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Fortestatin amide derivatives and their preparation method and application

A technology of tenacin amides and derivatives, which is applied in the field of pancreatic lipase inhibitors, and can solve the problems of no reports on the activity of tenacin amide derivatives, etc.

Inactive Publication Date: 2017-12-01
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] So far, there are no reports of stasisin amide derivatives and their activities in the prior art

Method used

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  • Fortestatin amide derivatives and their preparation method and application
  • Fortestatin amide derivatives and their preparation method and application
  • Fortestatin amide derivatives and their preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0071] Inhibition of pancreatic lipase in vitro:

[0072] 1. Determination of Drugs and Compounds

[0073] The assay compound is vibralactone steastin amide derivatives obtained in Example 1, a total of 12 compounds; the positive drug is Orlistat (Orlistat, N-Formyl-L-leucine (1S)-1-[[(2S, 3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester) was purchased from Sigma; the compound and Orlistat were dissolved in dimethylsulfoxide (DMSO) and stored at 4°C. 2. Reagents and solutions

[0074] (1) Reagents

[0075] Porcine pancreatic lipase (PPL) was purchased from Aladdin Reagent Company; p-nitrophenyl butyrate (p-NPB) and Tris were purchased from Sigma Company; D-PBS was purchased from Hyclone Company; anhydrous calcium chloride was purchased from Chengdu Kelong Chemical Reagent factory products.

[0076] (2) Solution

[0077] Tris buffer containing 100mM Tris, 5mM CaCl 2 , pH value is 7.0, and stored at 4°C; PPL solution is made into 1000U / mL stock solution with D-PBS, aliquo...

Embodiment 3

[0094] The compound was prepared according to Example 1, and excipients were added according to the weight ratio of compound crystals and excipients at a ratio of 1:1, and then granulated and compressed into tablets.

Embodiment 4

[0096] The compound was prepared according to Example 1, and capsules were made into capsules according to conventional capsule preparation methods.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a vibralactone amide derivative shown in a (formula I), a pharmaceutical composition employing a compound represented by the general formula I or a pharmaceutically acceptable salt as an active component, preparation methods of the vibralactone amide derivative and the pharmaceutical composition, and applications of the vibralactone amide derivative and the pharmaceutical composition in preparation of medicines for preventing and treating obesity and other metabolic diseases such as diabetes. The formula is shown in the specification.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to stestatin amide derivatives as a class of potent pancreatic lipase inhibitors, which inhibit the activity of enzymes by combining with pancreatic lipase, and prevent triglycerides from being hydrolyzed into absorbable free Fatty acids and monoacylglycerols prevent them from being absorbed, thereby reducing caloric intake and controlling body weight. Background technique [0002] Obesity is a disease caused by disorders of appetite, energy intake, and metabolic regulation. It has obvious correlations with diabetes, cardiovascular disease, fatty liver, and certain tumors. It has become one of the main killers that endanger human health. Therefore, how to effectively reduce obesity has become an important research topic facing many countries. Dietary fat intake is one of the main causes of obesity. The main lipid component in food is triglycerides, which are hydrolyzed into cor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D305/14A61K31/365A61P3/04A61P3/10
CPCC07D305/14
Inventor 刘吉开韦堃汪钢强白雪李正辉董泽军汪秋安陈贺平冯涛文春南
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI