Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

  • Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92. doi: 10.1016/j.bmcl.2009.08.071.
Christopher J Burns  1 ,  David G Bourke ,  Laura Andrau ,  Xianyong Bu ,  Susan A Charman ,  Andrew C Donohue ,  Emmanuelle Fantino ,  Michelle Farrugia ,  John T Feutrill ,  Max Joffe ,  Marcel R Kling ,  Margarita Kurek ,  Tracy L Nero ,  Thao Nguyen ,  James T Palmer ,  Ian Phillips ,  David M Shackleford ,  Harrison Sikanyika ,  Michelle Styles ,  Stephen Su ,  Herbert Treutlein ,  Jun Zeng ,  Andrew F Wilks
Affiliations
  • 1. Cytopia Research Pty Ltd, 576 Swan St, Richmond, VIC 3121, Australia.
PMID: 19762238 DOI: 10.1016/j.bmcl.2009.08.071
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.

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