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Compound and medicinal application thereof

A compound, drug technology

Inactive Publication Date: 2010-07-07
PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Salvianolic acid A is the most active compound in Danshen (Du Guanhua [Basic Medicine and Clinic, 2000, 20(5): 10-14], Hu Yiyang [Acta Pharmacology of Traditional Chinese Medicine, 1997, 18(5): 478-480] ), our hospital has developed it into a drug (Chinese patent 200610170267.0, 200610145453.9), but we found in the process of drug research that the structure of salvianolic acid A determines some of its defects, such as poor stability, poor membrane permeability, Low bioavailability, salvianolic acid A is a compound with strong antioxidant activity in nature, easy to be oxidized, unstable in aqueous solution, and easier to degrade during high temperature sterilization; salvianolic acid A is very soluble in water, its Membrane permeability is very poor; therefore, a lot of work is needed to develop salvianolic acid A into a medicine. If starting from the pharmaceutical excipients, although the above problems can be solved and salvianolic acid A can be made into a medicine, a large amount of work is required. However, its stability and membrane permeability are still not very ideal. Therefore, it is of broad and scientific significance to transform the structural defects of salvianolic acid A and find new compounds; many medical workers hope that through structural Transformation, in order to achieve the purpose of changing these defects

Method used

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  • Compound and medicinal application thereof
  • Compound and medicinal application thereof
  • Compound and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0221] The raw material is: salvianolic acid A;

[0222] Preparation method: Take raw materials, add water to dissolve, add KOH solution, adjust pH value to 3-5, place at low temperature, crystallization occurs, filter, dry to obtain compound:

[0223]

[0224] Composing a pharmaceutical composition with the obtained compound as an active ingredient, or preparing it into a pharmaceutical preparation;

[0225] The obtained compound spectrum data are as follows:

[0226] Hydrogen spectrum (ppm): 6.83, 7.14, 7.82, 6.27, 6.69, 6.71, 6.82, 2.97, 2.82, 4.93, 7.03, 6.61, 6.44, 6.59, 7.03.

[0227] 碳谱(ppm):124.1、129.50、146.25、147.85、114.97、119.56、145.44、115.59、166.70、129.11、116.98、144.24、143.77、116.35、119.13、37.24、74.94、172.50、127.28、113.42、146.03、144.55、 115.90, 120.42, 135.94, 119.61.

Embodiment 2

[0229] The raw material is: salvianolic acid A;

[0230] Preparation method: add dichloromethane, raw materials, phenol, DCC and DMAP to a dry round bottom flask under nitrogen protection, a white flocculent precipitate is formed, stir at room temperature for 5 hours, TLC detects that the reaction is complete (developing agent: chloroform: methanol: formic acid =4:1:0.2). Suction filtration, wash the filtrate with dilute alkaline solution 3 times, then wash with saturated NaCl solution until neutral, dry over anhydrous sodium sulfate, filter, spin the filtrate, purify by column chromatography, collect the product phase, spin evaporate until dry to shallow Yellow foamy solid, yielding compound:

[0231]

[0232] Composing a pharmaceutical composition with the obtained compound as an active ingredient, or preparing it into a pharmaceutical preparation;

[0233] The obtained compound spectrum data are as follows:

[0234] Hydrogen spectrum (ppm): 6.86, 7.22, 8.05, 6.33, 6.7...

Embodiment 3

[0237] The raw material is: salvianolic acid A;

[0238] Preparation method: add the raw materials into dichloromethane under nitrogen protection, stir to dissolve, add triethylamine, drop the temperature to 0°C, add 1 propionic anhydride dropwise, after the dropwise addition, continue to react for 3 hours, TLC detects that the reaction is complete (developing agent: chloroform : methanol: formic acid=4:1:0.2). Add water dropwise to the reaction solution, separate the liquid, wash the organic phase with water, dry over anhydrous sodium sulfate, filter, spin the filtrate, purify by column chromatography, collect the product phase, spin evaporate to dryness to obtain a light yellow solid, and obtain the compound:

[0239]

[0240] Composing a pharmaceutical composition with the obtained compound as an active ingredient, or preparing it into a pharmaceutical preparation;

[0241] The obtained compound spectrum data are as follows:

[0242] Hydrogen spectrum (ppm): 7.24, 7.31...

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Abstract

The invention discloses a newly-discovered compound and medicinal application thereof. The newly-discovered compound is characterized in that the new compound with good stability and membrane permeability and high bioavailability can be screened by reforming the structure of salvianolic acid A in salvia sclarea and carrying out stability experiment, Lop determination, pharmacodynamic experiment and the like and has better pharmacological effects in the aspect of treating cardiovascular and cerebrovascular diseases and other diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a series of novel compounds and their medicinal uses. Background technique [0002] The material basis for natural medicines to prevent and treat diseases lies in the active ingredients they contain. However, many natural active ingredients have structural defects, resulting in poor stability, solubility, absorption, incorrect distribution, and short metabolic and biological half-lives. problems and cannot be fully utilized therapeutically. Although some disadvantages can be overcome by appropriate pharmaceutical composition (i.e. formulation technology), thereby obtaining desired pharmaceutical products, such as sustained and controlled release technology or by other routes of administration such as rectal administration, epidermal administration, etc. Drugs, etc., but some problems cannot be solved by pharmaceutical compositions, and can only be solved by chemically modifying...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/73A61K31/225A61P1/16A61P9/06A61P3/06A61P35/00A61P25/28
Inventor 顾群孙学伟李志刚孙德杰米长江金治刚徐春霞
Owner PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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