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Carbowax alcoholized ramification of TimopEntin, combination of medication and application

A PEGylation and polyethylene glycol technology, applied in the field of compounds, can solve problems such as the lack of thymopentin, and achieve the effects of novel chemical structure, good application prospects and stable biological activity

Inactive Publication Date: 2005-06-15
INST OF BASIC MEDICAL SCI ACAD OF MILITARY MEDICAL SCI OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Peptide drugs and protein drugs have many similarities in structure and properties. The research on pegylation modification of peptide drugs is later than that of protein drugs, and good results have been achieved so far. PEGylated peptide drugs have good application prospects, but there is no report of PEGylated thymopentin

Method used

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  • Carbowax alcoholized ramification of TimopEntin, combination of medication and application
  • Carbowax alcoholized ramification of TimopEntin, combination of medication and application
  • Carbowax alcoholized ramification of TimopEntin, combination of medication and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 mPEG 5000 -NHCOCH 2 CH 2 Synthesis of CO-TP5

[0045] Weigh mPEG 2000 -OH 40.0g (20mmol) was placed in a 250ml reaction bottle, and 100ml CH was added 2 Cl 2 , after the solid dissolves, add 15mlEt 3 N (100mmmol) and 19.0g Ts-Cl (100mmol) were reacted with stirring at room temperature. After TLC monitors that the reaction is complete, the solvent is removed by rotary evaporation, and 100ml of anhydrous ether is added to precipitate a solid to obtain 28.5gmPEG 2000 -OTs, yield 71%

[0046] 18.0gmPEG 2000 -OTs (9 mmol) was dissolved in 50 ml of DMF, 5.0 g (27 mmol) of phthalimide potassium salt was added, and reacted at 120° C. for 4 hours. The solvent was distilled off under reduced pressure, the residue was dissolved in 50ml of absolute ethanol, 13.5ml of hydrazine hydrate was added, and the mixture was refluxed for 4 hours. The solvent was removed by rotary evaporation and the residue was dissolved in CH 2 Cl 2 , Precipitate the solid wit...

Embodiment 2

[0050] Implementation of 2 mPEG 5000 -NHCOCH 2 CH 2 Synthesis of CO-TP5

[0051] Weigh mPEG 2000 -OH 50.0g (10mmol) was placed in a 250ml reaction bottle, and 50ml CH was added 2 Cl 2 , the solid dissolved and then added 7.5ml Et 3 N (50mmmol) and 9.5g Ts-Cl (50mmol), stirred at room temperature. After TLC monitors that the reaction is complete, the solvent is removed by rotary evaporation, and 100ml of anhydrous ether is added to precipitate a solid to obtain 33.5gmPEG 5000 -OTs, yield 67%

[0052] 30.0g mPEG 5000 -OTs (6mmol) was dissolved in 30ml of DME, 3.33g (18mmol) of phthalimide potassium salt was added, and reacted at 120°C for 4 hours. The solvent was distilled off under reduced pressure, the residue was dissolved in 50ml of absolute ethanol, 4.0ml of hydrazine hydrate was added, and the mixture was refluxed for 4 hours. The solvent was removed by rotary evaporation and the residue was dissolved in CH 2 Cl 2 , Precipitate the solid with anhydrous et...

Embodiment 3

[0056] Implementation of 3 Cys (mPEG 2000 Synthesis of -MAL)-TP5

[0057] 5.0gmPEG 2000 -NH 2 Dissolve in 10ml of dioxane, add 2.0g of maleic anhydride, stir and react at 80°C for 30min. The solvent was evaporated under reduced pressure, 50ml of anhydrous diethyl ether was added, the solid was precipitated by cooling, and the solid was collected by filtration and dried to obtain 4.9g. The obtained solid was dissolved in 15ml of acetic anhydride, 5.0g of sodium acetate was added, and the reaction was stirred at 100°C for 45min. Evaporate the solvent under reduced pressure, dissolve the residue with dichloromethane, filter off the insoluble matter, add an appropriate amount of activated carbon to the filtrate, let it stand for 30 minutes, filter out the activated carbon, concentrate the filtrate to dryness, add anhydrous ether, precipitate a solid, filter After collection and drying, light yellow solid 2.5gmPEG was obtained 2000 -MAL, yield 50%.

[0058] With 100mg ...

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Abstract

A polyglycolized derivative of thymopeptide-5, which can be used to prepaer the medicines for preventing and treating rheumatoid arthritis, allergic dermatisis, tumor, viral infection, and the diseases associated with immune deficiency and hypoimmunofunction, is disclosed. Said derivative features that the polyglycol, polyglycol modified amino acid, cysteine, maleamido glycol, vinyl glycol, or iodoacetylglycol is introduced or coupled to the N or C terminal of thymopeptide-5.

Description

technical field [0001] The present invention relates to a compound, in particular to a pegylated derivative of thymopentin, and also relates to a pharmaceutical composition and application thereof. Background technique [0002] Thymopoietin (Thymopoietin) is a polypeptide hormone containing 49 amino acid residues secreted by thymus epithelial cells. Thymopentin (TP5) is a 32-36 amino acid fragment of thymopoietin. TP5 is the active site of thymopoietin, and its function is the same as that of thymopoietin. It is an immune enhancer for T lymphocytes, which can promote the maturation and differentiation of T cells, and promote the secretion of various lymphokines by mature T cells. (such as interleukin-2 and γ-interferon, etc.), can also promote the production of interleukin-2 receptors. In animal models of impaired immune balance, TP5 has properties that balance it out. Whether the immune response is too high or too low, TP5 can achieve balance regulation, making it very pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61L15/44A61P17/00A61P19/02A61P29/00A61P31/12A61P35/00A61P37/02C07K7/06C07K17/08
Inventor 潘和平王良友邵宁生柳川高亚萍
Owner INST OF BASIC MEDICAL SCI ACAD OF MILITARY MEDICAL SCI OF PLA
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