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WO2006060533A3 - Conjugates of 1, 8-bis-naphthalimides with an antibody - Google Patents

Conjugates of 1, 8-bis-naphthalimides with an antibody Download PDF

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Publication number
WO2006060533A3
WO2006060533A3 PCT/US2005/043409 US2005043409W WO2006060533A3 WO 2006060533 A3 WO2006060533 A3 WO 2006060533A3 US 2005043409 W US2005043409 W US 2005043409W WO 2006060533 A3 WO2006060533 A3 WO 2006060533A3
Authority
WO
WIPO (PCT)
Prior art keywords
antibody
adc
formula
relates
bis
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/US2005/043409
Other languages
French (fr)
Other versions
WO2006060533A2 (en
Inventor
Lewis J Gazzard
Edward Hyungsuk Ha
David Y Jackson
Joann Um
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.)
Genentech Inc
Original Assignee
Genentech Inc
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 Genentech Inc filed Critical Genentech Inc
Priority to JP2007544495A priority Critical patent/JP4993645B2/en
Priority to EP05852595A priority patent/EP1817059A2/en
Publication of WO2006060533A2 publication Critical patent/WO2006060533A2/en
Anticipated expiration legal-status Critical
Publication of WO2006060533A3 publication Critical patent/WO2006060533A3/en
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
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6849—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Investigating Or Analysing Materials By The Use Of Chemical Reactions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention relates to antibody drug conjugate (ADC) compounds represented by Formula:(I) where one or more 1,8 bis-naphthalimide drug moieties (D) having Formulas (IIa) and (Ilb)are covalently linked by a linker (L) to an antibody (Ab). The invention also relates to pharmaceutical compositions comprising an effective amount of a Formula I ADC for treatment of hyperproliferative disorders and other disorders. The invention also relates to methods for killing or inhibiting the multiplication of a tumor cell or cancer cell including administering to a patient an effective amount of a Formula (I) ADC.
PCT/US2005/043409 2004-12-01 2005-11-29 Conjugates of 1, 8-bis-naphthalimides with an antibody Ceased WO2006060533A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2007544495A JP4993645B2 (en) 2004-12-01 2005-11-29 Antibody drug conjugates and methods
EP05852595A EP1817059A2 (en) 2004-12-01 2005-11-29 Conjugates of 1,8-bis-naphthalimides with an antibody

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63261304P 2004-12-01 2004-12-01
US60/632,613 2004-12-01

Publications (2)

Publication Number Publication Date
WO2006060533A2 WO2006060533A2 (en) 2006-06-08
WO2006060533A3 true WO2006060533A3 (en) 2007-07-26

Family

ID=36263731

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2005/043409 Ceased WO2006060533A2 (en) 2004-12-01 2005-11-29 Conjugates of 1, 8-bis-naphthalimides with an antibody

Country Status (3)

Country Link
EP (1) EP1817059A2 (en)
JP (1) JP4993645B2 (en)
WO (1) WO2006060533A2 (en)

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US8008316B2 (en) 2006-09-12 2011-08-30 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Azonafide derived tumor and cancer targeting compounds
US8562693B2 (en) 2006-03-24 2013-10-22 L'oreal Method of dyeing and lightening keratin materials in the presence of a reducing agent comprising a fluorescent deisulphide dye
US8911732B2 (en) 2010-12-20 2014-12-16 Genentech, Inc. Anti-mesothelin antibodies and immunoconjugates
US9056910B2 (en) 2012-05-01 2015-06-16 Genentech, Inc. Anti-PMEL17 antibodies and immunoconjugates
US9175089B2 (en) 2012-03-30 2015-11-03 Genentech, Inc. Anti-LGR5 antibodies and immunoconjugates
US10981987B2 (en) 2007-07-16 2021-04-20 Genentech, Inc. Humanized anti-CD79b antibodies and immunoconjugates and methods of use
US11000510B2 (en) 2014-09-23 2021-05-11 Genentech, Inc. Methods of using anti-CD79b immunoconjugates

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US7947839B2 (en) 2004-12-01 2011-05-24 Genentech, Inc. Heterocyclic-substituted bis-1,8 naphthalimide compounds, antibody drug conjugates, and methods of use
US20070134243A1 (en) * 2004-12-01 2007-06-14 Gazzard Lewis J Antibody drug conjugates and methods
FR2898902B1 (en) * 2006-03-24 2010-09-10 Oreal PARTICULAR DYES OF THE NAPHTHALIMIDE TYPE, TINCTORIAL COMPOSITION COMPRISING AT LEAST ONE SUCH COLOR, PROCESS FOR CARRYING OUT AND USES
US8070830B2 (en) 2006-03-24 2011-12-06 L'oreal S.A. Fluorescent entity, dyeing composition containing at least one fluorescent entity comprising at least one heterocycle, with at least one internal cationic charge, and method for lightening keratin materials using said at least one fluorescent entity
WO2007110531A2 (en) * 2006-03-24 2007-10-04 L'oréal Dyeing composition containing a thiol/disulphide naphthylimide fluorescent colorant, and method for lightening keratin materials using said colorant
DK2176296T3 (en) 2007-07-16 2012-05-21 Genentech Inc Anti-CD79B antibodies and immune conjugates and methods of use.
FR2921381B1 (en) 2007-09-21 2009-10-30 Oreal HEMICYANINE STYRYLE THIOL / DISULFIDE DYE, TINCTORIAL COMPOSITION COMPRISING THE DYE, METHOD OF CLEANING KERATINIC MATERIALS FROM THAT COLORANT
FR2921377B1 (en) 2007-09-21 2009-10-30 Oreal STYRYL COMPOUND HAVING HYDROXY (CYCLO) ALKYLAMINO THIOL / DISULFIDE PATTERN, PROCESS FOR LIGHTENING KERATINIC MATERIALS THEREFROM
FR2921376B1 (en) 2007-09-21 2009-10-30 Oreal STYRYL TETRAHYDROQUINOLINIUM THIOL / DISULFIDE COMPOUND, PROCESS FOR CLEANING KERATINIC MATERIALS FROM THAT COLORANT
FR2921373B1 (en) 2007-09-21 2009-10-30 Oreal LINK ALKYLENE STYRYL INDOLE DERIVATIVE DYE, TINCTORIAL COMPOSITION COMPRISING THE DYE, METHOD FOR LIGHTENING KERATINIC MATERIALS FROM THAT COLORANT
US8119656B2 (en) 2007-12-07 2012-02-21 The Board Of Regents Of The University Of Texas System Inhibitors of the influenza virus non-structural 1 protein
US8420665B2 (en) 2008-01-11 2013-04-16 Northwestern University Anti-cancer compounds
DK2247620T3 (en) 2008-01-31 2016-08-22 Genentech Inc ANTI-CD79b ANTIBODIES AND IMMUNOCONJUGATES AND METHODS OF USE
WO2009144205A1 (en) 2008-05-30 2009-12-03 Basf Se Rylene-based semiconductor materials and methods of preparation and use thereof
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US9540486B2 (en) * 2012-05-02 2017-01-10 Lubrizol Advanced Materials, Inc. Aromatic dispersant composition
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