1002106-16-2Relevant academic research and scientific papers
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors
Kunz, Roxanne K.,Rumfelt, Shannon,Chen, Ning,Zhang, Dawei,Tasker, Andrew S.,Buerli, Roland,Hungate, Randall,Yu, Violeta,Nguyen, Yen,Whittington, Douglas A.,Meagher, Kristin L.,Plant, Matthew,Tudor, Yanyan,Schrag, Michael,Xu, Yang,Ng, Gordon Y.,Hu, Essa
scheme or table, p. 5115 - 5117 (2009/05/26)
Deregulation of the receptor tyrosine kinase c-Kit is associated with an increasing number of human diseases, including certain cancers and mast cell diseases. Interference of c-Kit signaling with multi-kinase inhibitors has been shown clinically to successfully treat gastrointestinal stromal tumors and mastocytosis. Targeted therapy of c-Kit activity may provide therapeutic advantages against off-target effects for non-oncology applications. A new structural class of c-Kit inhibitors is described, including in vitro c-Kit potency, kinase selectivity, and the observed binding mode.
DI-AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page/Page column 33, (2008/06/13)
The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various fibrotic and mast cell related diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6, X and Y are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
