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Piperidine medicine for preventing and treating fatty liver diseases and related diseases

A technology for fatty liver disease and steatohepatitis, which is applied in the field of preventive and therapeutic drugs for fatty liver disease and its related diseases, can solve the problems of unclear effect, and the prevention or reversal effect of fatty liver disease has not yet been found, so as to achieve the disease Significant improvement, fast onset, and broad application prospects

Inactive Publication Date: 2020-04-14
南京沿溯大数据有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the molecule or its structural analogs have not been found to prevent or reverse fatty liver disease
It is not yet clear whether the therapeutic mechanism of this molecule for fatty liver disease is through PAR-1 or through other off-targets, and the role of PAR-1 in fatty liver disease is not clear, and there is no evidence to inhibit the activity or function of PAR-1 , must be able to alleviate or reverse fatty liver disease

Method used

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  • Piperidine medicine for preventing and treating fatty liver diseases and related diseases
  • Piperidine medicine for preventing and treating fatty liver diseases and related diseases
  • Piperidine medicine for preventing and treating fatty liver diseases and related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1: Therapeutic or preventive effect of compound YS000003 on mice with fatty liver, liver fibrosis or liver cirrhosis

[0042] 1. Experimental materials

[0043] 1.1 Animals: male C57BL / 6 mice, 7-8 weeks old.

[0044] 1.2 Model: MCD-induced NASH model in C57BL / 6 mice: After the animals were fed adaptively within the SPF barrier for 3-7 days, the MCD feed was replaced, and the feeding cycle was 8 weeks.

[0045] 1.3 Treatment and control: YS000003 molecules are dissolved in water; the control group is water.

[0046] 2. Experimental method

[0047] 2.1 Establishment of scoring system for fatty liver severity

[0048] The fatty liver disease severity scoring system (NAS) commonly used in the world for humans and animals consists of three parts: Steatosis, Lobular Inflammation and HepatocyteBallooning. In this example, the significance of the treatment effect is determined by comparing the fatty liver disease severity scores calculated after liver tissue slice...

Embodiment 2

[0060] Embodiment 2: The treatment or prevention of fatty liver, liver fibrosis or liver cirrhosis mice by piperidine derivative compound YS000006 Anti-effect

[0061] 1. Experimental materials

[0062] The molecule (YS000006) whose two-dimensional structural molecular fingerprint and the Tanimoto similarity of YS000003 is more than 80% was selected as the research object. The molecule is a piperidine derivative, Pubchem accession number CID: 68778045.

[0063] 1.1 Animals: male C57BL / 6 mice, 7-8 weeks old.

[0064] 1.2 Model: MCD-induced NASH model in C57BL / 6 mice: After the animals were fed adaptively within the SPF barrier for 3-7 days, the MCD feed was replaced, and the feeding cycle was 8 weeks.

[0065] 1.3 Treatment and control: YS000006 molecules are dissolved in water; the control group is water.

[0066] 2. Experimental method

[0067] Refer to Example 1 for the establishment method of the MCD model.

[0068] The present invention demonstrates the therapeuti...

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Abstract

The invention relates to applications of a compound YS000003, a structural analogues, a corresponding medicinal isomer, a salt, a solvate and a polymorphic substance thereof in prevention or treatmentof fatty liver diseases and related diseases (such as non-alcoholic fatty liver diseases, steatohepatitis, liver fibrosis or liver cirrhosis and the like). According to the invention, the results prove that the compound YS000003 can obviously improve the degree of fatty liver diseases, liver fibrosis or liver cirrhosis and relieve liver injury, is good in safety and has good clinical applicationprospect.

Description

technical field [0001] The invention relates to preventive and therapeutic drugs for fatty liver disease and related diseases. In particular, the present invention relates to the use of compound YS000003 and compounds with a structural similarity of more than 80% in the prevention and treatment of fatty liver, steatohepatitis, liver fibrosis or liver cirrhosis. Background technique [0002] Fatty liver refers to the lesion of excessive accumulation of fat in liver cells caused by various reasons. It is a common pathological change of the liver, that is, fatty changes of the liver. Fatty liver disease is seriously threatening the health of Chinese people and has become the second largest liver disease after viral hepatitis. The incidence rate is constantly increasing, and the age of onset is getting younger and younger. It is a new challenge in the field of liver diseases in the 21st century. [0003] At present, the U.S. FDA has not approved any drug for non-alcoholic fatty...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/541A61P1/16
CPCA61K31/541A61P1/16Y02A50/30
Inventor 不公告发明人
Owner 南京沿溯大数据有限公司
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