Corticotropin-releasing factor 1 receptor antagonists: a patent review

Author： Williams John P  

Publisher： Informa Healthcare

ISSN： 1354-3776

Source： Expert Opinion on Therapeutic Patents, Vol.23, Iss.8, 2013-08, pp. : 1057-1068

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

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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.

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