Antithrombotic compounds as well as preparation methods and applications of antithrombotic compounds

A technology of antithrombotic drugs and compounds, applied in the field of medicine, can solve problems such as high bleeding risk

Inactive Publication Date: 2014-10-08
庞庆国
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of these drugs is the greater risk of bleeding

Method used

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  • Antithrombotic compounds as well as preparation methods and applications of antithrombotic compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] .

[0022] Reaction raw materials: self-made, conventional method.

[0023] 1.06 g (10 mmol) of compound II and 1.16 g (10 mmol) of compound III were dissolved in 20 mL of glacial acetic acid and heated to reflux overnight. After the reaction mixture was slightly cooled, it was poured into 200 mL of ice water, stirred, and the solid was collected by suction filtration, recrystallized from absolute ethanol, and vacuum-dried at room temperature to obtain product IV as white crystals. MS, m / z = 205 ([M+H]+).

[0024] 1.02 g (5 mmol) of compound IV, 1.85 g (5 mmol) of compound V and 2.07 g (15 mmol) of solid potassium carbonate were stirred overnight in 15 mL of acetonitrile, and then heated to reflux for 3 hours.

[0025] The reaction mixture was cooled slightly and poured into 200 mL ice water, stirred, adjusted to pH = 4 with concentrated hydrochloric acid, extracted with 50 mL × 3 dichloromethane, combined organic phases, washed with brine, dried over anhydrous sodi...

Embodiment 2

[0026] Example 2 In vitro platelet aggregation inhibition test

[0027] sample Inhibition of Platelet Aggregation IC50 (nM) Compound I 2.7

[0028] It can be seen from the above table that compound I of the present invention exhibits obvious inhibitory effect on platelet aggregation.

Embodiment 3

[0030] Dosage / tablet

[0031] Compound I 10 mg

[0032] Microcrystalline Cellulose 80 mg

[0033] Pregelatinized starch 70 mg

[0034] Polyvinylpyrrolidone 6 mg

[0035] Carboxymethyl starch sodium salt 5 mg

[0036] Magnesium stearate 2 mg

[0037] Talc 2 mg.

[0038] Sieve the active ingredient, pregelatinized starch and microcrystalline cellulose, mix well, add polyvinylpyrrolidone solution, mix, make soft material, sieve, make wet granules, dry at 50-60°C, carboxymethyl Sodium starch salt, magnesium stearate and talc powder are pre-screened and then added to the above granules for tableting.

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Abstract

The invention belongs to the technical field of medicines and relates to PAR (Protease Activated Receptor)-1 antagonists with structures as shown in the formula I, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine. Specifically, it relates to a novel structure of PAR-1 antagonists, a preparation method thereof, a pharmaceutical composition containing them and their use in the preparation of drugs for treating thrombotic diseases. Background technique [0002] Protease Activated Acceptor-1 (PAR-1) is a new target of anti-platelet antithrombotic drugs discovered recently. Protease-activated receptor 1 is also called thrombin receptor. After thrombin is activated by the coagulation chain, it acts on platelets through PAR-1 receptors to activate platelets, causing platelet aggregation and causing thrombus and coagulation. The thrombus induced by PAR-1 is rich in platelet components, which is the main cause of arterial thrombus. PAR-1 antagonists can block thrombin from activating platelets, thereby blocking arterial thrombus formation, and can be used to treat acute coronary syndrome (Acute Coronary Syndrome...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D249/12A61K31/5377A61P7/02
CPCC07D249/12
Inventor 张远强
Owner 庞庆国
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