KR102642432B1 - 약물-중합체 접합체 - Google Patents

약물-중합체 접합체 Download PDF

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KR102642432B1
KR102642432B1 KR1020197027318A KR20197027318A KR102642432B1 KR 102642432 B1 KR102642432 B1 KR 102642432B1 KR 1020197027318 A KR1020197027318 A KR 1020197027318A KR 20197027318 A KR20197027318 A KR 20197027318A KR 102642432 B1 KR102642432 B1 KR 102642432B1
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South Korea
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formula
group
polymer
alkyl
drug
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KR20190124243A (ko
Inventor
스티븐 론즈데일 벌켓
앤드류 크레이그 도나휴
아샤 마리나 드소자
사라 맨 이 엔지
에이드리언 슐리스티오
러셀 존 테이트
데이비드 벨레이드
앨런 네일러
제이슨 와틀링
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폴리액티바 피티와이 리미티드
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Priority claimed from US15/458,546 external-priority patent/US10113033B2/en
Priority claimed from AU2017900888A external-priority patent/AU2017900888A0/en
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    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G73/00—Macromolecular compounds obtained by reactions forming a linkage containing nitrogen with or without oxygen or carbon in the main chain of the macromolecule, not provided for in groups C08G12/00 - C08G71/00
    • C08G73/06—Polycondensates having nitrogen-containing heterocyclic rings in the main chain of the macromolecule
    • C08G73/08—Polyhydrazides; Polytriazoles; Polyaminotriazoles; Polyoxadiazoles
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61K47/593—Polyesters, e.g. PLGA or polylactide-co-glycolide
    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/5575—Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
    • 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
    • A61K47/595—Polyamides, e.g. nylon
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A61K9/0051—Ocular inserts or implants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Polymers & Plastics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020197027318A 2017-03-14 2018-03-14 약물-중합체 접합체 Active KR102642432B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US15/458,546 2017-03-14
US15/458,546 US10113033B2 (en) 2013-03-08 2017-03-14 Polymer conjugate for delivery of a bioactive agent
AU2017900888A AU2017900888A0 (en) 2017-03-14 Biodegradable drug-polymer conjugate
AU2017900888 2017-03-14
PCT/AU2018/050233 WO2018165710A1 (en) 2017-03-14 2018-03-14 Drug-polymer conjugate

Publications (2)

Publication Number Publication Date
KR20190124243A KR20190124243A (ko) 2019-11-04
KR102642432B1 true KR102642432B1 (ko) 2024-02-28

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Application Number Title Priority Date Filing Date
KR1020197027318A Active KR102642432B1 (ko) 2017-03-14 2018-03-14 약물-중합체 접합체
KR1020197029230A Active KR102642433B1 (ko) 2017-03-14 2018-03-14 생체분해성 약물-중합체 접합체의 제조

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KR1020197029230A Active KR102642433B1 (ko) 2017-03-14 2018-03-14 생체분해성 약물-중합체 접합체의 제조

Country Status (14)

Country Link
US (2) US11787906B2 (https=)
EP (2) EP3595670A4 (https=)
JP (2) JP7355649B2 (https=)
KR (2) KR102642432B1 (https=)
CN (4) CN110461336A (https=)
AU (2) AU2018233158B2 (https=)
CA (1) CA3054084A1 (https=)
CL (1) CL2019002600A1 (https=)
IL (2) IL269321B (https=)
MX (2) MX2019010837A (https=)
NZ (2) NZ756626A (https=)
SG (2) SG11201907956UA (https=)
WO (2) WO2018165710A1 (https=)
ZA (2) ZA201905589B (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
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US11696955B2 (en) 2017-03-14 2023-07-11 Polyactiva Pty Ltd Drug-polymer conjugate
MX2019010837A (es) * 2017-03-14 2019-12-19 Polyactiva Pty Ltd Conjugado biodegradable de farmaco-polimero.
WO2021024041A1 (en) 2019-08-07 2021-02-11 Ripple Therapeutics Corporation Controlled release drug dimers
CA3154867A1 (en) * 2019-09-19 2021-03-25 Polyactiva Pty Ltd Biodegradable drug-polymer conjugate
MX2022013665A (es) 2020-05-01 2022-11-30 Ripple Therapeutics Corp Composiciones y metodos heterodimeros para el tratamiento de trastornos oculares.
WO2024084056A1 (en) * 2022-10-21 2024-04-25 Etherna Immunotherapies Nv Ionizable lipids

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016515099A (ja) 2013-03-08 2016-05-26 ポリアクティヴァ・プロプライエタリー・リミテッド 生物活性剤を送達するためのポリマーコンジュゲート

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IT1044797B (it) 1974-10-15 1980-04-21 Ferruti Paolo Alti polimeri contenenti radicali prostaglandinici processo per la loro preparazione e loro impiego
JPH03220201A (ja) 1988-11-18 1991-09-27 Eisai Co Ltd プロスタグランジン類と多糖類の結合体
JP4419368B2 (ja) 2002-07-25 2010-02-24 小野薬品工業株式会社 プロスタグランジン誘導体およびその誘導体を有効成分として含有する薬剤
CA2617907A1 (en) 2005-08-05 2007-02-15 Syntarga B.V. Triazole-containing releasable linkers and conjugates comprising the same
MY155629A (en) 2008-10-10 2015-11-13 Polyactiva Pty Ltd Biodegradable polymer-bioactive moiety conjugates
SI2340271T1 (sl) 2008-10-10 2019-08-30 Polyactiva Pty Ltd. Konjugati polimer-bioaktivnega sredstva
US8535655B2 (en) * 2008-10-10 2013-09-17 Polyactiva Pty Ltd. Biodegradable polymer—bioactive moiety conjugates
US20100104654A1 (en) 2008-10-27 2010-04-29 Allergan, Inc. Prostaglandin and prostamide drug delivery systems and intraocular therapeutic uses thereof
US20120130045A1 (en) 2009-06-01 2012-05-24 Ablitech, Inc. Biomolecule-polymer conjugates and methods of making same
FR2961694B1 (fr) 2010-06-29 2013-01-25 Thea Lab Systeme de delivrance polymerique d'une solution non visqueuse a base de prostaglandine sans conservateur
WO2012075117A2 (en) 2010-12-01 2012-06-07 Ablitech, Inc. Small molecule-polymer conjugates and methods of making same
WO2012139164A1 (en) * 2011-04-12 2012-10-18 Polyactiva Pty Ltd Polymer conjugated prostaglandin analogues
JP2013035802A (ja) 2011-08-10 2013-02-21 D Western Therapeutics Institute Inc 緑内障又は高眼圧症の予防又は治療剤
MY190370A (en) * 2012-06-26 2022-04-18 Polyactiva Pty Ltd Polymer-nsaid conjugate
US10113033B2 (en) 2013-03-08 2018-10-30 Polyactiva Pty Ltd Polymer conjugate for delivery of a bioactive agent
MX2019010837A (es) * 2017-03-14 2019-12-19 Polyactiva Pty Ltd Conjugado biodegradable de farmaco-polimero.
US11696955B2 (en) 2017-03-14 2023-07-11 Polyactiva Pty Ltd Drug-polymer conjugate
US11207417B2 (en) 2017-03-14 2021-12-28 Polyactiva Pty Ltd Drug-polymer conjugate

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
JP2016515099A (ja) 2013-03-08 2016-05-26 ポリアクティヴァ・プロプライエタリー・リミテッド 生物活性剤を送達するためのポリマーコンジュゲート

Also Published As

Publication number Publication date
EP3595728A1 (en) 2020-01-22
WO2018165711A1 (en) 2018-09-20
JP2020510690A (ja) 2020-04-09
JP2020510692A (ja) 2020-04-09
WO2018165710A1 (en) 2018-09-20
JP7204661B2 (ja) 2023-01-16
IL269323A (en) 2019-11-28
CA3054084A1 (en) 2018-09-20
BR112019018914A2 (pt) 2020-06-30
IL269321B (en) 2022-07-01
CN120919337A (zh) 2025-11-11
AU2018233158A1 (en) 2019-09-12
KR20190124243A (ko) 2019-11-04
CN110662561A (zh) 2020-01-07
ZA201906133B (en) 2021-04-28
CN110461336A (zh) 2019-11-15
US11787906B2 (en) 2023-10-17
CA3054328A1 (en) 2018-09-20
US20240247106A1 (en) 2024-07-25
AU2018233159B8 (en) 2024-08-01
AU2018233159A1 (en) 2019-09-12
AU2018233159B2 (en) 2024-05-02
US12503553B2 (en) 2025-12-23
CL2019002600A1 (es) 2020-04-03
EP3595670A4 (en) 2021-05-12
KR20190123776A (ko) 2019-11-01
CN120919336A (zh) 2025-11-11
IL269323B (en) 2022-07-01
IL269321A (en) 2019-11-28
MX2019010904A (es) 2019-12-09
SG11201907956UA (en) 2019-09-27
SG11201907931WA (en) 2019-09-27
JP7355649B2 (ja) 2023-10-03
KR102642433B1 (ko) 2024-02-28
AU2018233158B2 (en) 2024-04-11
NZ756626A (en) 2022-10-28
ZA201905589B (en) 2020-07-29
EP3595670A1 (en) 2020-01-22
NZ757356A (en) 2022-10-28
AU2018233159C1 (en) 2025-01-02
AU2018233159A8 (en) 2024-08-01
US20200123322A1 (en) 2020-04-23
MX2019010837A (es) 2019-12-19
EP3595728A4 (en) 2021-05-05

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