CN100337689C - 聚亚烷基二醇酸加合物 - Google Patents

聚亚烷基二醇酸加合物 Download PDF

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Publication number
CN100337689C
CN100337689C CNB038175088A CN03817508A CN100337689C CN 100337689 C CN100337689 C CN 100337689C CN B038175088 A CNB038175088 A CN B038175088A CN 03817508 A CN03817508 A CN 03817508A CN 100337689 C CN100337689 C CN 100337689C
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formula
pag
ester
compound
residue
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Expired - Fee Related
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CNB038175088A
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English (en)
Chinese (zh)
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CN1671422A (zh
Inventor
P·S·拜隆
C-Y·王
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • 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
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • C08G65/329Polymers modified by chemical after-treatment with organic 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
    • C08G65/329Polymers modified by chemical after-treatment with organic compounds
    • C08G65/331Polymers modified by chemical after-treatment with organic compounds containing oxygen
    • C08G65/332Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides, or esters thereof
    • C08G65/3322Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides, or esters thereof acyclic
    • 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
    • C08G65/329Polymers modified by chemical after-treatment with organic compounds
    • C08G65/337Polymers modified by chemical after-treatment with organic compounds containing other elements
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2203/00Applications
    • C08L2203/02Applications for biomedical use

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Polyethers (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNB038175088A 2002-07-24 2003-07-16 聚亚烷基二醇酸加合物 Expired - Fee Related CN100337689C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39813702P 2002-07-24 2002-07-24
US60/398,137 2002-07-24

Publications (2)

Publication Number Publication Date
CN1671422A CN1671422A (zh) 2005-09-21
CN100337689C true CN100337689C (zh) 2007-09-19

Family

ID=31495718

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB038175088A Expired - Fee Related CN100337689C (zh) 2002-07-24 2003-07-16 聚亚烷基二醇酸加合物

Country Status (13)

Country Link
US (2) US7193031B2 (enExample)
EP (1) EP1526872A1 (enExample)
JP (2) JP4451308B2 (enExample)
KR (1) KR100608415B1 (enExample)
CN (1) CN100337689C (enExample)
AR (1) AR040654A1 (enExample)
AU (1) AU2003258518B2 (enExample)
BR (1) BR0313212A (enExample)
CA (1) CA2492775C (enExample)
MX (1) MXPA05000796A (enExample)
PL (1) PL375265A1 (enExample)
RU (1) RU2318004C2 (enExample)
WO (1) WO2004012773A1 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6057287A (en) 1994-01-11 2000-05-02 Dyax Corp. Kallikrein-binding "Kunitz domain" proteins and analogues thereof
ATE477020T1 (de) 2002-06-07 2010-08-15 Dyax Corp Prevention und verringerung von ischemia
US7153829B2 (en) 2002-06-07 2006-12-26 Dyax Corp. Kallikrein-inhibitor therapies
JP4451308B2 (ja) * 2002-07-24 2010-04-14 エフ.ホフマン−ラ ロシュ アーゲー ポリアルキレングリコール酸添加剤
WO2005021557A2 (en) * 2003-08-29 2005-03-10 Dyax Corp. Poly-pegylated protease inhibitors
CA2537113A1 (en) * 2003-08-29 2005-03-10 Dyax Corp. Modified protease inhibitors
KR101276422B1 (ko) 2004-03-15 2013-06-19 넥타르 테라퓨틱스 Hiv 유입 억제제의 중합체-기재 조성물 및 콘쥬게이트
CA2567630A1 (en) * 2004-05-17 2005-11-24 Mcmaster University Biological molecule-reactive hydrophilic silicone surface
ATE491475T1 (de) * 2004-07-16 2011-01-15 Nektar Therapeutics Konjugate enthaltend gm-csf und ein polymer
US7235530B2 (en) 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
ATE425204T1 (de) * 2005-08-26 2009-03-15 Novo Nordisk As Verfahren zur modifizierung eines makromolekularen systems
US8133707B2 (en) * 2006-01-17 2012-03-13 Enzon Pharmaceuticals, Inc. Methods of preparing activated polymers having alpha nitrogen groups
AR067536A1 (es) 2007-07-17 2009-10-14 Hoffmann La Roche Metodo para obtener una eritropoyetina mono-pegilada en una forma sustancialmente homogenea
CL2008002053A1 (es) * 2007-07-17 2009-05-22 Hoffmann La Roche Metodo para la purificacion de una eritropoyetina monopeguilada (epompeg) que consiste en proporcionar una solucion que contiene eritropoyetina mono, poli y no peguilada y hacerla pasar por dos pasos de cromatografia de intercambio cationico y metodo para producir epo mpeg que incluye metodo de purificacion.
US20090075887A1 (en) * 2007-08-21 2009-03-19 Genzyme Corporation Treatment with Kallikrein Inhibitors
KR101671537B1 (ko) 2008-08-11 2016-11-01 넥타르 테라퓨틱스 다분지형 중합체 알카노에이트 컨쥬게이트
EP2385843A4 (en) 2009-01-06 2013-02-27 Dyax Corp TREATMENT OF MUZOSITIS WITH CALLICINE INHIBITORS
EP4011917A1 (en) 2010-01-06 2022-06-15 Takeda Pharmaceutical Company Limited Plasma kallikrein binding proteins
US10040761B2 (en) * 2010-06-25 2018-08-07 Nof Corporation Branched hetero polyethylene glycol and intermediate
WO2012088422A1 (en) 2010-12-22 2012-06-28 Nektar Therapeutics Multi-arm polymeric prodrug conjugates of taxane-based compounds
WO2012088445A1 (en) 2010-12-22 2012-06-28 Nektar Therapeutics Multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds
AU2012204202A1 (en) 2011-01-06 2013-07-11 Dyax Corp. Plasma kallikrein binding proteins
MX358784B (es) 2012-04-03 2018-09-04 Sangart Inc Compuestos de nitroxilo activados con succinimida y metodos para el uso de los mismos para nitroxilacion de proteinas.
CN102816227A (zh) * 2012-08-30 2012-12-12 深圳赛保尔生物药业有限公司 回收促红细胞生成素的方法
EP2968597B1 (en) 2013-03-15 2021-08-18 Schindler, William Polyalkylene oxide valerate hemoglobin conjugates
KR20230109785A (ko) 2014-03-27 2023-07-20 다케다 파머수티컬 컴패니 리미티드 당뇨병성 황반 부종의 치료를 위한 조성물 및 방법
IL311156A (en) 2015-12-11 2024-04-01 Takeda Pharmaceuticals Co Plasma kallikrein inhibitors and uses thereof for treating hereditary angioedema attack
CN113631631B (zh) * 2019-03-29 2023-04-18 日油株式会社 含末端羧基的聚乙二醇的制备方法以及活化聚乙二醇的制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4670417A (en) * 1985-06-19 1987-06-02 Ajinomoto Co., Inc. Hemoglobin combined with a poly(alkylene oxide)
WO1995013090A1 (en) * 1993-11-10 1995-05-18 Enzon, Inc. Improved interferon polymer conjugates
CN1211578A (zh) * 1992-08-26 1999-03-24 霍夫曼-拉罗奇有限公司 聚乙二醇-干扰素结合物
WO2001046291A1 (en) * 1999-12-22 2001-06-28 Shearwater Corporation Sterically hindered derivatives of water soluble polymers
WO2002049673A2 (en) * 2000-12-20 2002-06-27 F. Hoffmann-La Roche Ag Conjugates of erythropoietin (pep) with polyethylene glycol (peg)

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5849450B2 (ja) * 1975-07-09 1983-11-04 株式会社日立製作所 スイリヨクシキカプセルユソウソウチノ ボウシクホウ
JP2531661B2 (ja) 1987-02-25 1996-09-04 味の素株式会社 酸素運搬剤
US5595732A (en) 1991-03-25 1997-01-21 Hoffmann-La Roche Inc. Polyethylene-protein conjugates
US5672662A (en) * 1995-07-07 1997-09-30 Shearwater Polymers, Inc. Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications
TW517067B (en) 1996-05-31 2003-01-11 Hoffmann La Roche Interferon conjugates
PT957929E (pt) * 1996-10-25 2006-06-30 Gilead Sciences Inc Complexos de ligandos de acido nucleico do factor de crescimento endotelial vascular
CN1376164A (zh) 1999-01-29 2002-10-23 霍夫曼-拉罗奇有限公司 Gcsf缀合物
PE20001548A1 (es) 1999-03-02 2001-01-16 Schering Corp Uso de interferon alfa pegilado para el tratamiento de vih-1
CZ299516B6 (cs) 1999-07-02 2008-08-20 F. Hoffmann-La Roche Ag Konjugát erythropoetinového glykoproteinu, zpusobjeho výroby a použití a farmaceutická kompozice sjeho obsahem
CN1284603C (zh) 1999-10-08 2006-11-15 内科塔治疗亚拉巴马公司 杂双官能聚乙二醇衍生物和它们的制备方法
US20020065397A1 (en) 2000-10-12 2002-05-30 Joseph Roberts Protecting therapeutic compositions from host-mediated inactivation
JP4451308B2 (ja) * 2002-07-24 2010-04-14 エフ.ホフマン−ラ ロシュ アーゲー ポリアルキレングリコール酸添加剤

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4670417A (en) * 1985-06-19 1987-06-02 Ajinomoto Co., Inc. Hemoglobin combined with a poly(alkylene oxide)
CN1211578A (zh) * 1992-08-26 1999-03-24 霍夫曼-拉罗奇有限公司 聚乙二醇-干扰素结合物
WO1995013090A1 (en) * 1993-11-10 1995-05-18 Enzon, Inc. Improved interferon polymer conjugates
WO2001046291A1 (en) * 1999-12-22 2001-06-28 Shearwater Corporation Sterically hindered derivatives of water soluble polymers
WO2002049673A2 (en) * 2000-12-20 2002-06-27 F. Hoffmann-La Roche Ag Conjugates of erythropoietin (pep) with polyethylene glycol (peg)

Also Published As

Publication number Publication date
PL375265A1 (en) 2005-11-28
US20060167218A1 (en) 2006-07-27
AU2003258518A1 (en) 2004-02-23
JP5112203B2 (ja) 2013-01-09
RU2005105580A (ru) 2006-01-20
US7504477B2 (en) 2009-03-17
KR100608415B1 (ko) 2006-08-02
AU2003258518B2 (en) 2007-01-18
CN1671422A (zh) 2005-09-21
JP2006502250A (ja) 2006-01-19
US20040106747A1 (en) 2004-06-03
JP4451308B2 (ja) 2010-04-14
BR0313212A (pt) 2005-06-28
AR040654A1 (es) 2005-04-13
RU2318004C2 (ru) 2008-02-27
KR20050025663A (ko) 2005-03-14
US7193031B2 (en) 2007-03-20
CA2492775A1 (en) 2004-02-12
MXPA05000796A (es) 2005-04-19
WO2004012773A1 (en) 2004-02-12
CA2492775C (en) 2011-06-21
EP1526872A1 (en) 2005-05-04
JP2009062516A (ja) 2009-03-26

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