Multi-branched polymeric prodrugs and their applications

A multi-branched and drug-based technology, applied in the field of medicine, can solve problems such as changes

Active Publication Date: 2018-07-10
JIANGSU HANSOH PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, protein-based compounds include mixtures of isomers, where and how many polymer chains bind to a particular protein often vary, leading to reproducibility issues when preparing these components

Method used

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  • Multi-branched polymeric prodrugs and their applications
  • Multi-branched polymeric prodrugs and their applications
  • Multi-branched polymeric prodrugs and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0189] step one:

[0190]

[0191] Add compound 2-1 (5g, 0.026mol, 1.0 equivalent), iron powder (4.30g, 0.078mol, 3.0 equivalent), ammonium chloride (6.96g, 0.13mol, 5.0 equivalent), water (150mL ) and methanol (50mL), N 2 Reflux for 2 hours under protection. LC-MS monitored the complete conversion of raw materials, stopped the reaction, cooled to room temperature, filtered, washed the filter cake with ethyl acetate, separated the liquid, extracted the aqueous phase with ethyl acetate (30mL×5), combined the organic phases, and used anhydrous Dried over sodium sulfate, filtered, and spin-dried, the crude product was separated by column chromatography (petroleum ether: ethyl acetate: 5:1). 2.0 g, yellow solid, yield 50%.

[0192] ESI:m / e + :166[M+H + ].

[0193] Step two:

[0194]

[0195] Add compound 1-1 (0.15g, 0.57mmol, 1.0eq) and acetic acid (4mL) into a 25mL single-necked flask, heat to 80°C under nitrogen protection, and drop compound 2-2 (0.122g, 0.74mmol, ...

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Abstract

The present invention relates to multi-branched polymeric prodrugs and applications thereof. Specifically, the present invention relates to a multi-branched polymeric prodrug having a structure of formula (I) or a pharmaceutically acceptable salt thereof, which is effective for topoisomerase I-related diseases in mammalian subjects, In particular, solid tumors in mammalian subjects have very good therapeutic effects. In the case of the same in vitro activity as inhibiting the proliferation of cancer cells, it has a more reasonable half-life and residence time of the drug in the body, greatly reduces the clearance rate, is more conducive to determining the way of drug administration, and reduces the number of administrations. It is expected to be developed into a new drug. A generation of antineoplastic drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a novel multi-branched polymer drug prodrug or a pharmaceutically acceptable salt thereof and application thereof. Background technique [0002] Camptothecin (CPT) is a cytotoxic alkaloid extracted from Camptotheca acuminata in 1966. It has obvious anti-tumor activity, especially for digestive tract tumors, leukemia, bladder cancer, etc. Stronger, and later found that camptothecin and its derivatives can inhibit topoisomerases necessary for DNA rotation and relaxation in molecular activities such as replication and transcription. Camptothecin stabilizes and forms a reversible enzyme-camptothecin-DNA ternary compound, i.e. the formation of this cleavable compound prevents the recombination step during the split / combination cycle of the topoisomerase reaction, whereas prior art Topoisomerase I inhibitors have been reported to be effective in the treatment of HIV. However, its ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/48A61K47/60A61K31/4745A61P35/00
Inventor 钟慧娟喻红平赵志明黄志强徐耀昌
Owner JIANGSU HANSOH PHARMA CO LTD
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