Medicinal Chemistry, Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP) Berlin, Berlin, 13125, Germany.
Roche Pharma Research & Early Development, Roche Innovation Center Basel, F Hoffmann-La Roche Ltd, Basel, 4070, Switzerland.
Pharm Pat Anal. 2021 May;10(3):111-163. doi: 10.4155/ppa-2021-0002. Epub 2021 Jun 11.
The G-protein-coupled cannabinoid receptor type 2 (CBR) is a key element of the endocannabinoid (EC) system. EC/CBR signaling has significant therapeutic potential in major pathologies affecting humans such as allergies, neurodegenerative disorders, inflammation or ocular diseases. CBR agonism exerts anti-inflammatory and tissue protective effects in preclinical animal models of cardiovascular, gastrointestinal, liver, kidney, lung and neurodegenerative disorders. Existing ligands can be subdivided into endocannabinoids, cannabinoid-like and synthetic CBR ligands that possess various degrees of potency on and selectivity against the cannabinoid receptor type 1. This review is an account of granted CBR ligand patents from 2010 up to the present, which were surveyed using Derwent Innovation.
G 蛋白偶联型大麻素受体 2(CBR)是内源性大麻素(EC)系统的关键组成部分。EC/CBR 信号在影响人类的主要疾病(如过敏、神经退行性疾病、炎症或眼部疾病)的治疗中具有重要的潜力。在心血管、胃肠道、肝脏、肾脏、肺部和神经退行性疾病的临床前动物模型中,CBR 激动剂发挥抗炎和组织保护作用。现有的配体可分为内源性大麻素、类大麻素和合成 CBR 配体,它们对大麻素受体 1 具有不同程度的效力和选择性。本综述介绍了截至目前(2023 年 7 月)已授权的 CBR 配体专利,这些专利是使用德温特创新专利数据库检索到的。