Furancarbonylguanidine derivatives, their preparation and...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 307/68 (2006.01)

Patent

CA 2549506

The present invention relates to furancarbonylguanidine derivatives, a preparation method thereof and a pharmaceutical composition comprising the same. Furancarbonylguanidine derivatives of the present invention inhibit NHE- 1 (sodium-hydrogen exchanger isoform 1), which helps recovery of heart function damaged from ischemia/ reperfusion and decreases myocardial infarction rate, indicating that they have protective effect on myocardial cells. Thus, furancarbonylguanidine derivatives of the present invention can be ef~fectively used for the prevention and the treatment of ischemic heart diseases such as myocardial infarction, arrhythmia, angina pectoris, etc, and also a promising candidate for a heart protecting agent applied to reperfusion therapy including thrombolytics or cardiac surgery including coronary artery bypass graft, percutaneous transluminal coronary angioplasty, etc.

La présente invention se rapporte à des dérivés de furancarbonylguanidine, à un procédé de préparation de ces dérivés et à une composition pharmaceutique les contenant. Les dérivés de furancarbonylguanidine de la présente invention inhibent NHE-1 (isoforme 1 d'échangeur sodium-hydrogène), ce qui facilite une récupération de la fonction cardiaque endommagée suite à une ischémie/reperfusion et réduit le taux d'infarctus du myocarde, ceci indiquant que ces dérivés présentent un effet protecteur sur les cellules du myocarde. Ainsi, les dérivés de furancarbonylguanidine de la présente invention peuvent être utilisés efficacement pour la prévention et le traitement des maladies cardiaques ischémiques du type infarctus du myocarde, arythmie, angine de poitrine, etc., et également constituer un candidat prometteur en tant qu'agent de protection du coeur appliqué à une thérapie de reperfusion, et notamment à une chirurgie thrombolytique ou cardiaque du type pontage aortocoronarien, à une angioplastie coronarienne transluminale percutanée, etc..

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