大麻素受体 1 拮抗剂专利更新（2015-2018）。
A patent update on cannabinoid receptor 1 antagonists (2015-2018).
机构信息
a Center for Drug Discovery , RTI International , RTP , NC , USA.
出版信息
Expert Opin Ther Pat. 2019 Apr;29(4):261-269. doi: 10.1080/13543776.2019.1597851. Epub 2019 Apr 8.
Abstract
INTRODUCTION
The endocannabinoid system is an important regulator of various physiological processes. Preclinical and clinical studies indicate that attenuation of the endocannabinoid system via antagonism of the type 1 cannabinoid receptor (CB1) is an excellent strategy to treat obesity, metabolic syndrome and associated disorders. However, centrally acting antagonists of CB1 also produce adverse effects like depression and anxiety. Current efforts are geared towards discovery and optimization of antagonists and modulators of CB1 that have limited brain penetration.
AREAS COVERED
Several recent publications and patent applications support the development of peripherally acting CB1 receptor antagonists and modulators. In this review, recent patents and applications (2015-2018) are summarized and discussed.
EXPERT OPINION
Approximately 30 new inventions have been reported since 2015, along with 3 recent commercial deals, highlighting the importance of this class of therapeutics. Taken together, peripherally acting CB1 receptor antagonists and modulators are an emerging class of drugs for metabolic syndrome, non-alcoholic steatohepatitis (NASH) and other important disorders where this receptor has been implicated.
摘要
简介
内源性大麻素系统是各种生理过程的重要调节剂。临床前和临床研究表明，通过拮抗 1 型大麻素受体（CB1）来减弱内源性大麻素系统是治疗肥胖症、代谢综合征和相关疾病的一种极好策略。然而，中枢作用的 CB1 拮抗剂也会产生抑郁和焦虑等不良反应。目前的努力方向是发现和优化具有有限脑穿透性的 CB1 拮抗剂和调节剂。
涵盖领域
几项最近的出版物和专利申请支持开发外周作用的 CB1 受体拮抗剂和调节剂。在这篇综述中，总结和讨论了最近的专利和申请（2015-2018 年）。
专家意见
自 2015 年以来，大约有 30 项新发明被报道，此外还有 3 项最近的商业交易，突出了这类治疗药物的重要性。总之，外周作用的 CB1 受体拮抗剂和调节剂是一种新兴的治疗代谢综合征、非酒精性脂肪性肝炎（NASH）和其他重要疾病的药物，这些疾病与该受体有关。
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