Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor

Journal of Medicinal Chemistry
Yoshinori TakahashiMasahiro Yonaga

Abstract

Design, synthesis, and structure-activity relationships of a series of 3-dialkylamino-7-phenyl pyrazolo[1,5-a]pyridines (I) as selective antagonists of the corticotropin-releasing factor 1 (CRF(1)) receptor are described. The most prominent compound to emerge from this work, 46 (E2508), exhibits potent in vitro activity, excellent drug-like properties, and robust oral efficacy in animal models of stress-related disorders. It has advanced into clinical trials.

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Citations

Dec 30, 2014·European Journal of Medicinal Chemistry·Oscar DelgadoAndrés A Trabanco
Aug 12, 2014·European Journal of Medicinal Chemistry·Meng Li, Bao-Xiang Zhao
Feb 14, 2015·Organic & Biomolecular Chemistry·Darapaneni Chandra MohanSubbarayappa Adimurthy

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