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Pyridines compound and application of pyridines compound in preparation of medicine for treating liver diseases

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

Active Publication Date: 2018-03-13
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 pyridine compound which can be used for liver diseases such as fatty liver, Treatment and / or prevention of liver cirrhosis, liver fibrosis, liver cancer, etc.

Method used

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  • Pyridines compound and application of pyridines compound in preparation of medicine for treating liver diseases
  • Pyridines compound and application of pyridines compound in preparation of medicine for treating liver diseases
  • Pyridines compound and application of pyridines compound in preparation of medicine for treating liver diseases

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] The preparation of embodiment 1 compound I-1

[0058]

[0059] Compound I-a1 (267mg, 1.1mmol), Compound I-b1 (162mg, 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 212 mg of off-white solid (54.9% yield), That is the product compound I-1. (LC / MS: [M+H] + 387).

Embodiment 2

[0060] The preparation of embodiment 2 compound 1-2

[0061] The preparation method of compound 1-2 was experimented 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 compound I-2 respectively, and the products were verified by LC / MS. Compound I-2 (LC / MS: [M+H] + 401).

Embodiment 3

[0062] The preparation of embodiment 3 compound 1-3

[0063] The preparation method of compound 1-3 was experimented in a manner similar to that of Example 1, but the starting material compounds used were different. After the reaction, the products were separated to obtain compound I-3 respectively, and the products were verified by LC / MS. Compound I-3 (LC / MS: [M+H] + 429).

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Abstract

The invention discloses a pyridines compound for treating liver diseases. The compound is a compound as shown in a formula I, pharmacologically acceptable salt, a hydrate, a solvate or a metabolite ofthe compound. The compound can be used for preparing a medicine for treating and / or preventing the liver diseases.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to pyridine compounds 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 costs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14C07D417/14C07D471/04A61K31/4439A61P1/16A61P35/00
CPCC07D401/14C07D417/14C07D471/04
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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