Synthesis and use of kinase inhibitors
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United States of America Patent
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Nov 29, 2016
Grant Date -
Aug 21, 2014
app pub date -
Aug 7, 2013
filing date -
Jun 30, 2010
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Abstract
An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.
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