治疗炎症性疾病的 P2X7 受体拮抗剂专利回顾(2018 年至今)。

IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Expert Opinion on Therapeutic Patents Pub Date : 2024-04-01 Epub Date: 2024-06-11 DOI:10.1080/13543776.2024.2363885
Jamshed Iqbal, Sehrish Bano, Imtiaz Ali Khan, Qing Huang
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引用次数: 0

摘要

简介嘌呤能 P2×7 受体表达于许多不同类型的细胞表面,包括免疫细胞。用拮抗剂靶向 P2×7 受体对多种炎症性疾病具有潜在的治疗作用。它在控制炎症反应中起着至关重要的作用:许多化学物质,包括羧酰胺、苯酰胺、含氮杂环衍生物和金刚烷羰基硫脲化合物,都对 P2×7 受体具有良好的抑制潜力。本综述讨论了2018年至今获得专利的P2×7受体拮抗剂的化学和临床应用:嘌呤能受体抑制剂的发现和应用已显示出治疗干预的潜力,药理学研究也证明了这一点。尽管晶体学和化学生物学方面的突破增加了人们对嘌呤能信号转导及其疾病后果的了解,但授权用于临床的化学模式却寥寥无几。数十年来,许多研究项目和制药运动维持着活跃的 P2X 受体计划,这证明了嘌呤能研究的治疗价值和学术坚持。P2×7 受体是一个令人感兴趣的治疗靶点,也可能是癌症、疼痛和炎症的生物标志物。尽管默克(Merck)和阿斯利康(AstraZeneca)等几家公司已经公布了 P2×3 拮抗剂的专利,但对 P2×7receptor (P2X7R) 拮抗剂的探索并未停止。许多制药公司已经公开了不同的支架,其中一些分子目前正在进行临床研究。
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A patent review of P2X7 receptor antagonists to treat inflammatory diseases (2018-present).

Introduction: The purinergic P2X7 receptor (P2X7R) is expressed on the surface of many different types of cells, including immune cells. Targeting P2X7R with antagonists has been studied for its potential therapeutic effects in a variety of inflammatory illnesses.

Area covered: Many chemical substances, including carboxamides, benzamides and nitrogen containing heterocyclic derivatives have demonstrated promising inhibitory potential for P2X7 receptor. The chemistry and clinical applications of P2X7R antagonists patented from 2018- present are discussed in this review.

Expert opinion: Purinergic receptor inhibitor discovery and application has demonstrated the potential for therapeutic intervention, as demonstrated by pharmacological research. Few chemical modalities have been authorized for use in clinical settings, despite the fact that breakthroughs in crystallography and chemical biology have increased the knowledge of purinergic signaling and its consequences in disease. The many research projects and pharmaceutical movements that sustain dynamic P2X receptor programs over decades are evidence of the therapeutic values and academic persistence in purinergic study. P2X7R is an intriguing therapeutic target and possible biomarker for inflammation. Although several companies like Merck and AstraZeneca have published patents on P2X3 antagonists, the search for P2X7R antagonists has not stopped. Numerous pharmaceutical companies have disclosed different scaffolds, and some molecules are presently being studied in clinical studies.

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来源期刊
CiteScore
12.10
自引率
1.50%
发文量
50
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.
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