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Edoxaban tosilate hydrate

A technology of p-toluenesulfonic acid and edoxaban, applied in organic chemistry, drug combination, blood diseases, etc., can solve the problem of weak inhibitory activity and achieve the effect of low impurity content

Active Publication Date: 2016-07-20
海思科制药(眉山)有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In vitro, edoxaban p-toluenesulfonate competitively and selectively inhibits FXa, but has weak inhibitory activity against serine proteases of other related coagulation factors

Method used

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  • Edoxaban tosilate hydrate
  • Edoxaban tosilate hydrate
  • Edoxaban tosilate hydrate

Examples

Experimental program
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Effect test

Embodiment 2

[0022] The formulation of embodiment 2-quality research and quality standard of compound of the present invention

[0023] The specific degradation impurities contained in edoxaban p-toluenesulfonate are impurities L, M, N, O. Among them, impurities L and M are hydrolysis products of edoxaban, which are easier to produce under alkaline conditions; impurities N and O are oxidation products.

[0024] According to the results of influencing factor tests and stability tests, the main impurities produced by self-produced and commercially available products during the storage process are oxidized impurities N and O, which will increase under high temperature and high humidity conditions.

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Abstract

The invention provides edoxaban tosilate hydrate. Edoxaban is a micromolecule oral anticoagulant drug, and is a blood coagulation factor X(FXa) retarding agent. In the process of blood coagulation, the activated coagulation factor X(FXa) activates prothrombin (FII) into thrombin (FIIa), formation of fibrin is promoted, and thrombus is formed, so that FXa is developed as a main target of a new generation anticoagulant drug. Edoxaban is the oral anticoagulant drug by selectively, reversibly and directly inhibiting FXa in order to inhibit formation of thrombus.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to an edoxaban p-toluenesulfonate compound. Background technique [0002] Edoxaban p-toluenesulfonate, the chemical name is N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(dimethylaminocarbonyl)-2-( 5-Methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamido)cyclohexyl]oxalamide (p-toluenesulfonate) monohydrate [0003] Chemical Structure: [0004] [0005] Molecular formula: C24H30ClN7O4S C7H8O3S H2O, molecular weight: 738.27 [0006] Thrombosis can cause stenosis and occlusion of the vascular lumen, leading to ischemia and infarction of major organs, thereby causing various diseases, such as myocardial infarction, ischemic cerebral infarction, and venous thromboembolism. Venous thromboembolism (VTE), including deep vein thrombosis (deep vein thrombosis, DVT) and pulmonary embolism (pulmonary embolism, PE), has become a common disease that seriously threate...

Claims

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Application Information

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IPC IPC(8): C07D513/04A61K31/444A61P7/02
Inventor 易仕旭
Owner 海思科制药(眉山)有限公司
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