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Application of N-(4,5-dihydro-2-thiazole)-2-(4-methyl benzol phenoxy methyl) thiazole-4-formamide

A technology of methylphenoxymethyl and formamide, which is applied to the compound N--2-thiazole-4-carboxamide, the field of pharmaceutical compositions of the compound, has broad application prospects and good anti-atherosclerosis effect Effect

Active Publication Date: 2015-02-11
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

N-(4,5-dihydro-2-thiazole)-2-(4-methylphenoxymethyl)thiazole-4-carboxamide has no literature report on the anti-atherosclerosis effect, which is the patent Application for first discovery

Method used

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  • Application of N-(4,5-dihydro-2-thiazole)-2-(4-methyl benzol phenoxy methyl) thiazole-4-formamide
  • Application of N-(4,5-dihydro-2-thiazole)-2-(4-methyl benzol phenoxy methyl) thiazole-4-formamide
  • Application of N-(4,5-dihydro-2-thiazole)-2-(4-methyl benzol phenoxy methyl) thiazole-4-formamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 The EC50 determination of the compound of the present invention on the ABCA1 up-regulation screening model

[0036] The compound was dissolved in DMSO to make a 10 mg / ml stock solution. ABCA1-LUC HepG2 cells in 5×10 4 Each cell / well was 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 once with PBS. Compounds diluted with serum-free RPMI1640 or MEM were made into a series of concentrations, 0.001-100 μmol / L, 200 μl / well. Wells with a final concentration of 0.1% DMSO medium were used as blank controls. 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. Add cell lysate (20 μl / well) (Promega), after 15-30min, observe under the microscope that the cell lysis is complete, add luciferase (60 μl / well), immediately measure luciferase activity (microplate read...

Embodiment 2

[0037] Example 2 Determination of the impact of the compound of the present invention on the expression level of ABCA1 protein

[0038] The effect of the compound on the expression of ABCA1 protein was detected by western blot method as before. HepG2 cells were plated in a six-well plate (Costar), and a drug-dosed group T61 (0.05, 0.24, 1.20, 6.0 μg / ml) and a negative control group (no sample to be tested) were set up. RIPA cell lysate was used to extract total cell protein, and BCA kit (Pierce) was used for protein quantification, followed by 10% SDS-PAGE electrophoresis, 30 μg protein per well. Concentration of each protein antibody used: ABCA1 (NB400-105; 1:500dilution; Novus Biologicals Inc., San Jose, CA); β-actin (1:5000; Invitrogen); peroxidase (HRP)-conjugated goat anti-rabbit IgG antibody (1:3000 dilution; Santa Cruz); peroxidase (HRP)-conjugated rabbit anti-mouse IgG antibody (1:3000 dilution; Santa Cruz). It was detected by chemiluminescence (ECL, Millipore) kit a...

Embodiment 3

[0039] Embodiment three in apoE - / - Pharmacodynamic evaluation in mice

[0040] apoE - / - Establishment of mouse arteriosclerosis model

[0041] apoE - / - Mice, 7 weeks old, were fed with common feed for one week;

[0042] apoE - / - The mice were weighed, randomly grouped, and divided into 4 groups (model group, drug administration group, negative control group), with 6-8 mice in each group;

[0043] From the age of 8 weeks, the model group and the treatment group were fed with high-fat feed, and the negative control group continued to be fed with common feed;

[0044] T61 (20mg / Kg) was administered by intragastric administration; the negative control group and the model group were given sodium carboxymethyl cellulose solution, administered by intragastric administration; administration for 8 weeks;

[0045] 8 weeks of apoE will be administered - / - The mice were fasted for 6 hours; the eyeballs were removed to collect blood, and the blood was collected in EP tubes rinsed w...

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Abstract

The invention discloses application of a compound which is named as N-(4,5-dihydro-2-thiazole)-2-(4-methyl benzol phenoxy methyl)thiazole-4-formamide (as shown in the formula (I)), and belongs to the field of pharmacy. The compound shown in the formula (I) is ABCA1 up regulation agents and can be used for regulating blood lipids and used for treating or preventing the atherosclerosis. The application is further suitable for a medicine composition of the compound applied to up regulation of the ABCA1 expression activity, blood lipid regulation and treatment and / or prevention; and the medicine composition contains selected active ingredients in effective treatment amount and optional pharmaceutical acceptable carriers.

Description

technical field [0001] The present invention relates to compound N-(4,5-dihydro-2-thiazole)-2-(4-methylphenoxymethyl)thiazole-4-carboxamide, which is used in the treatment and treatment of atherosclerotic cardiovascular diseases / or prevention, belonging to the field of pharmacy; the compound of the present invention is used for the preparation of ABCA1 up-regulators, blood lipid drugs, and the prevention and / or treatment of anti-atherosclerosis; the present invention also relates to the pharmaceutical composition of the 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/427A61P9/10A61P3/06
CPCA61K31/427
Inventor 司书毅许艳妮李永臻姜威贺晓波刘畅刘祺王潇冯婷婷巫晔翔
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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