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Polypeptide compound with aza-containing heterocyclic modified and its application

A technology for polypeptides and compounds, applied to polypeptide compounds and their application fields, can solve problems such as damage, failure to prevent the occurrence and development of diseases, and unclearness

Inactive Publication Date: 2007-07-18
TSINGHUA UNIV
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  • 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

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  • Polypeptide compound with aza-containing heterocyclic modified and its application
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  • Polypeptide compound with aza-containing heterocyclic modified and its application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1, the preparation of polypeptide compound

[0034] Synthesizing the polypeptide compound of the present invention (molecular formula sees formula IV), comprises the following steps:

[0035] a. Synthesize the monomer [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecyl-1-yl] acetic acid containing Cyclen, the method is: with Cyclen (purchased Acros company in the United States) as raw material, 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-tetraaze 3Boc-Cyelen (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 Chemicai 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, Pr...

Embodiment 2

[0042] Embodiment 2, the preparation of polypeptide compound

[0043] Synthesizing the polypeptide compound of the present invention (molecular formula sees formula V), comprises the following steps:

[0044] a. Amino acids (phenylalanine, phenylalanine, valine, leucine, lysine, glycine) were linked to Wang resin one by one by the same method as in Example 1.

[0045] b. Combine the monomer containing Cyclen [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecyl-1-yl]acetic acid with the Wang-containing resin obtained in step a The small peptides are connected, and the connection conditions are in the presence of coupling agents HBTU and HOBt (mixing ratio: 4 times the amount of monomers containing Cyclen, 1 times the amount of small peptides containing Wang resin, 4 times the amount of coupling agents HBTU and 4 times Amount of HOBt) was reacted at room temperature for 3 hours to obtain the target product.

[0046] c. Use the cleavage reagent trifluoroacetic acid (TF...

Embodiment 3

[0050] Embodiment 3, the preparation of polypeptide compound

[0051] Synthetic polypeptide compound of the present invention (molecular formula sees formula VI), comprises the following steps:

[0052] a. Link amino acids (aspartic acid, phenylalanine, valine, leucine) to Wang resin one by one.

[0053] b. Combine the monomer containing Cyclen [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecyl-1-yl]acetic acid with the Wang-containing resin obtained in step a The small peptides are connected, and the connection conditions are in the presence of coupling agents HBTU and HOBt (mixing ratio: 4 times the amount of monomers containing Cyclen, 1 times the amount of small peptides containing Wang resin, 4 times the amount of coupling agents HBTU and 4 times Amount of HOBt) was reacted at room temperature for 3 hours to obtain the target product.

[0054] c. Using the cleavage reagent trifluoroacetic acid (TFA) used in the synthesis of the polypeptide to separate the pol...

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Abstract

The present invention discloses one kind of nitrogen heterocycle modified polypeptide compound and its application in preparing medicine for preventing and treating Alzheimerdis, Parkinson's disease and other degenerative nerve system diseases and medicine for preventing and treating type II diabetes. Research shows that the nitrogen heterocycle modified polypeptide compound can inhibit Abeta aggregation, disaggregate Abeta, hydrolyze to eliminate Abeta protein and inhibit and eliminate Abeta toxicity, and possesses wide application foreground in pharmaceutical field.

Description

technical field [0001] The present invention relates to polypeptide compounds and applications thereof, in particular to polypeptide compounds modified with nitrogen-containing heterocycles and their use in the preparation of drugs for the treatment and prevention of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and type 2 diabetes in the application. Background technique [0002] Neurodegenerative diseases 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, clinically manifested as cognitive impairment, memory loss, and eventually loss of thinking ability, movement disorders, and life. Can not take care of themselves. The pathological features are mainly senile plaque (SP), neurofibrillary tangles (neurofibrillary tangles, NFT) and selective loss of neurons an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K47/48A61K38/08A61P25/28A61P3/10A61K47/58
Inventor 李艳梅吴为辉雷鹏苏小阳胡笳
Owner TSINGHUA UNIV
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