Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist |
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| Authors: | Zheng Changsheng Cao Ganfeng Xia Michael Feng Hao Glenn Joseph Anand Rajan Zhang Ke Huang Taisheng Wang Anlai Kong Ling Li Mei Galya Laurine Hughes Robert O Devraj Rajesh Morton Phillip A Rogier D Joseph Covington Maryanne Baribaud Fred Shin Niu Scherle Peggy Diamond Sharon Yeleswaram Swamy Vaddi Kris Newton Robert Hollis Greg Friedman Steven Metcalf Brian Xue Chu-Biao |
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| Affiliation: | a Incyte Corporation, Experimental Station E336, Wilmington, DE 19880, USA
b Pfizer Global Research and Development, Chesterfield Parkway West, St. Louis, MO 63017, USA |
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| 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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| Keywords: | CCR2 CCR5 Chemokine Antagonist |
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