RU2008126209A - Дендример-пэг с четырьмя ветками для конъюгирования с белками и пептидами - Google Patents

Дендример-пэг с четырьмя ветками для конъюгирования с белками и пептидами Download PDF

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RU2008126209A
RU2008126209A RU2008126209/04A RU2008126209A RU2008126209A RU 2008126209 A RU2008126209 A RU 2008126209A RU 2008126209/04 A RU2008126209/04 A RU 2008126209/04A RU 2008126209 A RU2008126209 A RU 2008126209A RU 2008126209 A RU2008126209 A RU 2008126209A
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ЭРНАНДЕС Хосе Анхел РАМОН (CU)
Эрнандес Хосе Анхел Рамон
ОДИО Фидель Рауль КАСТРО (CU)
Одио Фидель Рауль Кастро
МАРТИНЕС Вивиан Мария САЕС (CU)
Мартинес Вивиан Мария Саес
МЕЙРЕЛЕС Роландо ПАЕС (CU)
МЕЙРЕЛЕС Роландо ПАЕС
САНЧЕС Эдуардо ФЕРНАНДЕС (CU)
Санчес Эдуардо Фернандес
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Сентро Де Инхеньерия Хенетика И Биотекнолохия (Cu)
Сентро Де Инхеньерия Хенетика И Биотекнолохия
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    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32Polymers modified by chemical after-treatment
    • AHUMAN NECESSITIES
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    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/26Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32Polymers modified by chemical after-treatment
    • C08G65/321Polymers modified by chemical after-treatment with inorganic compounds
    • C08G65/325Polymers modified by chemical after-treatment with inorganic compounds containing nitrogen

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  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Polymers & Plastics (AREA)
  • Inorganic Chemistry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Polyethers (AREA)
  • Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)

Abstract

1. Полимерная дендример-подобная структура, включающая четыре ветви монометоксиполиэтиленгликоля, которая может быть представлена как: ! ! для получения конъюгатов, представляющих фармацевтический интерес. ! 2. Полимерная структура по п.1, где молекулярная масса каждой ПЭГ-цепи находится между 5000 и 30000 Д, а общая молекулярная масса находится между 20000 и 120000 Д. ! 3. Полимерная структура по п.2, активированная для конъюгирования с нуклеофильными группами, полученная функциональной активацией карбоксильной группы. ! 4. Конъюгат, включающий полимерную структуру по п.1 и нуклеофильную группу. ! 5. Конъюгат по п.4, где нуклеофильная группа содержится в биомолекуле, выбранной из группы, состоящей из белков, пептидов и полипептидов. ! 6. Конъюгат по п.5, где белок выбран из группы, состоящей из интерферона альфа 2-b, стрептокиназы, гранулоцитарного колониестимулирующего фактора, эритропоэтина и эпидермального ростового фактора.

Claims (6)

1. Полимерная дендример-подобная структура, включающая четыре ветви монометоксиполиэтиленгликоля, которая может быть представлена как:
Figure 00000001
для получения конъюгатов, представляющих фармацевтический интерес.
2. Полимерная структура по п.1, где молекулярная масса каждой ПЭГ-цепи находится между 5000 и 30000 Д, а общая молекулярная масса находится между 20000 и 120000 Д.
3. Полимерная структура по п.2, активированная для конъюгирования с нуклеофильными группами, полученная функциональной активацией карбоксильной группы.
4. Конъюгат, включающий полимерную структуру по п.1 и нуклеофильную группу.
5. Конъюгат по п.4, где нуклеофильная группа содержится в биомолекуле, выбранной из группы, состоящей из белков, пептидов и полипептидов.
6. Конъюгат по п.5, где белок выбран из группы, состоящей из интерферона альфа 2-b, стрептокиназы, гранулоцитарного колониестимулирующего фактора, эритропоэтина и эпидермального ростового фактора.
RU2008126209/05A 2005-11-30 2006-11-20 Дендример-пэг с четырьмя ветками для конъюгирования с белками и пептидами RU2409389C2 (ru)

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CU20050241A CU23556A1 (es) 2005-11-30 2005-11-30 Estructura polimérica semejante a dendrímero para la obtención de conjugados de interés farmacéutico

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Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2636599C (en) * 2006-01-20 2014-07-15 Starpharma Pty Limited Modified macromolecule
US8252834B2 (en) * 2008-03-12 2012-08-28 The Regents Of The University Of Michigan Dendrimer conjugates
WO2010039861A2 (en) 2008-09-30 2010-04-08 The Regents Of The University Of Michigan Dendrimer conjugates
US9017644B2 (en) 2008-11-07 2015-04-28 The Regents Of The University Of Michigan Methods of treating autoimmune disorders and/or inflammatory disorders
US20100158850A1 (en) * 2008-12-23 2010-06-24 The Regents Of The University Of Michigan Dendrimer based modular platforms
WO2011059609A2 (en) * 2009-10-13 2011-05-19 The Regents Of The University Of Michigan Dendrimer compositions and methods of synthesis
WO2011059586A2 (en) 2009-10-30 2011-05-19 The Regents Of The University Of Michigan Multifunctional small molecules
WO2013085718A1 (en) 2011-12-08 2013-06-13 The Regents Of The University Of Michigan Multifunctional small molecules
WO2013096388A1 (en) 2011-12-21 2013-06-27 The Regents Of The University Of California Telodendrimers with enhanced drug delivery
US9642916B2 (en) 2012-12-12 2017-05-09 The Regents Of The University Of California Porphyrin modified telodendrimers
MY186423A (en) * 2013-03-05 2021-07-22 Hanmi Pharm Ind Co Ltd Improved preparation method for high-yield production of physiologically active polypeptide conjugate
EP2786766A1 (en) * 2013-04-05 2014-10-08 Ufpeptides S.r.l. Supramolecular aggregates comprising maleimido cores
EP3013790A1 (en) 2013-06-27 2016-05-04 Mylan Laboratories Ltd. Process for the preparation of nepafenac
CU20140003A7 (es) * 2014-01-08 2015-08-27 Ct De Inmunología Molecular Biofarmacuba Conjugado que comprende eritropoyetina y una estructura polimérica ramificada
SI3183264T1 (sl) 2014-08-19 2021-03-31 Biogen Ma Inc. Metoda pegilacije
US20160361426A1 (en) * 2015-06-11 2016-12-15 Prolong Pharmaceuticals, LLC Pegylated granulocyte colony stimulating factor (gcsf)
EP3385383B1 (en) 2015-12-04 2021-04-07 Zenyaku Kogyo Co., Ltd. Anti-il-17 aptamer having improved retention in blood
AU2017205273C1 (en) 2016-01-08 2022-12-01 Ascendis Pharma Growth Disorders A/S Controlled-release CNP agonists with reduced side-effects
BR112018011008A2 (pt) 2016-01-08 2018-12-04 Ascendis Pharma Growth Disorders As agonistas de cnp de liberação controlada com ligação a npr-c baixa
EP3400022A1 (en) 2016-01-08 2018-11-14 Ascendis Pharma Growth Disorders A/S Controlled-release cnp agonists with low initial npr-b activity
WO2017118693A1 (en) * 2016-01-08 2017-07-13 Ascendis Pharma Growth Disorders A/S Cnp prodrugs with large carrier moieties
WO2017118700A1 (en) 2016-01-08 2017-07-13 Ascendis Pharma Growth Disorders A/S Controlled-release cnp agonists with increased nep stability
EP3400019B1 (en) 2016-01-08 2022-09-28 Ascendis Pharma Growth Disorders A/S Cnp prodrugs with carrier attachment at the ring moiety
JP7102005B2 (ja) 2016-09-15 2022-07-19 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 改善されたハイブリッドテロデンドリマー
KR102531327B1 (ko) 2016-09-29 2023-05-11 아센디스 파마 그로우쓰 디스오더스 에이/에스 조절 방출 cnp 아고니스트를 사용한 병용 요법
CN109134282B (zh) * 2017-06-28 2021-03-16 北京键凯科技股份有限公司 一种树状多缩乙二醇衍生物及其制备方法和应用
WO2019001473A1 (zh) * 2017-06-28 2019-01-03 北京键凯科技股份有限公司 一种树状多缩乙二醇衍生物及其制备方法和应用

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4732863A (en) 1984-12-31 1988-03-22 University Of New Mexico PEG-modified antibody with reduced affinity for cell surface Fc receptors
US5951974A (en) * 1993-11-10 1999-09-14 Enzon, Inc. Interferon polymer conjugates
US5932462A (en) * 1995-01-10 1999-08-03 Shearwater Polymers, Inc. Multiarmed, monofunctional, polymer for coupling to molecules and surfaces
US5985263A (en) * 1997-12-19 1999-11-16 Enzon, Inc. Substantially pure histidine-linked protein polymer conjugates
JP5170931B2 (ja) 2000-10-16 2013-03-27 中外製薬株式会社 Peg修飾エリスロポエチン
JP4758608B2 (ja) * 2001-11-07 2011-08-31 ネクター セラピューティックス 分枝ポリマーおよびそれらの結合体
US7144978B2 (en) * 2002-01-15 2006-12-05 Pan Asia Bio Co., Ltd. Multidrop tree branching functional polyethylene glycol, methods of preparing and using same
CN1176137C (zh) * 2002-01-15 2004-11-17 泛亚生物技术有限公司 多臂树杈型功能化聚乙二醇制备方法及它在药物中的应用
CN1569892A (zh) * 2004-04-30 2005-01-26 新峰生物科技(上海)有限公司 多臂树杈型聚乙二醇与蛋白质或多肽的结合物及其制备方法
ITMI20020951A1 (it) 2002-05-06 2003-11-06 Univ Degli Studi Trieste Derivati multifunzionali del polietilenglicole loro preparazione ed impiego
CA2510040C (en) 2003-05-23 2012-01-03 Nektar Therapeutics Al, Corporation Polymeric reagents and polymer-biomolecule conjugates comprising carbamate linkages
JP2007501811A (ja) * 2003-08-08 2007-02-01 ノボ ノルディスク ヘルス ケア アクチェンゲゼルシャフト 治療的な関心対象のタンパク質に対する遅延分子の選択的な化学物質接合のためのガラクトースオキシダーゼの使用。
CA2552892C (en) * 2004-01-08 2014-08-05 Neose Technologies, Inc. O-linked glycosylation of peptides
EP1768700B1 (en) 2004-07-16 2010-12-15 Nektar Therapeutics Conjugates comprising gm-csf and a polymer
EP1848461A2 (en) 2005-02-16 2007-10-31 Nektar Therapeutics Al, Corporation Conjugates of an epo moiety and a polymer
AU2006215566A1 (en) * 2005-02-16 2006-08-24 Novo Nordisk A/S Insulinotropic agents conjugated with structurally well defined branched polymers

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WO2007062610A2 (es) 2007-06-07
EP1967212B1 (en) 2016-09-21
AU2006319636B2 (en) 2012-10-18
JP5123201B2 (ja) 2013-01-23
EP1967212A2 (en) 2008-09-10
CA2631335A1 (en) 2007-06-07
ZA200804694B (en) 2009-03-25
KR101134983B1 (ko) 2012-04-09
UA91575C2 (ru) 2010-08-10
UY29981A1 (es) 2007-06-29
BRPI0604313A (pt) 2007-01-30
US20090082537A1 (en) 2009-03-26
CA2631335C (en) 2013-07-16
CU23556A1 (es) 2010-07-20
CN101389354A (zh) 2009-03-18
AU2006319636A1 (en) 2007-06-07
US8703893B2 (en) 2014-04-22
EG26619A (en) 2014-04-08
MY150739A (en) 2014-02-28
KR20080072960A (ko) 2008-08-07
CN104906594A (zh) 2015-09-16
CN104906594B (zh) 2016-12-28
JP2009517414A (ja) 2009-04-30
RU2409389C2 (ru) 2011-01-20
WO2007062610A3 (es) 2007-09-20

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