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

Info

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
Authority
CN
China
Prior art keywords
peg
tumor
prodrug
polymer
treatment
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201980060783.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN112996533A (zh
Inventor
M·乔尔内
I·阿尔费里夫
G·M·布罗德
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Childrens Hospital of Philadelphia CHOP
Original Assignee
Childrens Hospital of Philadelphia CHOP
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Childrens Hospital of Philadelphia CHOP filed Critical Childrens Hospital of Philadelphia CHOP
Priority to CN202510008384.XA priority Critical patent/CN119950749A/zh
Publication of CN112996533A publication Critical patent/CN112996533A/zh
Application granted granted Critical
Publication of CN112996533B publication Critical patent/CN112996533B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • 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)

Priority Applications (1)

Application Number Priority Date Filing Date Title
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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202510008384.XA Division CN119950749A (zh) 2018-09-17 2019-09-17 基于聚合物的大分子前药

Publications (2)

Publication Number Publication Date
CN112996533A CN112996533A (zh) 2021-06-18
CN112996533B true CN112996533B (zh) 2025-01-10

Family

ID=69887739

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201980060783.3A Active CN112996533B (zh) 2018-09-17 2019-09-17 基于聚合物的大分子前药
CN202510008384.XA Pending CN119950749A (zh) 2018-09-17 2019-09-17 基于聚合物的大分子前药

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202510008384.XA Pending CN119950749A (zh) 2018-09-17 2019-09-17 基于聚合物的大分子前药

Country Status (10)

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

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112996533B (zh) * 2018-09-17 2025-01-10 费城儿童医院 基于聚合物的大分子前药
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
KR101200729B1 (ko) 2003-09-17 2012-11-13 넥타르 테라퓨틱스 다분지형 고분자 전구약물
US8394365B2 (en) 2003-09-17 2013-03-12 Nektar Therapeutics Multi-arm polymer prodrugs
CA2543722C (en) * 2003-10-29 2011-01-04 Sonus Pharmaceuticals, Inc. Tocopherol-modified therapeutic drug compounds
WO2007106549A2 (en) * 2006-03-15 2007-09-20 Alza Corporation Method for treating brain cancer
CA2662973A1 (en) * 2006-09-15 2008-03-20 Enzon Pharmaceuticals, Inc. Lysine-based polymeric linkers
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
CN102159250B (zh) * 2008-08-11 2014-08-06 尼克塔治疗公司 多臂的聚合烷酸酯偶联物
PT2349346T (pt) 2008-09-23 2019-10-24 Nektar Therapeutics Método de dosagem metronómica com profármacos de camptotecina (e.g. peg-irinotecano).
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
EP2456464A4 (en) 2009-07-22 2013-02-20 Enzon Pharmaceuticals Inc METHODS OF TREATING POSITIVE HER2 CANCER WITH HER2 RECEPTOR ANTAGONIST IN COMBINATION WITH 7-ETHYL-10-HYDROXYCAMPTOTHECIN MULTI-ARM POLYMERIC CONJUGATES
HUE043689T2 (hu) 2009-11-18 2019-09-30 Nektar Therapeutics Polimer-gyógyszer savas sói
WO2012083197A1 (en) 2010-12-17 2012-06-21 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
CN104813167B (zh) 2012-11-28 2019-04-09 尼克塔治疗公司 用于评估和预测用一种长效拓扑异构酶i抑制剂进行乳腺癌治疗的疗效的方法
WO2014194289A1 (en) 2013-05-31 2014-12-04 Nektar Therapeutics Method for predicting and evaluating responsiveness to cancer treatment with dna-damaging chemotherapeutic agents
US10016411B2 (en) * 2013-10-04 2018-07-10 Prolynx Llc Slow-release conjugates of 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
WO2016050210A1 (zh) 2014-10-01 2016-04-07 厦门赛诺邦格生物科技有限公司 一种多官能化聚乙二醇衍生物及其制备方法
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
WO2018048859A1 (en) 2016-09-06 2018-03-15 Cerebral Therapeutics Direct brain administration of chemotherapeutics to the csf for patients with primary and secondary brain tumors
AU2018255458B2 (en) 2017-04-21 2020-06-25 Brightgene Bio-Medical Technology Co., Ltd. Multi-arm targeted anti-cancer conjugate
CN111328330B (zh) 2017-09-08 2024-03-08 普罗蒙托里治疗有限公司 作为免疫调节剂的磷铂化合物及其治疗用途
WO2019090141A1 (en) 2017-11-02 2019-05-09 Vicus Therapeutics, Llc Combination drug therapies for cancer and methods of making and using them
US20190375732A1 (en) 2018-05-14 2019-12-12 David Hung Anti-cancer nuclear hormone receptor-targeting compounds
CN112996533B (zh) * 2018-09-17 2025-01-10 费城儿童医院 基于聚合物的大分子前药
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
KR20220008869A (ko) 2019-05-14 2022-01-21 누베이션 바이오 인크. 항암 핵 호르몬 수용체-표적화 화합물

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 *

Also Published As

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

Similar Documents

Publication Publication Date Title
US12311028B2 (en) Polymer-based macromolecular prodrugs
US10238630B2 (en) Use of eribulin and poly (ADP ribose) polymerase (PARP) inhibitors as combination therapy for the treatment of cancer
Shiah et al. Combination chemotherapy and photodynamic therapy of targetable N-(2-hydroxypropyl) methacrylamide copolymer–doxorubicin/mesochlorin e6-OV-TL 16 antibody immunoconjugates
NZ745069A (en) Pyrrolobenzodiazepines and conjugates thereof
US8088412B2 (en) Intralymphatic chemotherapy drug carriers
EP2341774B1 (en) Treatment of neuroblastoma with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin
EP3565553B1 (en) Intratumoral administration of sirolimus for treatment of prostate cancer
US10376591B2 (en) Formulations and carrier systems including farnesylthiosalicylic moieties
WO2011087548A2 (en) Therapeutic compositions and methods for targeted delivery of active agents
JP2002507571A (ja) アントラサイクリン誘導体とカンプトテシン誘導体の相乗組合せを含有する抗腫瘍組成物
Shi et al. An esterase-activatable prodrug formulated liposome strategy: potentiating the anticancer therapeutic efficacy and drug safety
US20230414762A1 (en) Prostate-specific membrane antigen (psma)-targeted prodrug for selective killing of cells expressing psma
CN104981245B (zh) 无副作用的抗癌剂
EA045198B1 (ru) Макромолекулярные пролекарства на полимерной основе
Gritli et al. Polymeric nanoparticles and cancer: Lessons learnt from CRLX101
JP5843086B2 (ja) 治療活性物質の作用を増強するための高分子化環状ニトロキシドラジカル化合物の使用
WO2010083154A3 (en) Heterofunctional segment-poly(ethylene glycol) polymers as delivery vehicles
WO2025101904A1 (en) Norepinephrine transporter-targeted prodrugs for cancer therapy
CN119950745B (zh) 一种药物组合物及其在制备抗肿瘤药物中的应用
CN107921282A (zh) 选择性抑制肠羧酸酯酶2酶活性的组合物及方法
HK1214145B (en) Anticancer agent having no side effects

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant