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Sesterterpene compounds and use thereof

A technology for disesquiterpenes and compounds, applied in the field of novel disesquiterpenes, can solve problems such as incompatibility, and achieve the effects of inhibiting the production of fatty acids in the liver, inhibiting the differentiation of adipocytes, and reducing the accumulation of fat

Inactive Publication Date: 2014-01-15
SEOUL大学校产学协力财团
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the currently developed LXR active substances are not suitable as a single preparation for the treatment of hyperlipidemia, arteriosclerosis and Alzheimer's disease because they can cause complications similar to diabetes or liver disease (such as fatty liver) therapeutic agent

Method used

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  • Sesterterpene compounds and use thereof
  • Sesterterpene compounds and use thereof
  • Sesterterpene compounds and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Embodiment 1. Synthesis of compound 1

[0115]

[0116] PhorbaketalA (phorbaketalA, A) (10 mg, 0.025 mmol, Rho et.al., Organic Letters, 2009, 11, 5590-5593 (Rho et al., 2009, 11, 5590-5593)) was dissolved in dichloromethane, and added p-TsCL (5.4 mg, 1.2 eq) and triethylamine (0.01 mmol) were stirred for 5 hours. with saturated NaHCO 3 Aqueous solution and water (40ml) quenched the reaction. The organic solvent layer was washed twice with water, using Na 2 SO 4 After drying, it was concentrated with an evaporator. Compound 1 was obtained by purification with silica gel column chromatography. MS m / z554[M+H] +

Embodiment 2

[0117] Embodiment 2. Synthesis of compound 2

[0118]

[0119] Dissolve compound 1 (10 mg, 0.018 mmol) in dimethylformamide (DMF, dimethylformamide, 5 ml), add NaN 3 (11.7mg, 10mmol) and react at 70°C for 8 hours under nitrogen. After the reaction solution was cooled, ice water was added, and the organic solvent layer was separated after washing with water. will use Na 2 SO 4 The residue obtained by drying and distilling under reduced pressure was purified by silica gel column chromatography to obtain Compound 2. MS m / z424[M+H] +

Embodiment 3

[0120] Embodiment 3. Synthesis of compound 3

[0121]

[0122] Dissolve compound 2 (10mg, 0.023mmol) in acetonitrile (5ml) and add NaI (0.20mmol) and FeCl 3 (0.032 mmol). After stirring the reaction solution for 20 minutes, chloroform (5 ml) was added to terminate the reaction. Utilize Na 2 SO 3 Aqueous solution and NaHCO 3 Washed with aqueous solution, and the obtained organic solvent layer was washed with brine. The organic solvent layer was washed with Na 2 SO 4 The residue obtained by drying and distilling under reduced pressure was purified by silica gel column chromatography to obtain compound 3. MS m / z398[M+H] +

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PUM

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Abstract

The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.

Description

technical field [0001] The present invention relates to novel sesquiterpene compounds and the effects of the sesquiterpene compounds on diabetes, obesity, fatty liver disease (alcoholic, non-alcoholic and viral fatty liver disease), cardiovascular disease, atherosclerosis and Prevention and treatment of brain diseases (Parkinson's disease and Alzheimer's disease). The sesquiterpene compound of the present invention can be used as a combination for the prevention and treatment of type 2 diabetes and other complications caused by diabetes (renal insufficiency, foot ulcer, etc.) by regulating the expression of proteins with antidiabetic function and intracellular signals The active ingredient of the drug is used. And the sesquiterpene compound of the present invention can inhibit the production of fatty acids in the liver, consume the fatty acids accumulated in the liver, promote the beta-oxidation discharged by heat, and significantly reduce the accumulation of fat in the liver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/10C07D493/20A61K31/352A61P3/00A61P9/00
CPCC07D493/10C07D493/20C07D519/00C07F7/1804C07F9/65615C07H15/26C07H19/01A61P1/16A61P3/00A61P3/04A61P3/06A61P3/10A61P9/00A61P9/10A61P13/12A61P25/00A61P25/16A61P25/18A61P25/24A61P25/28A61P43/00A61K31/352A61K31/4184A61K31/4192A61K31/422A61K31/453A61K31/496A61K31/541A61K31/665A61K31/7048A61K45/06C07H17/04
Inventor 姜宪中元东焕梁仁豪金恩吾金正雅阿瓦度·阿让德拉·吉里芬卡·雷迪·玛勒帕里
Owner SEOUL大学校产学协力财团
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