CN111867633B - 用于实现延长的局部麻醉的共价麻醉药-聚合物缀合物 - Google Patents

用于实现延长的局部麻醉的共价麻醉药-聚合物缀合物 Download PDF

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CN111867633B
CN111867633B CN201880085421.5A CN201880085421A CN111867633B CN 111867633 B CN111867633 B CN 111867633B CN 201880085421 A CN201880085421 A CN 201880085421A CN 111867633 B CN111867633 B CN 111867633B
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ttx
conjugate
anesthetic
pgs
peg
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CN111867633A (zh
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D·S·寇汉
赵超
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Boston Childrens Hospital
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Boston Childrens Hospital
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    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Anesthesiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880085421.5A 2017-12-01 2018-12-03 用于实现延长的局部麻醉的共价麻醉药-聚合物缀合物 Active CN111867633B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762593784P 2017-12-01 2017-12-01
US62/593,784 2017-12-01
PCT/US2018/063573 WO2019109065A1 (en) 2017-12-01 2018-12-03 Covalent anesthetic-polymer conjugates for prolonged local anesthesia

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CN111867633A CN111867633A (zh) 2020-10-30
CN111867633B true CN111867633B (zh) 2023-09-22

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US (2) US20210275678A1 (https=)
EP (1) EP3717017B1 (https=)
JP (2) JP7601375B2 (https=)
CN (1) CN111867633B (https=)
AU (1) AU2018375002B2 (https=)
CA (1) CA3084034C (https=)
WO (1) WO2019109065A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4090374A4 (en) * 2020-01-17 2024-10-09 Children's Medical Center Corporation MACROMOLECULAR PRODRUGS FOR LIGHT EMITTING DIODES AND THEIR USES
CN113805326A (zh) * 2021-09-18 2021-12-17 吉林大学 原位拉伸多光子激光共聚焦成像仪、实时原位三维观测共混聚合物内部结构的方法
US20250099421A1 (en) * 2023-09-27 2025-03-27 Relevium Medical Analgesic Therapeutics Based on conjugation of Biocompatible Polymers to Ion Channel Modulators
CN119345382B (zh) * 2024-12-23 2025-03-21 上海华之沃生物医药科技有限公司 替曲朵辛偶联物、制备方法和应用

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996034599A1 (en) * 1995-05-01 1996-11-07 Children's Medical Center Corporation Prolonged nerve blockage by the combination of local anesthetics and glucocorticoids
US6326020B1 (en) * 1997-05-16 2001-12-04 Children's Medical Center Corporation Local anesthetic formulations
CN103857440A (zh) * 2011-06-22 2014-06-11 维奥姆生物科学有限公司 基于缀合物的抗真菌和抗细菌前药
CN103932972A (zh) * 2009-03-30 2014-07-23 天蓝制药公司 聚合物-药剂缀合物、颗粒、组合物和相关使用方法
CN104427987A (zh) * 2012-04-23 2015-03-18 儿童医学中心公司 延缓慢性神经病理性疼痛发作的调配物和方法
CN105142625A (zh) * 2013-03-15 2015-12-09 儿童医学中心公司 用于长效局部麻醉的新蛤蚌毒素组合配制品
CN105748412A (zh) * 2014-09-26 2016-07-13 柯惠Lp公司 针对术后慢性疼痛的药物负载微球

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4001413A (en) 1973-06-12 1977-01-04 Astra Pharmaceutical Products, Inc. Pharmaceutical local anesthetic composition employing saxitoxin
GB0218830D0 (en) * 2002-08-13 2002-09-18 Syngenix Ltd Anaesthetic conjugate
US20040228831A1 (en) * 2003-05-15 2004-11-18 Belinka Benjamin A. Polymeric conjugates for tissue activated drug delivery
US8980317B2 (en) * 2008-12-23 2015-03-17 Warsaw Orthopedic, Inc. Methods and compositions for treating infections comprising a local anesthetic
CN106310289B (zh) * 2015-06-24 2020-10-13 天津键凯科技有限公司 一种聚乙二醇和麻醉药的结合物及其制备方法

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996034599A1 (en) * 1995-05-01 1996-11-07 Children's Medical Center Corporation Prolonged nerve blockage by the combination of local anesthetics and glucocorticoids
US6326020B1 (en) * 1997-05-16 2001-12-04 Children's Medical Center Corporation Local anesthetic formulations
CN103932972A (zh) * 2009-03-30 2014-07-23 天蓝制药公司 聚合物-药剂缀合物、颗粒、组合物和相关使用方法
CN103857440A (zh) * 2011-06-22 2014-06-11 维奥姆生物科学有限公司 基于缀合物的抗真菌和抗细菌前药
CN104427987A (zh) * 2012-04-23 2015-03-18 儿童医学中心公司 延缓慢性神经病理性疼痛发作的调配物和方法
CN105142625A (zh) * 2013-03-15 2015-12-09 儿童医学中心公司 用于长效局部麻醉的新蛤蚌毒素组合配制品
CN105748412A (zh) * 2014-09-26 2016-07-13 柯惠Lp公司 针对术后慢性疼痛的药物负载微球

Non-Patent Citations (9)

* Cited by examiner, † Cited by third party
Title
Alpesh Patel等.Highly elastomeric poly(glycerol sebacate)-co-poly(ethylene glycol) amphiphilic block copolymers.《Biomaterials》.2013,第34卷(第16期),第3970-3983页. *
Highly elastomeric poly(glycerol sebacate)-co-poly(ethylene glycol) amphiphilic block copolymers;Alpesh Patel等;《Biomaterials》;第34卷(第16期);第3970页左栏第4行至右栏第12行、第3971页左栏第1-3行及第13-15行、第3972页右栏第39-44行、第3981页左栏第22-31行、图1a *
Injectable biodegradable hydrogels and microgels based on methacrylated poly(ethylene glycol)-co-poly(glycerol sebacate) multi-block copolymers: synthesis, characterization, and cell encapsulation;Wu Yaobin等;《Journal of Materials Chemistry B》;第2卷(第23期);第3674-3685页 *
Janus PEG-Based Dendrimers for Use in Combination Therapy: Controlled Multi-Drug Loading and Sequential Release;Aaron L. Acton等;《Biomacromolecules》;第14卷(第2期);第564-574页 *
Synthesis and evaluation of hydrolyzable hyaluronan-tethered bupivacaine delivery systems;Diego A Gianoli等;《Bioconjugate Chemistry》;第16卷(第6期);摘要部分第1-5行、第1513页左栏第57-59行、第1515页左栏第12-33行及右栏第6-10行、图3和图6 *
可生物降解缓释技术在镇痛释药系统的应用;陆蕾等;《国际药学研究杂志》;第35卷(第5期);第364-368页 *
姚静主编.注射剂中辅料的应用.《药用辅料应用指南》.中国医药科技出版社,2011,第303-304页. *
缓释微球制剂的研究进展;李勋等;《北京化工大学学报(自然科学版)》;第44卷(第6期);第1-11页 *
罗哌卡因聚乙二醇—聚乳酸微球对大鼠切口痛模型坐骨神经阻滞的时效;黄海真;《中国优秀硕士学位论文全文数据库 医药卫生科技辑》(第11期);第E066-52页 *

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JP2024114970A (ja) 2024-08-23
AU2018375002B2 (en) 2021-11-11
JP7601375B2 (ja) 2024-12-17
JP2021505550A (ja) 2021-02-18
EP3717017B1 (en) 2026-02-25
WO2019109065A1 (en) 2019-06-06
AU2018375002A1 (en) 2020-07-02
CA3084034A1 (en) 2019-06-06
CA3084034C (en) 2022-08-16
EP3717017A1 (en) 2020-10-07
US20250195671A1 (en) 2025-06-19
CN111867633A (zh) 2020-10-30
US20210275678A1 (en) 2021-09-09

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