1380434-33-2Relevant articles and documents
Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: Potent and orally active antagonists of corticotropin-releasing factor 1 receptor
Takahashi, Yoshinori,Hibi, Shigeki,Hoshino, Yorihisa,Kikuchi, Koichi,Shin, Kogyoku,Murata-Tai, Kaoru,Fujisawa, Masae,Ino, Mitsuhiro,Shibata, Hisashi,Yonaga, Masahiro
, p. 5255 - 5269 (2012/08/27)
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.