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1.发明授权BENZOTHIOPHEN-2-CARBONYLGUANIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 有权苯并噻吩-2- CARBONYLGUANIDINDERIVATE，生产，药品成分包含此
公开(公告)号：EP1831192B1
公开(公告)日：2011-08-24
申请号：EP05822428.8
申请日：2005-12-27
发明人： YI, Kyu Yang , LEE, SunKyung , SUH, Jee Hee , KIM, Nak Jeong , LEE, Hyunsuk , LEE, Byung-Ho , YOO, Sung-eun , LEE, Kyung-Hee, 204-1005 Pureunmaeul Byucksan Apt. , LEE, Yong Oh
IPC分类号： C07D333/70
CPC分类号： C07D333/70
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.
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2.发明公开BENZOTHIOPHEN-2-CARBONYLGUANIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 有权苯并噻吩-2- CARBONYLGUANIDINDERIVATE，生产，药品成分包含此
公开(公告)号：EP1831192A1
公开(公告)日：2007-09-12
申请号：EP05822428.8
申请日：2005-12-27
发明人： YI, Kyu Yang , LEE, SunKyung , SUH, Jee Hee , KIM, Nak Jeong , LEE, Hyunsuk , LEE, Byung-Ho , YOO, Sung-eun , LEE, Kyung-Hee, 204-1005 Pureunmaeul Byucksan Apt. , LEE, Yong Oh
IPC分类号： C07D333/70
CPC分类号： C07D333/70
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.
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