Synthetic micromolecule compound capable of conveying bioactive substances and application thereof

A technology of biologically active substances and small molecule compounds, which is applied in the field of small molecule compounds, can solve the problems of unsatisfactory oral delivery of hydrophilic macromolecular drugs, poor stability, and failure to achieve, and achieve convenient oral administration, improved stability, The effect of improving the absorption rate

Active Publication Date: 2013-06-05
SANSURE (SHANGHAI) GENE TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in these microparticle carrier delivery systems, the lipid drug delivery system cannot achieve a high encapsulation efficiency for hydrophilic macromolecular drugs
In addition, they are less stable in the digestive tract
Ordinary liposomes and microemulsions are basically unable to meet the oral delivery of hydrophilic macromolecular drugs

Method used

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  • Synthetic micromolecule compound capable of conveying bioactive substances and application thereof
  • Synthetic micromolecule compound capable of conveying bioactive substances and application thereof
  • Synthetic micromolecule compound capable of conveying bioactive substances and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0032] (1) Examples of preparation methods of small molecular compounds

[0033]

[0034] Preparation of compound 1: 2-benzyloxyphenylfluoromethyl diethyl phosphate (1.5 equivalents) was dissolved in anhydrous tetrahydrofuran (50 ml), and the solution was cooled in an ice bath under the protection of nitrogen. Subsequently, sodium hydride (60%, 1.75 equiv) was added in portions. After all had been added, the reaction mixture was stirred at 0°C for 20 minutes, then methyl 9-oxononanoate (1.0 eq) dissolved in anhydrous THF (15 mL) was added slowly over 20 minutes using an addition funnel. Subsequently, the reaction mixture was gradually warmed to room temperature and stirred at room temperature for 18 hours, water (20 ml) was slowly added to the reaction mixture, and transferred to a separatory funnel, extracted with ethyl acetate (3 × 20 ml), organic The layers were washed with water (20 ml) and saturated sodium chloride (30 ml), respectively. Subsequently, it was dried ov...

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PUM

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Abstract

The invention relates to a synthetic micromolecule compound capable of conveying bioactive substances and application thereof. The general formula of the micromolecule compound or any medicinal salt thereof is disclosed in the specification, wherein R4 is an aromatic ring of C6-C10 or a heteroaromatic ring of C2-C9; R5 is a -(CH2)n-, a naphthenic group of C3-C5, an aromatic ring of -(CH2)n-C6-C10or a heteroaromatic ring of C2-C9; and R6 is a carboxyl group (COOH), -CONHOH, tetrazole, OH and -SO3H.

Description

[0001] This application is a divisional application with an application date of May 22, 2009, an application number of 200910043494.0, and an invention title of "Synthetic Small Molecular Compounds Capable of Transporting Biologically Active Substances and Their Applications". technical field [0002] The present invention relates to a small molecular compound capable of transporting biologically active substances (including chemically synthesized active substances) into organisms and applications thereof. Background technique [0003] Substances with biological activity can be transported into organisms through several ways, but which method can achieve the purpose of delivery is often subject to the objective conditions of delivery. [0004] Most of the biologically active substances (such as calcitonin, interferon, insulin, special mucopolysaccharides, heparin, heparin analogs, etc.) Relatively single, and frequent administration, poor patient compliance. Currently, the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C59/56C07D257/04A61K47/12A61K47/22
Inventor 邢东霞戴立忠
Owner SANSURE (SHANGHAI) GENE TECH LTD
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