Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

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Abstract

A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported. © 2009 Elsevier Ltd. All rights reserved.

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Burns, C. J., Bourke, D. G., Andrau, L., Bu, X., Charman, S. A., Donohue, A. C., … Wilks, A. F. (2009). Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorganic and Medicinal Chemistry Letters, 19(20), 5887–5892. https://doi.org/10.1016/j.bmcl.2009.08.071

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