Unlock instant, AI-driven research and patent intelligence for your innovation.

Synthesized micromolecule compound capable of conveying bioactivator and application thereof

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

Active Publication Date: 2012-06-20
SANSURE (SHANGHAI) GENE TECH LTD
View PDF1 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

preparation example Construction

[0033] (1) Examples of Preparation Methods of Small Molecular Compounds

[0034]

[0035] Preparation of compound 5: 1-(3-dimethylaminopropyl)-3-ethyl Carbodiimide hydrochloride (1.0 equivalents) and 4-dimethylaminopyridine (2 equivalents), the solution was stirred at 0°C for 20 minutes, and the solution was added to the solution containing methyl 4-aminobutyrate (1.0 equivalents). ) in dichloromethane (10 mL), after addition, the reaction mixture was gradually warmed to room temperature and stirred at room temperature for 12 hours.

[0036] The solution was transferred to a separatory funnel, washed with 1 N hydrochloric acid solution (2×20 ml), water (2×20 ml), saturated sodium bicarbonate solution (2×20 ml), and saturated brine (40 ml) respectively, It was dried over anhydrous magnesium sulfate, filtered, and concentrated in vacuo. Subsequently, the residue was dissolved in tetrahydrofuran (30 mL) and sodium hydroxide solution (2 eq.) was added. The mixture was stirre...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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: wherein, R1 is C6-C10 aromatic ring or C2-C9 hetero-aromatic ring; R2 is -(CH2)n-, C3-C6 naphthenic group, -(CH2)n-C6-C10 aromatic ring or C2-C9 hetero-aromatic ring; R3 is carboxylic group (COOH), -CONHOH, tetrazole, OH, -SO3H. The micromolecule compound of the invention can effectively deliver substance with biological activity by ways of mouth, colon and so on to an organism body, realize the organism body administration, improve the stability of drugs, improve the absorption rate in gastrointestinal tract, directionally deliver the drugs to a target part in the body, and achieve the slowly-released long effective purpose through the degradation of biodegradable polymer.

Description

technical field [0001] 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 [0002] 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. [0003] 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 biggest problem with oral administration of such substances is that the body's physical, chemical and biological barriers affect their delivery. For example, protein drugs cannot be administered orally, mainly because such drugs are often hydrolyzed by strong gastric acid or deg...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(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