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New compound containing anthracycline structure as well as preparation method and application of new compound containing anthracycline structure

An anthracycline and compound technology, which is applied in the fields of new compounds containing anthracycline drug structures and the fields of preparation and use

Inactive Publication Date: 2014-10-29
张雅珍
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no definite report on the application of anthracycline antibiotics in retinal vein occlusion, and there is no report on the new polymer of the present invention. The final product prepared by this patent is far more effective than other drug treatments when used for the treatment of eye diseases

Method used

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  • New compound containing anthracycline structure as well as preparation method and application of new compound containing anthracycline structure
  • New compound containing anthracycline structure as well as preparation method and application of new compound containing anthracycline structure
  • New compound containing anthracycline structure as well as preparation method and application of new compound containing anthracycline structure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] 1) A mixture of 2 g of sebacic acid in 25 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0049] 2) 5 g of compound A, 60 mg of compound B, 200 mg of dicyclohexylcarbodiimide and 10 mg of pyridine were mixed with 30 ml of dichloromethane, stirred at room temperature overnight; then washed with ether and dried under vacuum to obtain a polymer;

[0050] 3) Mix the products of step 1) and step 2) into a flask, and react at 150°C for 1 hour; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried;

[0051]4) Put doxorubicin and the polymer of step 3) into a solution mixed with 10ml of dichloromethane and 6ml of dimethyl sulfoxide; then put it in an oven for 2 hours; minutes; the product was put into 5% cholic acid solution and stirred at 400 rpm for 2 hours; it was collected by centrifugation and freeze-dried to obtain the final product.

Embodiment 2

[0053] 1. Mix 2.5g of compound A, 47mg of compound B, 200mg of dicyclohexylcarbodiimide and 8mg of pyridine, add 20ml of dichloromethane, and stir overnight at room temperature;

[0054] It was then washed with ether and dried under vacuum;

[0055] 2. Mix 1 g of acetyl-sebacic acid (commercially available) and the product of step 1 into a flask, and react at 120°C for 1.5 hours; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried to obtain a polymer thing;

[0056] 3 Put pirarubicin and the polymer into a solution mixed with 5ml of methanol and 5ml of dichloromethane; then put it in an oven for 4 hours; at minus 10-20 degrees, ultrasonic for 20 minutes; put the product in 3% Stir in the cholic acid solution at 400 rpm for 2 hours; collect by centrifugation and freeze-dry to obtain the final product.

Embodiment 3

[0058] 1 The mixture of 2 g of sebacic acid in 20 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0059] 2 2.5 g of compound A, 42 mg of compound B, 150 mg of dicyclohexylcarbodiimide and tetrahydrofuran were mixed with 15 ml of chloroform, stirred at room temperature overnight; then washed with ether and dried under vacuum to obtain a polymer;

[0060] 3 Mix the products of step 1 and step 2 into a flask, and react at 150°C for 1 hour; when the polymer is cooled to room temperature, dissolve it with chloroform, wash with petroleum ether and dry;

[0061] 4 Put arubicin and the polymer in step 3 into a solution mixed with 10ml of dichloromethane and 6ml of dimethyl sulfoxide; then put it in an oven for 8 hours; at minus 20-30 degrees, ultrasonic for 20 minutes The product was put into 5% cholic acid solution and stirred at 400 rpm for 2 hours; it was collected by centrifugation and freeze-dried to obtain the final product.

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Abstract

The invention discloses a new compound containing an anthracycline structure as well as a preparation method and application of the new compound containing the anthracycline structure. The anthracycline antibiotic, namely the new compound containing the anthracycline structure, is coupled with non-linear multi-segmented copolymer and has better effect in treatment of a retina vein occlusion disease compared with medicines or medicaments in other forms.

Description

technical field [0001] The invention discloses a new compound containing an anthracycline antibiotic drug structure, a preparation method and an application of the compound. Background technique [0002] Anthracyclines are antimitotic and extremely cytotoxic drugs. Anthracyclines can successfully inhibit a variety of malignancies, including acute leukemia, lymphoma, soft tissue and osteosarcoma, childhood malignancies, and adult solid tumors. Its mechanism of action is that the drug can penetrate into the cell and bind to the chromosome. The planar loop in the drug structure is inserted between the base pairs to form a complex with DNA, which seriously interferes with DNA synthesis, RNA synthesis and protein synthesis. In addition, anthracycline antibiotics are also related to the redox effect, and can participate in the reaction to obtain cytotoxic compounds, such as peroxides, active hydroxyl groups and hydrogen peroxide. At present, the pharmacodynamic effects of anthr...

Claims

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Application Information

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IPC IPC(8): C08G67/04C08G65/00A61K47/48A61K31/704A61K31/7048A61P9/10A61P27/02
Inventor 张雅珍李铁力白毅
Owner 张雅珍
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