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Application of flavone derivative in preparation of medicine for preventing or treating acute lung injury and/or acute respiratory distress syndrome

A technology for acute respiratory distress and acute lung injury, applied in the field of pharmaceutical research and development, can solve the problems of low curative effect, suppressing pulmonary edema dosage, etc., and achieve the effect of low dosage, suppressing pulmonary edema, and reducing the generation of pulmonary effusion

Pending Publication Date: 2022-05-06
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Therefore, the object of the present invention is to solve the problem that the drugs in the prior art cannot inhibit pulmonary edema while anti-inflammation, and there is a problem of high dosage and low curative effect, thereby providing a kind of flavone derivatives used in the preparation of prevention or treatment of acute Use of Drugs for Lung Injury and / or Acute Respiratory Distress Syndrome

Method used

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  • Application of flavone derivative in preparation of medicine for preventing or treating acute lung injury and/or acute respiratory distress syndrome
  • Application of flavone derivative in preparation of medicine for preventing or treating acute lung injury and/or acute respiratory distress syndrome
  • Application of flavone derivative in preparation of medicine for preventing or treating acute lung injury and/or acute respiratory distress syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The present embodiment provides a kind of flavonoid derivative, its reaction equation and preparation method are as follows:

[0045]

[0046] Weigh 20g of scutellarein and 25g of dichlorodiphenylmethane into 400mL of diphenyl ether, heat and stir at 180°C for 30 minutes, cool to room temperature, add 2L of petroleum ether dropwise, and filter out the solid. The solid was dissolved in ethyl acetate and mixed with silica gel (dry loading), and the silica gel column was used to Purification, followed by eluting with a mixture of petroleum ether and ethyl acetate with a volume ratio of 10:1, 3:1, and 1:1, and collecting petroleum ether and ethyl acetate with a volume ratio of 3:1 according to the TLC results The eluate obtained as the eluent was concentrated and crystallized to obtain compound 1 (25.13 g, yield 79.6%) as a yellow solid.

Embodiment 2

[0048] The present embodiment provides a kind of flavonoid derivative, its reaction equation and preparation method are as follows:

[0049]

[0050] Weigh 500 mg of compound 1 prepared in Example 1, add it to 25 mL of DMF, add 260 mg of potassium carbonate, and then add 200 μl of benzyl bromide to obtain a mixture, which is stirred in an ice-water bath (0° C.) for 2 h, and left at room temperature for 12 hours. The mixture was dissolved in 150 mL of water, extracted 3 times with ethyl acetate, 80 mL each time, the collected organic layer was washed with 200 mL of saturated brine, dried over sodium sulfate, and concentrated under reduced pressure to obtain a crude solid, which was dissolved in ethyl acetate Mix the sample with silica gel (dry loading), then pass through the silica gel column Purify, using the mixed solution of petroleum ether and ethyl acetate that volume ratio is 10:1, 5:1, 2:1, 1:1 successively as eluent to carry out gradient elution, collect according t...

Embodiment 3-8

[0052] This example provides a series of flavonoid derivatives, which are all prepared by the following reaction equation and preparation method, the difference is that the raw materials H-R 3 And the consumption of this raw material is different, thereby obtains different products, specifically see the following table:

[0053] The raw material of embodiment 3-8, product and reaction yield

[0054]

[0055] Embodiment 3-8 all adopts following reaction equation and preparation method as follows:

[0056]

[0057] Weigh the corresponding raw materials H-R according to the quality in Table 1 3 , weigh 8ml of DMF (dimethylformamide) and add to 500mlCCl 4 In the solution, after stirring at room temperature for 30min, add CCl containing 120g bis(trichloromethyl)carbonate dropwise. 4 Solution 200ml. The mixture was slowly refluxed at 75°C for 6 hours, and naturally cooled to room temperature. After the reaction solution was concentrated under reduced pressure, the crude r...

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Abstract

The invention relates to the technical field of medicine research and development, in particular to application of a flavone derivative in preparation of a medicine for preventing or treating acute lung injury and / or acute respiratory distress syndrome, the flavone derivative has a structure shown as a formula I, R1 is selected from one of H, C1-C8 alkyl and C3-C10 cycloalkyl, R2 is selected from one of C1-C8 alkyl and C3-C10 cycloalkyl, and R3 is selected from one of C1-C8 alkyl and C3-C10 cycloalkyl. And R2 is selected from aryl groups of C5-C20 or substituted aryl groups of C5-C20. The flavone derivative provided by the invention can obviously inhibit inflammatory response, inhibit release of inflammatory factors, reduce the content of inflammatory factors in alveolar lavage fluid and serum, obviously inhibit pulmonary edema, reduce generation of pulmonary effusion, reduce lung wet weight and inhibit the rising degree of the ratio of the lung wet weight to the lung dry weight caused by acute lung injury; therefore, the effects of resisting inflammation and inhibiting lung edema are achieved.

Description

technical field [0001] The invention relates to the technical field of medical research and development, in particular to the application of a flavonoid derivative in the preparation of drugs for preventing or treating acute lung injury and / or acute respiratory distress syndrome. Background technique [0002] Acute lung injury (ALI) / acute respiratory distress syndrome (ARDS) is a common clinical critical illness with a high mortality rate, which seriously threatens the lives of critically ill patients. According to statistics, more than 10% of ALI patients need to be admitted to intensive care unit for treatment, and the fatality rate is as high as 32%-55%. bronchial asthma or myocardial infarction etc. on a par. The basic pathophysiological change of ALS / ARDS is non-cardiogenic pulmonary edema caused by increased permeability of alveolar epithelial cells and pulmonary capillary endothelium. Due to alveolar edema and alveolar collapse, severe ventilation / blood flow imbalanc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P11/00
CPCA61K31/352A61P11/00
Inventor 申凯孙俊哲温尧林
Owner CATCH BIO SCI & TECH
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