Kyu Yang Yi,SunKyung Lee,Jee Hee Suh,Nak Jeong Kim,Hyunsuk Lee,Byung-Ho Lee,Sung-eun Yoo,Kyung-Hee Lee,Yong Oh Lee
申请号：
US11794238
公开号：
US08143307B2
申请日:
2005.12.27
申请国别(地区):
US
年份:
2012
代理人:
摘要：
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.
