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Multiple-arm polyethylene glycol with functional group at long chain end, its preparation method and uses

A technology of multi-arm polyethylene glycol and polyethylene glycol, which is applied in the field of multi-arm polyethylene glycol and its preparation, can solve problems such as difficulty in controlling the quality of conjugates, achieve high biological activity and reduce immune response Effects that occur and increase the chance of collision

Inactive Publication Date: 2007-07-11
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The third is that for proteins with multiple reaction sites, it is generally difficult to control the reaction site well, which makes it difficult to control the quality of the conjugate

Method used

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  • Multiple-arm polyethylene glycol with functional group at long chain end, its preparation method and uses
  • Multiple-arm polyethylene glycol with functional group at long chain end, its preparation method and uses
  • Multiple-arm polyethylene glycol with functional group at long chain end, its preparation method and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] mPEG with different arm lengths 3 -Lys-PEG-NH 2 Preparation (p-nitrophenol ester activation method)

[0034] Dissolve lysine (439 mg, 3 mmol) in 20 ml of water with a pH value of 8.0 to 8.3, and then add mPEG to it in batches within 3 hours 2 -Lys-CO 2 PhNO 2 (two-arm mPEG p-nitrophenol ester, molecular weight 10000, wherein one arm is 7000, the other arm is 3000, 10g, 1mmol), while maintaining the pH value of the system at 8.3 with 0.2mol / L NaOH. After stirring overnight at room temperature, the reactant was cooled to 0° C., and the pH value of the system was adjusted to 3 with 2 mol / L hydrochloric acid. Now use diethyl ether to extract impurities from water, and then use chloroform to continuously extract three times. After the extract is concentrated, it is added dropwise into anhydrous diethyl ether to obtain a white precipitate. 2 Mono-substituted lysine (mPEG 2 -mono-Lysine). The product was characterized by amino titration, GPC and MALDI, and its purity re...

Embodiment 2

[0038] mPEG with different arm lengths 3 -Lys-PEG-NH 2 Preparation (N-hydroxysuccinimide ester activation method)

[0039] It is enough to change the p-nitrophenol in the above-mentioned embodiment 1 into an equivalent amount of N-hydroxysuccinimide.

Embodiment 3

[0041] mPEG with different arm lengths 4 -Lys-PEG-NH 2 Preparation (p-nitrophenol ester activation method)

[0042] To be dissolved with the product mPEG described in embodiment 1 2 - Mono-Lysine (molecular weight 10000, 9g, 0.9mmol) in anhydrous dichloromethane (20mL), add triethylamine (TEA) until the pH value reaches 8. mPEG 2 CO 2 PhNO 2 (Molecular weight 10000, one arm is 6000, the other arm is 4000, 10.5g, 1.05mmol) was added to the reaction solution in batches within three hours, while maintaining the pH value of the system at about 8 with TEA. After reflux for 72 hours, the reactant was cooled to room temperature, concentrated, filtered, precipitated with ether, and then recrystallized with a small amount of ethanol. excess mPEG 2 -CO 2 PhNO 2 After being stirred overnight in a buffer solution with a pH value of 9-10, it is hydrolyzed, the solution is cooled to 0°C, and the pH value is adjusted to 3 with 2mol / L hydrochloric acid system. The p-nitrophenol in t...

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PUM

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Abstract

The invention discloses a new multiple-arm carbowax and making method and application in the macromolecular material technical domain, which is characterized by the following: possessing active functional group on one end of arm; fitting for decorating micromolecular drug, protein and peptide drug; modifying the solubility, stability and immunity of drug; lengthening the half-life of drug.

Description

technical field [0001] The invention belongs to the technical field of polymer materials, and in particular relates to a multi-arm polyethylene glycol with active functional groups at the end of the long chain, a preparation method thereof and an application in medicine preparation. Background technique [0002] At present, there are many kinds of antineoplastic drugs, which can be generally divided into two categories according to their molecular weight: one class has a lower molecular weight, usually below 1000, most of which are commonly used chemically synthesized drugs and some natural drugs, such as Nitrogen mustard, cisplatin, 5-fluorouracil, paclitaxel, etc. all belong to this category; the other category has a larger molecular weight, and most protein and polypeptide drugs produced by genetic engineering belong to the second category. However, both small molecule drugs and macromolecular drugs have disadvantages such as high toxicity, poor solubility, and short half...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48A61K47/48A61K47/60
Inventor 黄骏廉任勇徐学伟
Owner FUDAN UNIV
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