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Self-assembled diblock copolymers composed of pegmema and drug bearing polymeric segments

A technology of block copolymers and polymers, used in anticancer agents for cancer treatment, 3] In order to solve the above problems, in the field of treatment of diseases, it can solve problems such as unclear structures and unexpected biological interactions

Pending Publication Date: 2019-07-05
RS研究教育咨询医学工业贸易股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This protocol does not fully couple the drug to the polymer backbone due to steric hindrance, which leads to ambiguity in the final structure
Furthermore, the reactive groups remaining on the polymer backbone due to incomplete coupling may be the most important disadvantage of this post-polymerization coupling strategy, as there may be undesired biological interactions in vivo

Method used

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  • Self-assembled diblock copolymers composed of pegmema and drug bearing polymeric segments
  • Self-assembled diblock copolymers composed of pegmema and drug bearing polymeric segments
  • Self-assembled diblock copolymers composed of pegmema and drug bearing polymeric segments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1A

[0222] Example 1A: Synthesis of polymerizable Compretin-A4 monomer (CombMA)

[0223] In the case of N2, compretidine-A4 (300mg, 0.95mmol), triethylamine (TEA, 191mg, 1.89mmol), methacryloyl chloride (198mg, 1.89mmol) were dissolved in a 25mL round bottom flask Dry in dichloromethane (DCM, 10 mL). The reaction was stirred at room temperature for 16 hours. Use saturated NaHCO 3 (20mL x 2) and distilled water (20mL x 2) to extract the crude product. Na for organic layer 2 SO 4 Drying is performed and the solvent is evaporated. CombMA monomer was purified using column chromatography on silica with hexane.

Embodiment 1B

[0224] Example 1B: Preparation of Chain Transfer Agents (CTAs) with Reactive Functional Groups

[0225] 4-cyanopentanoic acid dithiovalerate (CPDB) is the CTA, and this CTA is modified with N-hydroxysuccinimide (NHS) according to the following procedure, NHS being the reactive functional group;

[0226] Briefly, CPADB (200 mg, 0.72 mmol) and N-hydroxysuccinimide (125 mg, 1.07 mmol) were dissolved in anhydrous DCM (4 mL). Dicyclohexylcarbodiimide (DCC) (177 mg, 0.86 mmol) was dissolved in anhydrous DCM (1 mL). The two solution mixtures were then combined, and the reaction mixture was stirred at room temperature in the dark for 16 hours. The insoluble white by-product dicyclohexylurea (DCU) was removed by filtration. The obtained solution was dried under vacuum and the crude product was purified by column chromatography on silica with hexane and EtOAC.

Embodiment 1C

[0227] Example 1C: Synthesis of POEGMEMA and NHS-POEGMEMA Homopolymers

[0228] Reversible addition-fragmentation chain transfer (RAFT) was used to synthesize POEGMEMA and NHS-activated POEGMEMA (NHS-POEGMEMA) homopolymers. To synthesize POEGMEMA polymer, to a solution of OEGMA (600 mg, 2.0 mmol) and CPADB (20.12 mg, 0.072 mmol) in DMF (3 mL) was added AIBN (1.31 mg, 0.008 mmol). use N 2 Sweep the mixture to remove O 2 and polymerized with stirring at 70°C. Polymerization was stopped by cooling and air exposure. POEGMEMA polymer was purified by precipitation in diethyl ether. The polymer precipitate was dried under vacuum to afford about 350 EGMEMA repeating units (460 mg, 77% yield). NHS-POEGMEMA polymer was synthesized using the same procedure using SCPDB (27.10 mg, 0.072 mmol) as a chain transfer agent to provide approximately 35 OEGMEMA repeating units (480 mg, 80% yield).

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Abstract

The invention relates to polymer drug conjugates according to formula I, and their use for treatment of diseases such as cancer.

Description

[0001] The present invention relates to polymer drug conjugates of formula I, components consisting of polymer drug conjugates of formula I, methods for preparing the drug-polymer conjugates and components, and their use in the treatment of diseases (such as cancer). Background technique [0002] Chemotherapeutic agents used to treat cancer are mostly cytotoxic. In addition to the targeted area, these agents may accumulate in body tissues, which in turn leads to reduced therapeutic benefit and undesired distribution of the drug throughout healthy body tissues. The uncontrolled distribution of these agents throughout the body causes serious side effects for patients. [0003] To address the above problems, drug delivery systems that can deliver drugs to targeted areas of the body have been developed. For example, in some cancer treatments, these systems exploit enhanced permeability and retention (EPR), which means that drug carriers with high molecular weight and large hydro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/58A61K47/60A61P35/00C08F220/28
CPCC08F293/005A61K47/6835A61K47/64A61K47/58A61K47/60A61K31/7068A61K31/09A61K31/513A61P35/00C08F2438/01C08F2438/03C08F220/286A61K47/6907A61K47/65A61K47/6883A61K47/6929A61K31/704C08F8/00A61K47/6889
Inventor R·桑雅尔A·桑雅尔S·卡加
Owner RS研究教育咨询医学工业贸易股份有限公司
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