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Treatment effect of 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative on thrombi

A technology of pyridine derivatives and tetrahydrothiophene, which is applied in the field of medicine, can solve the problems of long antithrombotic time, single action target, and patients giving up treatment, and achieve good anticoagulant effect, quick effect, and good bioavailability Effect

Inactive Publication Date: 2018-09-25
RIZHAO PUDA PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Western medicines include clopidogrel, aspirin, etc., but their targets are single, and multiple drugs such as thrombolysis, neuroprotection, anti-inflammation, and nutrition should be used in combination for each lesion, and the cost is high
Traditional Chinese medicine has the advantages of strong long-term effect, strong drug resistance, safety and non-toxicity, and is very suitable for long-term use of middle-aged and elderly patients with thrombosis. However, the anti-thrombotic time is long, and it is easy for patients to give up treatment. Therefore, it is necessary to continue to explore and develop new treatments for thrombosis. medicine

Method used

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  • Treatment effect of 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative on thrombi
  • Treatment effect of 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative on thrombi
  • Treatment effect of 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative on thrombi

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Synthesis of 2-acetoxy-5-(α-methylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine.

[0052]

[0053] The synthetic route is:

[0054] .

[0055] The synthesis steps are:

[0056] Dissolve 4-thio-hexahydropyrazole-2-acetic acid (compound 1) (10g) in a mixed solvent of propylene oxide (60ml) and ether (20ml), add sodium hydroxide solution (10ml), trichloro Phosphate (1.1g) and liquid chlorine (20ml) are fully stirred and mixed, and under the action of sodium hydroxide solution and phosphorus trichloride, α-halogen substitution reaction of carboxylic acid occurs with liquid chlorine at 65-100°C, reaction 6 -10h, 4-thio-hexahydropyrazole-2-chloroacetic acid (compound 2) (10.21g) was obtained;

[0057] 4-Thio-hexahydropyrazole-2-chloroacetic acid (compound 2) (10.21g) was dissolved in tetrahydrofuran (80ml) in the presence of potassium carbonate (0.7g) and iodine (0.05g), and 1-methyl -3-Bromo-3-(2-fluorophenyl)-2-propanone (compound 3) (12g), heate...

Embodiment 2

[0062] Synthesis of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-benzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine.

[0063]

[0064] The synthetic route is:

[0065] .

[0066] The synthesis steps are:

[0067] Dissolve 4-thio-hexahydropyrazole-2-acetic acid (compound 1) (20g) in a mixed solvent of propylene oxide (100ml) and ether (20ml), add sodium hydroxide solution (15ml), trichloro Phosphate (1.6g) and liquid chlorine (35ml) are fully stirred and mixed, and under the action of sodium hydroxide solution and phosphorus trichloride, an α-halogen substitution reaction of carboxylic acid occurs with liquid chlorine at 65-100°C. Reaction 6 -10h, 4-thio-hexahydropyrazole-2-chloroacetic acid (compound 2) (20.38g) was obtained;

[0068] 4-Thio-hexahydropyrazole-2-chloroacetic acid (compound 2) (20.38g) was dissolved in tetrahydrofuran (150ml) in the presence of potassium carbonate (1.0g) and iodine (0.08g), and 1-cyclopropane was added Base-3-bromo-3-(2-phenyl)-2-propanone (compou...

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Abstract

The invention provides a treatment effect of a 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative on thrombi. The 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative has the following generalformula structure: (with reference to the specification), wherein R<1> represents C1-C6 alkyl acyloxy; R<2> and R<3> can be the same or different, and are respectively independently selected from C1-C6 alkyl, C1-C6 alkoxy, a halo substituent of C1-C6 alkyl, C1-C6 naphthenic base, C1-C6 alkyl sulphanyl, aryl, a substituent group of aryl, heteroaryl, a substituent group of heteroaryl or heterocyclic alkyl. According to the invention, the new 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative is synthesized, which is a blood platelet adenosine diphosphate receptor inhibitor and is used fortreating thrombi; active molecules are formed in a body and are combined with a blood platelet P2Y12 receptor to exert effects; the 4,5,6,7-tetrahydrothiophene-[3,2-c] pyridine derivative has an excellent anticoagulant effect and meanwhile, has excellent bioavailability.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular, the invention relates to the therapeutic effect of a 4,5,6,7-tetrahydrothieno[3,2-c]pyridine derivative on thrombus. Background technique [0002] A thrombus is a small piece of blood that forms on the surface of a vessel in the cardiovascular system where the lining has been peeled off or repaired. Thrombosis is the abnormal accumulation of blood components in local blood vessels of the human body. With the continuous improvement of people's living standards, the incidence of thrombotic diseases is increasing year by year. The causes of thrombosis include damage to the intima of the heart and blood vessels, changes in blood flow, and changes in blood properties. The formation process is a multi-factorial change process that interacts and affects each other with genetic factors and environmental factors. The normal blood coagulation of the body mainly depends on the complete stru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/4545A61K31/4375A61P7/02
CPCA61P7/02C07D495/04
Inventor 不公告发明人
Owner RIZHAO PUDA PHARMA TECH CO LTD
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