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用于治疗分枝杆菌感染的化合物:专利评价(WO2014049107A1)。

Compounds for use in the treatment of mycobacterial infections: a patent evaluation (WO2014049107A1).

机构信息

Unité de Service et de Recherche CNRS - Pierre Fabre n°3388 ETaC - Epigenetic Targeting of Cancer , CRDPF, 3 avenue Hubert Curien, 31035 Toulouse Cedex 01 , France

出版信息

Expert Opin Ther Pat. 2015 Jun;25(6):729-35. doi: 10.1517/13543776.2015.1021333. Epub 2015 Mar 10.

Abstract

Tuberculosis is one of the main causes of mortality with 1.5 million deaths a year worldwide. The growing emergence of multi- and extremely resistant strains highlights the urgent need of novel antibiotic strategies. Ethionamide, interfering with the mycobacterial membrane biosynthesis, is used in second-line treatment. This molecule is a prodrug, which requires activation by EthA. The patent described in this evaluation (WO2014049107A1) claimed a new family of molecules and their use as antibiotic treatment against mycobacteria such as Mycobacterium tuberculosis, M. leprae and atypical mycobacteria, either as a single active agent or in combination with antibiotics activable by EthA pathway.

摘要

结核病是导致全球每年 150 万人死亡的主要原因之一。越来越多的多药和极端耐药菌株的出现凸显了新型抗生素策略的迫切需求。乙硫异烟胺通过干扰分枝杆菌细胞膜的生物合成,用于二线治疗。该分子是一种前药,需要 EthA 激活。本评价中描述的专利(WO2014049107A1)要求一种新的分子家族及其作为抗生素治疗分枝杆菌(如结核分枝杆菌、麻风分枝杆菌和非典型分枝杆菌)的用途,无论是作为单一活性成分还是与 EthA 途径激活的抗生素联合使用。

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