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Warfarin-aspirin conjugates, their synthesis, antithrombotic activity and applications

A technology of aspirin and warfarin, applied in application, application in preparation of vitamin K antagonist and field of manufacture

Inactive Publication Date: 2021-03-30
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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However, it has not been possible

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  • Warfarin-aspirin conjugates, their synthesis, antithrombotic activity and applications
  • Warfarin-aspirin conjugates, their synthesis, antithrombotic activity and applications
  • Warfarin-aspirin conjugates, their synthesis, antithrombotic activity and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 prepares warfarin-aspirin

[0024] Dissolve 0.51 g (2.7 mmol) of aspirin in 10 mL of anhydrous tetrahydrofuran under ice cooling, add 0.02 g (0.11 mmol) of DMAP, and mix well to obtain reaction solution 1. Dissolve 0.98 g (2.7 mmol) of warfarin in 10 mL of anhydrous tetrahydrofuran, add to reaction solution 1 and stir for 5 min to obtain reaction solution 2. 0.73g (3.4mmol) of DCC was dissolved in 10mL of anhydrous tetrahydrofuran under ice cooling and added dropwise to the reaction solution 2, and stirred for 2 hours to complete the reaction. During stirring, dicyclohexyl urea (DCU) precipitated out. After the reaction, DCU was filtered off. The filtrate was concentrated under reduced pressure to remove THF, the residue was dissolved in dichloromethane, DCU was filtered off, the filtrate was concentrated under reduced pressure, and purified by chromatography to obtain 0.91 g (70%) of warfarin-aspirin as a colorless solid. Mp: 69-70°C. ESI-MS(m / e):493[...

Embodiment 2

[0025] Example 2 Evaluation of the antithrombotic effect of warfarin-aspirin

[0026] Experimental Materials

[0027] Urethane (Sinopharm Chemical Reagent Co., Ltd.), heparin sodium (Bailingwei Technology Co., Ltd.), normal saline (Shijiazhuang No.4 Medicine Co., Ltd.).

[0028] experimental animals

[0029] SD strain rats, male, 200±20g, were purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.

[0030] Bypass cannula

[0031] The bypass intubation tube is composed of three sections. The polyethylene tube with an inner diameter of 1.0 mm and an outer diameter of 2.0 mm is heated and drawn into a thin tube with an oblique opening at one end, and the length is 10.0 cm. The two ends of the bypass cannula; the middle section is composed of polyethylene tube with an inner diameter of 3.5mm, and the length is 8.0cm; the silk thread with rough surface is 6.0cm long and weighs 4.0±0.1mg.

[0032] The inner walls of the three sections of polyethylene tubes...

Embodiment 3

[0042] Embodiment 3 evaluates the antivenous thrombosis effect of warfarin-aspirin

[0043] Experimental Materials

[0044] Urethane (urethane, CAS: 51-79-6, Sinopharm Chemical Reagent Co., Ltd.), normal saline (Shijiazhuang No.4 Medicine Co., Ltd.) warfarin sodium (CAS: 129-06-6, Bailingwei Technology Co., Ltd. ).

[0045] experimental animals

[0046] SD strain rats, male, 250±20g, were purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.

[0047] Experimental method The rat model of inferior vena cava ligation was used in the experiment.

[0048] Grouping and dosage:

[0049] The dose of the compound warfarin-aspirin of the present invention is 0.1 μmol / kg, the dose of the positive control warfarin is 4.87 μmol / kg, and the negative control is physiological saline.

[0050] Reagent preparation

[0051] The anesthetic was 20% urethane solution prepared in normal saline.

[0052] Experimental operation:

[0053] Before the operation, the rats w...

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Abstract

The invention discloses a warfarin-aspirin conjugate and its preparation method, arterial thrombosis-resistant activity, venous thrombosis-resistant activity, internal vitamin K content reduction activity, internal blood coagulation factor II content reduction activity, platelet aggregation inhibiting activity and the advantage of no bleeding risk caused by warfarin. The invention also discloses a use of the warfarin-aspirin conjugate in preparation of arterial thrombosis-resistant drugs, venous thrombosis-resistant drugs, platelet aggregation inhibiting drugs, a vitamin K antagonist and a blood coagulation factor II antagonist.

Description

technical field [0001] The present invention relates to a novel warfarin-aspirin, to its preparation method, to its anti-arterial thrombosis activity, to its anti-venous thrombosis activity, to its function of reducing the content of vitamin K in the body, and to its function of reducing blood coagulation in the body The effect of factor II levels, related to its inhibitory effect on platelet aggregation, related to its no advantage in reducing the risk of warfarin-like bleeding. Thus the present invention relates to its application in the preparation of anti-arterial thrombosis drugs, its application in the preparation of anti-venous thrombosis drugs, its application in the preparation of platelet aggregation inhibiting drugs, its application in the preparation of vitamin K antagonists and its use in the preparation of coagulation factor II Antagonist applications. The invention belongs to the field of biomedicine. Background technique [0002] Both arterial thrombosis an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/56A61K31/37A61P7/02A61P3/00
CPCC07D311/56
Inventor 彭师奇赵明吴建辉王玉记张薪
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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