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Polyethylene glycol modified nemifitide and preparation method

A technology of nanopeptide and polyethylene glycol, which is applied in the field of peptide or protein modification and its preparation, can solve the problems of unstable physical and chemical properties and reduced bioavailability, achieve single product, long half-life, and improve biological The effect of utilization

Inactive Publication Date: 2009-11-04
NANJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, nanopeptides are protein polypeptide drugs, which are easily hydrolyzed by proteases in the body, resulting in unstable physical and chemical properties and reduced bioavailability

Method used

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  • Polyethylene glycol modified nemifitide and preparation method
  • Polyethylene glycol modified nemifitide and preparation method
  • Polyethylene glycol modified nemifitide and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Preparation method of PEG-modified nano-non-peptide complexes. In this example, the PEG is mPEG-CH 2 CHO, with a molecular weight of 2KD.

[0043] In the first step, the nano-non-peptide precursor was prepared with 0.1 mmol of Rink Amide MBHA resin;

[0044] In the second step, 0.1 mmol of mPEG-CH with a molecular weight of 2KD 2 CHO was dissolved in 150 mmol pH 6 DMF solution, the nano-non-peptide precursor prepared in the first step was added, mixed to form a reaction mixture, and the reaction was carried out at 20 °C for 6 h;

[0045] In the third step, 0.1 mmol of sodium triacetoxyborohydride was slowly added to the reaction system of the second step, and the reaction was continued for 6 h;

[0046]After the fourth step, the PEG-coupled resin was repeatedly washed with methanol to remove unreacted sodium triacetoxyborohydride and mPEG-CH3CHO, etc., and the resin and amino acid side chain protecting groups were cleaved, precipitated with glacial ether, and frozen....

Embodiment 2

[0049] Preparation method of PEG-modified nano-non-peptide complexes. In this example, the PEG is mPEG-CH 2 CHO, with a molecular weight of 2KD.

[0050] The first step is to prepare the nano-non-peptide precursor with 0.1 mmol of RinkAmide MBHA resin;

[0051] In the second step, 0.1 mmol of mPEG-CH with a molecular weight of 2KD 2 CHO was dissolved in 150 mmol pH 6 DMF solution, the nano-non-peptide precursor prepared in the first step was added, mixed to form a reaction mixture, and the reaction was carried out at 60 °C for 6 h;

[0052] In the third step, 0.1 mmol of sodium triacetoxyborohydride was slowly added to the reaction system of the second step, and the reaction was continued for 18 h;

[0053] After the fourth step, the PEG-coupled resin was repeatedly washed with methanol to remove unreacted sodium triacetoxyborohydride and mPEG-CH3CHO, etc., and the resin and amino acid side chain protecting groups were cleaved, precipitated with glacial ether, and frozen. ...

Embodiment 3

[0056] Preparation method of PEG-modified nano-non-peptide complexes. In this example, the PEG is mPEG-CH 2 CHO, with a molecular weight of 2KD.

[0057] The first step is to prepare the nano-non-peptide precursor with 0.1 mmol of RinkAmide MBHA resin;

[0058] In the second step, 0.1 mmol of mPEG-CH with a molecular weight of 2KD 2 CHO was dissolved in 150 mmol pH 6 DMF solution, the nano-non-peptide precursor prepared in the first step was added, mixed to form a reaction mixture, and the reaction was carried out at 90 °C for 6 h;

[0059] In the third step, 0.1 mmol of sodium triacetoxyborohydride was slowly added to the second step reaction system, and the reaction was continued for 30h;

[0060] After the fourth step, the PEG-coupled resin was repeatedly washed with methanol to remove unreacted sodium triacetoxyborohydride and mPEG-CH3CHO, etc., and the resin and amino acid side chain protecting groups were cleaved, precipitated with glacial ether, and frozen. After dr...

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Abstract

The invention discloses a monomethoxypolyethylene glycol derivative modified nemifitide compound and a preparation method thereof, which belong to the technical field of modification and preparation of peptides or proteins. The compound consists of nemifitide and a monomethoxypolyethylene glycol derivative, wherein the nemifitide and the monomethoxypolyethylene glycol derivative are linked by amido bonds formed by the bonding of free amino in the nemifitide and active ethyl aldehyde in the monomethoxypolyethylene glycol derivative. The molecular weight of the compound is between 2.7 and 10.7 KD. The free amino is terminal alpha-NH2 in the nemifitide and the active group is ethyl aldehyde in m PEG-CH2CHO. A free amino-containing nemifitide and resin compound precursor prepared by a solid phase synthesis method and the ethyl aldehyde-containing the m PEG-CH2CHO undergo a modification reaction to form a coarse product of a m PEG modified nemifitide and resin compound; and a pure product of the m PEG modified nemifitide and resin compound can be obtained by washing, cutting, precipitation by glacial aether, ultrafilter concentration and freeze drying.

Description

technical field [0001] The present invention relates to a polyethylene glycol-modified nano-non-peptide and a preparation method thereof, to be precise, to a monomethoxy polyethylene glycol derivative, namely an mPEG-modified nano-non-pentapeptide complex and its preparation The method belongs to the technical field of peptide or protein modification and preparation thereof. Background technique [0002] Unipolar depression is a common mental disorder caused by chemical changes in the central nervous system and is classified as endogenous depression. The use of antidepressants to treat unipolar depression is well established in the medical community. Nemifitide is a synthetic pentapeptide compound with a structure of 4-fluoro-L-phenylalanyl-(trans) 4-OH-L-prolyl-L-arginyl- Glycyl-L-tryptophanamide, which is effective in treating depression. At present, the US Tetragenex pharmaceuticals (formerly Innapharma) is conducting Phase III clinical trials of the drug, and its anti...

Claims

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Application Information

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IPC IPC(8): C07K17/08A61K38/08A61K47/48A61P25/24A61K47/60
Inventor 韦萍朱颐申蒋正新王亚利
Owner NANJING UNIV OF TECH
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