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The use of a group of carbamoylbenzenesulfonyl compounds

A carbamoylbenzenesulfonyl compound technology, applied in the pharmaceutical field, can solve the problems of lack of specific atherosclerotic drugs, severe side effects, etc., and achieve the effects of good anti-atherosclerosis effect, unique mechanism of action and novel structure

Active Publication Date: 2017-04-12
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In conclusion, clinically used statin drugs also have serious side effects, and currently there is no specific drug for the treatment of atherosclerosis.

Method used

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  • The use of a group of carbamoylbenzenesulfonyl compounds
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  • The use of a group of carbamoylbenzenesulfonyl compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 The activity of the compound of the present invention on ABCA1 up-regulation screening model

[0047] ABCA1-LUC HepG2 cells in 5×10 4 Inoculate each well in a 96-well cell culture plate. After the cells adhere to the wall for about 6 hours, remove the serum-containing medium, gently rinse the cells once with PBS, and add serum-free MEM-EBSS medium to each experimental well. 200 μl, and then add 2 μl of the compound sample to be tested (final concentration 2.5 or 10 μg / ml), and the well with the final concentration of 0.1% DMSO medium is used as a blank control. After continuing to culture at 37° C. and 5% CO 2 for 18-24 h, the plate was washed twice with PBS (200 μl / well), and the PBS was discarded. Cell lysate (20 μl / well) (Promega) was added, and after 15-30 min, the complete cell lysis was observed under a microscope, then luciferase (60 μl / well) was added, and the luciferase activity was immediately measured (read by microplate reader).

[0048] Use the ...

Embodiment 2

[0051] Example 2 The activity of the compound of the present invention on the CLA-1 upregulator screening model

[0052] CLAP-LUC HepG2 cells in 5×10 4 Cells / well were seeded in a 96-well cell culture plate. After the cells adhered to the wall for about 6 hours, the serum-containing medium was removed, and the cells were gently rinsed with PBS once. Serum-free MEM-EBSS was added to each experimental well for culture. Base 200 μl, and then add 2 μl of the compound sample to be tested (final concentration 2.5 or 10 μg / ml), and the wells with the final concentration of 0.1% DMSO medium are used as blank control. After continuing to culture at 37°C and 5% CO2 for 18 hours, the plate was washed twice with PBS (200 μl / well), and the PBS was discarded. Cell lysate (20 μl / well) (Promega) was added, and after 15-30 min, the cell cleavage was observed under a microscope, then luciferase (60 μl / well) was added, and the luciferase activity was immediately measured (read by microplate rea...

Embodiment 3

[0056] Example 3 EC50 Determination of Compounds of the Present Invention on ABCA1 and CLA-1 Up-regulation Model

[0057] The compound was dissolved in DMSO to make a 10 mg / ml stock solution. ABCA1p-LUC HepG2 and CLA-1p-LUC HepG2 cells were plated on a 96-well white plate (Costar), and the method was the same as before. Compounds diluted with serum-free RPMI1640 or MEM were made into a series of concentrations, 0.001-100 μmol / L, 200 μl / well. After 18-24h, the cell luciferase activity was measured, and the EC was calculated using Origin8.5 50 .

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Abstract

The invention discloses a new use of a group of carbamyl phenylsulfonyl compounds, and belongs to the field of pharmacy. The invention relates to the application of the group of carbamyl phenylsulfonyl compounds or pharmaceutical compositions thereof in resisting atherosclerosis cardiovascular diseases. The compounds or the compositions thereof are used for preparation of ABCA1 and CLA-1 up-regulators and lipid-lowering and cholesterol-lowering drugs. The pharmaceutical compositions of the compounds used for treatment and / or prevention of atherosclerosis cardiovascular diseases contain the selected active ingredient with a therapeutically effective amount and an optionally pharmaceutically acceptable carrier.

Description

technical field [0001] The invention relates to a group of carbamoylbenzenesulfonyl compounds, which are used in the treatment and / or prevention of atherosclerotic cardiovascular diseases and belong to the field of pharmacy; the compounds of the invention are used to prepare ABCA1, CLA1 up-regulators and lipid-lowering agents 1. The use of cholesterol-lowering drugs; the present invention also relates to the pharmaceutical composition of said compound. Background technique [0002] Cardiovascular disease is the main killer of human health in developed countries and most developing countries. In recent years, with the improvement of people's material living standards, the incidence of cardiovascular and cerebrovascular diseases has shown an obvious upward trend, and the death rate of cardiovascular and cerebrovascular diseases accounts for the The composition of population death has reached 1 / 3. Atherosclerosis (AS) is a chronic inflammatory disease, which is the pathologica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D417/04C07D277/46C07D277/28C07D277/82C07D235/06C07D233/74C07D235/30C07D235/08C07D513/04C07C311/18C07D277/60A61K31/427A61K31/426A61K31/428A61K31/4166A61K31/4184A61K31/437A61K31/18A61P9/10A61P3/06
CPCC07C311/18C07D233/74C07D235/06C07D235/08C07D235/30C07D277/28C07D277/46C07D277/60C07D277/82C07D417/04C07D513/04
Inventor 司书毅许艳妮李永臻姜威刘畅王潇冯婷婷李霓李东升巫晔翔
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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