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Disubstituted tetrazole acetophenone compound, its preparation method and use

A technology of compounds and uses, which is applied in the field of drugs related to thrombosis diseases, and can solve problems such as high bleeding risk

Inactive Publication Date: 2015-10-14
XUZHOU FENGRUN BIOLOGICAL ORGANIC FERTILIZER TECH DEV CO LTD
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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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  • Disubstituted tetrazole acetophenone compound, its preparation method and use
  • Disubstituted tetrazole acetophenone compound, its preparation method and use
  • Disubstituted tetrazole acetophenone compound, its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] .

[0029] Reaction materials: homemade, conventional methods.

[0030] 2.20 g (10 mmol) compound II-1 , 3.70 g (10 mmol) compound III-1 And 4.15 g (30 mmol) solid potassium carbonate were stirred overnight in 20 mL acetonitrile, and then heated to reflux for 3 hours.

[0031] The reaction mixture was slightly cooled and poured into 200 mL ice water, stirred, adjusted to pH = 4 with concentrated hydrochloric acid, extracted with 50 mL × 3 dichloromethane, combined the organic phases, washed with brine, dried with anhydrous sodium sulfate, and placed on a rotary evaporator. Evaporate the solvent on top, and the residue obtained is purified by column chromatography to obtain pure product I-1 , White solid, MS, m / z = 518 ([M+Na] + ).

Embodiment 2-4

[0033] According to the method of Example 1, synthesized with the general formula I The following compounds:

[0034] .

Embodiment 5

[0035] Example 5 In vitro platelet aggregation inhibition test

[0036] "In a 96-well plate, the pharmacological test of the substance was performed in the platelet aggregation induced by TRAP (thrombin receptor activating peptide). 3.13% sodium citrate solution was added to the syringe in advance, and then 20 mL of healthy volunteers’ blood was drawn into the syringe. g After centrifugation for 20 minutes, platelet-rich plasma (PRP) was separated and treated with 1 μL PGE1 solution (500 μg / mL ethanol solution) / mL PRP. After incubating for 5 minutes at room temperature, it was centrifuged at 1200 g for 20 minutes to remove leukocytes. PRP without leukocytes was transferred to 15 mL PP tubes in 5 mL / parts, and centrifuged at 3600 g to pellet platelets. Then, the upper plasma was decanted and the platelet pellet obtained from 5 mL PRP was resuspended in 1 mL Tyrode (120 mM NaCl, 2.6 mM KCl, 12 mM NaHCO3, 0.39 mM NaH2PO4, 10 mM HEPES, 0.35% BSA, 5.5 mM Glucose, pH = 7.4), and use...

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Abstract

The invention relates to the field of medicines related to thrombotic diseases, in particular to a disubstituted PAR-1 (Protease Activated Acceptor-1) agonist containing a tetrazole acetophenone structure, a preparation method thereof, a medicine composition containing the PAR-1 agonist and application of the PAR-1 agonist to preparation of medicines for treating thrombotic diseases. The formula (I) and the definition of R group are shown in the specification.

Description

technical field [0001] The invention relates to the field of drugs related to thrombosis diseases. Specifically, the present invention relates to a class of disubstituted tetrazoleacetophenone-containing PAR-1 antagonists that have a therapeutic effect on thrombotic diseases, a preparation method thereof, and a pharmaceutical composition containing them. 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D257/04A61K31/5377A61P7/02
CPCC07D257/04
Inventor 张远强
Owner XUZHOU FENGRUN BIOLOGICAL ORGANIC FERTILIZER TECH DEV CO LTD
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