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Compounds and uses thereof for treating atherosclerosis

A compound and composition technology, applied in the field of medicine, can solve the problems of niacin patients' compliance troubles, side effects, flushing, etc.

Active Publication Date: 2019-04-09
XIAN PEIHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Even so, however, statins achieve only about one-third of the risk reduction in the treatment and prevention of atherosclerosis and its associated vascular complications
In addition, the drugs themselves have certain drawbacks, for example niacin suffers from patient compliance issues, partly due to side effects such as flushing etc.

Method used

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  • Compounds and uses thereof for treating atherosclerosis
  • Compounds and uses thereof for treating atherosclerosis
  • Compounds and uses thereof for treating atherosclerosis

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach

[0059] Hereinafter, the present invention is described in more detail to facilitate understanding of the present invention.

[0060] Those skilled in the art will recognize that the chemical reactions described herein can be used to suitably prepare many other compounds of the invention and that other methods for preparing the compounds of the invention are considered to be within the scope of the invention Inside. For example, the synthesis of those non-exemplified compounds according to the present invention can be successfully accomplished by those skilled in the art through modification methods, such as appropriate protection of interfering groups, by using other known reagents in addition to those described in the present invention, or by incorporating Reaction conditions with some routine modifications. In addition, reactions disclosed herein or known reaction conditions are also recognized to be applicable to the preparation of other compounds of this invention.

Embodiment 1

[0061] Example 1: 2-(6-methylthien[2,3-d]pyrimidin-5-ylamino)quinazolin-4(3H)-one (compound TPQZ-1)

[0062]

[0063] Add 2-aminoquinazolin-4(3H)-one (5.0mmol), 5-bromo-6-methylthien[2,3-d]pyrimidine (5.0mmol) to 50mL N,N-dimethyl Add 60% NaH (10.0mmol) to the above mixture in batches under stirring in formamide, and add 60% NaH (10.0mmol) in batches to room temperature, then continue the reaction for 5 hours. After the reaction is complete, add 2 mL of glacial acetic acid to terminate the reaction . The reaction solution was poured into 100 mL of saturated sodium bicarbonate solution, the precipitated solid was filtered, washed with water, and the filter cake was dried and recrystallized with ethyl acetate to obtain 1.22 g of the target product with a yield of 79.5%.

[0064] Mass Spectrum (ESI): 310.35[M+H] +

[0065] Elemental analysis: theoretical value C, 58.24; H, 3.58; N, 22.64; O, 5.17; S, 10.37

[0066] Found value C, 58.15; H, 3.78; N, 22.48; O, 5.06; S, 10.53...

Embodiment 2

[0068] Example 2: 2-(6-amino-2-methylthiophene [2,3-d]pyrimidin-5-ylamino)-5,7-dimethoxyquinazolin-4(3H)-one ( Compound TPQZ-2)

[0069]

[0070] 2-amino-5,7-dimethoxyquinazolin-4(3H)-one (5.0mmol), 5-bromo-2-methylthien[2,3-d]pyrimidin-6-amine ( 5.0mmol) was added to 50mL N,N-dimethylformamide, cooled to 0°C in an ice bath, and 60% NaH (10.0mmol) was added to the above mixture in batches under stirring, and the temperature was naturally raised to room temperature, and then continued The reaction was carried out for 7 hours. After the reaction was complete, 2 mL of glacial acetic acid was added to terminate the reaction. The reaction solution was poured into 100 mL of saturated sodium bicarbonate solution, the precipitated solid was filtered, washed with water, and the filter cake was dried and then recrystallized with toluene to obtain 1.43 g of the target product with a yield of 74.6%.

[0071] Mass Spectrum (ESI): 385.41[M+H] +

[0072] Elemental analysis: theoretica...

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Abstract

The invention relates to a quinolinone compound for treating atherosclerosis, and an application of the compound in preparing medicine for treating atherosclerosis. The compound of the present invention can improve the uptake rate of liver cells for low-density lipoprotein LDL, can reduce serum total cholesterol (TC), serum triglyceride (TG), serum low-density lipoprotein cholesterol (LDL-C) of rats, shows The compound of the present invention can greatly reduce blood fat, so it can be used for preventing and treating atherosclerosis. Furthermore, the above-mentioned effects of the compounds of the invention are comparable or even superior to those of simvastatin.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a compound for treating atherosclerosis and the application of the compound in the preparation of medicine for treating atherosclerosis. Background technique [0002] Atherosclerosis (AS) is a systemic disease related to lipid metabolism disorders, characterized by lipid deposition in the intima of large and medium arteries, atherosclerotic plaque formation, fibrous tissue hyperplasia, and arterial wall sclerosis. Atherosclerosis and its associated vascular complications are a major cause of cardiovascular and cerebrovascular diseases leading to heart attack and stroke. Over time, plaque deposits within the arteries increase in size, preventing oxygen from reaching downstream organs. When a vital artery in the heart becomes blocked, it can cause angina and heart attack, and can lead to death. Atherosclerosis also affects the arteries leading to the brain, causing blood clots in ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D495/04A61K31/519A61P9/10A61P3/06
CPCA61P3/06A61P9/10C07D495/04
Inventor 柳蔚孟姣陈玉华
Owner XIAN PEIHUA UNIV
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