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ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226. eCollection 2015 Aug 13.

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

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1
Bristol-Myers Squibb R&D , US Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.

Abstract

JAK2 kinase inhibitors are a promising new class of agents for the treatment of myeloproliferative neoplasms and have potential for the treatment of other diseases possessing a deregulated JAK2-STAT pathway. X-ray structure and ADME guided refinement of C-4 heterocycles to address metabolic liability present in dialkylthiazole 1 led to the discovery of a clinical candidate, BMS-911543 (11), with excellent kinome selectivity, in vivo PD activity, and safety profile.

KEYWORDS:

BMS-911543; JAK2; myeloproliferative neoplasm; selective inhibitor; structure-guided design

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