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Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs) |
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| 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 |
| Affiliation: | 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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