1044656-17-8Relevant academic research and scientific papers
Imidazo[1,2-a]pyrazine diaryl ureas: Inhibitors of the receptor tyrosine kinase EphB4
Mitchell, Scott A.,Danca, Mihaela Diana,Blomgren, Peter A.,Darrow, James W.,Currie, Kevin S.,Kropf, Jeffrey E.,Lee, Seung H.,Gallion, Steven L.,Xiong, Jin-Ming,Pippin, Douglas A.,DeSimone, Robert W.,Brittelli, David R.,Eustice, David C.,Bourret, Aaron,Hill-Drzewi, Melissa,Maciejewski, Patricia M.,Elkin, Lisa L.
experimental part, p. 6991 - 6995 (2010/07/15)
Inhibition of receptor tyrosine kinases (RTKs) such as vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs) has been validated by recently launched small molecules Sutent and Nexavar/
CERTAIN SUBSTITUTED IMIDAZO[1,2-A]PYRAZINES, AS MODULATORS OF KINASE ACTIVITY
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Page/Page column 57, (2010/02/11)
Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically-acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
