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Naphthalene acetamide compound

A technology for compounds and diseases, applied in the field of medicine, can solve problems such as unsatisfactory effects

Active Publication Date: 2016-07-06
河北久鹏制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, this type of drug is widely used in the world, but it is more appropriate as a preventive drug than a therapeutic drug, because the effect of using this type of drug in the acute stage of stroke is not ideal

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Embodiment 1: the preparation of each compound:

[0014] Because the compounds described herein have strong coherence, in order to describe the preparation method of each compound in detail, accurately and conveniently, it is expressed with 1 embodiment, and the serial number of the compound is indicated below each compound of the following synthetic route, for more Concise descriptions are replaced by serial numbers in the following preparation methods:

[0015]

[0016] (1) Synthesis of Compound 3:

[0017] Accurately weigh 93.1 grams of raw material 2 and add it to 200.0 mL of thionyl chloride, stir the reaction at 80°C for 6 hours, stop the reaction, cool the reaction solution to room temperature, add 75.7 grams of triethylamine and 300 mL of tetrahydrofuran, and stir for 20 minutes. Dissolve 1.0 gram of L-proline methyl ester in 200 mL of tetrahydrofuran, slowly add it dropwise to the above reaction solution, continue the reaction for 4 hours, stop the reaction...

Embodiment 2

[0025]Example 2: Effects of Compound 1a and Compound D1 in Example 1 on Cerebral Infarction Volume in Rats with Focal Cerebral Ischemia

[0026] (1) Experimental materials and methods

[0027] Wistar rats, body weight 250-280g. They were reared separately before and after the operation, the room temperature was kept at 23-25°C, and they had their own food and water. The tMCAO model was prepared according to the method of Longa et al. Rats were anesthetized with 10% chloral hydrate (350mg / kg, i.p.), the body temperature was maintained at 37±0.5°C, and the supine position was fixed on the operating table. The skin was incised along the midline of the neck, and the right common carotid artery (CCA), external carotid artery (ECA), and internal carotid artery (ICA) were carefully separated. Cut the ECA ligation and straighten it to be in line with the ICA. Cut a small opening on the ECA, and insert a 4.0cm-long, 0.26mm-diameter round siliconized nylon rope (coated with 0.1% pol...

Embodiment 3

[0038] Example 3: Effects of compound 1a and compound D1 on sleep in rats:

[0039] sleep improvement test

[0040] Animal source: Kunming white mice, 18-22 grams, male. Experimental animal breeding room temperature 22 ± 2 ℃, relative humidity 50-70%. In this experiment, the dose of compound 1a was set at 25 mg / kg, and a distilled water control group was also set up.

[0041] Sample treatment: Take 25mg of each sample and add distilled water to 20ml to make a uniform suspension for testing.

[0042] Way of giving samples: gavage

[0043] Experimental method: pentobarbital sodium suprathreshold dose hypnosis test:

[0044] Select 30 male mice with a body weight of 18-22g, and randomly divide them into 3 groups, 10 in each group, give samples continuously for 30 days, and give each group of animals 50 mg / kg. Barbital sodium was injected intraperitoneally, and the injection volume was 0.2ml / 20g.b.w. The mouse's righting reflex disappeared for more than 1 minute as the criter...

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Abstract

The invention relates to a new naphthalene acetamide compound as shown in formula I and the salt of the naphthalene acetamide compound.Experiments prove that the naphthalene acetamide compound can be used for treating and preventing cerebral ischemic disease and improving sleep.When R=H, the naphthalene acetamide compound can react with alkali metal such as sodium, magnesium, potassium and calcium and tromethamine, diethylamine, triethylamine and the like to generate the salt which is capable of treating and preventing the cerebral ischemic disease and improving the sleep. The influence of the naphthalene acetamide compound on ischemic cerebral infarction volume is larger than that of a control group, the blood concentration of the naphthalene acetamide compound in brain tissue is higher than that of the control group, and the half-life period is prolonged evidently.

Description

technical field [0001] The invention belongs to the field of medicine, relates to a novel amide compound and its salt, and discloses its preparation method and application. Background technique [0002] Drugs for the treatment of ischemic stroke: the first category is vasodilators (such as dipyridamole, etc.). In the past, it was believed that as long as the drug can dilate the blood vessels in the brain, it can make the blood flow more from the blocked blood vessels. However, it was found that the vasodilators not only cannot do this, but also cause the blood in the diseased part to flow back into the healthy brain tissue (this is called intracerebral steal syndrome), so the use of such drugs is no longer advocated. The second category is drugs that improve microcirculation and expand blood volume (such as low molecular weight dextran, etc.). At present, this kind of medicine is widely used, but patients with heart disease should use it with caution, otherwise it may caus...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/16A61K31/401A61P25/20A61P9/10
CPCA61K31/401C07D207/09C07D207/16
Inventor 陈秀兰王明霞史美娟
Owner 河北久鹏制药有限公司
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