Patent review of cannabinoid receptor type 2 (CB₂R) modulators (2016-present).

IF 5.4 2区医学 Q1 CHEMISTRY, MEDICINAL

Expert Opinion on Therapeutic Patents Pub Date : 2024-08-01 Epub Date: 2024-07-02 DOI:10.1080/13543776.2024.2368745

Miroslav Kosar, Leonard Mach, Erick M Carreira, Marc Nazaré, Pal Pacher, Uwe Grether

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引用次数: 0

Abstract

Introduction: Cannabinoid receptor type 2 (CB₂R), 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.

Areas covered: This review is an account of patents from 2016 up to 2023 which describes novel CB₂R ligands, therapeutic applications, synthesis, as well as formulations of CB₂R modulators.

Expert opinion: The patents cover a vast, structurally diverse chemical space. The focus of CB₂R ligand development has shifted from unselective dual-cannabinoid receptor type 1 (CB₁R) and 2 agonists toward agonists with high selectivity over CB₁R, particularly for indications associated with inflammation and tissue injury. Currently, there are at least eight CB₂R agonists and one antagonist in active clinical development. A better understanding of the endocannabinoid system (ECS) and in particular of CB₂R pharmacology is required to unlock the receptor's full therapeutic potential.

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大麻素受体 2 型（CB2R）调节剂专利回顾（2016 年至今）。

简介大麻素受体 2 型（CB2R）主要在免疫组织中表达，被认为在人体保护机制中发挥着至关重要的作用。对它的调节为治疗各种非生物疾病带来了巨大希望，包括心血管、胃肠道、肝脏、肾脏、神经退行性疾病、精神疾病、骨骼、皮肤和自身免疫性疾病，以及肺部疾病、癌症和疼痛治疗：本综述收录了 2016 年至 2023 年的专利，介绍了新型 CB2R 配体、治疗应用、合成以及 CB2R 调节剂的制剂：这些专利涵盖了广阔的、结构多样的化学空间。CB2R 配体开发的重点已从无选择性的 1 型和 2 型大麻素受体（CB1R）双重激动剂转向对 CB1R 具有高选择性的激动剂，特别是针对与炎症和组织损伤相关的适应症。目前，至少有八种 CB2R 激动剂和一种拮抗剂正在积极进行临床开发。我们需要更好地了解内源性大麻素系统（ECS），尤其是 CB2R 的药理学，以充分挖掘该受体的治疗潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Expert Opinion on Therapeutic Patents 医学-药学

CiteScore

12.10

自引率

1.50%

发文量

审稿时长

6-12 weeks

期刊介绍： Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.