1. Academic Validation
  2. Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist

  • Bioorg Med Chem Lett. 2011 Mar 1;21(5):1442-6. doi: 10.1016/j.bmcl.2011.01.015.
Changsheng Zheng 1 Ganfeng Cao Michael Xia Hao Feng Joseph Glenn Rajan Anand Ke Zhang Taisheng Huang Anlai Wang Ling Kong Mei Li Laurine Galya Robert O Hughes Rajesh Devraj Phillip A Morton D Joseph Rogier Maryanne Covington Fred Baribaud Niu Shin Peggy Scherle Sharon Diamond Swamy Yeleswaram Kris Vaddi Robert Newton Greg Hollis Steven Friedman Brian Metcalf Chu-Biao Xue
Affiliations

Affiliation

  • 1 Incyte Corporation, Experimental Station E336, Wilmington, DE 19880, USA.
Abstract

We report the discovery of a potent, selective, and orally bioavailable dual CCR2 and CCR5 Antagonist (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl]-3-methoxytetrahydro-2H-pyran-4-amine (19). After evaluation in 28-day toxicology studies, compound 19 (INCB10820/PF-4178903) was selected as a clinical candidate.

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