dushin

William Howard Roark

Thomas R Belliotti

Gregg Brian Feigelson

Howard D Showalter

Ellen Myra Dobrusin

Lawrence Nathan Tumey

David W Fry

Magda Asselin

David Michael Blum

Dennis W Powell

Howard Daniel Hollis Showalter

Mark Robert Barvian

Michael D Mullican

Ali Fattaey

Richard Dennis Dyer

Amarnauth Shastrie Prashad

Karen Sutherland

Jay Thomas Afragola

Diane Marie Joseph-McCarthy

Henry Strong

Asaf Ragim Alimardanov

Howard Glenn Welgus

Chuan S Niu

Zhipei Wu

Steve Lawrence Johnson

Susanne Andrea Trumpp-Kallmeyer

Joan Chen

Sony S Khatana

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

This invention relates to compounds having the structure of Formula I wherein R, R, R, and Rare described herein.

4-(2,4-dichloro-5-methoxyphenyl)amino-6-methoxy-7-{[5-substituted-amino)methyl]-3-furyl}-3-quinolinecarbonitriles as kinase inhibitors

This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

Process for preparation of 4-amino-3-quinolinecarbonitriles

This invention provides compounds of Formula (1)&#x2013;(1), II wherein:

Thieno[3,2-b]pyridine-6-carbonitriles and thieno[2,3-b]pyridine-5-carbonitriles as protein kinase inhibitors

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

This invention provides compounds of Formula (1a)-(1f)wherein:

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

Pyrido&lsqb;2,3-D&rsqb;pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation

Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation.

Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation

The present invention provides a method of inhibiting connective tissue degradation that comprises administering to a patient having a condition in which connective tissue is degraded a therapeutically effective amount of a compound having the formula

Method of inhibiting connective tissue degradation

Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. ##STR1## The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular

6-Aryl pyrido�2,3-d!pyrimidine 7-imines, 7-ones, and 7-thiones are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

Pyrido�2, 3-d!pyrimidines for inhibiting protein tyrosine kinase

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Plymouth, MI, United States of America

Diane H Boschelli