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Triazole derivative, and its application in preparation of medicines for treating liver diseases

A drug and pharmacy technology, applied in the field of biomedicine, which can solve the problem of no suitable therapeutic drugs for indications

Active Publication Date: 2018-04-13
武汉九州钰民医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a novel triazole compound, which can be used for liver diseases such as fat Treatment and / or prevention of liver, liver cirrhosis, liver fibrosis, liver cancer, etc.

Method used

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  • Triazole derivative, and its application in preparation of medicines for treating liver diseases
  • Triazole derivative, and its application in preparation of medicines for treating liver diseases
  • Triazole derivative, and its application in preparation of medicines for treating liver diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The preparation of embodiment 1 compound I-1

[0055]

[0056] Compound I-a1 (440mg, 1.05mmol), Compound I-b1 (203mg, 1.0mmol), (2-(7-aza-1H-benzotriazol-1-yl)-1,1,3, 3-Tetramethyluronium hexafluorophosphate (HATU) (456mg, 1.2mmol) and N-methylmorpholine (13μL, 1.2mmol) were added to DMF, kept at 70°C and stirred for 8 hours. Concentrated under reduced pressure to remove the solvent, the The residue was suspended in acetonitrile and the solid product was isolated by filtration, washed with water (80 mL), acetonitrile (80 mL), acetone (80 mL) and dried under vacuum to afford 374 mg of off-white solid (62% yield), That is the product compound I-1. (LC / MS: [M+H] + 605).

Embodiment 2～ Embodiment 5

[0057] The preparation of embodiment 2~embodiment 5 compound I-2~I-5

[0058] The preparation methods of compounds I-2 to I-5 were tested in a manner similar to that of Example 1, but the starting material compounds used were different. After the reaction was completed, the products were separated to obtain compounds I-2 to I-5 respectively, and the products were verified by LC / MS.

[0059] Compound I-2 (LC / MS: [M+H] + 523).

[0060] Compound I-3 (LC / MS: [M+H] + 568).

[0061] Compound I-4 (LC / MS: [M+H] + 565).

[0062] Compound I-5 (LC / MS: [M+H] + 549).

Embodiment 6

[0063] Example 6 Effects of Compounds of the Present Invention in LDL Receptor Gene Knockout Mouse NASH Model

[0064] The present invention investigates the development of high fat / high cholesterol diet (Western diet)-loaded LDL receptor knockout mice known to have fatty liver and hepatitis, which are characteristic of NASH (Yoshimatsu M. et al., Int. J. Exp. Path., 85, 335-43 (2004)).

[0065] Animals used: Male LDL receptor knockout mice were used in the experiments. During 13 weeks from about 8 weeks old, they were given a high-fat / high-cholesterol diet ad libitum to suffer from NASH. The mice were loaded with a high-fat / high-cholesterol diet, and blood collection and body weight measurements were performed 1 week later.

[0066] Divide into the following groups according to the mode that there is no difference on lipid and body weight in blood plasma between the groups: control group (0.5% methylcellulose aqueous solution), compound 0.25mg / kg shown in the present invent...

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PUM

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Abstract

The invention discloses a triazole compound for treating liver diseases. The compound is a compound represented by formula I, or a pharmaceutically acceptable salt, a hydrate, a solvate or a metabolite thereof. The compound can be used to prepare medicines for treating and / or preventing the liver diseases.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to triazole derivatives and their application in the preparation of medicines for treating liver diseases. Background technique [0002] Liver disease is a common and frequently-occurring disease in our country, including fatty liver, various acute and chronic hepatitis, liver fibrosis, liver cirrhosis, liver cancer and other series of diseases. Most of these liver diseases are caused by obesity, drugs, excessive drinking, hepatitis B and C caused by hepatitis virus infection. According to the estimates of the World Health Organization, the number of deaths caused by various types of hepatitis is about 1.4 million to 1.5 million each year, ranking seventh among various diseases. And the World Health Organization warned that hepatitis will soon overtake AIDS to become the sixth largest health killer for human beings. my country has become the country that pays the most social cos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/14A61K31/4427A61P1/16A61P35/00
CPCC07D413/14
Inventor 许勇范昭泽于静
Owner 武汉九州钰民医药科技有限公司
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