AU2018375002B2 - Covalent anesthetic-polymer conjugates for prolonged local anesthesia - Google Patents

Covalent anesthetic-polymer conjugates for prolonged local anesthesia Download PDF

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Publication number
AU2018375002B2
AU2018375002B2 AU2018375002A AU2018375002A AU2018375002B2 AU 2018375002 B2 AU2018375002 B2 AU 2018375002B2 AU 2018375002 A AU2018375002 A AU 2018375002A AU 2018375002 A AU2018375002 A AU 2018375002A AU 2018375002 B2 AU2018375002 B2 AU 2018375002B2
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Australia
Prior art keywords
ttx
anesthetic
peg
polymer
pgs
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AU2018375002A
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AU2018375002A1 (en
Inventor
Daniel S. Kohane
Chao Zhao
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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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Anesthesiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
AU2018375002A 2017-12-01 2018-12-03 Covalent anesthetic-polymer conjugates for prolonged local anesthesia Active AU2018375002B2 (en)

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

Publications (2)

Publication Number Publication Date
AU2018375002A1 AU2018375002A1 (en) 2020-07-02
AU2018375002B2 true AU2018375002B2 (en) 2021-11-11

Family

ID=64734233

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018375002A Active AU2018375002B2 (en) 2017-12-01 2018-12-03 Covalent anesthetic-polymer conjugates for prolonged local anesthesia

Country Status (7)

Country Link
US (2) US20210275678A1 (enExample)
EP (1) EP3717017A1 (enExample)
JP (2) JP7601375B2 (enExample)
CN (1) CN111867633B (enExample)
AU (1) AU2018375002B2 (enExample)
CA (1) CA3084034C (enExample)
WO (1) WO2019109065A1 (enExample)

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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014350A2 (en) * 2002-08-13 2004-02-19 Sirus Pharmaceuticals Ltd Polymer conjugates of a local anaesthetic drug
WO2016206549A1 (zh) * 2015-06-24 2016-12-29 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

Family Cites Families (10)

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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
US5700485A (en) * 1992-09-10 1997-12-23 Children's Medical Center Corporation Prolonged nerve blockade by the combination of local anesthetic and glucocorticoid
AU7389098A (en) * 1997-05-16 1998-12-08 Brigham And Women's Hospital Local anesthetic formulations
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
AU2010234916A1 (en) * 2009-03-30 2011-10-13 Cerulean Pharma Inc. Polymer-agent conjugates, particles, compositions, and related methods of use
EA032840B8 (ru) 2011-06-22 2020-06-18 Вайоми Терапеутикс Лимитед Пролекарства на основе конъюгатов противогрибковых агентов и их применение
JP2015514805A (ja) * 2012-04-23 2015-05-21 ザ チルドレンズ メディカル センター コーポレイション 慢性神経因性疼痛の発症を遅延させるための製剤および方法
NZ710890A (en) * 2013-03-15 2016-11-25 Childrens Medical Ct Corp Neosaxitoxin combination formulations for prolonged local anesthesia
US10449152B2 (en) * 2014-09-26 2019-10-22 Covidien Lp Drug loaded microspheres for post-operative chronic pain

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014350A2 (en) * 2002-08-13 2004-02-19 Sirus Pharmaceuticals Ltd Polymer conjugates of a local anaesthetic drug
WO2016206549A1 (zh) * 2015-06-24 2016-12-29 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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DIEGO A. GIANOLIO ET AL, "Synthesis and Evaluation of Hydrolyzable Hyaluronan-Tethered Bupivacaine Delivery Systems", BIOCONJUGATE CHEMISTRY, US, (2005-11-01), vol. 16, no. 6, doi:10.1021/bc050239a, ISSN 1043-1802, pages 1512 - 1518 *
KOHANE D S et al., "Prolonged duration local anesthesia from tetrodotoxin-enhanced local anesthetic microspheres", Pain, (2003-07-01), vol. 104, no. 1, pages 415 - 421, ISSN 0304-3959. <doi:10.1016/S0304-3959(03)00049-6> *

Also Published As

Publication number Publication date
US20250195671A1 (en) 2025-06-19
EP3717017A1 (en) 2020-10-07
CN111867633B (zh) 2023-09-22
AU2018375002A1 (en) 2020-07-02
CA3084034A1 (en) 2019-06-06
JP7601375B2 (ja) 2024-12-17
US20210275678A1 (en) 2021-09-09
JP2024114970A (ja) 2024-08-23
CN111867633A (zh) 2020-10-30
CA3084034C (en) 2022-08-16
JP2021505550A (ja) 2021-02-18
WO2019109065A1 (en) 2019-06-06

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