CN112996533B - 基于聚合物的大分子前药 - Google Patents

基于聚合物的大分子前药 Download PDF

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Publication number
CN112996533B
CN112996533B CN201980060783.3A CN201980060783A CN112996533B CN 112996533 B CN112996533 B CN 112996533B CN 201980060783 A CN201980060783 A CN 201980060783A CN 112996533 B CN112996533 B CN 112996533B
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peg
tumor
prodrug
polymer
treatment
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Chinese (zh)
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CN112996533A (zh
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M·乔尔内
I·阿尔费里夫
G·M·布罗德
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Childrens Hospital of Philadelphia CHOP
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Childrens Hospital of Philadelphia CHOP
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
CN201980060783.3A 2018-09-17 2019-09-17 基于聚合物的大分子前药 Active CN112996533B (zh)

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CN202510008384.XA CN119950749A (zh) 2018-09-17 2019-09-17 基于聚合物的大分子前药

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862732199P 2018-09-17 2018-09-17
US62/732,199 2018-09-17
PCT/US2019/051457 WO2020061007A1 (en) 2018-09-17 2019-09-17 Polymer-based macromolecular prodrugs

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CN112996533B true CN112996533B (zh) 2025-01-10

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US (4) US11253603B2 (https=)
EP (1) EP3852793B1 (https=)
JP (1) JP7546552B2 (https=)
KR (1) KR20210072002A (https=)
CN (2) CN112996533B (https=)
AU (1) AU2019344783B2 (https=)
CA (1) CA3112778A1 (https=)
EA (1) EA202190799A1 (https=)
MX (1) MX2021003116A (https=)
WO (1) WO2020061007A1 (https=)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3112778A1 (en) * 2018-09-17 2020-03-26 The Children's Hospital Of Philadelphia Polymer-based macromolecular prodrugs
CN115443947B (zh) * 2022-10-12 2023-11-21 江苏省人民医院（南京医科大学第一附属医院） 高血压动物模型的制备方法
WO2025101904A1 (en) * 2023-11-08 2025-05-15 The Children's Hospital Of Philadelphia Norepinephrine transporter-targeted prodrugs for cancer therapy

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999052861A1 (de) * 1998-04-09 1999-10-21 Institut für Diagnostikforschung GmbH an der Freien Universität Berlin Neue benzylguanidinderivate für die therapie, in-vivo- und in-vitro-diagnostik
CN102215688A (zh) * 2008-10-21 2011-10-12 安龙制药公司 用7-乙基-10-羟基喜树碱的多臂聚合物对神经母细胞瘤的治疗

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002255821A (ja) 2001-03-06 2002-09-11 Yakult Honsha Co Ltd 抗癌剤耐性癌に対する治療剤
US7591994B2 (en) 2002-12-13 2009-09-22 Immunomedics, Inc. Camptothecin-binding moiety conjugates
US20040258754A1 (en) * 2003-06-18 2004-12-23 Valery Alakhov Compositions for oral administration of camptothecin and its analogs
CA2537336C (en) 2003-09-17 2013-02-26 Nektar Therapeutics Al, Corporation Multi-arm polymer prodrugs
US8394365B2 (en) 2003-09-17 2013-03-12 Nektar Therapeutics Multi-arm polymer prodrugs
WO2005042539A1 (en) * 2003-10-29 2005-05-12 Sonus Pharmaceuticals, Inc. Tocopherol-modified therapeutic drug compounds
WO2007106549A2 (en) * 2006-03-15 2007-09-20 Alza Corporation Method for treating brain cancer
BRPI0716808A2 (pt) * 2006-09-15 2013-11-05 Enzon Pharmaceuticals Inc Ligantes poliméricos baseados em lisina
US20090074074A1 (en) 2007-06-29 2009-03-19 The Hong Kong University Of Science And Technology Multiple description encoder and decoder for transmitting multiple descriptions
AU2009282413B2 (en) * 2008-08-11 2014-07-17 Nektar Therapeutics Multi-arm polymeric alkanoate conjugates
LT2349346T (lt) 2008-09-23 2019-09-25 Nektar Therapeutics Kamptotecino provaistų (pvz., peg-irinotekano) metronominio dozavimo būdas
CN101385860B (zh) * 2008-10-31 2011-11-02 美国草药泉有限责任公司 喜树碱及其衍生物的非线性聚乙二醇前药
US20120171201A1 (en) 2009-07-22 2012-07-05 Enzon Pharmaceuticals, Inc. Methods of treating her2 positive cancer with her2 receptor antagonist in combination with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin
PT2501413T (pt) 2009-11-18 2019-07-10 Nektar Therapeutics Formas de sal de ácido de conjugados de polímero-fármaco
US20140371258A1 (en) 2010-12-17 2014-12-18 Nektar Therapeutics Water-Soluble Polymer Conjugates of Topotecan
CN102626518B (zh) * 2012-05-09 2014-05-28 中国药科大学 一种包载难溶性药物的泊洛沙姆/两亲性多糖混合胶束的制备和应用
WO2014085571A1 (en) 2012-11-28 2014-06-05 Nektar Therapeutics Method for assessing and predicting efficacy of breast cancer treatment with a long-acting topoisomerase i inhibitor
WO2014194289A1 (en) 2013-05-31 2014-12-04 Nektar Therapeutics Method for predicting and evaluating responsiveness to cancer treatment with dna-damaging chemotherapeutic agents
MX371201B (es) 2013-10-04 2020-01-22 Prolynx Llc Conjugados de liberación lenta de sn-38.
WO2015191583A2 (en) 2014-06-09 2015-12-17 Biomed Valley Discoveries, Inc. Combination therapies targeting tumor-associated stroma or tumor cells and topoisomerase
WO2016040848A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
US11324827B2 (en) 2014-10-01 2022-05-10 Xiamen Sinopeg Biotech Co., Ltd. Multifunctionalized polyethylene glycol derivative and preparation method therefor
CN104877127B (zh) 2015-06-23 2017-11-10 厦门赛诺邦格生物科技股份有限公司 一种八臂聚乙二醇衍生物、制备方法及其修饰的生物相关物质
CN107375288B (zh) 2016-05-16 2019-08-23 博瑞生物医药（苏州）股份有限公司 多臂的聚合靶向抗癌偶联物
US20200163956A1 (en) 2016-09-06 2020-05-28 Cerebral Therapeutics LLC Direct brain administration of chemotherapeutics to the csf for patients with primary and secondary brain tumors
KR102279429B1 (ko) 2017-04-21 2021-07-20 브라이트제네 바이오-메디컬 테크놀로지 코., 엘티디. 멀티 암 표적 항암 콘쥬게이트
JP7381083B2 (ja) 2017-09-08 2023-11-15 フォスプラティン テラピューティクス インコーポレイテッド 免疫調節剤としてのホスファプラチン化合物およびその治療的使用
WO2019090141A1 (en) 2017-11-02 2019-05-09 Vicus Therapeutics, Llc Combination drug therapies for cancer and methods of making and using them
CA3099155A1 (en) 2018-05-14 2019-11-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
CA3112778A1 (en) 2018-09-17 2020-03-26 The Children's Hospital Of Philadelphia Polymer-based macromolecular prodrugs
CN111603567B (zh) 2019-02-22 2024-12-27 赣江新区博瑞创新医药有限公司 Cd44靶向多臂偶联物
CA3138197A1 (en) 2019-05-14 2020-11-19 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999052861A1 (de) * 1998-04-09 1999-10-21 Institut für Diagnostikforschung GmbH an der Freien Universität Berlin Neue benzylguanidinderivate für die therapie, in-vivo- und in-vitro-diagnostik
CN102215688A (zh) * 2008-10-21 2011-10-12 安龙制药公司 用7-乙基-10-羟基喜树碱的多臂聚合物对神经母细胞瘤的治疗

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
argeted drug delivery with polymers and magnetic nanoparticles: covalent and noncovalent approaches, release control, and clinical studies;Ulbrich K et al.;《Chemical reviews》;第116卷(第9期);第5369页第4.2.4节 *
Radiolabeled phenethylguanidines: novel imaging agents for cardiac sympathetic neurons and adrenergic tumors;Raffel D M et al.;《Journal of medicinal chemistry》;第50卷(第9期);摘要 *

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Publication number Publication date
WO2020061007A1 (en) 2020-03-26
EA202190799A1 (ru) 2021-06-22
CN119950749A (zh) 2025-05-09
CA3112778A1 (en) 2020-03-26
JP2022501341A (ja) 2022-01-06
NZ773863A (en) 2024-10-25
EP3852793A4 (en) 2022-07-13
US20210000967A1 (en) 2021-01-07
US20230414766A1 (en) 2023-12-28
US12311028B2 (en) 2025-05-27
CN112996533A (zh) 2021-06-18
EP3852793C0 (en) 2025-11-19
JP7546552B2 (ja) 2024-09-06
KR20210072002A (ko) 2021-06-16
EP3852793B1 (en) 2025-11-19
EP3852793A1 (en) 2021-07-28
US11642414B2 (en) 2023-05-09
AU2019344783A1 (en) 2021-04-08
US20220160886A1 (en) 2022-05-26
US20250387496A1 (en) 2025-12-25
MX2021003116A (es) 2021-05-14
US11253603B2 (en) 2022-02-22
AU2019344783B2 (en) 2025-10-23

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