CN101076353B - 基于脂肪族生物可降解的接头的可释放的聚合物共轭物 - Google Patents

基于脂肪族生物可降解的接头的可释放的聚合物共轭物 Download PDF

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Publication number
CN101076353B
CN101076353B CN200580042661XA CN200580042661A CN101076353B CN 101076353 B CN101076353 B CN 101076353B CN 200580042661X A CN200580042661X A CN 200580042661XA CN 200580042661 A CN200580042661 A CN 200580042661A CN 101076353 B CN101076353 B CN 101076353B
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alkynyl
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CN101076353A (zh
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赵洪
理查德·B·格林沃尔德
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Viskase Holdings Inc
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Enzon Pharmaceuticals Inc
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    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/12—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/16—Sulfur atoms
    • 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
    • A61K31/325—Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Preparation (AREA)
  • Polyethers (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Polyamides (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Peptides Or Proteins (AREA)
CN200580042661XA 2004-12-14 2005-12-13 基于脂肪族生物可降解的接头的可释放的聚合物共轭物 Expired - Fee Related CN101076353B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11/011,818 2004-12-14
US11/011,818 US7413738B2 (en) 2002-08-13 2004-12-14 Releasable polymeric conjugates based on biodegradable linkers
PCT/US2005/045467 WO2006066020A2 (en) 2004-12-14 2005-12-13 Releasable polymeric conjugates based on aliphatic biodegradable linkers

Publications (2)

Publication Number Publication Date
CN101076353A CN101076353A (zh) 2007-11-21
CN101076353B true CN101076353B (zh) 2010-12-08

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CN200580042661XA Expired - Fee Related CN101076353B (zh) 2004-12-14 2005-12-13 基于脂肪族生物可降解的接头的可释放的聚合物共轭物

Country Status (12)

Country Link
US (2) US7413738B2 (enExample)
EP (1) EP1827497A4 (enExample)
JP (1) JP5405746B2 (enExample)
KR (1) KR20070089739A (enExample)
CN (1) CN101076353B (enExample)
AU (1) AU2005316520B2 (enExample)
CA (1) CA2589975C (enExample)
IL (1) IL183582A0 (enExample)
MX (1) MX2007007034A (enExample)
RU (1) RU2007126802A (enExample)
TW (1) TWI375556B (enExample)
WO (1) WO2006066020A2 (enExample)

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US7413738B2 (en) * 2002-08-13 2008-08-19 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on biodegradable linkers
US7122189B2 (en) * 2002-08-13 2006-10-17 Enzon, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7087229B2 (en) * 2003-05-30 2006-08-08 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7365127B2 (en) * 2005-02-04 2008-04-29 Enzon Pharmaceuticals, Inc. Process for the preparation of polymer conjugates
CN101166761A (zh) * 2005-05-04 2008-04-23 隆萨股份公司 肽合成法
GB2427360A (en) * 2005-06-22 2006-12-27 Complex Biosystems Gmbh Aliphatic prodrug linker
US8133707B2 (en) 2006-01-17 2012-03-13 Enzon Pharmaceuticals, Inc. Methods of preparing activated polymers having alpha nitrogen groups
US20090156629A1 (en) * 2006-06-09 2009-06-18 Enzon Pharmaceuticals, Inc. Indenoisoquinoline-releasable polymer conjugates
CA2662520A1 (en) * 2006-09-15 2008-03-20 Enzon Pharmaceuticals, Inc. Polymeric conjugates containing positively-charged moieties
US8110559B2 (en) * 2006-09-15 2012-02-07 Enzon Pharmaceuticals, Inc. Hindered ester-based biodegradable linkers for oligonucleotide delivery
WO2008034120A2 (en) * 2006-09-15 2008-03-20 Enzon Pharmaceuticals, Inc. Lysine-based polymeric linkers
CA2662962A1 (en) * 2006-09-15 2008-03-20 Enzon Pharmaceuticals, Inc. Polyalkylene oxides having hindered ester-based biodegradable linkers
US20100279408A1 (en) * 2006-11-27 2010-11-04 Enzon Pharmaceuticals, Inc. Polymeric short interfering rna conjugates
JP2010514803A (ja) * 2006-12-29 2010-05-06 エンゾン ファーマスーティカルズ インコーポレイテッド 肺疾患を治療するためのアデノシンデアミナーゼの使用方法
HUE027603T2 (en) * 2007-04-20 2016-10-28 Sigma-Tau Rare Disease Ltd Stable, recombinant adenosine deaminase
PL2147122T3 (pl) * 2007-04-20 2015-05-29 Leadiant Biosciences Ltd Enzymatyczna terapia przeciwnowotworowa
BRPI0721948A2 (pt) * 2007-08-20 2014-04-08 Enzon Pharmaceuticals Inc Ligantes poliméricos contendo frações dissulfeto de piridila
PT3057585T (pt) 2013-10-15 2020-10-21 Seagen Inc Fármaco-ligadores peguilados para farmacocinética melhorada de conjugados de fármaco-ligando
EP3433278A4 (en) 2016-03-25 2019-11-06 Seattle Genetics, Inc. METHOD FOR THE PRODUCTION OF PEGYLATED ACTIVE LINKERS AND INTERMEDIATE PRODUCTS THEREOF
JP7527787B2 (ja) 2017-03-24 2024-08-05 シージェン インコーポレイテッド グルクロニド薬物－リンカーの調製のためのプロセスおよびその中間体

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US4179337A (en) 1973-07-20 1979-12-18 Davis Frank F Non-immunogenic polypeptides
DE4135115A1 (de) 1991-10-24 1993-04-29 Trigon Chemie Gmbh Kationaktive tenside
US5679711A (en) 1993-10-08 1997-10-21 Fhj Scientific, Inc. Hydroxyl ions as novel therapeutic agents and compounds that modulate these ions, compositions employing these agents, therapeutic methods for using such agents
US5643575A (en) 1993-10-27 1997-07-01 Enzon, Inc. Non-antigenic branched polymer conjugates
US5919455A (en) 1993-10-27 1999-07-06 Enzon, Inc. Non-antigenic branched polymer conjugates
MXPA04007809A (es) 2002-02-25 2004-10-15 Kudos Pharm Ltd Piranonas utiles como inhibidores de ataxia-telangetaxia mutada.
US7087229B2 (en) * 2003-05-30 2006-08-08 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7122189B2 (en) 2002-08-13 2006-10-17 Enzon, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7413738B2 (en) 2002-08-13 2008-08-19 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on biodegradable linkers
AU2003287605A1 (en) 2002-11-12 2004-06-03 Enzon Pharmaceuticals, Inc. Polymeric prodrugs of vancomycin
US7332164B2 (en) 2003-03-21 2008-02-19 Enzon Pharmaceuticals, Inc. Heterobifunctional polymeric bioconjugates
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Non-Patent Citations (2)

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GREENWALD等.A new aliphatic amino prodrug system for the delivery of smallmolecules and proteions utilizing novel PEG derivatives.J. Med. Chem.47 3.2004,47(3),726-734.
GREENWALD等.A new aliphatic amino prodrug system for the delivery of smallmolecules and proteions utilizing novel PEG derivatives.J. Med. Chem.47 3.2004,47(3),726-734. *

Also Published As

Publication number Publication date
AU2005316520B2 (en) 2011-09-29
KR20070089739A (ko) 2007-08-31
IL183582A0 (en) 2007-09-20
WO2006066020A2 (en) 2006-06-22
CA2589975A1 (en) 2006-06-22
JP2008523239A (ja) 2008-07-03
AU2005316520A1 (en) 2006-06-22
TWI375556B (en) 2012-11-01
WO2006066020A3 (en) 2006-08-10
RU2007126802A (ru) 2009-01-27
US7413738B2 (en) 2008-08-19
EP1827497A2 (en) 2007-09-05
MX2007007034A (es) 2007-08-03
CN101076353A (zh) 2007-11-21
JP5405746B2 (ja) 2014-02-05
US8192743B2 (en) 2012-06-05
CA2589975C (en) 2013-12-10
US20080305070A1 (en) 2008-12-11
TW200635576A (en) 2006-10-16
US20050197290A1 (en) 2005-09-08
EP1827497A4 (en) 2010-09-29

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Granted publication date: 20101208

Termination date: 20131213