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Applications of benzylidene barbiturate compound in serving as PCSK9 antagonist and reducing low-density lipoprotein

A technology of benzylidenebarbital and compounds, which is applied in the direction of medical preparations containing active ingredients, drug combinations, metabolic diseases, etc., can solve problems such as inconvenient use, and achieve the effects of convenient manufacture, reduced concentration, and easy manufacture

Active Publication Date: 2017-09-15
VIVA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current research on PCSK9 antagonists is still focused on the direction of monoclonal antibodies. However, monoclonal antibodies are used as drugs in clinical practice, and there are many inconveniences in use.

Method used

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  • Applications of benzylidene barbiturate compound in serving as PCSK9 antagonist and reducing low-density lipoprotein
  • Applications of benzylidene barbiturate compound in serving as PCSK9 antagonist and reducing low-density lipoprotein
  • Applications of benzylidene barbiturate compound in serving as PCSK9 antagonist and reducing low-density lipoprotein

Examples

Experimental program
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Embodiment Construction

[0027] The specific implementation manners of the present invention will be described below in conjunction with the accompanying drawings.

[0028] This embodiment provides an application of a compound in reducing low-density lipoprotein in blood. Included in this application are administering to a subject an effective amount of the LDL-lowering compounds, mixtures and compositions herein.

[0029] 1. The compound of the present invention has the structure of V in the figure:

[0030]

[0031] Among them, R 1 , R 2 independently H, -OR', -OC(O)R", -OSO2R", -OC(O)NR'R", -O-alkylene-OR', -O-alkylene-NR 'R', -SO2R', -S(O)R, -SR, -NR'R", -NHC(O)R', -NHC(O)OR', -NHC(O)NR'R", -NR'C(O)R", -NR'C(O)OR", -NR'C(O)NR"R"', or substituted or unsubstituted alkyl, cycloalkyl, alkenyl , alkynyl, aryl, heteroaryl.

[0032] Wherein, X is substituted or unsubstituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl.

[0033] Wherein, Y is substituted or unsubstituted alkyl, cycloal...

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Abstract

The invention provides application of a benzylidene barbiturate compound in serving as a PCSK9 antagonist, and further provides application of the benzylidene barbiturate compound in reducing the low-density lipoprotein. The invention provides a small-molecule benzylidene barbiturate compound serving as the PCSK9 antagonist, and the benzylidene barbiturate compound can effectively reduce the concentration of low-density lipoprotein.

Description

technical field [0001] The invention relates to the application of a benzylidene barbiturate compound as a PCSK9 antagonist, and also relates to the application of a benzylidene barbiturate compound in reducing low-density lipoprotein, which belongs to the field of medicine. Background technique [0002] PCSK9 is a soluble endogenous serine protease and a member of the mammalian proprotein convertase family. It is mainly synthesized in the liver, but also expressed at low levels in the intestine, kidney and brain. PCSK9 exists in an inactive form in hepatocytes, and once released into the blood, it can bind to LDL receptors, enter hepatocytes through endocytosis, and then degrade. LDL receptors on the surface of liver cells will be reduced, and too much LDL in the blood will lead to increased blood lipid levels. Low incidence of hyperlipidemia in people with congenital PCSK9 variants. The current research on PCSK9 antagonists is still focused on the direction of monoclona...

Claims

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Application Information

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IPC IPC(8): A61K31/515A61P3/06
CPCA61K31/515
Inventor 丁悦周晶方芳房丽燕钱冬明姜启阳安治星杨晶晶刘彬崔荣蓉周立宏胡亮蔡建华王增全叶志雄任德林程学恒
Owner VIVA BIOTECH
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