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Anticoagulated small-molecule compound, application thereof and drug including compound

A small molecular compound and small molecule technology, applied in the field of biomedicine, can solve the problems of narrow drug treatment window, easy to cause bleeding complications, etc., achieve the effect of small bleeding side effects, solve bleeding side complications, and prolong thromboplastin time

Active Publication Date: 2019-04-16
深圳市龙华区中心医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Whether it is traditional blood coagulation drugs such as warfarin and heparin or FXa inhibitors (rivaroxaban, apixaban, etc.) Although new drugs such as dabitran etexilate and hirudin have good blood coagulation effects, they all have a fatal deficiency. The drug treatment window is relatively narrow, which easily causes bleeding complications.

Method used

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  • Anticoagulated small-molecule compound, application thereof and drug including compound
  • Anticoagulated small-molecule compound, application thereof and drug including compound
  • Anticoagulated small-molecule compound, application thereof and drug including compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The synthetic equation of the anticoagulant small molecular compound that selectively inhibits blood coagulation factor XIa is as follows:

[0039]

[0040] Will with CH 2 (COOH) 2 According to the molar ratio of 1:1.1, the reaction is carried out at 76 degrees Celsius to obtain then With ethanol according to the molar ratio of 1:1, react at 6 degrees Celsius to get

[0041] 2) Will According to the molar ratio of 1:22 with thionyl chloride, react under the condition of 79 degrees Celsius to obtain

[0042] 3) The obtained in step 1) and obtained in step 2) According to the molar ratio of 1:1, the reaction is carried out at 0 degrees Celsius to obtain

Embodiment 2

[0044] Anticoagulant activity of the anticoagulant small molecular compound provided by the invention

[0045] The anticoagulant activity of the anticoagulant small molecular compound provided by the invention is observed by detecting activated partial thromboplastin time (aPTT) and prothrombin time (PT).

[0046] Determination of prothrombin time (PT): Prepare 1 part of anticoagulant small molecule compound with different concentrations and 4 parts of normal human plasma, mix well and incubate at 37°C for 15 minutes, then use a coagulation instrument S5100 (SYSMEX, Japan), and set the measurement parameters as follows: mix Plasma 50ul+50ul original aPTT reagent+50ul original calcium chloride reagent. The instrument reads the result. Each concentration was repeated twice, and the average value was taken. Experimental results such as figure 1 shown.

[0047] Determination of prothrombin time (PT): Prepare 1 part of anticoagulant small molecule compound with different concen...

Embodiment 3

[0051] Effects of Anticoagulant Small Molecular Compounds on Coagulation Time in Rats

[0052] 40 SPF grade SD rats (provided by the Experimental Animal Center of Guangdong Medical University), weighing 250 ± 50g, were randomly divided into 4 groups, namely blank control group (distilled water), low-dose anticoagulant small molecule group (20mg / kg), Anticoagulant small molecule medium dose group (40mg / kg) and anticoagulant small molecule high dose group (80mg / kg), 10 rats in each group. Rats were intragastrically administered, and after 3 hours, blood was taken from the tail vein or eyeballs, injected into a plastic tube added with 3.8% sodium citrate (blood: anticoagulant = 9:1), and shaken gently. Centrifuge at 1500Xg for 10min to separate the plasma. Determination of aPTT and PT, the measurement method is as described in (2). The results are shown in Table 1

[0053] the result shows

[0054] Anticoagulant small molecule compounds can significantly prolong plasma activa...

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Abstract

The invention relates to an anticoagulated small-molecule compound, application thereof and a drug including the compound. A structural formula of the anticoagulated small-molecule compound is shown in the description, and the anticoagulated small-molecule compound can selectively inhibit a coagulation factor XIa, has high anticoagulation activity, can obviously prolong the thrombin time of a activated part of plasma, generates little influence on the prothrombin time and has no influence on the thrombin time. Small molecules have an excellent antithrombotic effect, and the compound can be absorbed orally and used for preparing oral drugs for preventing and treating thrombotic diseases and have a small side effect.

Description

technical field [0001] The invention belongs to the field of biomedicine. Specifically, the present invention relates to a class of anticoagulant polypeptides and the application of the anticoagulant polypeptides in the prevention and treatment of thrombotic diseases. Background technique [0002] At present, the most important and common complication in the prevention and treatment of clinical antithrombotic drugs is bleeding. Therefore, there is a very urgent clinical need to find effective anticoagulant and antithrombotic drugs with low bleeding risk. In recent years, through clinical research on hemophilia C (FXI deficiency syndrome), animal experiments of knocking out FXI gene and antithrombotic experiments of FXIa inhibitors have shown that: FXI, as a new target for antithrombotic prevention and treatment, has a wide window of drug treatment and anti-hemorrhage The side effects are small, but the current research on fXIa inhibitors as new drugs has only recently recei...

Claims

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Application Information

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IPC IPC(8): C07D235/06C07D261/20A61K31/4184A61K31/423A61P7/02
CPCA61P7/02C07D235/06C07D261/20
Inventor 李少金肖水秀张肄鹏邵正梁旭玲杨宜球何小奇
Owner 深圳市龙华区中心医院
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