Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 11, Pages 5255-5269Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm300259r
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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 (CRF1) 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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