Heteroaryl‐Substituted 4‐(1<i>H</i>‐pyrazol‐1‐yl)‐5,6‐dihydro‐1<i>H</i>‐pyrrolo[2,3‐<i>d</i>]pyrimidine Derivatives as Potent and Selective Corticotropin‐Releasing Factor Receptor‐1 Antagonists

Abstract

Potent and selective CRF1 receptor antagonists based on the 5,6-dihydro-1H-pyrrolo[2,3-d]pyrimidines 2 were discovered and characterized. Identification of two complementary synthetic pathways allowed an efficient SAR exploration, which was facilitated by computational methods that allowed the rational design of target compounds within a defined drug-like physicochemical space.