Mycobacterium tuberculosis inhibitors: an updated patent review (2021-present).

IF 5.4 2区医学 Q1 CHEMISTRY, MEDICINAL

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-18 DOI:10.1080/13543776.2024.2419826

Salvucci Benedetta, Francesco Vallini, Michela Guida, Chiara Tammaro, Mariangela Biava, Giovanna Poce

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引用次数: 0

Abstract

Introduction: Tuberculosis (TB) remains a major global health issue, causing around 10 million new cases and 1.3 million deaths in 2022. The challenge is compounded by multidrug-resistant (MDR) and extensively drug-resistant (XDR) TB strains, and co-infection with HIV.

Areas covered: The present review examines significant patent literature on TB chemotherapeutics from September 2021 to the present using the following databases, reaxys, google patent and espacenet. Only patents reporting compounds with a minimum inhibitory concentration (MIC) on whole Mycobacterium tuberculosis cells of ≤5 µM were selected for review.

Expert opinion: The fight against TB is advancing with the development of promising new compounds due to the challenge of drug-resistant strains. Notable among those reviewed in this paper are the benzothiazinones, showing high efficacy against both drug-sensitive and resistant TB strains. Additionally, Q203 analogues, demonstrate strong antitubercular activity, good microsomal stability, and favorable safety profiles. Finally, LysRS inhibitors also show significant promise in vivo models. These advancements underscore the importance of novel targets and innovative strategies in developing effective, resistance-resistant TB treatments.

查看原文本刊更多论文

结核分枝杆菌抑制剂：最新专利回顾（2021 年至今）。

导言：结核病（TB）仍然是一个重大的全球健康问题，2022 年将导致约 1000 万新病例和 130 万人死亡。耐多药（MDR）和广泛耐药（XDR）结核菌株以及合并感染艾滋病毒使这一挑战更加严峻：本综述使用以下数据库：reaxys、google patent 和 espacenet，研究了 2021 年 9 月至今有关结核病化疗药物的重要专利文献。本综述只选取报告了对结核分枝杆菌整个细胞的最低抑制浓度（MIC）≤5 µM的化合物的专利进行审查：专家观点：由于耐药菌株的挑战，抗击结核病的斗争正随着有前景的新化合物的开发而不断向前推进。在本文评述的化合物中，苯并噻嗪酮类化合物对药物敏感型和耐药型结核菌株都有很高的疗效。此外，Q203 类似物具有很强的抗结核活性、良好的微粒体稳定性和良好的安全性。最后，LysRS 抑制剂在体内模型中也显示出巨大的前景。这些进展凸显了新靶点和创新策略在开发有效的抗耐药性结核病治疗方法中的重要性。

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.