Sugen Incorporated

Pharmacia & Upjohn Company

Connie Li Sun

Peng Cho Tang

Congxin Liang

Chung Chen Wei

Asaad S Nematalla

Tomas Vojkovsky

Ping Huang

Marcel Koenig

G Davis Harris, Jr

Huiping Guan

Yong Zhou

Gerald McMahon

Jingrong Jean Cui

Klaus Peter Hirth

Laura Kay Shawver

Todd Anthony Miller

John Yudhistir Ramphal

Michael John Hawley

Xiaoyuan Li

Shahrzad Shirazian

The present invention relates to pyrrole substituted-2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Pyrrole substituted 2-indolinone protein kinase inhibitors

The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1' position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.

Indolinone combinatorial libraries and related products and methods for the treatment of disease

The present invention relates to substituted imidazopyrazines of the general Formula I which modulate the activity of protein kinases ('PKs'). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors

The present invention relates to 8-amino-aryl-substituted imidazopyrazines which modulate the activity of protein kinases ('PKs'). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives

The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.

5-aralkysufonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors

Growing community of inventors

Foster City, CA, United States of America

Connie Li Sun