Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Compound of styryl with axa-containing heterocyclic modified and use thereof

A technology of styrene-based compounds, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, organic chemistry, etc., can solve the problems of inability to prevent the occurrence and development of diseases, damage, and unclearness

Inactive Publication Date: 2007-07-18
TSINGHUA UNIV
View PDF0 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For many years, the main drug for clinical treatment of this disease is cholinesterase inhibitor, which acts on the cholinergic nervous system and has a relieving effect on the disease, but it cannot prevent the occurrence and development of the disease
At present, the pathogenesis of Alzheimer's disease is not very clear, but it is generally believed that the key cause of the disease is the aggregate (SP) formed by misfolding of excess β-amyloid peptide (Aβ). main component) damages cell membranes, synapses and axons, and causes neurofibrillary tangles

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
  • Compound of styryl with axa-containing heterocyclic modified and use thereof
  • Compound of styryl with axa-containing heterocyclic modified and use thereof
  • Compound of styryl with axa-containing heterocyclic modified and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1. Preparation of styryl compounds

[0036] The synthesis of the styryl compound of the present invention includes the following steps:

[0037] a. Synthesis of Cyclen-containing monomer [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecano-1-yl]acetic acid, the method is: Cyclen (purchased Starting from Acros Company in the United States, first react with Boc20 (di-tert-butyl dicarbonate, purchased from Shanghai Gil Biochemical Company) to obtain 1,4,7-tri-tert-butoxycarbonyl-1,4,7,10-tetraaza 3Boc-Cyclen (see Eiichi Kimura, Shin Aoki, Tohru Koike, and Motoo Shiro, A Tris (ZnII-1, 4, 7, 10-tetraazacyclododecane) Complex as a New Receptor for Phosphate Dianions in Aqueous Solution, Journal of American Chemical Society, 1997, Vol 119, 3068-3076), and then react the product with ethyl bromoacetate (see Joong Won Jeon, SangJun Son, Chang Eun Yoo, In Seok Hong, Jung Bae Song, and Junghun Suh, Protein-Cleaving Catalyst Selective for Protein Substrate, Organic Le...

Embodiment 2

[0043] Example 2. Preparation of styryl compounds

[0044] The synthesis of the styryl compound (formula VII) of the present invention includes the following steps:

[0045] a. Combining benzoic acid (purchased from Sigma in the United States) with Cyclen-containing monomer [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecano-1-yl ] Acetic acid coupling, the connection conditions are the presence of coupling agent EDC (purchased from Shanghai Yanchang Biochemical Company), HOBt (purchased from Shanghai Gil Biochemical Company) and catalyst DMAP (mixing ratio: 4 times the amount of monomer containing Cyclen, 1 times The amount of benzoic acid, 4 times the amount of coupling agent EDC and 4 times the amount of HOBt) react at room temperature for 15 hours to obtain the target product.

[0046] c. The crude product obtained after the reaction in step b is separated with a silica gel column (column separation conditions are: ethyl acetate: petroleum ether (1:4)), and the prod...

Embodiment 3

[0051] Example 3. Preparation of styryl compounds

[0052] The synthesis of the styryl compound of the present invention (see formula VIII for the molecular formula) includes the following steps:

[0053] a. Preparation of Trpn-containing monomer [3(3',3"-di-tert-butoxycarbonyl-3',3"-diamino)aminopropylamino]acetic acid: The synthesis method is: Trpn (purchased from the United States) Acros company) as the raw material, firstly react with Boc20 (di-tert-butyl dicarbonate, purchased from Shanghai Gil Biochemical Company) to obtain 3',3"-di-tert-butoxycarbonyl-3,3',3"-triaminopropyl Amine (2Boc-Trpn) (see Eiichi Kimura, Shin Aoki, Tohru Koike, and Motoo Shiro, ATris (ZnII-1, 4, 7, 10-tetraazacyclododecane) Complex as a New Receptor for Phosphate Dianions in Aqueous Solution, Journal of American Chemical Society, 1997, Vol 119, 3068-3076), and then react the product with ethyl bromoacetate (see Joong Won Jeon, Sang Jun Son, Chang Eun Yoo, In Seok Hong, Jung Bae Song, and Junghun Suh,...

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

This invention relates to an azacyclo-modified styrene compounds and its applications. Its purpose is to provide an azacyclo-modified styrene compounds, and its applications in the preparation of Alzheimer's disease, Parkinson's disease and other degenerative nervous system disease or type two diabetes prevention and therapeutic drug. Studies show that the invention can inhibit aggregation of A beta, also can make the A beta aggregate depolymerizate, and will eventually hydrolysis and eliminate A beta protein, inhibited and removal of A beta toxicity, in the field of medicine has broad application prospects.

Description

Technical field [0001] The present invention relates to a styryl compound and its application, in particular to a styryl compound modified with a nitrogen-containing heterocycle and its preparation, treatment and prevention of Alzheimer’s disease, Parkinson’s disease, type 2 diabetes and other nervous systems Application in degenerative disease drugs. Background technique [0002] Degenerative diseases of the nervous system such as Alzheimer's disease and Parkinson's disease and type 2 diabetes are protein conformation diseases. Among them, Alzheimer's disease (AD), also known as Alzheimer's disease, is a degenerative disease of the central nervous system, which is clinically manifested as cognitive impairment, memory decline, and eventually loss of thinking ability, movement disorders, and life Can't take care of themselves. The pathological features are mainly senile plaque (SP), neurofibrillary tangles (NFT), and loss of selective neurons and synapses. With the aging of the gl...

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
IPC IPC(8): C07D225/02C07C229/16C07C237/06A61K47/48A61K31/19A61K31/665A61K31/216A61P25/28A61P25/16A61P3/10A61K47/54
Inventor 李艳梅吴为辉雷鹏苏小阳胡笳
Owner TSINGHUA UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com