An orally active corticotropin releasing factor 1 receptor antagonist from 8 -aryl -1,3a,7,8 -tetraaza -cyclopenta[a]indenes

Abstract 8-Aryl-1,3a,7,8-tetraaza-cyclopenta[ a ]indenes represent a novel series of high-affinity corticotropin-releasing factor-1 receptor (CRF1R) antagonists. Herein we report the synthesis and SAR around the tricyclic core and the anxiolytic activity of an orally dosed exemplary compound 9d ( K i  = 8.0 nM) in a mouse canopy model.