Cannabinoid receptor 2 (CB₂) agonists and antagonists: a patent update

ABSTRACT

Introduction: Modulation of the CB₂ receptor is an interesting approach for pain and inflammation, arthritis, addictions, neuroprotection, and cancer, among other possible therapeutic applications, and is devoid of central side effects.

Areas covered: This review highlights the novel scaffolds for CB₂ ligands and the diverse therapeutic applications for CB₂ modulators disclosed in patents published since 2012.

Expert opinion: Structural diversity of CB₂ modulator scaffolds characterized the patent literature. Several CB₂ agonists reached clinical Phase II for pain management and inflammation. Other therapeutic applications need to be explored such as neuroprotection and/or neurodegeneration.

KEYWORDS:

• Cannabinoid receptor 2
• cancer
• endometriosis
• HIV
• inflammation
• organ transplant
• osteoarthritis
• pain

Article highlights

• The number of patent applications on CB₂ modulators during these last 4 years is maintained compared to the period 2009-2012.

• Patents of pharmaceutical companies are in general more oriented to claim large and structurally diverse series of CB₂ agonists.

• Academic researchers are generally focussing on new therapeutic applications of CB₂ modulators.

• The efficacy of CB₂ selective agonists in the clinic for pain management and inflammation still needs to be proved.

This box summarizes key points contained in the article.

Declaration of interest

This work was supported by Spanish grants from the Spanish Ministry MINECO (SAF2012-40075-C02-02 and SAF2015-68580-C2) and from the Madrid Autonomic Community CAM S2010/BMD-2308. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.