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Bioorg Med Chem. 2011 Sep 15;19(18):5432-45. doi: 10.1016/j.bmc.2011.07.055. Epub 2011 Jul 31.

6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists.

Author information

1
Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan. te.saitou@ono.co.jp

Abstract

To identify an orally active corticotropin-releasing factor 1 receptor antagonist, a series of 6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives were designed, synthesized and evaluated. An in vitro study followed by in vivo and pharmacokinetic studies of these heterotricyclic compounds led us to the discovery of an orally active CRF1 receptor antagonist. The results of a structure-activity relationship study are presented.

PMID:
21865047
DOI:
10.1016/j.bmc.2011.07.055
[Indexed for MEDLINE]

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