Corticotropin-releasing factor 1 receptor antagonists: a patent review

Abstract

Introduction: Corticotropin-releasing factor (CRF) is a 41 amino acid peptide hypothalamic factor that plays a key role in the body's response to stress. The receptors for CRF (CRF₁ and CRF₂) are members of the class B G-protein coupled receptor family and several small molecule antagonists have been evaluated clinically in stress-related disorders.

Areas covered: The present review covers the disclosures of non-peptide CRF₁ antagonists in the patent literature since 2006.

Expert opinion: Antagonists of the CRF₁ receptor have failed to demonstrate clinical utility. All of the compounds evaluated are similar structures and are allosteric inhibitors of the CRF₁ receptor. Further clinical evaluation of new compounds appears unlikely unless novel structures are identified that interact with the receptor distinct to the first-generation antagonists.