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Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)
Authors:Christopher J Burns  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  Andrew F Wilks
Institution:1. Cytopia Research Pty Ltd, 576 Swan St, Richmond, VIC 3121, Australia;2. Centre for Drug Candidate Optimisation, Faculty of Pharmacy and Pharmaceutical Sciences, Monash University, 381 Royal Pde, Parkville, VIC 3052, Australia
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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