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1. WO2021036654 - GRAPHENE ALKALI TARGETING DNA MAJOR GROOVE AND INHIBITING TOPOISOMERASE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

Publication Number WO/2021/036654
Publication Date 04.03.2021
International Application No. PCT/CN2020/105360
International Filing Date 29.07.2020
IPC
A61K 33/44 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
33Medicinal preparations containing inorganic active ingredients
44Elemental carbon, e.g. charcoal, carbon black
A61K 47/55 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
55the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
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
B82Y 30/00 2011.01
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE  OR TREATMENT OF NANOSTRUCTURES
30Nanotechnology for materials or surface science, e.g. nanocomposites
CPC
A61K 33/44
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
33Medicinal preparations containing inorganic active ingredients
44Elemental carbon, e.g. charcoal, carbon black
A61K 47/55
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
55the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
B82Y 20/00
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
20Nanooptics, e.g. quantum optics or photonic crystals
B82Y 30/00
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
30Nanotechnology for materials or surface science, e.g. nanocomposites
Applicants
  • 上海大学 SHANGHAI UNIVERSITY [CN]/[CN]
Inventors
  • 潘登余 PAN, Dengyu
  • 耿弼江 GENG, Bijiang
Agents
  • 上海宛林专利代理事务所(普通合伙) SHANGHAI WANLIN PATENT AGENCY (GENERAL PARTNERSHIP)
Priority Data
201910809745.529.08.2019CN
202010638282.306.07.2020CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) GRAPHENE ALKALI TARGETING DNA MAJOR GROOVE AND INHIBITING TOPOISOMERASE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
(FR) ALCALI DE GRAPHÈNE CIBLANT UNE RAINURE PRINCIPALE D'ADN ET INHIBANT LA TOPOISOMÉRASE, PROCÉDÉ DE PRÉPARATION S'Y RAPPORTANT ET APPLICATION ASSOCIÉE
(ZH) 靶向DNA大沟并抑制拓扑异构酶的石墨烯碱及其制法和用途
Abstract
(EN)
Disclosed are a graphene alkali that targets a DNA major groove and that inhibits topoisomerase, a preparation method therefor and an application thereof. The graphene alkali that targets a DNA major groove and that inhibits topoisomerase serves as an anticancer active ingredient and comprises a graphene skeleton of only several nano sizes and having a planar structure, and nitrogen heterocyclic clusters located around the graphene skeleton. The graphene alkali containing bioactive nanoparticles is simple in structure and easy to synthesize, has a precise targeting function on a nuclear DNA major groove and also has efficient inhibitory activity on topoisomerase I and topoisomerase II. Particularly in the situation in which no small-molecule drug component is contained and no grafted special targeting molecule is contained, the nanoparticles may show higher anticancer activity than chemotherapy drugs.
(FR)
L'invention concerne un alcali de graphène qui cible une rainure principale d'ADN et qui inhibe la topoisomérase, un procédé de préparation s'y rapportant et une application associée. L'alcali de graphène qui cible une rainure principale d'ADN et qui inhibe la topoisomérase sert de principe actif anticancéreux et comprend un squelette de graphène de seulement quelques nano-tailles et comportant une structure plane, et des groupes hétérocycliques d'azote situés autour du squelette de graphène. L'alcali de graphène contenant des nanoparticules bioactives présente une structure simple et est facile à synthétiser, possède une fonction de ciblage précise sur une rainure principale d'ADN nucléaire et possède également une activité inhibitrice efficace sur la topoisomérase I et la topoisomérase II. En particulier en cas d'absence d'un constituant de médicament à petite molécule et d'absence d'une molécule de ciblage spéciale greffée, les nanoparticules peuvent démontrer une activité anticancéreuse plus élevée que les médicaments de chimiothérapie.
(ZH)
公开了一种靶向DNA大沟并抑制拓扑异构酶的石墨烯碱及其制法和用途,所述靶向DNA大沟并抑制拓扑异构酶的石墨烯碱作为抗癌活性成分,其包括仅几个纳米尺寸、具有平面结构的石墨烯骨架和位于所述石墨烯骨架周围的氮杂环簇。该生物活性纳米粒子的石墨烯碱,结构简单、易于合成,其不仅拥有对核DNA大沟的精准靶向功能,而且具有对拓扑异构酶I和II的高效抑制活性,尤其是在不含小分子药物成分且不含嫁接的特殊靶向分子的情况下纳米粒子本身就能显示高于化疗药物的抗癌活性。
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