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Medicine for preventing and treating myocardial ischemia and preparation method thereof

A pharmacy and compound technology, applied in the field of medicine, can solve problems such as abnormal heart failure, atrioventricular block, and clinical application limitations

Active Publication Date: 2017-08-18
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many contraindications in clinical application, including airway blockage, atrioventricular block and abnormal heart failure, etc., and the clinical application is limited.

Method used

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  • Medicine for preventing and treating myocardial ischemia and preparation method thereof
  • Medicine for preventing and treating myocardial ischemia and preparation method thereof
  • Medicine for preventing and treating myocardial ischemia and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056]

[0057] Potassium tert-butoxide (5.60 g, 50 mmol) was added to a solution of 5,6-dimethylpyrazin-2-amine (1.23 g, 10 mmol) in 250 mL of anhydrous THF at room temperature under nitrogen. After stirring for 15 minutes, a solution of 2-nitrothiazole-4-oyl chloride (2.10 g, 11 mmol) in 50 mL of anhydrous THF was added dropwise. The reaction mixture was stirred at room temperature for 4 h, then poured into saturated NaHCO 3 aqueous solution and extracted with EtOAc. The organic phase was washed with saturated NaCl aqueous solution, washed with anhydrous NaCl 2 SO 4 Dried and concentrated to dryness. Purification by flash chromatography on silica gel (cyclohexane / EtOAc: 90 / 10 to 50 / 50) gave N-(5,6-dimethylpyrazin-2-yl)-2-nitrothiazole as a white solid -4-amide 1.69 g (yield: 61.0%).

[0058] The catalyst tetrakis(triphenylphosphine)palladium (0.63mg, 0.55mmol) and potassium acetate (0.98g, 10mmol) were added to N-(5,6-dimethylpyrazine in a microwave reactor) under ni...

Embodiment 2

[0064]

[0065] Potassium tert-butoxide (5.60 g, 50 mmol) was added to a solution of 6-phenylpyrazin-2-amine (1.71 g, 10 mmol) in 250 mL of anhydrous THF at room temperature under nitrogen. After stirring for 15 minutes, a solution of 2-aminothiazole-4-oyl chloride (1.77 g, 11 mmol) in 40 mL of anhydrous THF was added dropwise. The reaction mixture was stirred at room temperature for 5 h, then poured into saturated NaHCO 3 aqueous solution and extracted with EtOAc. The organic phase was washed with saturated NaCl aqueous solution, washed with anhydrous NaCl 2 SO 4 Dried and concentrated to dryness. After purification by flash chromatography on silica gel (n-Hexane / EtOAc: 95 / 5 to 40 / 60), N-(6-phenylpyrazin-2-yl)-2-aminothiazole-4-amide 1.74 was obtained as a gray solid. g (yield: 58.9%).

[0066] The catalyst tetrakis(triphenylphosphine)palladium (0.63mg, 0.55mmol) and potassium acetate (0.98g, 10mmol) were added to N-(6-phenylpyrazine-2- In a solution of (1.48 g, 5 mm...

Embodiment 3

[0073]

[0074] ESI-MS: 313.00[M+H] +

[0075] Elemental analysis: theoretical value / measured value, C(38.46 / 38.51), H(2.58 / 2.55), N(17.94 / 17.88), O(20.49 / 20.59), S(20.53 / 20.47)

[0076] 1 HNMR (400MHz, CDCl 3 )δ: 8.05(s,1H), 7.63(s,1H), 4.02(s,3H), 3.47(s,3H).

[0077] 13 C NMR (400MHz, CDCl 3 )δ: 157.2, 154.1, 153.4, 151.0, 141.4, 139.3, 135.7, 133.6, 133.0, 54.9.

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Abstract

The invention relates to a medicine for preventing and treating myocardial ischemia and a preparation method and application thereof, in particular to a compound with a formula (I) and a pharmaceutically acceptable salt thereof. The formula (I) is shown in the description. The compound with the formula (I) has the advantages that the excellent myocardial ischemia resisting function is realized; in a rat acute myocardial infarction model, the compound can obviously reduce the myocardial infarction area of the rat with the myocardial infarction, and the activities of CK (creatine kinase), AST (aspartate aminotransferase) and LDH (lactate dehydrogenase) in serum are obviously reduced; the function of preventing and treating the myocardial infarction is obvious, and the medicine can be applied to prevent and treat the myocardial infarction.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a medicine for preventing and treating myocardial ischemia and its preparation method and application. Background technique [0002] Heart disease is one of the diseases that seriously threaten human health. Worldwide, cardiovascular disease is the No. 1 cause of death in most Western developed countries; in developing countries cardiovascular disease currently accounts for a quarter of deaths but is expected to reach one third by 2020 one. The World Health Organization has predicted that by 2020, cardiovascular disease will become the first cause of death in the world. Myocardial ischemia is the cause of most cardiovascular diseases. [0003] The common cause of myocardial ischemia is coronary atherosclerosis, followed by inflammation (rheumatism, syphilis, Kawasaki disease and vaso-occlusive vasculitis, etc.), spasm, embolism, connective tissue disease, trauma and congenital malforma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D513/14A61K31/4985A61K31/5377A61P9/10
Inventor 刘世娟侯甲福李雪梅周雪吴宜艳赵聪佟雷张朝立刘佳维崔新宇
Owner MUDANJIANG MEDICAL UNIV
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