Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

Christopher Burns, David G Bourke, Laura Andrau, Xianyong Bu, Susan Ann Charman, Andrew C Donohue, Emmanuelle Fantino, Michelle Farrugia, John T Feutrill, Max Joffe, R Marcel Kling, Margarita Kurek, Tracy L Nero, Thao Nguyen, James T Palmer, Ian D Phillips, David Shackleford, Harrison Sikanyika, Michelle Styles, Stephen SuH R Treutlein, Jun Zeng, Andrew Frederick Wilks

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Abstract

The 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.
Original languageEnglish
Pages (from-to)5887 - 5892
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number20
Publication statusPublished - 2009

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