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Aminosugar derivate, preparation method and medical application thereof

A drug and pharmaceutical technology, applied in the field of inhibition of neovascularization of chicken embryo allantoic membrane, compound N--3--acrylamide, can solve the complex structure of carbohydrate compounds, difficult industrial production, difficult analysis and preparation, etc. problem, to achieve a strong effect of chick embryo allantoic membrane neovascularization

Inactive Publication Date: 2009-12-30
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these sugar compounds have complex structures, are difficult to analyze and prepare, and are difficult to carry out industrial production.

Method used

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  • Aminosugar derivate, preparation method and medical application thereof
  • Aminosugar derivate, preparation method and medical application thereof
  • Aminosugar derivate, preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] N-(2,3,4,6-tetra-O-acetyl-1-deoxy-β-D-galactopyranosyl)-3-(2,4-dichlorophenyl)-2-acrylamide Preparation of (I) 2-benzylidene-1,3,4,6-tetrahydroxy-2-deoxy-β-D-galactopyranose (4)

[0041] Add 10g (46mmol) of 1,3,4,6-tetrahydroxy-2-deoxy-D-galactopyranosamine hydrochloride to 47mL aqueous solution containing 2.2g (55mmol) of NaOH at 0°C, under mechanical stirring Slowly add 5.4mL (53mmol) of benzaldehyde, a white solid precipitates out quickly, continue to stir for 1h and then stop the reaction, place it at 0°C for 12h, filter, then mix with water, V (ether): V (ethanol) = 4:1 Washed with solvent and dried under infrared light to obtain 10 g of white solid mixture, which was directly used in the next reaction without purification.

[0042] 2-Benzylidene-1,3,4,6-tetra-O-acetyl-2-deoxy-β-D-galactopyranose (5)

[0043] Add 10 g of the mixture containing intermediate 4 into 60 mL of pyridine, add 42 mL (0.46 mol) of acetic anhydride while stirring in an ice-water bath, rais...

Embodiment 2

[0056] tablet

[0057] Get compound I 500mg obtained in Example 1, starch 2g, dextrin 1g mix, make soft material with appropriate amount of 30% ethanol as wetting agent, conventional method granulate, add appropriate amount of magnesium stearate, make tablet.

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PUM

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Abstract

The invention relates to the field of medicinal chemistry, an aminosugar derivate, a preparation method and a medical application thereof, in particular to a compound N-(1, 3, 4, 6-fourth-O-galloylhyperin acetyl-2-deoxidizing-beta D-pyranoid galactosyl)-3-(2,4-dichlorophenyl)-acrylamide (I). Pharmacological experiments show that the compound (I) can inhibit the neovascularization of chick chorioallantoic membrane, therefore, the compound can be used for treating tumors or chronic inflammation clinically.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the compound N-(1,3,4,6-tetra-O-acetyl-2-deoxy-β-D-galactopyranosyl)-3-(2,4- Dichlorophenyl)-acrylamide, its preparation method, and its inhibitory effect on neovascularization of chicken embryo allantoic membrane. Background technique [0002] Tumor Angiogenesis Inhibitors (Tumor Angiogenesis Inhibitor, TAI) can destroy or inhibit angiogenesis, effectively prevent tumor growth, metastasis and recurrence, and show great advantages compared with traditional anti-tumor drugs. Currently known TAIs can be divided into drugs with specific mechanism of action and multi-target drugs acting on a single signaling pathway based on their mechanism of action. Mechanism-specific drugs include, for example, Bevacizumab, a VEGF / VEGFR signaling pathway inhibitor. Multi-target drugs include multi-target tyrosine kinase inhibitors Sorafenib (Sorafenib), Thalidomide (Thailidomide), etc. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H13/04A61K31/7024A61P29/00A61P35/00
Inventor 靳娜庄毅超董缙徐云根陈王露王琳薛鑫张宇宋巧杨波何俏军
Owner CHINA PHARM UNIV
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