Literature DB >> 21295478

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

Changsheng Zheng1, 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.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2011        PMID： 21295478     DOI： 10.1016/j.bmcl.2011.01.015

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Targeting CCR5 for anti-HIV research.

Authors:  W-G Gu; X-Q Chen
Journal:  Eur J Clin Microbiol Infect Dis       Date:  2014-06-11       Impact factor: 3.267

2.  Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Authors:  Chu-Biao Xue; Anlai Wang; Qi Han; Yingxin Zhang; Ganfeng Cao; Hao Feng; Taisheng Huang; Changsheng Zheng; Michael Xia; Ke Zhang; Lingquan Kong; Joseph Glenn; Rajan Anand; David Meloni; D J Robinson; Lixin Shao; Lou Storace; Mei Li; Robert O Hughes; Rajesh Devraj; Philip A Morton; D Joseph Rogier; Maryanne Covington; Peggy Scherle; Sharon Diamond; Tom Emm; Swamy Yeleswaram; Nancy Contel; Kris Vaddi; Robert Newton; Greg Hollis; Brian Metcalf
Journal:  ACS Med Chem Lett       Date:  2011-10-05       Impact factor: 4.345

Review 3.  CCR5 receptor antagonists in preclinical to phase II clinical development for treatment of HIV.

Authors:  Michelle B Kim; Kyle E Giesler; Yesim A Tahirovic; Valarie M Truax; Dennis C Liotta; Lawrence J Wilson
Journal:  Expert Opin Investig Drugs       Date:  2016-12       Impact factor: 6.206

4.  Structural insights from binding poses of CCR2 and CCR5 with clinically important antagonists: a combined in silico study.

Authors:  Gugan Kothandan; Changdev G Gadhe; Seung Joo Cho
Journal:  PLoS One       Date:  2012-03-27       Impact factor: 3.240

Review 5.  Targeting the CCL2/CCR2 Axis in Cancer Immunotherapy: One Stone, Three Birds?

Authors:  Liyang Fei; Xiaochen Ren; Haijia Yu; Yifan Zhan
Journal:  Front Immunol       Date:  2021-11-03       Impact factor: 7.561

Review 6.  International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors.

Authors:  Francoise Bachelerie; Adit Ben-Baruch; Amanda M Burkhardt; Christophe Combadiere; Joshua M Farber; Gerard J Graham; Richard Horuk; Alexander Hovard Sparre-Ulrich; Massimo Locati; Andrew D Luster; Alberto Mantovani; Kouji Matsushima; Philip M Murphy; Robert Nibbs; Hisayuki Nomiyama; Christine A Power; Amanda E I Proudfoot; Mette M Rosenkilde; Antal Rot; Silvano Sozzani; Marcus Thelen; Osamu Yoshie; Albert Zlotnik
Journal:  Pharmacol Rev       Date:  2013-11-11       Impact factor: 25.468
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.