Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity
ACS Medicinal Chemistry Letters2010Vol. 1(9), pp. 483–487
Citations Over Time
Chu‐Biao Xue, Lihua Chen, Ganfeng Cao, Ke Zhang, Anlai Wang, David Meloni, Joseph Glenn, Rajan Anand, Michael Xia, Ling Kong, Taisheng Huang, Hao Feng, Changsheng Zheng, Mei Li, Laurine G. Galya, Jiacheng Zhou, Niu Shin, Fredric Baribaud, Kim Solomon, Peggy Scherle, Bitao Zhao, Sharon Diamond, Tom Emm, Douglas A. Keller, Nancy Contel, Swamy Yeleswaram, Kris Vaddi, Gregory Hollis, Robert Newton, Steven Friedman, Brian Metcalf
Abstract
To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high affinity for CCR5, potent anti-HIV-1 activity, high receptor selectivity, excellent oral bioavailability, and a tolerated safety profile. INCB9471 has entered human clinical trials.
Related Papers
- → 4-(Pyrrolidinyl)methoxybenzoic Acid Derivatives as a Potent, Orally Active VLA-4 Antagonist(2006)16 cited
- → In Vivo Pharmacologic Profile of ONO-1078: A Potent, Selective and Orally Active Peptide Leukotriene (LT) Antagonist.(1992)86 cited
- → In Vivo Pharmacologic Profile of ONO-1078: A Potent, Selective and Orally Active Peptide Leukotriene (LT) Antagonist(1992)20 cited
- Studies of an orally active leukotriene antagonist L-649,923 in normal man.(1987)
- → ChemInform Abstract: The Identification of Novel Orally Active mGluR5 Antagonist GSK2210875.(2011)