Anticoagulant compound, preparation method and application of anticoagulant compound and drug composition containing anticoagulant compound

A compound and drug technology, applied in the field of pharmaceutical compositions containing the compound and anticoagulant compounds, can solve problems such as thrombus, and achieve the effects of high safety, good application prospects and novel structure

Inactive Publication Date: 2015-03-18
北京赛而生物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But if the clot dislodges, it is likely to become a thrombus

Method used

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  • Anticoagulant compound, preparation method and application of anticoagulant compound and drug composition containing anticoagulant compound
  • Anticoagulant compound, preparation method and application of anticoagulant compound and drug composition containing anticoagulant compound
  • Anticoagulant compound, preparation method and application of anticoagulant compound and drug composition containing anticoagulant compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Example 1TM 1 preparation of

[0072]

[0073] Such as figure 1 As shown, the synthesis steps are as follows:

[0074] 1) Add 350mL dry tetrahydrofuran to the reaction flask, add N G -Nitro-N 2 -Boc-L-arginine (31.9g, 0.1mol, purchased from Jill Biochemical (Shanghai) Co., Ltd.), cooling the reaction solution to -20°C, adding triethylamine (10.1g, 0.1mol) and Isobutyl chloroformate (13.6 g, 0.1 mol). After 30 minutes, (2R, 4R)-4-methyl-2-piperidinecarboxylic acid ethyl ester (20.5g, 0.12mol) was added to the reaction solution, and the temperature of the reaction solution was lowered after stirring for 30 minutes at -20°C. Return to room temperature. After the reaction solution was concentrated under reduced pressure, 350 mL of ethyl acetate was added, and after dissolution, the organic layer was washed with 200 mL of water, 100 mL of 5% sodium bicarbonate solution, 100 mL of 10% citric acid solution and 200 mL of water. Ethyl acetate was dried over anhydrous s...

Embodiment 2

[0084] Example 2TM 2 preparation of

[0085]

[0086] Such as figure 2 As shown, the synthesis steps are as follows:

[0087] 1) Dissolve L-proline methyl ester hydrochloride (44.1g, 0.267mol) in dichloromethane, add 37.10ml triethylamine under stirring condition, white flocs are formed, filter the precipitate, and the filtrate is reduced Concentrate under reduced pressure to obtain white solid L-proline methyl ester, which is directly used for the next reaction without further treatment.

[0088] Add 300 mL of dry tetrahydrofuran to the reaction flask, add N G -Nitro-N 2 -Boc-L-arginine (28.4g, 0.089mol), cooled the reaction solution to -20°C, and added triethylamine (9.0g, 0.089mol) and isobutyl chloroformate (12.1g, 0.089 mol). After 30 minutes, L-proline methyl ester was added to the reaction solution, stirred at -20° C. for 30 minutes, and then the temperature of the reaction solution was returned to room temperature. After the reaction solution was concentrate...

Embodiment 3

[0094] Example 3TM 1 injection

[0095] Specifications and composition:

[0096] The capacity of each injection is 2.5mL, and each 1mL injection contains 100mg TM 1 , 300mg D-sorbitol and 400mg absolute ethanol.

[0097] Preparation:

[0098] Add 200g water for injection into a 1000mL beaker, add 300g D-sorbitol to it, stir to dissolve (heat if necessary); then add 400g absolute ethanol, stir and add 100g TM 1 , and stir until completely dissolved. Sterilized by filtration, filled to get 2.5mL / bottle, each 1mL contains 100mg TM 1 injection.

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PUM

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Abstract

The invention relates to a compound shown in a general formula (I) in the specification and a stereoisomer or physiologically acceptable salts thereof and also relates to a preparation method and application of the compound. Besides, the invention also relates to a drug composition containing the compound and an application of the drug composition. The compound which is provided by the invention and can serve as a thrombin inhibitor has good in-vitro human thrombin inhibiting effects and does not have obvious toxicity. Besides, the compound provided by the invention has a novel structure and good biological activity, is simple and convenient to synthesize and is a thrombin inhibitor with a good application prospect.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to an anticoagulant compound that can be used as a thrombin inhibitor, its preparation method and use, and a pharmaceutical composition containing the compound and its use. Background technique [0002] A thrombus is a blood clot that forms in a blood vessel, impeding or blocking blood flow in the circulatory system. When a blood vessel is damaged, platelets and fibrin in the blood will aggregate to form a blood clot to repair it, so as to avoid blood loss or further damage to the blood vessel due to the impact of blood flow. But if the blood clot breaks off, it is more likely to become a thrombus. As a serious peripheral vascular disease, thrombosis is a systemic disease with a wide range of pathogenesis, which can affect upper limbs, lower limbs, visceral blood vessels and carotid arteries; when thrombosis occurs in the heart, myocardial infarction can occur; When it occurs in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/107C07K5/068C07K5/078A61K38/05A61K38/07A61P7/02A61P9/10
CPCY02P20/55
Inventor 马骉杜欣孔双泉
Owner 北京赛而生物药业有限公司
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