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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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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Enzon Pharmaceuticals 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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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US7087229B2 (en) * 2003-05-30 2006-08-08 Enzon Pharmaceuticals, 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
US7122189B2 (en) * 2002-08-13 2006-10-17 Enzon, 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
ATE440856T1 (de) * 2005-05-04 2009-09-15 Lonza Ag Festphasengebundenes thymosin-alpha1 und dessen synthese
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
JP2009539879A (ja) * 2006-06-09 2009-11-19 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 インデノイソキノリン放出性ポリマー複合体
US8110559B2 (en) * 2006-09-15 2012-02-07 Enzon Pharmaceuticals, Inc. Hindered ester-based biodegradable linkers for oligonucleotide delivery
BRPI0716823A2 (pt) * 2006-09-15 2015-05-26 Enzon Pharmaceuticals Inc Conjunto poliméricos contendo porções positivamente carregadas
EP2063912A4 (en) * 2006-09-15 2010-07-28 Enzon Pharmaceuticals Inc POLYALKYLENE OXIDES HAVING BIODEGRADABLE BOND SEGMENTS BASED ON COARSE ESTER
BRPI0716808A2 (pt) * 2006-09-15 2013-11-05 Enzon Pharmaceuticals Inc Ligantes poliméricos baseados em lisina
US20100279408A1 (en) * 2006-11-27 2010-11-04 Enzon Pharmaceuticals, Inc. Polymeric short interfering rna conjugates
CA2671209A1 (en) * 2006-12-29 2008-07-10 Enzon Pharmaceuticals, Inc. Use of adenosine deaminase for treating pulmonary disease
PL2147116T3 (pl) * 2007-04-20 2016-08-31 Leadiant Biosciences Ltd Stabilna rekombinowana dezaminaza adenozynowa
TWI486169B (zh) * 2007-04-20 2015-06-01 Sigma Tau Rare Diseases S A 酵素性抗癌療法
JP2010536986A (ja) * 2007-08-20 2010-12-02 エンゾン ファーマシューティカルズ，インコーポレーテッド ピリジルジスルフィド部分を含有するポリマーリンカー
NZ758050A (en) 2013-10-15 2024-03-22 Seagen Inc Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics
JP7073266B2 (ja) 2016-03-25 2022-05-23 シージェン インコーポレイテッド Ｐｅｇ化薬物リンカー及びその中間体を調製するためのプロセス
KR102648564B1 (ko) 2017-03-24 2024-03-19 씨젠 인크. 글루쿠로니드 약물-링커의 제조 공정 및 그 중간물

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DE4135115A1 (de) 1991-10-24 1993-04-29 Trigon Chemie Gmbh Kationaktive tenside
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US5919455A (en) 1993-10-27 1999-07-06 Enzon, Inc. Non-antigenic branched polymer conjugates
US5643575A (en) 1993-10-27 1997-07-01 Enzon, Inc. Non-antigenic branched polymer conjugates
EP2174939A1 (en) 2002-02-25 2010-04-14 Kudos Pharmaceuticals Limited Pyranones useful as ATM inhibitors
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
US7087229B2 (en) 2003-05-30 2006-08-08 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7273845B2 (en) 2002-11-12 2007-09-25 Enzon Pharmaceuticals, Inc. Polymeric prodrugs of vancomycin
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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. *

Also Published As

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

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Granted publication date: 20101208

Termination date: 20131213