306296-78-6Relevant academic research and scientific papers
Discovery of INCB9471, a potent, selective, and orally bioavailable CCR5 antagonist with potent anti-HIV-1 activity
Xue, Chu-Biao,Chen, Lihua,Cao, Ganfeng,Zhang, Ke,Wang, Anlai,Meloni, David,Glenn, Joseph,Anand, Rajan,Xia, Michael,Kong, Ling,Huang, Taisheng,Feng, Hao,Zheng, Changsheng,Li, Mei,Galya, Laurine,Zhou, Jiacheng,Shin, Niu,Baribaud, Fredric,Solomon, Kim,Scherle, Peggy,Zhao, Bitao,Diamond, Sharon,Emm, Tom,Keller, Douglas,Contel, Nancy,Yeleswaram, Swamy,Vaddi, Kris,Hollis, Gregory,Newton, Robert,Friedman, Steven,Metcalf, Brian
scheme or table, p. 483 - 487 (2011/03/20)
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 affinit
Piperazine derivatives
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Page/Page column 12-13, (2009/10/31)
This invention relates to novel compounds that are piperazine derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel piperazine compounds that are derivatives of the chemokine CCR5 receptor antagonist
Forward- and reverse-synthesis of piperazinopiperidine amide analogs: A general access to structurally diverse 4-piperazinopiperidine-based CCR5 antagonists
Feng, Dong-Zhi,Song, Yan-Li,Jiang, Xiao-Hua,Chen, Li,Long, Ya-Qiu
, p. 2690 - 2697 (2008/03/12)
Piperazinopiperidine amide analogs are among the most promising CCR5 antagonists. As an effective extension of a previously-reported methodology to synthesize such compounds, forward- and reverse-syntheses were successfully developed in which the convergent synthesis of the piperazinopiperidine nucleus, with a building block of 4-substituent-4-aminopiperidine, served as a common key step. The two-way approach affords a comprehensive access to the piperazinopiperidine templated library with variation on the pharmacophore sites. Thus, a SAR study of our synthesized piperazinopiperidine-based CCR5 antagonists was conducted with respect to the structure and configuration of the substituent on the piperazine ring. The S-configuration of the benzylic-substituent is vital for the CCR5 binding, and the bulky or aryl substituent on the 2-position in the piperazine ring is detrimental to the activity. By using the forward-synthesis approach, the best compound in the chiral piperazine-based CCR5 antagonist series, Sch-D (Vicriviroc), was conveniently synthesized in an excellent yield. The Royal Society of Chemistry.
Piperazinylpiperidine derivatives as chemokine receptor antagonists
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Page/Page column 13; 30, (2008/06/13)
The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR
Piperidine derivatives useful as CCR5 antagonists
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Page/Page column 16; 18, (2010/02/07)
The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present invention also provides pharmaceutical compositions containing
