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  • Title: Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor.
    Author: Takahashi Y, Hibi S, Hoshino Y, Kikuchi K, Shin K, Murata-Tai K, Fujisawa M, Ino M, Shibata H, Yonaga M.
    Journal: J Med Chem; 2012 Jun 14; 55(11):5255-69. PubMed ID: 22587443.
    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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