A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents

• Published in: Expert opinion on therapeutic patents Vol. 25; no. 10; p. 1093
• Main Authors: Sharma, Mayank Kumar, Murumkar, Prashant R, Barmade, Mahesh A, Giridhar, Rajani, Yadav, Mange Ram
• Format: Journal Article
• Language: English
• Published: England 03.10.2015
• Subjects: Animals; Anti-Obesity Agents - adverse effects; Anti-Obesity Agents - pharmacology; Cannabinoid Receptor Antagonists - adverse effects; Cannabinoid Receptor Antagonists - pharmacology; Drug Design; Humans; Obesity - drug therapy; Obesity - physiopathology; Patents as Topic; Receptor, Cannabinoid, CB1 - antagonists & inhibitors; Receptor, Cannabinoid, CB1 - metabolism; peripherally acting; CB1 receptor antagonists; rimonabant; endocannabinoid system; cannabinoid; obesity
• ISSN: 1744-7674
• DOI: 10.1517/13543776.2015.1064898

Obesity is a rapidly expanding worldwide health problem. Various targets are investigated presently for the treatment of obesity, but there remains an unmet need for an effective drug therapy with acceptable efficacy levels and reduced side effects. Targeting peripherally located cannabinoid 1 (CB1) receptors is an attractive strategy as these receptors play a vital role in energy homeostasis. CB1 receptor antagonists constitute one of the most important categories of compounds of interest for the control of obesity. In this review, the authors focus on recent advances (since 2007) in diverse chemical classes of patented compounds belonging to the category of CB1 receptor antagonists. Safer CB1 receptor antagonists for the treatment of obesity can be discovered by developing such compounds that act peripherally. Increasing the polar service area, decreasing the lipophilicity and designing of neutral antagonists and allosteric inhibitors are some interesting strategies that could offer promising results.