Patent review of cannabinoid receptor type 2 (CB<sub>2</sub>R) modulators (2016-present)
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Cannabinoid receptor type 2 (CB<sub>2</sub>R), predominantly expressed in immune tissues, is believed to play a crucial role within the body’s protective mechanisms. Its modulation holds immense therapeutic promise for addressing a wide spectrum of dysbiotic conditions, including cardiovascular, gastrointestinal, liver, kidney, neurodegenerative, psychiatric, bone, skin, and autoimmune diseases, as well as lung disorders, cancer, and pain management. This review is an account of patents from 2016 up to 2023 which describes novel CB<sub>2</sub>R ligands, therapeutic applications, synthesis, as well as formulations of CB<sub>2</sub>R modulators. The patents cover a vast, structurally diverse chemical space. The focus of CB<sub>2</sub>R ligand development has shifted from unselective dual-cannabinoid receptor type 1 (CB<sub>1</sub>R) and 2 agonists toward agonists with high selectivity over CB<sub>1</sub>R, particularly for indications associated with inflammation and tissue injury. Currently, there are at least eight CB<sub>2</sub>R agonists and one antagonist in active clinical development. A better understanding of the endocannabinoid system (ECS) and in particular of CB<sub>2</sub>R pharmacology is required to unlock the receptor’s full therapeutic potential.
