2. Academic Validation
  3. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

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

Affiliation

  • 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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