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WO2005021043A3 - High-molecular-mass prodrugs - Google Patents

High-molecular-mass prodrugs Download PDF

Info

Publication number
WO2005021043A3
WO2005021043A3 PCT/FR2004/002162 FR2004002162W WO2005021043A3 WO 2005021043 A3 WO2005021043 A3 WO 2005021043A3 FR 2004002162 W FR2004002162 W FR 2004002162W WO 2005021043 A3 WO2005021043 A3 WO 2005021043A3
Authority
WO
WIPO (PCT)
Prior art keywords
prodrugs
molecular
mass
spacer
prodrug form
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/FR2004/002162
Other languages
French (fr)
Other versions
WO2005021043A2 (en
Inventor
Andre Trouet
Vincent Dubois
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.)
Diatos SA
Original Assignee
Diatos SA
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
Application filed by Diatos SA filed Critical Diatos SA
Priority to AU2004268405A priority Critical patent/AU2004268405A1/en
Priority to JP2006523656A priority patent/JP2007503382A/en
Priority to EP04786328A priority patent/EP1701743A2/en
Priority to CA002536442A priority patent/CA2536442A1/en
Priority to BRPI0413843-0A priority patent/BRPI0413843A/en
Publication of WO2005021043A2 publication Critical patent/WO2005021043A2/en
Priority to IL173760A priority patent/IL173760A0/en
Priority to US11/357,966 priority patent/US20060281897A1/en
Anticipated expiration legal-status Critical
Publication of WO2005021043A3 publication Critical patent/WO2005021043A3/en
Ceased legal-status Critical Current

Links

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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)

Abstract

The invention relates to a modified prodrug form. According to the invention, a typical prodrug form comprises a bulky group, a spacer, a cleavable structure in the circulatory system and a therapeutic agent or a marker, said spacer enabling or facilitating the cleavage of the cleavable structure.
PCT/FR2004/002162 2003-08-22 2004-08-19 High-molecular-mass prodrugs Ceased WO2005021043A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
AU2004268405A AU2004268405A1 (en) 2003-08-22 2004-08-19 Potentiation of the activation of high-molecular-mass prodrugs
JP2006523656A JP2007503382A (en) 2003-08-22 2004-08-19 Possible activation of high molecular weight prodrugs
EP04786328A EP1701743A2 (en) 2003-08-22 2004-08-19 Potentiation of the activation of high-molecular-mass prodrugs
CA002536442A CA2536442A1 (en) 2003-08-22 2004-08-19 Potentiation of the activation of high-molecular-mass prodrugs
BRPI0413843-0A BRPI0413843A (en) 2003-08-22 2004-08-19 enhancement of activation of high molecular weight prodrugs
IL173760A IL173760A0 (en) 2003-08-22 2006-02-16 Potentialization of the activation of high-molecular-mass prodrugs
US11/357,966 US20060281897A1 (en) 2003-08-22 2006-02-22 Potentialization of the activation of high molecular weight prodrugs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0310114A FR2858936A1 (en) 2003-08-22 2003-08-22 New active compound precursor, useful as therapeutic or diagnostic agent or tracer, includes cleavable component that increases half-life in the circulation, attached through hydrophilic spacer
FR0310114 2003-08-22

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/357,966 Continuation-In-Part US20060281897A1 (en) 2003-08-22 2006-02-22 Potentialization of the activation of high molecular weight prodrugs

Publications (2)

Publication Number Publication Date
WO2005021043A2 WO2005021043A2 (en) 2005-03-10
WO2005021043A3 true WO2005021043A3 (en) 2006-06-15

Family

ID=34112859

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/FR2004/002162 Ceased WO2005021043A2 (en) 2003-08-22 2004-08-19 High-molecular-mass prodrugs

Country Status (8)

Country Link
EP (1) EP1701743A2 (en)
JP (1) JP2007503382A (en)
AU (1) AU2004268405A1 (en)
BR (1) BRPI0413843A (en)
CA (1) CA2536442A1 (en)
FR (1) FR2858936A1 (en)
IL (1) IL173760A0 (en)
WO (1) WO2005021043A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007530569A (en) * 2004-03-23 2007-11-01 アムジエン・インコーポレーテツド Chemically modified protein composition and method
EP3660162A1 (en) * 2005-12-27 2020-06-03 McMaster University Enzyme measurement assay using a modified substrate comprising a substrate attached to a macromolecule via a spacer
CA2645347A1 (en) * 2006-03-10 2007-09-20 Diatos Anticancer drugs conjugated to antibody via an enzyme cleavable linker
AU2009302387B2 (en) 2008-10-07 2014-12-04 Rexahn Pharmaceuticals, Inc HPMA - docetaxel or gemcitabine conjugates and uses therefore
KR20100083632A (en) * 2009-01-14 2010-07-22 울산대학교 산학협력단 Anticancer prodrug sensitive to target protease
BR112012008772A2 (en) 2009-10-13 2017-06-20 Rexahn Pharmaceuticals Inc polymeric systems for releasing anti-cancer agents
US12358957B2 (en) 2017-01-12 2025-07-15 Revolo Biotherapeutics Limited Method for the acute treatment of atopic dermatitis and allergic skin hypersensitivity
GB201700555D0 (en) 2017-01-12 2017-03-01 Peptinnovate Ltd Method for the treatment of a relapsing-remitting condition
GB201700557D0 (en) * 2017-01-12 2017-03-01 Peptinnovate Ltd Novel peptides

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996005863A1 (en) * 1994-08-19 1996-02-29 La Region Wallonne Compounds, pharmaceutical composition and diagnostic device comprising same and their use
WO2001091798A2 (en) * 2000-06-01 2001-12-06 Universite Catholique De Louvain Tumor activated prodrug compounds
WO2001095945A2 (en) * 2000-06-14 2001-12-20 Medarex, Inc. Prodrug compounds cleavable by thimet oligopeptidase

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996005863A1 (en) * 1994-08-19 1996-02-29 La Region Wallonne Compounds, pharmaceutical composition and diagnostic device comprising same and their use
WO2001091798A2 (en) * 2000-06-01 2001-12-06 Universite Catholique De Louvain Tumor activated prodrug compounds
WO2001095945A2 (en) * 2000-06-14 2001-12-20 Medarex, Inc. Prodrug compounds cleavable by thimet oligopeptidase

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
GREENWALD R B ET AL: "Effective drug delivery by PEGylated drug conjugates", ADVANCED DRUG DELIVERY REVIEWS 10 FEB 2003 NETHERLANDS, vol. 55, no. 2, 10 February 2003 (2003-02-10), pages 217 - 250, XP002275066, ISSN: 0169-409X *
KRATZ FELIX ET AL: "Development and in vitro efficacy of novel MMP2 and MMP9 specific doxorubicin albumin conjugates", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 11, no. 15, 6 August 2001 (2001-08-06), pages 2001 - 2006, XP002360788, ISSN: 0960-894X *
MANSOUR AHMED M ET AL: "A new approach for the treatment of malignant melanoma: Enhanced antitumor efficacy of an albumin-binding doxorubicin prodrug that is cleaved by matrix metalloproteinase 2.", CANCER RESEARCH, vol. 63, no. 14, 15 July 2003 (2003-07-15), pages 4062 - 4066, XP002360787, ISSN: 0008-5472 *

Also Published As

Publication number Publication date
AU2004268405A1 (en) 2005-03-10
FR2858936A1 (en) 2005-02-25
JP2007503382A (en) 2007-02-22
BRPI0413843A (en) 2006-10-24
CA2536442A1 (en) 2005-03-10
WO2005021043A2 (en) 2005-03-10
IL173760A0 (en) 2006-07-05
EP1701743A2 (en) 2006-09-20

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