Cytopia Research Pty Ltd, 576 Swan St, Richmond, VIC 3121, Australia.
Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92. doi: 10.1016/j.bmcl.2009.08.071. Epub 2009 Aug 23.
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.
已鉴定出一系列苯氨基嘧啶类化合物为 Janus 激酶（JAK）抑制剂。该初始系列的开发导致了强效的 JAK2/JAK1 抑制剂 CYT387（N-(氰甲基)-4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]-苯甲酰胺）。报道了这些化合物的合成和 SAR 研究的详细信息。
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