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Application of anti-atherosclerotic thrombotic compounds in preparing medicine for treating vascular disfunction

The technology of a compound and a drug is applied in the field of use of an anti-atherosclerotic thrombosis compound in the preparation of a drug for the treatment of vascular disorders, and can solve the problems of platelet aggregation, blockage and the like

Inactive Publication Date: 2007-10-10
SERVIER LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The formed atherosclerotic plaque can rupture under stimulation of local inflammation and oxidative stress, causing aggregation of platelets on the surface, leading to obstruction

Method used

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  • Application of anti-atherosclerotic thrombotic compounds in preparing medicine for treating vascular disfunction
  • Application of anti-atherosclerotic thrombotic compounds in preparing medicine for treating vascular disfunction
  • Application of anti-atherosclerotic thrombotic compounds in preparing medicine for treating vascular disfunction

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Experimental program
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Embodiment Construction

[0035] preclinical data

[0036] The antithrombotic effect of the sodium salt of the (R) isomer of the compound of formula (I) was demonstrated in various models of carotid artery thrombosis, in vivo: vascular electrolysis (dog), mechanical injury (guinea pig) and electrical stimulation ( rat), in vitro (ex vivo): carotid-carotid arterial bypass via glass capillary: the sodium salt of the (R) isomer of the compound of formula (I) prolongs the occlusion time in a dose-dependent manner.

[0037] The antiproliferative, antiatherosclerotic and antiinflammatory effects of the sodium salt of the (R) isomer of the compound of formula (I) were investigated exploratoryly in experimental models: it significantly reduces the surface area of ​​atherosclerotic lesions, Vascular wall thickness and intima / media ratio without lowering serum cholesterol levels. It also inhibited the infiltration of macrophages into the vessel wall and the expression of adhesion molecules, especially markers s...

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Abstract

The present invention relates to the use of a specific antagonist of TP receptors in obtaining medicaments intended for the treatment of vascular disorders in patients having had a previous cerebral vascular accident, especially for reducing cerebrovascular and cardiovascular events in patients having had a previous cerebral ischaemic accident (CIA) or transitory ischaemic attack (TIA).

Description

technical field [0001] The present invention relates to the preparation of specific antagonists of thromboxane-prostaglandin (TP) receptors for the treatment of vascular disorders in patients previously suffering from cerebrovascular accidents (CVA), in particular for the treatment of patients previously suffering from cerebral ischemia Use of drugs to reduce cerebrovascular and cardiovascular events in patients with accident (CIA) or transient ischemic attack (TIA). Background technique [0002] Thromboxane A 2 (TXA 2 ) is an unstable metabolite of arachidonic acid, which is involved in the pathogenesis of many cardiovascular disorders. [0003] TXA 2 and other arachidonic acid metabolites such as endoperoxides (PGG 2 / PGH 2 ), HETEs and isoprostanes are ligands for a co-receptor known as the TP receptor (thromboxane-prostaglandin-endoperoxide). Their binding to TP receptors brings about deleterious effects: platelet activation and aggregation, endothelial dysfunction...

Claims

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Application Information

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IPC IPC(8): A61K31/196A61P9/00A61P9/10
CPCA61K31/196A61P25/00A61P29/00A61P7/00A61P7/02A61P9/00A61P9/10A61K31/64
Inventor M-D·弗拉塔奇A·德科尔杜L·勒龙T·韦伯朗A·吕潘G·拉维埃勒
Owner SERVIER LAB