Conjugate of paeonol and ozagrel, pharmaceutical composition and medical application of conjugate

A technology of paeonol and its composition, applied in the field of medicinal chemistry, can solve the problems of easy decomposition, poor drug compliance of patients, unstable aqueous solution, etc.

Inactive Publication Date: 2013-12-25
上海海虹实业(集团)巢湖今辰药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the drug is eliminated from the blood very quickly after the administration of ozagrel sodium injection, this product can only be administered clinically by continuous intravenous infusion, resulting in poor drug compliance of patients. In addition, the aqueous solution of this product is unstable and easily decomposed when exposed to light. , making its clinical application further limited

Method used

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  • Conjugate of paeonol and ozagrel, pharmaceutical composition and medical application of conjugate
  • Conjugate of paeonol and ozagrel, pharmaceutical composition and medical application of conjugate
  • Conjugate of paeonol and ozagrel, pharmaceutical composition and medical application of conjugate

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Experimental program
Comparison scheme
Effect test

preparation example Construction

[0019] The preparation method of the compound of the present invention is as follows:

[0020]

[0021] The compounds of the present invention can be made into common pharmaceutical preparations by adding pharmaceutically acceptable carriers, such as tablets, capsules, powders, syrups, liquids, suspensions, injections, spices, sweeteners, liquid or solid fillers can be added Or pharmaceutically acceptable pharmaceutical excipients such as diluents.

[0022] The clinical administration of the compound of the present invention can be oral administration, injection and the like.

[0023] Pharmacological tests prove that the compound of the present invention has the effect of preventing or treating cardiovascular and cerebrovascular diseases caused by platelet aggregation, especially can treat diseases such as thrombotic heart and brain ischemia or infarction.

[0024] Below is the pharmacological test and the result of compound of the present invention:

[0025] Experimental...

Embodiment 1

[0036] 1.1 Synthesis of (E)-3-(4-((1H-imidazolyl-1-yl)methyl)phenyl)acryloyl chloride

[0037] Reaction formula:

[0038]

[0039] Reaction steps:

[0040] Ozagrel (6.84g, 0.03mol), CH 2 Cl 2 (60ml) were mixed, 5 drops of DMF was added, and SOCl was added dropwise under stirring at room temperature 2 (15ml) in CH 2 Cl 2 The solution in (30ml) drips in about half an hour, and after dripping, the external temperature is heated to 70 degrees Celsius, and refluxes for 2.5 hours. The reaction solution was evaporated to dryness under reduced pressure to remove SOCl2 , CH 2 Cl 2 , the residue plus CH 2 Cl 2 (20ml) beating, suction filtration to obtain 7.51g of light yellow solid, yield 88.5%.

[0041] 1.2 Synthesis of (E)-2-acetyl-5-methoxyphenyl-3-(4-((1H-imidazolyl-1-yl)methyl)phenyl)acrylate

[0042] Reaction formula:

[0043]

[0044] Reaction steps:

[0045] Paeonol (3.67g, 0.022mol), CH 2 Cl 2 (60ml) and triethylamine (7.5ml) were mixed, and the product fro...

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PUM

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Abstract

The invention discloses a conjugate of paeonol and ozagrel, a pharmaceutical composition and medical application of the conjugate. The conjugate of paeonol and ozagrel has a structural formula shown in the specification. The invention also discloses application of the conjugate of paeonol and ozagrel in preparation of a medicine for preventing or treating cardiovascular and cerebrovascular diseases caused by platelet aggregation, and also discloses the pharmaceutical composition of the conjugate of paeonol and ozagrel, and a carrier containing the conjugate of paeonol and ozagrel or a pharmaceutically acceptable vector. The compound has the effect of preventing or treating cardiovascular and cerebrovascular diseases caused by platelet aggregation, and especially treating the thrombotic cardiovascular and cerebrovascular ischemia or infarct and other diseases.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a paeonol-ozagrel conjugate and a pharmaceutical composition containing them. Background technique [0002] Cardiovascular and cerebrovascular diseases are common and frequently-occurring diseases that seriously endanger human health. With the aging of the social population, the incidence rate is increasing day by day. [0003] Thromboembolism is one of the important factors leading to cardiovascular and cerebrovascular diseases. Coronary artery disease and its corresponding ischemic complications can cause a variety of clinical syndromes, such as stroke, myocardial infarction or peripheral arterial disease. The main cause is the formation of A blood clot blocks a blood vessel, causing severe ischemia. Thromboembolic diseases with coronary thrombosis and cerebral thrombosis as the core also have high morbidity and mortality in my country. Therefore, preventing thrombosis has b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/56A61K31/4174A61P7/02A61P9/10
Inventor 彭代银方国民陈卫东张先文李家明桂双英
Owner 上海海虹实业(集团)巢湖今辰药业有限公司
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