Melanocortin-4 receptor modulators for the treatment of obesity: a patent analysis (2008-2014).

The central melanocortin system and particularly the melanocortin-4 receptor (MC4R) subtype, plays an important role in the regulation of body weight. The discovery of orally active MC4R agonists suitable for evaluation in human clinical trials as weight loss agents has attracted considerable interest over the past decade, but has proved challenging, in part because of cardiovascular and behavioral side effects. Currently, the only MC4R agonist in clinical trials is a peptide identified as RM-493. To avoid some of the undesirable side effects associated with MC4R activation, new pharmacological approaches for modulating the MC system have been investigated. In this article, we provide a review of the MC4R patent landscape from 2008 to 2014 and analyze the physicochemical properties of compounds described herein.