Orexin receptor antagonists

Abstract

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.