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Application of benzotriazole compound in preparation of fat and weight reducing medicines

A technology of benzotriazoles and benzotriazoles, which is applied in the field of biological activity of compounds, can solve the problems of undisclosed biological activity, etc., and achieve the effects of inhibiting fat absorption, preventing fat accumulation, and promoting fat hydrolysis

Inactive Publication Date: 2016-08-17
张雪燕
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] CN105218532A discloses a benzotriazole small molecule compound or a pharmaceutically acceptable acid addition salt thereof, and also discloses the benzotriazole small molecule compound or a pharmaceutically acceptable acid addition salt thereof Medical use in the preparation of drugs for the treatment of various malignant tumor growth, metastasis and recurrence caused by RAS gene mutations, but it does not disclose the biological activity of this type of compound in reducing blood fat or losing weight

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Preparation of 1-phenylcarboxylic acid [2-(4-methoxyphenyl)-2H-benzotriazol-5-yl]-amide (RS014)

[0016] (1) Dissolve p-methoxyaniline (2.48g, 20.14mmol) in 48ml of hydrochloric acid aqueous solution (4M), add sodium nitrite (1.67g, 24.17mmol) under ice bath conditions, and react for half an hour. Ammonium sulfamate (3.16 g) was slowly added to the system at 0°C and stirring was continued for half an hour. The pH of the solution was adjusted to 5-6 with sodium acetate, and o-phenylenediamine hydrochloride (3.33 g, 18.42 mmol) was added to the reaction system under ice-bath conditions, and stirred overnight. After the completion of the reaction as detected by TLC, adjust the pH to greater than 14 with sodium hydroxide solution, extract with ethyl acetate and water, combine the organic phases, and distill under reduced pressure to obtain a dry crude azo compound. The azo compound was dissolved with 40ml of pyridine, and 10g of anhydrous copper sulfate was added...

Embodiment 2

[0019] Example 2: Effects of RS014 on body weight and blood lipids in obese mice with hyperlipidemia

[0020] Select 40 Kunming mice (half male and half female), weighing 20±2g. The experimental animals were kept in separate cages, and purified water was used for drinking. The temperature of the breeding environment is controlled at 20±3°C, the relative humidity is 60% to 70%, 12 hours of sunlight and 12 hours of darkness are alternated every day, and the working illumination is 150 LX to 300 LX. After the test started, 40 Kunming mice were randomly divided into four groups: normal control group, model control group, test sample RS014 group and weight loss drug orlistat administration group, with 10 mice in each group, half male and half female .

[0021] Normal control group: Mice were fed with full-price ordinary compound feed from the beginning of the experiment to the end of the experiment, and 1% sodium carboxymethylcellulose was orally gavaged every day (gavage volume ...

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PUM

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Abstract

The invention provides the application of benzotriazole compounds in the preparation of lipid-lowering and weight-loss drugs, and the benzotriazole compounds are 1-phenylcarboxylic acid [2-(4-methoxyphenyl)-2H ‑Benzotriazole‑5‑yl]‑amide. The present invention not only has the functions of inhibiting fat absorption and promoting fat hydrolysis, but also can promote fat hydrolysis and prevent fat accumulation without affecting the patient's appetite. Or drugs for nutritional diseases such as obesity.

Description

technical field [0001] The invention belongs to the technical field of biological activity application of compounds, in particular, relates to a new pharmaceutical application of benzotriazole compounds, especially 1-phenylcarboxylic acid [2-(4-methoxyphenyl)- Application of 2H-benzotriazol-5-yl]-amide in the preparation of lipid-lowering and weight-loss drugs. Background technique [0002] With the improvement of people's living standards and the change of original eating habits, obesity has become an epidemic in modern society. Other related diseases brought about by obesity, such as diabetes, atherosclerosis, coronary heart disease, hypertension, fat Liver and other cardiovascular and cerebrovascular diseases have seriously threatened human health. According to the results of the survey, the number of obese people in developed countries has increased significantly since 1996, and more than 60% of the population is troubled by obesity (Relling, David P a, Esberg. High-fat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4192A61P3/04A61P3/06A23L33/10
CPCA61K31/4192A23V2002/00A23V2200/332
Inventor 张雪燕
Owner 张雪燕
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