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Application of compound shown in formula I in preparation of drug for treating obesity and related symptoms

A technology for related diseases and compounds is applied in the field of use of the compound of formula I in the preparation of medicines for the treatment of obesity and related diseases, which can solve the problems of easy rebound, easy problems with insulin, and increased diabetes.

Inactive Publication Date: 2020-12-22
UNIVERSITY OF CHINESE ACADEMY OF SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

2. Diabetes: Obesity will cause excessive secretion of insulin in the blood. The more severe the obesity, the higher the insulin concentration on an empty stomach, and the secretion of insulin after eating cannot be relatively increased, so the phenomenon of elevated blood sugar is formed; and the experiment found that , obese people have fewer insulin receptors in their cells, or are prone to problems receiving insulin, so obese people increase the risk of diabetes
[0004] At present, weight loss methods usually include dieting, increasing exercise, adjusting diet structure, drug intervention, reducing absorption (such as laxatives), etc. These methods either need to be persisted for a long time, such as dieting, increasing exercise, and adjusting diet structure, which is a test of perseverance. Only few people can persist, so it is difficult to achieve effective weight loss; for those who lose weight through laxatives, as long as they stop taking the medicine, it is very easy to rebound

Method used

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  • Application of compound shown in formula I in preparation of drug for treating obesity and related symptoms
  • Application of compound shown in formula I in preparation of drug for treating obesity and related symptoms
  • Application of compound shown in formula I in preparation of drug for treating obesity and related symptoms

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Taking 8-10 week-old wild-type C57BL6 mice as research objects, fed with high-fat diet with a fat content of 62% by weight for 3 months, they were randomly divided into blank control group and GCN2iB treatment group, 5 mice in each group, two groups There was no significant difference in the initial weight of the figure 1 shown. On the first day of modeling, the drug GCN2iB was dissolved in olive oil and administered to mice in the GCN2iB treatment group by intragastric administration at a dose of 5 mg / (kg body weight) every 2 days for 4 weeks. The blank control group was given the same volume of olive oil every 2 days for 4 weeks. During the administration period, the mice in the two groups continued to be fed with high-fat diet, and their body weight was weighed every week. After the experiment, blood was taken from the eyeballs of the mice, and biochemical and histological analyzes were performed on the liver at the same time. The experimental results were as follo...

Embodiment 2

[0047] The homozygous mouse for leptin gene mutation (Lepob, usually written as ob or ob / ob) is a classic animal model of non-alcoholic fatty liver disease. Ob / ob mice aged 10-12 weeks were randomly divided into blank control group and GCN2iB treatment group, 5 mice in each group. There was no significant difference in body weight among the groups. The administration method and dosage are the same as in Example 1, and the duration is 6 weeks. Body weight was recorded during the experiment. At the end of the experiment, blood was taken from the eyeballs of the mice, and biochemical and histological analyzes were performed on the liver. The experimental results are as Figure 4 , Figure 5 A-5B and Image 6 A-6C shown. from Figure 4 It can be seen that oral administration of GCN2iB significantly reduced the body weight of ob / ob mice (* represents p Figure 5 In A and 5B, it can be seen that oral administration of GCN2iB significantly reduced alanine aminotransferase (ALT) ...

Embodiment 3

[0049] Leptin receptor mutant db / db mice have typical clinical symptoms of diabetes such as extreme obesity, polyphagia, thirst, and polyuria, and are also a typical animal model of fatty liver. db / db mice aged 6-8 weeks were selected and randomly divided into blank control group and GCN2iB treatment group with similar body weight. The administration method and dosage are the same as in Example 1, and the duration is 4 weeks. After the experiment, blood was taken from the eyeballs of the mice, and biochemical analysis was performed on the liver at the same time. The experimental results are as Figure 7 , Figure 8 A-8B and Figure 9 A-9C shown. from Figure 7 It can be seen that oral administration of GCN2iB can maintain the body weight of db / db mice basically unchanged, while the weight of db / db mice in the control group increased significantly (** represents p Figure 8 In A and 8B, it can be seen that oral administration of GCN2iB can significantly reduce the alanine a...

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Abstract

The invention provides application of a compound shown in a formula I in preparation of a drug for treating obesity and obesity-related symptoms, wherein R1, R2 and R3 are the same or different and are respectively selected from halogen elements; R4 is substituted or unsubstituted C1-C10 straight-chain or branched-chain alkyl; and R5 is a basic group. The research shows that the compound shown inthe formula I can effectively reduce the weight of high-fat diet-induced obese mice, OB mice and db / db mice, reduce the activity of glutamic-pyruvic transaminase ALT and glutamic oxalacetic transaminase AST and improve the fatty liver symptom. Therefore, the compound shown in the formula I has an improvement effect on obesity caused by bad dietary habits and obesity caused by genetic factors, andimproves the obesity-related symptoms such as fatty liver.

Description

technical field [0001] The present invention relates to the use of a compound of formula I in the preparation of medicines for treating obesity and obesity-related diseases. Background technique [0002] In recent decades, with the improvement of people's living standards and changes in lifestyle, the number of obese people is increasing, and there is a trend of younger people. The World Health Organization has defined obesity as a disease, which is the third biggest enemy to human health after cardiovascular and cerebrovascular diseases and cancer. [0003] Obesity can easily lead to the following symptoms: 1. Fatty liver: normal human liver tissue contains a small amount of fat, such as triglycerides, phospholipids, glycolipids and cholesterol, and its weight is about 3% to 5% of the liver weight. Fat accumulation is too much, more than 5% of liver weight or when more than 50% of liver cells have fatty degeneration in histology, it can be called fatty liver. 2. Diabetes:...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61P9/12A61P3/04A61P1/16A61P3/10A61P3/06A61P5/00A61P17/00A61P19/02A61P1/18A61P11/00
CPCA61K31/506A61P9/12A61P3/04A61P1/16A61P3/10A61P3/06A61P5/00A61P17/00A61P19/02A61P1/18A61P11/00
Inventor 陆忠兵
Owner UNIVERSITY OF CHINESE ACADEMY OF SCIENCES
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