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Hispidine compound and application thereof

A compound and milk technology, applied in the directions of active ingredients of heterocyclic compounds, organic chemistry, drug combinations, etc., can solve the problems of poor safety and efficacy of anti-obesity drugs, and achieve good adipocyte differentiation, inhibition of adipocyte differentiation, and good The effect of development prospects

Inactive Publication Date: 2018-03-13
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Another aspect of the present invention aims at the problem of poor safety and curative effect of existing anti-obesity drugs, and provides a drug for treating or preventing obesity containing a milky tree compound and / or a pharmaceutically acceptable salt thereof

Method used

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  • Hispidine compound and application thereof
  • Hispidine compound and application thereof
  • Hispidine compound and application thereof

Examples

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preparation example Construction

[0036] The preparation method of the milk tree compound of the present invention comprises the following steps: taking 4-hydroxyl-6-methyl-2-pyrone as raw material, passing dimethyl sulfate and potassium carbonate solvent under the condition of acetone, making Hydroxymethylated to get 4-methoxy-6-methyl-2-pyrone, then reacted with alkaline reagent magnesium methylate and corresponding aldehydes to get β-lactone milkythenic compounds, then reactant with Excessive 36% ammonia water and ethanol were reacted in a sealed tube at 120°C for 36 hours to obtain β-lactam milkythenic compounds.

[0037] The invention synthesizes the milky tree compound by using 4-hydroxy-6-methyl-2-pyrone as a raw material, the raw material is cheap and easy to obtain, the synthesis method is simple and easy to operate, the yield is high, and the product is stable.

[0038] The specific synthetic method of milkytheine compound 3-23 of the present invention is as follows:

[0039] Synthesis of 4-methoxy-...

Embodiment 1

[0067] This embodiment provides a medicament for preventing or treating obesity, which contains a pharmaceutically acceptable carrier and an effective amount of the above compound 20 and / or its pharmaceutically acceptable salt as an active ingredient.

Embodiment 2

[0069] This embodiment provides a medicament for preventing or treating obesity, which contains a pharmaceutically acceptable carrier and an effective amount of the above compound 21 and / or its pharmaceutically acceptable salt as an active ingredient.

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Abstract

The invention relates to the technical field of synthetic medicine, in particular to a hispidine compound and pharmaceutical salt thereof, and application to the aspect of treating and preventing obesity and hyperlipemia. The hispidine compound can obviously inhibit the accumulation of triglyceride and total fat in the 3T3-L1 preadipocyte differentiation process; the inhibition effect is superiorto that of a positive control compound of jamaicin; no obvious cytotoxicity exists. In addition, a beta-lactam hispidine compound can also regulate and control the phosphorylation of transcription factors AMPK and ACC of fat metabolism and the SIRT1 expression quantity, and can regulate and control the expression quantity of transcription factors PPAR-gamma, SREBP-1c and FABP4 of the adipocyte differentiation. Therefore the medicine containing the hispidine compound and / or the pharmaceutical salt has good effects of inhibiting the adipocyte differentiation and reducing oil drops and triglyceride in the adipocyte; good development prospects are realized in the aspects of treating or preventing obesity and reducing the blood fat.

Description

technical field [0001] The invention relates to the technical field of synthetic medicines, in particular to milky tree compounds and their medicinal salts, and their application in the treatment and prevention of obesity and hyperlipidemia. Background technique [0002] In recent years, with the changes in people's lifestyle and diet structure, the number of obesity and hyperlipidemia has increased sharply around the world, becoming a worldwide public health problem that threatens human health and quality of life. Obesity and hyperlipidemia may lead to high blood pressure, fatty liver, and certain cancers. Obesity is already the fifth leading cause of death in the world, and hyperlipidemia is also one of the top ten diseases that endanger the health of our people. Therefore, obesity and hyperlipidemia are extremely harmful to the health of our nationals, and the corresponding drug research and development issues are key scientific and technological issues that urgently need...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/69C07D405/06C07D409/06A61K31/44A61K31/443A61K31/4436A61P3/04A61P3/06
CPCC07D213/69C07D405/06C07D409/06
Inventor 顾琼李婵娟程宝徐峻
Owner SUN YAT SEN UNIV
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