Sugen Incorporated

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Asta Medica, Aktiengesellschaft

Yissum Research Development

New York University

Zentaris Gmbh

Zentaris Ag

Harald App

Peng Cho Tang

Gerald McMahon

Bernhard Kutscher

Heinz Weinberger

Alexander Levitzki

Aviv Gazit

Gerald M McMahon

Joseph Schlessinger

Klaus Peter Hirth

Benjamin L Margolis

Edward Y Skolnik

Jianming Tsai

Cho Peng Tang

Gerald M Mcmahon

The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to quinazoline compounds and pharmaceutical compositions comprising these compounds.

Methods of modulating serine/threonine protein kinase function with quinazoline-based compounds

The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with azabenzimidazole-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to azabenzimidazole compounds and pharmaceutical compositions comprising these compounds.

Methods of modulating serine/threonine protein kinase function with azabenzimidazole-based compounds

The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with 5-azaquinoxaline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to 5-azaquinoxaline compounds and pharmaceutical compositions comprising these compounds.

Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds

Methods of modulating serine/thereonine protein kinase function with quinazoline-based compounds

Methods of modulating serine/threonine protein kinase function with

The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described. The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.

Substituted phenylacrylonitrile compounds and compositions thereof for

The present invention relates to a novel method, based on direct expression cloning, for identifying target proteins capable of binding to and/or serving as substrates for receptor or cytoplasmic tyrosine kinases. The present invention also relates to novel proteins identified using this method, and to methods for identifying compounds that disrupt the interaction of such novel proteins with the receptor or cytoplasmic tyrosine kinases.

Expression-cloning method for identifying target proteins for eukaryotic

The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLX-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described. The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.

Compounds for the treament of disorders related to vasculogenesis and/or

Quinazoline compounds and compositions thereof for the treatment of

Compounds for the treatment of disorders related to vasculogenesis

The invention is directed to rapid and quantitative assay systems for screening test compounds for their ability to modulate tyrosine kinase or phosphatase activities involved in signal transduction by determining the tyrosine phosphorylation state of a protein substrate using an anti-phosphotyrosine antibody and an antibody specific for the protein substrate. These assays may be practiced in a whole cell or cell-free system. The assays can be used to identify test compounds for use in therapeutic applications to disease processes in which tyrosine kinase or phosphatase activity in a signal transduction pathway contributes to a pathological process.

Screening assays for compounds

Growing community of inventors

San Francisco, CA, United States of America

Harald App