WO2006069388A3 - Stabilized polymeric thiol reagents - Google Patents

Stabilized polymeric thiol reagents Download PDF

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Publication number
WO2006069388A3
WO2006069388A3 PCT/US2005/047337 US2005047337W WO2006069388A3 WO 2006069388 A3 WO2006069388 A3 WO 2006069388A3 US 2005047337 W US2005047337 W US 2005047337W WO 2006069388 A3 WO2006069388 A3 WO 2006069388A3
Authority
WO
WIPO (PCT)
Prior art keywords
water soluble
thiol
stabilized polymeric
thiol reagents
polymeric thiol
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2005/047337
Other languages
French (fr)
Other versions
WO2006069388A2 (en
Inventor
Antoni Kozlowski
Samuel Mcmanus
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nektar Therapeutics AL Corp
Original Assignee
Nektar Therapeutics AL Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36440883&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2006069388(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to KR1020077014146A priority Critical patent/KR101320936B1/en
Priority to CA2591233A priority patent/CA2591233C/en
Priority to AU2005318984A priority patent/AU2005318984B2/en
Priority to AT05855832T priority patent/ATE494012T1/en
Priority to JP2007548599A priority patent/JP5243041B2/en
Application filed by Nektar Therapeutics AL Corp filed Critical Nektar Therapeutics AL Corp
Priority to MX2007007471A priority patent/MX2007007471A/en
Priority to CN2005800475071A priority patent/CN101111267B/en
Priority to EP05855832.1A priority patent/EP1827501B2/en
Priority to DE602005025805T priority patent/DE602005025805D1/en
Publication of WO2006069388A2 publication Critical patent/WO2006069388A2/en
Publication of WO2006069388A3 publication Critical patent/WO2006069388A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • C07D213/71—Sulfur atoms to which a second hetero atom is attached
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/10—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C323/11—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/12—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Polyethers (AREA)
  • Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)

Abstract

Disclosed are water soluble polymeric reagents comprising the structure POLY-[Y-S-W]x,, where POLY is a water soluble polymer; Y is a hydrocarbon­based spacer group, x is 1 to 25, and S-W is a thiol, protected thiol, or thiol-reactive derivative. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are conjugates of such polymeric reagents with pharmaceutically relevant molecules, and methods of their formation and use.
PCT/US2005/047337 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents Ceased WO2006069388A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
DE602005025805T DE602005025805D1 (en) 2004-12-21 2005-12-21 STABILIZED POLYMER THIOL REAGENTS
CN2005800475071A CN101111267B (en) 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents
AU2005318984A AU2005318984B2 (en) 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents
AT05855832T ATE494012T1 (en) 2004-12-21 2005-12-21 STABILIZED POLYMER THIOL REAGENTS
JP2007548599A JP5243041B2 (en) 2004-12-21 2005-12-21 Stabilized polymer thiol reagent
KR1020077014146A KR101320936B1 (en) 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents
MX2007007471A MX2007007471A (en) 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents.
CA2591233A CA2591233C (en) 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents
EP05855832.1A EP1827501B2 (en) 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US63982304P 2004-12-21 2004-12-21
US60/639,823 2004-12-21
US70596805P 2005-08-04 2005-08-04
US60/705,968 2005-08-04

Publications (2)

Publication Number Publication Date
WO2006069388A2 WO2006069388A2 (en) 2006-06-29
WO2006069388A3 true WO2006069388A3 (en) 2007-05-31

Family

ID=36440883

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2005/047337 Ceased WO2006069388A2 (en) 2004-12-21 2005-12-21 Stabilized polymeric thiol reagents

Country Status (12)

Country Link
US (5) US7851565B2 (en)
EP (1) EP1827501B2 (en)
JP (1) JP5243041B2 (en)
KR (1) KR101320936B1 (en)
CN (1) CN101111267B (en)
AT (1) ATE494012T1 (en)
AU (1) AU2005318984B2 (en)
CA (1) CA2591233C (en)
DE (1) DE602005025805D1 (en)
ES (1) ES2357089T5 (en)
MX (1) MX2007007471A (en)
WO (1) WO2006069388A2 (en)

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US7771751B2 (en) 2005-08-31 2010-08-10 Abraxis Bioscience, Llc Compositions comprising poorly water soluble pharmaceutical agents and antimicrobial agents
US7981445B2 (en) 2005-08-31 2011-07-19 Abraxis Bioscience, Llc Compositions and methods for preparation of poorly water soluble drugs with increased stability

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JP5243041B2 (en) * 2004-12-21 2013-07-24 ネクター セラピューティックス Stabilized polymer thiol reagent
BRPI0614257A2 (en) * 2005-08-04 2011-03-15 Nektar Therapeutics Al Corp conjugates of a portion of g-csf and a polymer
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WO2009052148A1 (en) 2007-10-15 2009-04-23 California Institute Of Technology Functionalized polymers using protected thiols
WO2009103199A1 (en) * 2008-02-18 2009-08-27 江苏恒瑞医药股份有限公司 A g-csf conjugate modified by water-soluble polymer
WO2009143412A2 (en) * 2008-05-23 2009-11-26 Enzon Pharmaceuticals, Inc. Polymeric systems containing intracellular releasable disulfide linker for the delivery of oligonucleotides
US20120128587A1 (en) * 2009-07-31 2012-05-24 Endocyte, Inc. Folate-targeted diagnostics and treatment
CA2796729C (en) 2010-04-20 2020-06-23 Octapharma Ag Melezitose for stabilizing human blood plasma proteins
JP2019043961A (en) * 2010-04-20 2019-03-22 オクタファルマ・アーゲー Novel stabilizer for pharmaceutical proteins
CN101885841B (en) * 2010-07-02 2012-05-16 清华大学 A polymer that can undergo addition reactions with sulfhydryl groups and is bonded and hydrolytically stable
WO2012021791A2 (en) * 2010-08-13 2012-02-16 Scidose Llc Aqueous formulation with improved stability
UA116217C2 (en) 2012-10-09 2018-02-26 Санофі Exendin-4 derivatives as dual glp1/glucagon agonists
HUE035803T2 (en) 2012-12-21 2018-05-28 Sanofi Sa Dual glp1/gip or trigonal glp1/gip/glucagon agonists
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WO2015086730A1 (en) 2013-12-13 2015-06-18 Sanofi Non-acylated exendin-4 peptide analogues
WO2015086728A1 (en) 2013-12-13 2015-06-18 Sanofi Exendin-4 peptide analogues as dual glp-1/gip receptor agonists
TW201625669A (en) 2014-04-07 2016-07-16 賽諾菲公司 Peptidic dual GLP-1/glucagon receptor agonists derived from Exendin-4
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7771751B2 (en) 2005-08-31 2010-08-10 Abraxis Bioscience, Llc Compositions comprising poorly water soluble pharmaceutical agents and antimicrobial agents
US7981445B2 (en) 2005-08-31 2011-07-19 Abraxis Bioscience, Llc Compositions and methods for preparation of poorly water soluble drugs with increased stability
US8034765B2 (en) 2005-08-31 2011-10-11 Abraxis Bioscience, Llc Compositions and methods for preparation of poorly water soluble drugs with increased stability
US9308180B2 (en) 2005-08-31 2016-04-12 Abraxis Bioscience, Llc Compositions and methods for preparation of poorly water soluble drugs with increased stability

Also Published As

Publication number Publication date
ES2357089T5 (en) 2014-02-24
US20120258985A1 (en) 2012-10-11
US8217123B2 (en) 2012-07-10
US20110112277A1 (en) 2011-05-12
EP1827501A2 (en) 2007-09-05
ES2357089T3 (en) 2011-04-18
AU2005318984B2 (en) 2011-12-01
JP5243041B2 (en) 2013-07-24
CA2591233A1 (en) 2006-06-29
JP2008524338A (en) 2008-07-10
EP1827501B2 (en) 2013-11-20
US20140256951A1 (en) 2014-09-11
US20130280206A1 (en) 2013-10-24
ATE494012T1 (en) 2011-01-15
US8765883B2 (en) 2014-07-01
US20060135586A1 (en) 2006-06-22
US8492488B2 (en) 2013-07-23
KR101320936B1 (en) 2013-10-23
US9308274B2 (en) 2016-04-12
CA2591233C (en) 2014-10-07
US7851565B2 (en) 2010-12-14
CN101111267B (en) 2012-12-05
EP1827501B1 (en) 2011-01-05
WO2006069388A2 (en) 2006-06-29
CN101111267A (en) 2008-01-23
MX2007007471A (en) 2007-07-20
AU2005318984A1 (en) 2006-06-29
DE602005025805D1 (en) 2011-02-17
KR20070088727A (en) 2007-08-29

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