Flavone derivative and preparation method and medical application of flavone derivative

A technology of derivatives and flavones, which is applied in the field of flavone derivatives and their preparation, to achieve the effect of easy-to-obtain raw materials, high yield, and fewer steps

Active Publication Date: 2019-08-27
北京东方百奥医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, ED prevention and treatment drugs must be able to repair these ED pathophysiological changes in order to effectively restore erectile function, but there is no drug that can repair ED pathological changes and restore erectile function in clinical use. This is the current ED rehabilitation treatment research. major challenge

Method used

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  • Flavone derivative and preparation method and medical application of flavone derivative
  • Flavone derivative and preparation method and medical application of flavone derivative
  • Flavone derivative and preparation method and medical application of flavone derivative

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] The flavone derivatives provided by the present invention or their pharmaceutically acceptable salts have the following structure:

[0071]

[0072] in:

[0073] (1) R1 is independently selected from the following substituent groups: H, C1-C6 alkyl;

[0074] (2) R2 is independently selected from the following substituent groups: H, C1-C6 alkyl, C3-C8 cycloalkyl, C2-C6 alkenyl, C2-C6 fatty acyl, C7-C12 aroyl;

[0075] (3) R3 is independently selected from the following substituent groups: H, C1-C6 alkyl.

[0076] Further, the flavone derivatives provided by the present invention or pharmaceutically acceptable salts thereof are preferably R1=H, R2=C2-C6 alkenyl, R3=CH3.

Embodiment 2

[0078] The flavone derivatives provided by the present invention or their pharmaceutically acceptable salts are code-named YS10 and have the following structure:

[0079]

[0080] The synthesis of flavone derivative YS10 comprises the following steps:

[0081] (1) Mix 6g (16.3mmol) dehydrated icariin with 80mL DMF, add 3.38g (24.5mmol) anhydrous potassium carbonate to it, stir for 10 minutes and slowly add 1.97mL (19.6mmol) 3- Bromo-2-methylpropene, after addition, react at room temperature.

[0082] (2) TLC (petroleum ether: dichloromethane: methanol = 40:40:1) followed the reaction, and the reaction was complete after about 8 hours. After the reaction was completed, pour the reaction solution into 500 mL of ice water, stir and let stand for one hour, a large amount of light yellow solid precipitated, filtered with suction, washed the filter cake with water three times and dried to obtain the crude product of YS-10. Pass the crude product through a silica gel column (pet...

Embodiment 3

[0098] Use of the flavone derivative YS10 in a drug for preventing or treating erectile dysfunction.

[0099] The first part, in vitro experiment: the comparison of flavone derivative YS10 and dehydrated icariin on the activation of adipose stem cells.

[0100] Research Background:

[0101] Chronic diseases that endanger human health include complications caused by common diseases such as diabetes, hypertension, obesity, trauma, etc., which mainly occur in important parenchymal organs such as heart, brain, kidney, and genital tissues, blood vessels, nerves, and matrix. Death, degeneration, necrosis, and degenerative pathological changes cause related organ dysfunction. Therefore, exploring the pathophysiological mechanism of tissue damage repair and exploring drugs and methods that can prevent and treat these pathophysiological changes are currently major challenges to maintaining organ function, and this patent invention is based on this.

[0102] This study takes erectile ...

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Abstract

The invention relates to a flavone derivative and a preparation method and medical application of the flavone derivative. The flavone derivative is prepared through a mode that anhydroicaritin is taken as a mother nucleus, and group addition and reduction are conducted. It is proved through a pharmacological experiment that the flavone derivative has the pharmacological effect of activating endogenous stem cells in the body, achieves the effects of repairing injury-type pathological changes of blood vessel cells, nerve cells, endothelial cells and the matrix and recovering functions, can be used for preparing medicines for repairing the tissue-injury pathological changes and has a good prospect in preparing medicines for conducting rehabilitation treatment on erectile dysfunction pathological changes.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a class of flavonoid derivatives, a preparation method and medical application thereof. Background technique [0002] Chronic diseases that endanger human health include complications caused by common diseases such as diabetes, hypertension, obesity, trauma, etc., which mainly occur in important parenchymal organs such as heart, brain, kidney, and genital tissues, blood vessels, nerves, and matrix. Death, degeneration, necrosis, and degenerative pathological changes cause related organ dysfunction. Therefore, exploring the pathophysiological mechanism of tissue damage repair and exploring drugs and methods that can prevent and treat these pathophysiological changes are currently major challenges to maintaining organ function, and this patent invention is based on this. [0003] Erectile dysfunction (erectile dysfunction, ED) refers to the continuous inability of th...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61P15/10A61P13/12A61P15/00A61P27/02
CPCC07D493/04A61P15/10A61P13/12A61P15/00A61P27/02
Inventor 刘接卿林倩玉辛华顾静良姚正
Owner 北京东方百奥医药开发有限公司
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