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    • 6. 发明授权
    • Benzothiophen-2-carbonylguanidine derivatives, preparation thereof, and pharmaceutical composition containing the same
    • 苯并噻吩-2-羰基胍衍生物及其制备方法和含有它们的药物组合物
    • US08143307B2
    • 2012-03-27
    • US11794238
    • 2005-12-27
    • Kyu Yang YiSunKyung LeeJee Hee SuhNak Jeong KimHyunsuk LeeByung-Ho LeeSung-eun YooKyung-Hee LeeYong Oh Lee
    • Kyu Yang YiSunKyung LeeJee Hee SuhNak Jeong KimHyunsuk LeeByung-Ho LeeSung-eun YooKyung-Hee LeeYong Oh Lee
    • A61K31/381C07D333/56
    • C07D333/70
    • The present invention is related to benzothiophen-2-carbonylguanidine derivatives, a preparation method thereof, and pharmaceutical compositions containing the same. The derivatives have potent inhibitory effect on the sodium/hydrogen exchanger NHE-I, improve the functional recovery of ischemia/reperfusion-induced heart injury in isolated ischemic heart models, and significantly reduce the myocardiac infarct size in in vivo ischemic animal models, thereby showing excellent cardioprotective effects. Also, the derivatives are protective of both neuronal cells and the brain as proven by their protective effects on neuronal cells from necrosis and apoptosis and by their ability to significantly reduce cerebral infarct sizes in in vivo ischemic brain models. The derivatives can be effectively used for the prevention and treatment of ischemic heart diseases such as myocardiac infarction, arrhythmia, angina pectoris and the like, and cerebrovascular diseases such as cerebral stroke and be used as cardioprotective agents to the patients undergoing reperfusion therapy including chemicals such as thrombolytic agents, or surgery such as coronary artery bypass and percutaneous transluminal coronary angioplasty.
    • 本发明涉及苯并噻吩-2-羰基胍衍生物,其制备方法和含有它们的药物组合物。 该衍生物对钠/氢交换器NHE-1具有有效的抑制作用,改善了分离缺血心脏模型缺血/再灌注诱导的心脏损伤的功能恢复,并显着降低了体内缺血动物模型中的心肌梗死面积,从而显示 良好的心脏保护作用。 此外,衍生物保护神经元细胞和脑,如通过其对来自坏死和凋亡的神经元细胞的保护作用以及通过其在体内缺血性脑模型中显着降低脑梗塞大小的能力所证明的。 该衍生物可以有效地用于预防和治疗心肌梗塞,心律失常,心绞痛等缺血性心脏病,脑血管疾病如脑卒中,并用作心脏保护剂,用于接受再灌注治疗的患者,包括化学药剂 作为溶栓剂,或手术如冠状动脉旁路和经皮腔内冠状动脉成形术。