DK2306986T3 - PRODRUGS AND PHARMACEUTICAL Macromolecule Conjugates with Controlled Drug Release Rates - Google Patents

PRODRUGS AND PHARMACEUTICAL Macromolecule Conjugates with Controlled Drug Release Rates Download PDF

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Publication number
DK2306986T3
DK2306986T3 DK09771199.8T DK09771199T DK2306986T3 DK 2306986 T3 DK2306986 T3 DK 2306986T3 DK 09771199 T DK09771199 T DK 09771199T DK 2306986 T3 DK2306986 T3 DK 2306986T3
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Denmark
Prior art keywords
formula
drug
optionally substituted
compound
macromolecule
Prior art date
Application number
DK09771199.8T
Other languages
Danish (da)
English (en)
Inventor
Daniel V Santi
Gary Ashley
Brian Hearn
Original Assignee
Prolynx Llc
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 Prolynx Llc filed Critical Prolynx Llc
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Publication of DK2306986T3 publication Critical patent/DK2306986T3/en

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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
    • 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
    • A61K47/54—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 compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • 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
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333—Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C08G65/33303—Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group
    • C08G65/33317—Polymers modified by chemical after-treatment with organic compounds containing nitrogen containing amino group heterocyclic
    • 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
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/333—Polymers modified by chemical after-treatment with organic compounds containing nitrogen
    • C08G65/33396—Polymers modified by chemical after-treatment with organic compounds containing nitrogen having oxygen in addition to nitrogen
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2203/00—Applications
    • C08L2203/02—Applications for biomedical use

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Polymers & Plastics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
DK09771199.8T 2008-06-26 2009-06-26 PRODRUGS AND PHARMACEUTICAL Macromolecule Conjugates with Controlled Drug Release Rates DK2306986T3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13314808P 2008-06-26 2008-06-26
US19205008P 2008-09-15 2008-09-15
PCT/US2009/048943 WO2009158668A1 (en) 2008-06-26 2009-06-26 Prodrugs and drug-macromolecule conjugates having controlled drug release rates

Publications (1)

Publication Number Publication Date
DK2306986T3 true DK2306986T3 (en) 2018-06-18

Family

ID=41444985

Family Applications (1)

Application Number Title Priority Date Filing Date
DK09771199.8T DK2306986T3 (en) 2008-06-26 2009-06-26 PRODRUGS AND PHARMACEUTICAL Macromolecule Conjugates with Controlled Drug Release Rates

Country Status (7)

Country Link
US (2) US8680315B2 (enExample)
EP (1) EP2306986B1 (enExample)
JP (2) JP6084770B2 (enExample)
CN (1) CN102076331B (enExample)
DK (1) DK2306986T3 (enExample)
ES (1) ES2672526T3 (enExample)
WO (1) WO2009158668A1 (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011140376A1 (en) * 2010-05-05 2011-11-10 Prolynx Llc Controlled drug release from dendrimers
WO2011140393A1 (en) 2010-05-05 2011-11-10 Prolynx Llc Controlled release from macromolecular conjugates
EP2566334B1 (en) * 2010-05-05 2018-04-18 Prolynx, LLC Controlled drug release from solid supports
HUE052285T2 (hu) 2011-06-06 2021-04-28 Starpharma Pty Ltd Makromolekulák
WO2013036857A1 (en) * 2011-09-07 2013-03-14 Prolynx Llc Sulfone linkers
SG11201400444VA (en) 2011-09-07 2014-04-28 Prolynx Llc Hydrogels with biodegradable crosslinking
EP2768856A4 (en) * 2011-10-18 2015-05-27 Prolynx Llc PEG CONJUGATES OF EXENATIDE
US9545449B2 (en) * 2012-05-11 2017-01-17 Advanced Proteone Therapeutics Inc. Site-specific labeling and targeted delivery of proteins for the treatment of cancer
JP2016534064A (ja) 2013-10-22 2016-11-04 プロリンクス エルエルシー ソマトスタチン及びその類似体のコンジュゲート
CN105813653B (zh) 2013-12-19 2020-06-26 西雅图基因公司 与目标-药物偶联物并用的亚甲基氨基甲酸酯连接物
WO2016025752A1 (en) * 2014-08-14 2016-02-18 Prolynx Llc Reagents for thiol conjugation and conjugates formed therefrom
CN107001440A (zh) 2014-09-26 2017-08-01 拜耳制药股份公司 稳定化的肾上腺髓质素衍生物及其用途
GB201508024D0 (en) * 2015-05-11 2015-06-24 Haemostatix Ltd Haemostatic compositions
CA3016814A1 (en) 2016-03-16 2017-09-21 Prolynx Llc Extended release conjugates of exenatide analogs
CN106177977B (zh) * 2016-07-11 2020-09-04 天津科技大学 一种抗肿瘤药物三元偶联物及合成和应用
TWI773730B (zh) 2017-02-22 2022-08-11 瑞典商阿斯特捷利康公司 治療性樹枝狀聚合物
JP2021510702A (ja) 2018-01-12 2021-04-30 プロリンクス エルエルシー 相乗的がん治療
EP3823961A4 (en) 2018-07-19 2022-06-08 Starpharma Pty Limited THERAPEUTIC DENDRIMER
US12071517B2 (en) 2018-07-19 2024-08-27 Starpharma Pty Ltd. Therapeutic dendrimer
JPWO2020050378A1 (ja) * 2018-09-06 2021-08-30 生化学工業株式会社 第３級アミン化合物又はイミン化合物を結合させた、ポリマーコンジュゲートとその製造方法
WO2020067507A1 (ja) * 2018-09-28 2020-04-02 生化学工業株式会社 第１級アミン化合物又は第２級アミン化合物－酸性多糖コンジュゲートとその製造方法
MX2021011997A (es) * 2019-04-05 2021-11-04 Prolynx Llc Enlazadores de conjugacion mejorados.
WO2020219943A1 (en) 2019-04-26 2020-10-29 Prolynx Llc Slow-release cytokine conjugates
CA3143584A1 (en) 2019-06-18 2020-12-24 Bayer Aktiengesellschaft Adrenomedullin-analogues for long-term stabilization and their use
BR112022002308A2 (pt) 2019-08-07 2022-04-26 Prolynx Llc Esterilização a vapor de hidrogéis reticulados por ligantes beta-eliminativos
CN110423355B (zh) * 2019-08-29 2021-09-14 武汉轻工大学 羧甲基化莲藕多糖-曲古霉素a轭合物的制备方法
WO2021067458A1 (en) 2019-09-30 2021-04-08 Beijing Xuanyi Pharmasciences Co., Ltd. Protein-macromolecule conjugates and methods of use thereof
KR102986821B1 (ko) 2020-04-22 2026-07-06 머크 샤프 앤드 돔 엘엘씨 인터류킨-2 수용체 베타 감마c 이량체에 대해 편향되고 비펩티드성 수용성 중합체에 접합된 인간 인터류킨-2 접합체
EP4319821A4 (en) * 2021-04-09 2026-05-06 Nanjing University CONJUGATE AND ITS PREPARATION PROCESS AND ITS USE
EP4713024A1 (en) * 2023-05-16 2026-03-25 Nanjing University Conjugate and the preparation thereof
WO2026138790A1 (zh) * 2024-12-24 2026-07-02 长春金赛药业有限责任公司 一种具有可控的药物释放速率的前药和药物

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0270595B1 (en) 1986-05-16 1990-08-16 Eka Nobel Ab An optically active reagent and a method for the determination of enantiomeric amine compounds
US5101059A (en) * 1989-12-05 1992-03-31 Research Corporation Technologies, Inc. Amino acid protecting groups
DE4321946A1 (de) 1993-07-01 1995-01-12 Hoechst Ag Methylphosphonsäureester, Verfahren zu deren Herstellung und deren Verwendung
CA2262502C (en) * 1996-07-31 2002-11-26 Nikken Chemicals Co., Ltd. 6-phenyltetrahydro-1,3-oxazin-2-one derivatives and pharmaceutical composition containing the same
IL119029A0 (en) 1996-08-07 1996-11-14 Yeda Res & Dev Long-acting drugs and pharamaceutical compositions comprising them
JPH11130711A (ja) * 1997-10-24 1999-05-18 Teijin Ltd １α，２４，２５−トリヒドロキシビタミンＤ３類の合成中間体およびその製造法
AU1345600A (en) * 1998-11-12 2000-06-05 Merck & Co., Inc. Pyrimidinedione derivatives useful as alpha 1a adrenoceptor antagonists
US6114566A (en) * 1999-05-24 2000-09-05 Board Of Trustees Operating Michigan State University 4-cyano-3-hydroxybutanoyl hydrazines, derivatives and process for the preparation thereof
JP2003528939A (ja) * 1999-09-03 2003-09-30 スクール オブ ファーマシー， ユニヴァーシティ オブ ロンドン 分解性ポリマー
US6861162B2 (en) 2002-08-28 2005-03-01 Cityu Research Ltd. Organic electroluminescence devices using pyrazolo[3,4b]quinoxaline derivatives
WO2004089280A2 (en) * 2003-04-08 2004-10-21 Yeda Research And Development Co. Ltd. Reversible pegylated drugs
WO2004089279A2 (en) 2003-04-08 2004-10-21 Yeda Research And Development Co. Ltd. Long-acting derivatives of pyy agonists
US20070010573A1 (en) * 2003-06-23 2007-01-11 Xianqi Kong Methods and compositions for treating amyloid-related diseases
GB0319759D0 (en) 2003-08-22 2003-09-24 Astrazeneca Ab Chemical compounds
CA2786794C (en) 2004-03-23 2017-09-12 Complex Biosystems Gmbh Aromatic polymeric cascade prodrug linker reagent
JP2006067889A (ja) 2004-09-01 2006-03-16 Japan Science & Technology Agency Ｐｅｏと二本鎖核酸のコンジュゲート
JP5167473B2 (ja) 2005-03-03 2013-03-21 コヴェックス・テクノロジーズ・アイルランド・リミテッド 抗血管新生化合物
CN101287835A (zh) 2005-08-17 2008-10-15 株式会社百奥尼 用于siRNA细胞内输送的siRNA-亲水性聚合物结合物及其方法
JP5224016B2 (ja) * 2006-03-10 2013-07-03 晃二 有光 感活性エネルギー線塩基発生剤、感活性エネルギー線塩基発生剤組成物、塩基反応性組成物及びパターン形成方法
US20100168443A1 (en) 2006-11-02 2010-07-01 University Of Virginia Patent Foundation Ethoid-Containing Compounds, Methods for Preparing Ethoid-Containing Compounds, and Methods of Use
CA3004716C (en) * 2008-04-29 2022-04-12 Ascendis Pharma Endocrinology Division A/S Pegylated recombinant human growth hormone compounds

Also Published As

Publication number Publication date
EP2306986A4 (en) 2015-01-28
CN102076331B (zh) 2013-12-18
ES2672526T3 (es) 2018-06-14
WO2009158668A1 (en) 2009-12-30
EP2306986A1 (en) 2011-04-13
JP2011528654A (ja) 2011-11-24
EP2306986B1 (en) 2018-03-21
US9387254B2 (en) 2016-07-12
US20110263502A1 (en) 2011-10-27
US8680315B2 (en) 2014-03-25
CN102076331A (zh) 2011-05-25
JP2015172078A (ja) 2015-10-01
JP6084770B2 (ja) 2017-02-22
US20140296476A1 (en) 2014-10-02

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