WO2001007013A3 - Thioamide moiety-containing polymer drug conjugates - Google Patents

Thioamide moiety-containing polymer drug conjugates Download PDF

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Publication number
WO2001007013A3
WO2001007013A3 PCT/US2000/020090 US0020090W WO0107013A3 WO 2001007013 A3 WO2001007013 A3 WO 2001007013A3 US 0020090 W US0020090 W US 0020090W WO 0107013 A3 WO0107013 A3 WO 0107013A3
Authority
WO
WIPO (PCT)
Prior art keywords
polymer
thioamide
conjugate
therapeutic
agents
Prior art date
Application number
PCT/US2000/020090
Other languages
French (fr)
Other versions
WO2001007013A9 (en
WO2001007013A2 (en
Inventor
Stanley Stein
Guobao Zhang
Bo Qiu
Original Assignee
Univ New Jersey Med
Stanley Stein
Guobao Zhang
Bo Qiu
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
Priority claimed from US09/621,109 external-priority patent/US6468522B1/en
Application filed by Univ New Jersey Med, Stanley Stein, Guobao Zhang, Bo Qiu filed Critical Univ New Jersey Med
Priority to CA002380050A priority Critical patent/CA2380050A1/en
Priority to AU63685/00A priority patent/AU6368500A/en
Publication of WO2001007013A2 publication Critical patent/WO2001007013A2/en
Publication of WO2001007013A3 publication Critical patent/WO2001007013A3/en
Publication of WO2001007013A9 publication Critical patent/WO2001007013A9/en

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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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

This invention pertains to disulfide-linked conjugates of therapeutic agents containing at least one thioamide group with polymer comprising at least one thiol group, so as to provide a controlled release pharmaceutical composition for administration to animals for the prophylaxis or treatment of various conditions or diseases. The therapeutic agent conjugate may comprise an inactive or weakly active prodrug form which may be converted into the original therapeutic compound by the natural action of reducing agents in vivo. The composition may comprise a mixture of polymers each with a different thioamide-containing agent attached, or a polymer conjugated with a mixture of thioamide-containing agents. Modified properties of the therapeutic compound potentially provided by the polymer itself, as well as by other compounds also appended to the polymer, include but are not limited to greater water solubility, longer in vivo half-life (due to larger size of the conjugate), slower release from a sustained-release depot (due to larger size of the conjugate), better oral bioavailability and tissue-specific targeting.
PCT/US2000/020090 1999-07-22 2000-07-24 Thioamide moiety-containing polymer drug conjugates WO2001007013A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CA002380050A CA2380050A1 (en) 1999-07-22 2000-07-24 Materials and processes for controlled release of thioamide moiety-containing therapeutic agents by linking to thiol-containing polymers
AU63685/00A AU6368500A (en) 1999-07-22 2000-07-24 Materials and processes for controlled release of thioamide moiety-containing therapeutic agents by linking to thiol-containing polymers

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US35851599A 1999-07-22 1999-07-22
US09/358,515 1999-07-22
US09/621,109 2000-07-21
US09/621,109 US6468522B1 (en) 1999-07-22 2000-07-21 Controlled release of thioamide moiety-containing therapeutic agents

Publications (3)

Publication Number Publication Date
WO2001007013A2 WO2001007013A2 (en) 2001-02-01
WO2001007013A3 true WO2001007013A3 (en) 2001-10-25
WO2001007013A9 WO2001007013A9 (en) 2002-11-14

Family

ID=27000094

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/020090 WO2001007013A2 (en) 1999-07-22 2000-07-24 Thioamide moiety-containing polymer drug conjugates

Country Status (3)

Country Link
AU (1) AU6368500A (en)
CA (1) CA2380050A1 (en)
WO (1) WO2001007013A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101466409B (en) * 2006-06-09 2012-11-21 赛诺菲-安万特 Leptomycin derivatives

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1581582B2 (en) 2003-01-06 2017-06-07 Nektar Therapeutics Thiol-selective water-soluble polmer derivatives

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BORKOW G ET AL: "CHEMICAL BARRIERS TO HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION: RETROVIRUCIDAL ACTIVITY OF UC781, A THIOCARBOXANILIDE NONNUCLEOSIDE INHIBITOR OF HIV-1 REVERSE TRANSCRIPTASE", JOURNAL OF VIROLOGY,US,THE AMERICAN SOCIETY FOR MICROBIOLOGY, vol. 71, no. 4, 1 April 1997 (1997-04-01), pages 3023 - 3030, XP002037328, ISSN: 0022-538X *
HUANG ET AL: "A Polyethylene Glycol Copolymer for Carrying and Releasing Multiple Copies of Cysteine-Containing Peptides", BIOCONJUGATE CHEMISTRY,US,AMERICAN CHEMICAL SOCIETY, WASHINGTON, vol. 9, no. 5, 1998, pages 612 - 617, XP002117430, ISSN: 1043-1802 *
KIRPOTIN D ET AL: "LIPOSOMES WITH DETACHHABLE POLYMER COATING: DESTABILIZATION AND FUSION OF DIOLEOYLPHOSPHATIDYLETHANOLAMINE VESCLES TRIGGERED BY CLEAVAGE OF SURFACE-GRAFTED POLY(ETHYLENE GLYCOL)", FEBS LETTERS,ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM,NL, vol. 388, no. 2/03, 17 June 1996 (1996-06-17), pages 115 - 118, XP000858878, ISSN: 0014-5793 *
VINCENTELLI JEAN ET AL: "Poly(ethylene glycol) derivatized prodrugs through mixed disulfide bond formation: Preliminary report on captopril.", INTERNATIONAL JOURNAL OF PHARMACEUTICS (AMSTERDAM), vol. 134, no. 1-2, 1996, pages 147 - 155, XP000993165, ISSN: 0378-5173 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101466409B (en) * 2006-06-09 2012-11-21 赛诺菲-安万特 Leptomycin derivatives

Also Published As

Publication number Publication date
WO2001007013A9 (en) 2002-11-14
AU6368500A (en) 2001-02-13
CA2380050A1 (en) 2001-02-01
WO2001007013A2 (en) 2001-02-01

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