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1. WO2022001957 - PH-RESPONSIVE MEMBRANE-RUPTURING POLYMER MATERIAL, PREPARATION METHOD THEREFOR, AND USE THEREOF

Publication Number WO/2022/001957
Publication Date 06.01.2022
International Application No. PCT/CN2021/102758
International Filing Date 28.06.2021
IPC
A61K 31/785 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
74Synthetic polymeric materials
785Polymers containing nitrogen
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C08F 220/34 2006.1
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
220Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide, or nitrile thereof
02Monocarboxylic acids having less than ten carbon atoms; Derivatives thereof
10Esters
34Esters containing nitrogen
C08F 2/38 2006.1
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
2Processes of polymerisation
38Polymerisation using regulators, e.g. chain terminating agents
A61K 47/34 2017.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
Applicants
  • 华南理工大学 SOUTH CHINA UNIVERSITY OF TECHNOLOGY [CN]/[CN]
  • 中山大学孙逸仙纪念医院 SUN YAT-SEN MEMORIAL HOSPITAL , SUN YAT-SEN UNIVERSITY [CN]/[CN]
Inventors
  • 熊梦华 XIONG, Menghua
  • 鲍燕 BAO, Yan
  • 黄良琪 HUANG, Liangqi
  • 王晓川 WANG, Xiaochuan
  • 刘明冬 LIU, Mingdong
  • 梁阳彬 LIANG, Yangbin
  • 王均 WANG, Jun
Agents
  • 广州广典知识产权代理事务所(普通合伙) GUANGZHOU PRIME IP LAW OFFICE
Priority Data
202010611437.430.06.2020CN
202011633559.X31.12.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PH-RESPONSIVE MEMBRANE-RUPTURING POLYMER MATERIAL, PREPARATION METHOD THEREFOR, AND USE THEREOF
(FR) MATÉRIAU POLYMÈRE À RUPTURE DE MEMBRANE SENSIBLE AU PH, SON PROCÉDÉ DE PRÉPARATION ASSOCIÉ ET SON UTILISATION
(ZH) pH响应性破膜高分子材料及其制备方法与应用
Abstract
(EN) Provided in the present invention are a pH-responsive membrane-rupturing polymer material, a preparation method therefor, and the use thereof. The pH-responsive membrane-rupturing polymer material has a structure as represented by formula (I). The polymer material is hydrophobic and electrically neutral at a normal physiological pH, can be self-assembled into nanoparticles with PEG as a shell layer, and has weak interaction with a cell membrane; and when the pH is reduced, the polymer material can be protonized to form an amphiphilic structure consisting of a hydrophobic domain and a cationic domain, which has strong interaction with the cell membrane and has a strong membrane-rupturing activity, thereby killing tumor cells or bacteria with a high efficiency and a high selectivity.
(FR) La présente invention concerne un matériau polymère à rupture de membrane sensible au pH, un procédé de préparation de celui-ci et l’utilisation de celui-ci. Le matériau polymère à rupture de membrane sensible au pH a une structure telle que représentée par la formule (I) : Le matériau polymère est hydrophobe et électriquement neutre à un pH physiologique normal, peut être autoassemblé en nanoparticules avec du PEG sous la forme d’une couche d’enveloppe, et présente une interaction faible avec une membrane cellulaire ; et lorsque le pH est réduit, le matériau polymère peut être protoné pour former une structure amphiphile constituée d’un domaine hydrophobe et d’un domaine cationique, qui présente une forte interaction avec la membrane cellulaire et présente une forte activité de rupture de membrane, de façon à tuer des cellules tumorales ou des bactéries avec une efficacité élevée et une sélectivité élevée.
(ZH) 本发明提供了一种pH响应性破膜高分子材料及其制备方法与应用。该pH响应性破膜高分子材料具有式(I)所示结构。该高分子材料在正常生理pH下,呈疏水电中性,可自组装成PEG为壳层的纳米颗粒,与细胞膜的相互作用弱;当pH降低,可以质子化,形成疏水结构域和阳离子结构域组成的两亲性结构,与细胞膜具有强相互作用并且具有强破膜活性,因而可以高效、高选择性杀伤肿瘤细胞或细菌。
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