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抑制剂:最新专利综述(2021年至今)

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

作者信息

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

机构信息

Department of Chemistry and Technologies of Drugs, Sapienza University of Rome, Rome, Italy.

出版信息

Expert Opin Ther Pat. 2024 Dec;34(12):1215-1230. doi: 10.1080/13543776.2024.2419826. Epub 2024 Nov 18.

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 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 models. These advancements underscore the importance of novel targets and innovative strategies in developing effective, resistance-resistant TB treatments.

摘要

引言

结核病仍然是一个重大的全球健康问题,2022年导致约1000万新发病例和130万人死亡。耐多药(MDR)和广泛耐药(XDR)结核菌株以及与艾滋病毒的合并感染使这一挑战更加复杂。

涵盖领域

本综述使用以下数据库(reaxys、谷歌专利和欧洲专利局专利数据库)研究了2021年9月至今关于结核病化疗药物的重要专利文献。仅选择报告对全细胞最小抑菌浓度(MIC)≤5 μM的化合物的专利进行综述。

专家意见

由于耐药菌株的挑战,随着有前景的新化合物的开发,抗击结核病的斗争正在取得进展。本文综述的化合物中值得注意的是苯并噻嗪酮类,它们对药物敏感和耐药结核菌株均显示出高效。此外,Q203类似物表现出强大的抗结核活性、良好的微粒体稳定性和良好的安全性。最后,赖氨酰-tRNA合成酶(LysRS)抑制剂也显示出显著的前景。这些进展强调了新靶点和创新策略在开发有效、抗耐药结核病治疗方法中的重要性。

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