title: Corticotropin-releasing factor 1 receptor antagonists: a patent review.
abstract: BACKGROUND
  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.
  
  
  METHODS
  The present review covers the disclosures of non-peptide CRF₁ antagonists in the patent literature since 2006.
  
  
  CONCLUSIONS
  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.
authors: Neurocrine Biosciences, Medicinal Chemistry, 12780 El Camino Real, San Diego, CA 92130, USA. jwilliams@neurocrine.com
authors: John P
authors: JP
authors: Williams
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D001007:Anxiety / Q000188:drug therapy / Q000503:physiopathology; D003863:Depression / Q000188:drug therapy / Q000503:physiopathology; D015195:Drug Design; D006801:Humans; D010330:Patents as Topic; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013315:Stress, Psychological / Q000188:drug therapy* / Q000503:physiopathology; D000099052:CRF Receptor, Type 1
chemical_list: D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1