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Synthesized micromolecule compound capable of conveying bioactivator and application thereof

A technology for small molecular compounds and biologically active substances, applied in the field of small molecular compounds, can solve the problems of inability to meet the oral delivery of hydrophilic macromolecular drugs, poor stability, inability to achieve, etc., achieve convenient oral administration, improve stability, The effect of improving the absorption rate

Active Publication Date: 2009-10-14
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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  • Synthesized micromolecule compound capable of conveying bioactivator and application thereof
  • Synthesized micromolecule compound capable of conveying bioactivator and application thereof
  • Synthesized micromolecule compound capable of conveying bioactivator and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]

[0041] Preparation of compound 5: add 1-(3-dimethylaminopropyl)-3-ethyl to a solution of 2-hydroxy-5-isopropylbenzoic acid (1.0 equivalent) in dichloromethane (30 ml) Carbodiimide hydrochloride (1.0 equivalent) and 4-dimethylaminopyridine (2 equivalent). After stirring this solution at 0°C for 20 minutes, add methyl 4-aminobutyrate (1.0 equivalent) to the solution. ) In dichloromethane (10 mL). After the addition, the reaction mixture was gradually warmed to room temperature and stirred at room temperature for 12 hours.

[0042] The solution was transferred to a separatory funnel, and washed with 1 equivalent hydrochloric acid solution (2×20 mL), water (2×20 mL), saturated sodium bicarbonate solution (2×20 mL), and saturated brine (40 mL). It was dried with anhydrous magnesium sulfate, filtered, and concentrated in vacuo. Subsequently, the residue was dissolved in tetrahydrofuran (30 mL) and sodium hydroxide solution (2 equivalents) was added. The mixture was stirred at...

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Abstract

The invention relates to a synthesized micromolecule compound capable of conveying bioactivator and an application thereof. The micromolecule compound of the invention or any medicinal salt thereof are provided with the following general formula: A-B-X-C-D-E; wherein, A is C6-C10 aromatic ring or C2-C9 hetero-aromatic ring, B is C6-C10 aromatic ring or C2-C9 hetero-aromatic ring, X is O,NH, S or CH2 and C is -(CH2)n-, C3-C6 naphthene base, C6-C10 aromatic ring or C2-C9 hetero-aromatic ring. D is carboxylic acid group (COOH) or CONHOH, when C stands for -(CH2)n-; when C is C6-C10 aromatic ring or C2-C9 hetero-aromatic ring, D is -(CH2)n-, and E is negative charged carboxyl group (COOH), -CONHOH, tetrazole, OH or -SO3H.

Description

Technical field [0001] The invention relates to a small molecule compound capable of transporting biologically active substances (including chemically synthesized active substances) into organisms and applications thereof. Background technique [0002] Substances with biological activity can be delivered into the organism through several ways, but which method can achieve the purpose of delivery is often restricted by the objective conditions during delivery. [0003] Most of the biologically active substances (such as calcitonin, interferon, insulin, special mucopolysaccharides, heparin, heparin analogs, etc.) are commonly used in clinical administration for injection solutions and freeze-dried powder injections. Relatively single, and frequent administration, patient compliance is poor. At present, the biggest problem with oral administration of such substances is that the body's physical, chemical and biological barriers affect its delivery. For example, protein drugs cannot b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C235/60C07C59/56C07D257/04C07D263/32C07D277/30C07D498/04C07C309/51C07C259/10A61K47/16A61K47/12A61K47/22A61K47/20A61P43/00
Inventor 邢东霞戴立忠
Owner SANSURE (SHANGHAI) GENE TECH LTD
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