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4H-45-e14-58- Muti-substituted 4H-thiazolo45-e14diazepine-58-dione derivatives and use thereof

机译:4H- [45-e] [14] -58-多取代的4H-噻唑并[45-e] [14]二氮杂-58-二酮衍生物及其用途

摘要

The present invention relates to a poly-substituted 4H-thiazolo[4,5-e][1,4]diazepine-5,8-dione derivative represented by chemical formula 1, and a use of the same as a pharmaceutical composition for preventing or treating vascular inflammation-associated infections induced by the activation of HMGB1 protein containing the same as an effective component. As a result of screening for antiseptic effects through CLP-induced sepsis animal experiments, the poly-substituted 4H-thiazolo[4,5-e][1,4]diazepine-5,8-dione derivative of the present invention was found to increase the survival rate of patients with sepsis, and thus the pharmaceutical composition of the present invention, by comprising the poly-substituted 4H-thiazolo[4,5-e][1,4]diazepine-5,8-dione derivative or a pharmaceutically acceptable salt thereof as an effective component, may be beneficially used as a therapeutic agent for vascular inflammation and infection diseases including sepsis induced by the activation of HMGB1 protein.
机译:本发明涉及化学式1表示的多取代的4H-噻唑并[4,5-e] [1,4]二氮杂-5,8-二酮衍生物及其作为药物组合物的用途或治疗因含有有效成分的HMGB1蛋白活化而引起的与血管炎症相关的感染。通过CLP诱导的败血症动物实验筛选抗菌效果的结果,发现本发明的多取代的4H-噻唑并[4,5-e] [1,4]二氮杂-5,8-二酮衍生物具有通过包含多取代的4H-噻唑并[4,5-e] [1,4]二氮杂-5,8-二酮衍生物或α-吡咯烷酮来增加败血症患者的存活率,从而提高本发明的药物组合物其药学上可接受的盐作为有效成分,可以有利地用作血管炎和感染疾病的治疗剂,所述疾病包括通过激活HMGB1蛋白诱导的败血症。

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