Orexin receptor antagonists.
The orexin neuropeptides bind to two G protein-coupled receptors, orexin-1 and -2. Small-molecule antagonism of the receptors has potential therapeutic utility in a number of areas, most notably insomnia, for which the most advanced dual orexin receptor antagonist has now completed clinical trials. The purpose of this article is to comprehensively review small-molecule orexin antagonist patent activity during the period 2009-2011.
Heptares Therapeutics Limited, BioPark, Broadwater Road, Welwyn Garden City, Hertfordshire, AL7 3AX, UK. john.christopher@heptares.com.
John A
JA
Christopher
D000818:Animals; D002986:Clinical Trials as Topic; D015195:Drug Design; D006801:Humans; D006993:Hypnotics and Sedatives / Q000494:pharmacology*; D047908:Intracellular Signaling Peptides and Proteins / Q000378:metabolism; D009479:Neuropeptides / Q000378:metabolism; D000068796:Orexin Receptor Antagonists; D000068797:Orexins; D010330:Patents as Topic; D007319:Sleep Initiation and Maintenance Disorders / Q000188:drug therapy* / Q000503:physiopathology
D006993:Hypnotics and Sedatives; D047908:Intracellular Signaling Peptides and Proteins; D009479:Neuropeptides; D000068796:Orexin Receptor Antagonists; D000068797:Orexins