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1. WO2021043231 - DUAL-TARGETING MATERIAL AND USE THEREOF IN DRUG DELIVERY

Publication Number WO/2021/043231
Publication Date 11.03.2021
International Application No. PCT/CN2020/113360
International Filing Date 04.09.2020
IPC
A61K 47/34 2017.01
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
A61K 47/54 2017.01
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
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
B82Y 5/00 2011.01
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE  OR TREATMENT OF NANOSTRUCTURES
5Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
C08G 65/333 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
65Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
02from cyclic ethers by opening of the heterocyclic ring
32Polymers modified by chemical after-treatment
329with organic compounds
333containing nitrogen
C08G 65/332 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
65Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
02from cyclic ethers by opening of the heterocyclic ring
32Polymers modified by chemical after-treatment
329with organic compounds
331containing oxygen
332containing carboxyl groups, or halides or esters thereof
CPC
A61K 47/34
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
A61K 47/542
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
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
542Carboxylic acids, e.g. a fatty acid or an amino acid
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
B82Y 5/00
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
5Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
C08G 65/3322
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
65Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
02from cyclic ethers by opening of the heterocyclic ring
32Polymers modified by chemical after-treatment
329with organic compounds
331containing oxygen
332containing carboxyl groups, or halides, or esters thereof
3322acyclic
C08G 65/33313
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
65Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
02from cyclic ethers by opening of the heterocyclic ring
32Polymers modified by chemical after-treatment
329with organic compounds
333containing nitrogen
33303containing amino group
3331cyclic
33313aromatic
Applicants
  • 沈阳药科大学 SHENYANG PHARMACEUTICAL UNIVERSITY [CN]/[CN]
Inventors
  • 王永军 WANG, Yongjun
  • 王振杰 WANG, Zhenjie
  • 何仲贵 HE, Zhonggui
  • 刘洪卓 LIU, Hongzhuo
  • 孙进 SUN, Jin
Agents
  • 沈阳飞扬灵睿知识产权代理事务所(普通合伙) SHENYANG FEIYANG LINGRUI INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP)
Priority Data
201910840463.106.09.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) DUAL-TARGETING MATERIAL AND USE THEREOF IN DRUG DELIVERY
(FR) MATÉRIAU À DOUBLE CIBLAGE ET SON UTILISATION DANS L'ADMINISTRATION DE MÉDICAMENT
(ZH) 一种双靶向材料及其在药物传递中的应用
Abstract
(EN)
A novel amphiphilic dual-targeting functional material belonging to the field of new auxiliary materials and new dosage forms of drug preparations, and the use thereof as a targeting material in an active targeting drug delivery system. The structural general formula of the amphiphilic targeting material is as follows: wherein A and Linker are as claimed in the claims and the description. The amphiphilic targeting material uses tyrosine as a target head, and after chemical modification, the targeting material can self-assemble to form micelles or can also be modified to the surface of a liposome or a nanoparticle, and is used as a carrier for targeted delivery of anti-tumour drugs. The material can simultaneously interact with large and medium-sized amino acid transporter 1 (LAT1) and amino acid transporter ATB0,+ expressed on tumour cell membranes by means of surface-modified tyrosine, thereby effectively improving the cellular uptake and anti-tumour activity of the nano-preparation.
(FR)
L'invention concerne un nouveau matériau fonctionnel amphiphile à double ciblage appartenant au domaine des nouveaux matériaux auxiliaires et des nouvelles formes posologiques de préparations médicamenteuses, et son utilisation en tant que matériau de ciblage dans un système d'administration de médicament à ciblage actif. La formule générale structurelle du matériau de ciblage amphiphile est la suivante : A et le lieur étant tels que revendiqués dans les revendications et la description. Le matériau de ciblage amphiphile utilise la tyrosine en tant que tête de ciblage, et après modification chimique, le matériau de ciblage peut s'autoassembler pour former des micelles ou peut également être modifié à la surface d'un liposome ou d'une nanoparticule, et est utilisé en tant que support pour l'administration ciblée de médicaments antitumoraux. Le matériau peut simultanément interagir avec un transporteur d'acide aminé 1 de grande taille et de taille moyenne (LAT1) et un transporteur d'acide aminé ATB0,+ exprimé sur des membranes de cellules tumorales au moyen d'une tyrosine modifiée en surface, ce qui permet d'améliorer efficacement l'absorption cellulaire et l'activité antitumorale de la nanopréparation.
(ZH)
一种属于药物制剂新辅料和新剂型领域的新型两亲性双靶向功能材料,及其作为靶向材料在主动靶向药物传递系统中的应用。所述的两亲性靶向材料的结构通式如下:其中,A,Linker如权利要求和说明书所述。所述的两亲性靶向材料以酪氨酸为靶头,经化学修饰后,该靶向材料可以自组装形成胶束也可以修饰到脂质体、纳米粒表面,作为抗肿瘤药物靶向传递的载体。该材料通过表面修饰的酪氨酸能同时与肿瘤细胞膜上高表达的大中型氨基酸转运体1(LAT1)和氨基酸转运体ATB 0,+相互作用,有效提高纳米制剂的细胞摄取和抗肿瘤活性。
Also published as
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