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Use of imidazolone compounds for treating cardiovascular and cerebrovascular diseases

A technology for cardiovascular and cerebrovascular diseases and cerebrovascular diseases, applied in the field of medicine, can solve problems such as adverse reactions, unfavorable confrontation and balance, and damage to gastric mucosa

Inactive Publication Date: 2008-08-06
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, aspirin can also directly inhibit prostaglandin synthase in the blood vessel wall, reduce the synthesis of prostacyclins (PGs), tilt the metabolic balance of arachidonic acid in the body towards 5-LOX and COX-2, and produce a large number of inflammatory mediators such as LTs and PGE 2 etc., LTs and PGE 2 Inflammatory mediators such as inflammatory mediators have multiple biological activities, such as vasoconstriction, leukocyte adhesion, and induction of TNFs and ILs production, etc. , 62(11):1433-1438); at the same time, due to the inhibition of PGI by aspirin 2 The generation is not conducive to fighting and balancing TXA 2 Therefore, obvious gastrointestinal adverse reactions occur, damage the gastric mucosa, cause gastric bleeding; even cause side effects such as headache, tinnitus, dizziness, and vision loss.

Method used

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  • Use of imidazolone compounds for treating cardiovascular and cerebrovascular diseases
  • Use of imidazolone compounds for treating cardiovascular and cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] In vitro antiplatelet aggregation test

[0016] For male SD rats, the common carotid artery was isolated under anesthesia, blood was collected, and anticoagulated with heparin. Prepare platelet-rich plasma (PRP) and platelet-poor plasma (PPP) according to the literature (Xu Shuyun, Pharmacological Experimental Methodology, Third Edition, 2001: 1281), centrifuge the anticoagulated blood at 150×g for 10 minutes, and suck out the upper layer of plasma, which is PRP; the remaining blood was centrifuged at 3000×g for 15 minutes, and the supernatant was taken as PPP. Adjust the number of platelets in PRP with PPP to 5×10 8 / ml. Different inducers ADP (50 μM), arachidonic acid (300 μg·ml -1 ) and collagen (6μg·ml -1 ) to induce platelet aggregation, measure the maximum aggregation rate of platelets with NBY-6 platelet aggregation meter, and calculate the inhibition rate by formula: inhibition rate=(A model -A test ) / A model ×100%, the results showed that the compound ZL...

Embodiment 2

[0024] In vivo antiplatelet aggregation test

[0025] Male SD rats were randomly divided into model control group and aspirin group (30 mg·kg -1 ), CI-1004 (Darbufelone developed by Pfizer) group (5mg·kg -1 ) and ZLJ-6 high and low dose groups (10mg·kg -1 , 3mg·kg -1 ), 8 in each group. Continuous intragastric administration for 7 days. 2 hours after the last administration, blood was taken, anticoagulated with heparin, and the whole blood was allowed to stand still for 50-60 minutes. Take the blood sample and slowly inject it into a special siliconized test tube, add Tyrode's buffer, incubate at 37°C for 10 minutes, insert the sample tube into the measurement hole, put it into the stirring bar to stir, insert the electrode into the test tube until the digital display value is stable, and then adjust to zero. Then add aggregation inducer ADP solution (50 μM), arachidonic acid (300 μg·ml -1 ) or collagen (6μg·ml -1 ), timing. Record the maximum resistance value within 5...

Embodiment 3

[0031] Arteriovenous bypass thrombosis test in rats

[0032] Male SD rats were randomly divided into model control group and aspirin group (30 mg·kg -1 ), CI-1004 group (5mg·kg -1 ) and ZLJ-6 high and low dose groups (10mg·kg -1 , 3mg·kg -1 ), 8 in each group. Continuous intragastric administration for 7 days. Two hours after the last administration, the right common carotid artery and the left external jugular vein were separated under anesthesia, a 6 cm long and weighed silk thread was placed in the middle section of the polyethylene tube, and the lumen was filled with heparin saline, inserted and separated. In the out-flowing blood vessels, the silk thread was taken out and weighed after opening the blood flow for 15 minutes. The wet weight of the thrombus was subtracted from the total weight of the silk thread. Compared with the model group, the difference was significant (p<0.01), and the thrombus inhibition rate was equivalent to that of the positive control aspirin...

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Abstract

The invention relates to a medicine field, in particular relates to application of (Z)-1-methyl-1, 5-dihydro-2-amido-5-(4-(mesyl) benzal)-4H-imidazole-4-ketone and pharmaceutically acceptable salt thereof in the treatment of cardiovascular and cerebrovascular diseases of mammals; the compound and the salt of the compound can effectively prohibit formation of thrombus and are used for preventing or curing diseases such as coronary heart disease, atherosclerosis, artery and vein thrombosis, angina, myocardial infarction, coronary heart disease, myocarditis, ischemic cardiomyopathy, myocardial infarction, cardiovascular complications of diabetes, cerebral haemorrhage, cerebral thrombosis, cerebral embolism, cerebral infarction, brain stroke, lacunar infarction, transient ischemic attack, cerebral arteriosclerosis and peripheral vascular diseases such as obstructive vasculitis, aortoarteritis, hypercholesterolemia, or high blood lipids, etc.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to (Z)-1-methyl-1,5-dihydro-2-amino-5-[4-(methylsulfonyl)benzylidene]-4H-imidazole-4- Application of ketone or pharmaceutically acceptable salt thereof in treating cardiovascular and cerebrovascular diseases of mammals. Background technique [0002] In the inventor's previous research, a compound of structural formula I was prepared, chemical name: (Z)-1-methyl-1,5-dihydro-2-amino-5-[4-(methylsulfonyl)benzylidene ]-4H-imidazol-4-one. [0003] [0004] The compound of formula I has been disclosed in CN1389458A and CN1597673A, and it is disclosed that it has cyclooxygenase (COX) inhibitory activity and can be used for treating inflammatory diseases. [0005] Thrombotic disease mainly refers to arterial thrombotic disease and venous thrombotic disease, involving a variety of diseases of the blood and circulatory system, common coronary artery disease thrombosis caused myocardial in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4168A61P9/00A61P9/10A61P3/06
Inventor 季晖赖宜生李立文敖桂珍张奕华彭司勋陈颖
Owner CHINA PHARM UNIV
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