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

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.