RU2487877C2 - Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры) - Google Patents

Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры) Download PDF

Info

Publication number
RU2487877C2
RU2487877C2 RU2010148740/04A RU2010148740A RU2487877C2 RU 2487877 C2 RU2487877 C2 RU 2487877C2 RU 2010148740/04 A RU2010148740/04 A RU 2010148740/04A RU 2010148740 A RU2010148740 A RU 2010148740A RU 2487877 C2 RU2487877 C2 RU 2487877C2
Authority
RU
Russia
Prior art keywords
antibody
cells
carbon atoms
chain
cell
Prior art date
Application number
RU2010148740/04A
Other languages
English (en)
Russian (ru)
Other versions
RU2010148740A (ru
Inventor
Раджиева Сингх
Елена Ковтун
Шарон Д. ВИЛЬХЕЛЬМ
Рави В. Дж. Чари
Original Assignee
Иммьюноджен, Инк.
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 Иммьюноджен, Инк. filed Critical Иммьюноджен, Инк.
Publication of RU2010148740A publication Critical patent/RU2010148740A/ru
Application granted granted Critical
Publication of RU2487877C2 publication Critical patent/RU2487877C2/ru

Links

Images

Classifications

    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • 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
    • A61K47/54—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 compound
    • 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
    • A61K47/68—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
    • A61K47/6801—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
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • 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
    • A61K47/6843—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 material from animals or humans
    • 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
    • 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
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • 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
    • A61K47/6863—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 the tumour determinant being from stomach or intestines cancer 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
    • A61K47/6891—Pre-targeting systems involving an antibody for targeting specific cells
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
RU2010148740/04A 2008-04-30 2009-04-30 Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры) RU2487877C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4928908P 2008-04-30 2008-04-30
US61/049,289 2008-04-30
PCT/US2009/042259 WO2009134976A1 (en) 2008-04-30 2009-04-30 Potent conjugates and hydrophilic linkers

Publications (2)

Publication Number Publication Date
RU2010148740A RU2010148740A (ru) 2012-06-10
RU2487877C2 true RU2487877C2 (ru) 2013-07-20

Family

ID=41255418

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2010148740/04A RU2487877C2 (ru) 2008-04-30 2009-04-30 Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры)

Country Status (16)

Country Link
US (3) US9150649B2 (cg-RX-API-DMAC7.html)
EP (1) EP2276506A4 (cg-RX-API-DMAC7.html)
JP (2) JP2011523628A (cg-RX-API-DMAC7.html)
KR (1) KR20100137585A (cg-RX-API-DMAC7.html)
CN (2) CN102083461B (cg-RX-API-DMAC7.html)
AU (1) AU2009243009B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0911442A2 (cg-RX-API-DMAC7.html)
CA (1) CA2722109A1 (cg-RX-API-DMAC7.html)
IL (1) IL208937A0 (cg-RX-API-DMAC7.html)
MX (1) MX2010011808A (cg-RX-API-DMAC7.html)
NZ (1) NZ588851A (cg-RX-API-DMAC7.html)
RU (1) RU2487877C2 (cg-RX-API-DMAC7.html)
SG (1) SG189817A1 (cg-RX-API-DMAC7.html)
UA (1) UA108598C2 (cg-RX-API-DMAC7.html)
WO (2) WO2009134952A2 (cg-RX-API-DMAC7.html)
ZA (1) ZA201007806B (cg-RX-API-DMAC7.html)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2653443C2 (ru) * 2016-07-15 2018-05-08 Закрытое Акционерное Общество "Биокад" Биспецифичные анти-her2/анти-her3 антитела
RU2754369C2 (ru) * 2016-03-02 2021-09-01 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конъюгаты антитело-лекарственное средство на основе эрибулина и способы применения
RU2844753C2 (ru) * 2016-03-02 2025-08-05 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конъюгаты антитело-лекарственное средство на основе эрибулина и способы применения

Families Citing this family (181)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7276497B2 (en) * 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
EP1789391B1 (en) 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
WO2007024536A2 (en) 2005-08-24 2007-03-01 Immunogen, Inc. Process for preparing maytansinoid antibody conjugates
CA2680535C (en) 2007-03-14 2016-09-20 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
BRPI0809435A2 (pt) 2007-03-27 2014-09-09 Sea Lane Biotechnologies, Llc Constructos e bibliotecas que compreendem sequências de cadeia leve substituida de anticorpos
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
CA2690943A1 (en) 2007-06-25 2008-12-31 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
SG189817A1 (en) 2008-04-30 2013-05-31 Immunogen Inc Potent conjugates and hydrophilic linkers
KR20230003298A (ko) 2008-04-30 2023-01-05 이뮤노젠 아이엔씨 가교제 및 그 용도
CN102482345A (zh) 2009-05-13 2012-05-30 航道生物技术有限责任公司 针对流感病毒的中和分子
SG176068A1 (en) * 2009-06-03 2011-12-29 Immunogen Inc Conjugation methods
AU2015201534B2 (en) * 2009-06-03 2016-11-24 Immunogen, Inc. Conjugation methods
FR2947269B1 (fr) 2009-06-29 2013-01-18 Sanofi Aventis Nouveaux composes anticancereux
FR2949469A1 (fr) * 2009-08-25 2011-03-04 Sanofi Aventis Derives anticancereux, leur preparation et leur application en therapeutique
AU2010292172A1 (en) 2009-09-09 2012-05-03 Centrose, Llc Extracellular targeted drug conjugates
TW201117814A (en) * 2009-10-02 2011-06-01 Sanofi Aventis New maytansinoids and the use of said maytansinoids to prepare conjugates with an antibody
EP2486023A4 (en) * 2009-10-06 2014-05-07 Immunogen Inc EFFICIENT CONJUGATES AND HYDROPHILIC BINDER
RS55738B1 (sr) 2010-02-24 2017-07-31 Immunogen Inc Imunokonjugati protiv folatnog receptora 1 i njihove upotrebe
EP3620467A1 (en) 2010-03-12 2020-03-11 Debiopharm International SA Cd37-binding molecules and immunoconjugates thereof
FR2963007B1 (fr) 2010-07-26 2013-04-05 Sanofi Aventis Derives anticancereux, leur preparation et leur application therapeutique
WO2012019024A2 (en) 2010-08-04 2012-02-09 Immunogen, Inc. Her3-binding molecules and immunoconjugates thereof
TW201302793A (zh) 2010-09-03 2013-01-16 Glaxo Group Ltd 新穎之抗原結合蛋白
EA201390575A1 (ru) 2010-10-29 2014-01-30 Иммьюноджен, Инк. Неантагонистические egfr-связывающие молекулы и их иммуноконъюгаты
MX2013004761A (es) 2010-10-29 2013-08-27 Immunogen Inc Nuevas moleculas de union al receptor del factor de crecimiento epidermico (egfr) e inmunoconjugados de estas.
MX2013005046A (es) * 2010-11-03 2013-12-12 Immunogen Inc Agentes citotoxicos que comprenden nuevos derivados de ansamitocina.
CN103313990B (zh) * 2010-11-17 2016-07-20 基因泰克公司 丙氨酰美登醇抗体偶联物
CN103260406B (zh) 2010-12-09 2016-10-19 伊缪诺金公司 制备带电荷交联剂的方法
DK2675480T3 (en) 2011-02-15 2019-04-15 Immunogen Inc PROCEDURES FOR PREPARING CONJUGATES
WO2012122514A1 (en) * 2011-03-09 2012-09-13 Centrose, Llc Extracellular targeted drug conjugates
MY171008A (en) 2011-03-29 2019-09-23 Immunogen Inc Preparation of maytansinoid antibody conjugates by a one-step process
CN103717262B (zh) 2011-03-29 2017-09-15 伊缪诺金公司 通过一步法制备类美登素抗体缀合物
BR112013025415B1 (pt) 2011-04-01 2021-03-16 Immunogen, Inc uso de um imunoconjugado antirreceptor de folato 1 (folr1)
WO2012138749A1 (en) * 2011-04-04 2012-10-11 Immunogen, Inc. Methods for decreasing ocular toxicity of antibody drug conjugates
ME03071B (me) 2011-04-21 2019-01-20 Bristol Myers Squibb Co Polipeptidi antitela koji antagonizuju cd40
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
TWI597065B (zh) 2011-06-10 2017-09-01 梅爾莎納醫療公司 蛋白質－聚合物－藥物共軛體
US10300140B2 (en) 2011-07-28 2019-05-28 I2 Pharmaceuticals, Inc. Sur-binding proteins against ERBB3
MX2014006087A (es) 2011-11-21 2014-08-01 Immunogen Inc Metodo de tratamiento de tumores que son resistentes a terapias contra el receptor del factor de crecimiento epidermico (egfr) con agentes citotoxicos conjugados con anticuerpos dirigidos contra el receptor del factor de crecimiento epidermico.
WO2013096828A1 (en) 2011-12-22 2013-06-27 Sea Lane Biotechnologies, Llc Surrogate binding proteins
RU2624731C2 (ru) * 2012-01-27 2017-07-06 Ф. Хоффманн-Ля Рош Аг Конъюгаты антагонистов интегрина для нацеленной доставки к клеткам, экспрессирующим vla-4
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
MX362514B (es) 2012-08-31 2019-01-22 Immunogen Inc Kits y ensayos de diagnostico para la deteccion del receptor 1 de folato.
MX359599B (es) 2012-10-04 2018-09-12 Immunogen Inc Uso de una membrana de pvdf para purificar conjugados de agentes de unión celular y agentes citotóxicos.
US20150306242A1 (en) * 2012-10-04 2015-10-29 Immunogen, Inc. Process for preparing stable antibody maytansinoid conjugates
IN2015DN04147A (cg-RX-API-DMAC7.html) 2012-10-16 2015-10-16 Endocyte Inc
NO2789793T3 (cg-RX-API-DMAC7.html) * 2012-10-24 2018-01-27
IN2015DN02349A (cg-RX-API-DMAC7.html) * 2012-10-24 2015-08-28 Polytherics Ltd
EP2922818B1 (en) 2012-11-24 2018-09-05 Hangzhou Dac Biotech Co., Ltd Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
WO2014089177A2 (en) 2012-12-04 2014-06-12 Massachusetts Institute Of Technology Compounds, conjugates and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines
CN103288957B (zh) 2012-12-21 2015-01-28 百奥泰生物科技(广州)有限公司 一种抑制肿瘤生长的抗体药物衍生物及其制备方法和用途
CN104650113A (zh) * 2012-12-21 2015-05-27 百奥泰生物科技(广州)有限公司 类美登素衍生物及其制备方法和用途
US9968673B2 (en) * 2013-02-26 2018-05-15 Commissariat á l'ènergie atomique et aux ènergies alternatives Immunogenic composition in emulsion form comprising two dispersed phases, one comprising an antigen and the other comprising an immunostimulating agent
FR3002454B1 (fr) * 2013-02-26 2015-04-10 Commissariat Energie Atomique Composition immunogene sous forme d'emulsion
WO2014134483A2 (en) * 2013-02-28 2014-09-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
CN110143999B (zh) 2013-03-15 2023-12-05 酵活英属哥伦比亚省公司 具细胞毒性和抗有丝分裂的化合物以及其使用方法
MY183572A (en) 2013-03-15 2021-02-26 Regeneron Pharma Biologically active molecules, conjugates thereof, and therapeutic uses
MX370829B (es) * 2013-05-02 2020-01-08 Hoffmann La Roche Uso de un anticuerpo para cd20 afucosilado con un conjugado de anticuerpo para cd22-fármaco.
US10208125B2 (en) 2013-07-15 2019-02-19 University of Pittsburgh—of the Commonwealth System of Higher Education Anti-mucin 1 binding agents and uses thereof
TWI641620B (zh) * 2013-08-21 2018-11-21 再生元醫藥公司 抗－ｐｒｌｒ抗體及其用途
CN105530942B (zh) 2013-08-26 2019-10-11 瑞泽恩制药公司 一种包含大环内酯类非对映体的药物组合物、其制备方法和用途
PL3038650T3 (pl) 2013-08-30 2021-11-22 Immunogen, Inc. Przeciwciała i testy do wykrywania receptora folianu 1
SG10201801779XA (en) 2013-09-05 2018-04-27 Jackson Lab Compositions for rna-chromatin interaction analysis and uses thereof
IL298044B2 (en) 2013-10-08 2024-11-01 Immunogen Inc Dosing regimens of anti-FOLR1 immunoconjugate
CN105813655B (zh) 2013-10-11 2022-03-15 阿萨纳生物科技有限责任公司 蛋白-聚合物-药物缀合物
CN105979970B (zh) 2013-10-11 2019-09-10 梅尔莎纳医疗公司 蛋白质-聚合物-药物共轭物
CN103483357B (zh) * 2013-10-12 2015-11-18 齐鲁制药有限公司 一种抗体-美登素偶联物的中间体新晶型及其制备方法
WO2015081857A1 (en) * 2013-12-02 2015-06-11 Hong Kong Baptist University Anticancer maytansinoids with two fused macrocyclic rings
JP6560681B2 (ja) 2013-12-27 2019-08-14 ザイムワークス インコーポレイティド 薬物結合体のためのスルホンアミド含有連結系
AU2015210578B2 (en) * 2014-01-29 2020-04-16 Jiangsu Hengrui Medicine Co., Ltd. Ligand-cytotoxic drug conjugate, preparation method therefor, and uses thereof
MY178160A (en) 2014-03-11 2020-10-06 Regeneron Pharma Anti-egfrviii antibodies and uses thereof
JP6805425B2 (ja) 2014-03-24 2020-12-23 ザ・トラスティーズ・オブ・コランビア・ユニバーシティー・イン・ザ・シティー・オブ・ニューヨーク タグ付けされたヌクレオチドを製造するための化学的方法
EP3138568B1 (en) * 2014-04-29 2019-04-17 Genequantum Healthcare (Suzhou) Co., Ltd. New stable antibody-drug conjugate, preparation method therefor, and use thereof
CA2953371C (en) 2014-06-30 2021-08-24 Tarveda Therapeutics, Inc. Targeted conjugates and particles and formulations thereof
DK3160513T3 (da) 2014-06-30 2020-04-06 Glykos Finland Oy Saccharidderivat af en toksisk payload og antistofkonjugater deraf
CA2958882A1 (en) 2014-09-02 2016-03-10 Immunogen, Inc. Methods for formulating antibody drug conjugate compositions
WO2016036804A1 (en) 2014-09-03 2016-03-10 Immunogen, Inc. Cytotoxic benzodiazepine derivatives
EP3188733B1 (en) * 2014-09-03 2019-11-06 ImmunoGen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
SG11201701455SA (en) 2014-09-03 2017-03-30 Immunogen Inc Cytotoxic benzodiazepine derivatives
KR102494557B1 (ko) 2014-09-17 2023-02-02 자임워크스 비씨 인코포레이티드 세포독성 및 항유사분열성 화합물, 그리고 이를 이용하는 방법
MX386328B (es) 2015-03-27 2025-03-18 Regeneron Pharma Derivados de maitansinoide, conjugados de los mismos, y metodos de uso.
SG10202110908WA (en) 2015-05-04 2021-11-29 Cytomx Therapeutics Inc Anti-cd166 antibodies, activatable anti-cd166 antibodies, and methods of use thereof
US10449258B2 (en) 2015-06-09 2019-10-22 Xdcexplorer (Shanghai) Co., Ltd. Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
SI3313845T1 (sl) 2015-06-29 2021-01-29 Immunogen, Inc. Konjugati spremenjenih protiteles cisteina
JP6700321B2 (ja) * 2015-07-04 2020-05-27 ハンジョウ ディーエーシー バイオテック シーオー．，エルティディ．Ｈａｎｇｚｈｏｕ Ｄａｃ Ｂｉｏｔｅｃｈ Ｃｏ．，Ｌｔｄ． 細胞結合分子の特異的共役体
NZ737726A (en) 2015-07-06 2023-03-31 Regeneron Pharma Multispecific antigen-binding molecules and uses thereof
AU2016297087B2 (en) 2015-07-21 2021-02-18 Immunogen, Inc Methods of preparing cytotoxic benzodiazepine derivatives
US10509035B2 (en) 2015-08-07 2019-12-17 Gamamabs Pharma Sa Antibodies, antibody drug conjugates and methods of use
KR102700777B1 (ko) 2015-09-17 2024-08-29 이뮤노젠 아이엔씨 항-folr1 면역접합체를 포함하는 치료제 조합
CA3001712A1 (en) 2015-10-28 2017-05-04 Tarveda Therapeutics, Inc. Sstr-targeted conjugates and particles and formulations thereof
CN108495619A (zh) 2015-11-10 2018-09-04 儿研所儿童医学中心 棘霉素制剂及其制备方法和使用方法
PT3380525T (pt) 2015-11-25 2024-02-05 Immunogen Inc Formulações farmacêuticas e métodos que as utilizam
CN108602890A (zh) 2015-12-11 2018-09-28 瑞泽恩制药公司 用于减少或预防对egfr和/或erbb3阻滞剂具有抗性的肿瘤生长的方法
MX390630B (es) 2016-01-25 2025-03-21 Regeneron Pharma Derivados de maitansinoide, conjugados de los mismos y metodos de uso.
US11603346B2 (en) 2016-03-07 2023-03-14 Hanmi Pharm. Co., Ltd. Polyethylene glycol derivative and use thereof
EP3448891A1 (en) 2016-04-28 2019-03-06 Regeneron Pharmaceuticals, Inc. Methods of making multispecific antigen-binding molecules
US10918627B2 (en) 2016-05-11 2021-02-16 Massachusetts Institute Of Technology Convergent and enantioselective total synthesis of Communesin analogs
CN109963870B (zh) 2016-06-08 2023-07-28 艾伯维公司 抗b7-h3抗体和抗体药物偶联物
JP2019524687A (ja) 2016-07-01 2019-09-05 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ 抗体薬物複合体およびこれを用いた治療方法
US10772972B2 (en) 2016-09-23 2020-09-15 Regeneron Pharmaceuticals, Inc. Anti-STEAP2 antibody drug conjugates, and compositions and uses thereof
HRP20231281T1 (hr) 2016-09-23 2024-02-02 Regeneron Pharmaceuticals, Inc. Bispecifična anti-muc16-cd3 antitijela i konjugati anti-muc16 s lijekom
KR20190074310A (ko) 2016-11-08 2019-06-27 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체
TWI782930B (zh) 2016-11-16 2022-11-11 美商再生元醫藥公司 抗ｍｅｔ抗體，結合ｍｅｔ之雙特異性抗原結合分子及其使用方法
MA46887A (fr) 2016-11-23 2019-10-02 Immunogen Inc Sulfonation sélective de dérivés de benzodiazépine
IL266917B2 (en) 2016-11-29 2023-10-01 Regeneron Pharma Anti-human prolactin receptor (prlr) antibody-drug conjugates and use thereof in combination therapy of prlr positive breast cancer
EP3554544A4 (en) 2016-12-16 2020-07-29 Bluefin Biomedicine, Inc. ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE
LT3558391T (lt) 2016-12-23 2022-07-11 Immunogen, Inc. Imunokonjugatai, kurių taikinys yra adam9, ir jų naudojimo būdai
WO2018129029A1 (en) 2017-01-04 2018-07-12 Immunogen, Inc. Met antibodies and immunoconjugates and uses thereof
US20200061031A1 (en) 2017-02-28 2020-02-27 Kinki University Method for treating egfr-tki-resistant non-small cell lung cancer by administration of anti-her3 antibody-drug conjugate
KR102681168B1 (ko) 2017-02-28 2024-07-04 이뮤노젠 아이엔씨 자기희생적 펩티드 링커 및 이들의 접합체를 갖는 메이탄시노이드 유도체
EP3381474A1 (en) * 2017-03-27 2018-10-03 Alfasigma S.p.A. Histone deacetylase inhibitors-based antibody drug conjugates (adcs) and use in therapy
WO2018181059A1 (ja) 2017-03-30 2018-10-04 日油株式会社 ヘテロ二官能性単分散ポリエチレングリコール及びそれを用いた複合体
WO2018195243A1 (en) 2017-04-20 2018-10-25 Immunogen, Inc. Cytotoxic benzodiazepine derivatives and conjugates thereof
WO2018209239A1 (en) 2017-05-11 2018-11-15 Massachusetts Institute Of Technology Potent agelastatin derivatives as modulators for cancer invasion and metastasis
JP7364471B2 (ja) 2017-05-18 2023-10-18 レゲネロン ファーマシューティカルス，インコーポレーテッド シクロデキストリンタンパク質薬物コンジュゲート
CN111065622A (zh) 2017-05-18 2020-04-24 里珍纳龙药品有限公司 双八氢菲羧酰胺类化合物及其蛋白质偶联物
JP7348844B2 (ja) 2017-06-07 2023-09-21 リジェネロン・ファーマシューティカルズ・インコーポレイテッド 内部移行酵素のための組成物および方法
CA3067311A1 (en) * 2017-06-20 2018-12-27 Sorrento Therapeutics, Inc. Cd38 antibody drug conjugate
US10640508B2 (en) 2017-10-13 2020-05-05 Massachusetts Institute Of Technology Diazene directed modular synthesis of compounds with quaternary carbon centers
WO2019094395A2 (en) 2017-11-07 2019-05-16 Regeneron Pharmaceuticals, Inc. Hydrophilic linkers for antibody drug conjugates
CN109771658B (zh) * 2017-11-14 2021-12-10 博瑞生物医药（苏州）股份有限公司 靶向多臂偶联物
WO2019133652A1 (en) 2017-12-28 2019-07-04 Immunogen, Inc. Benzodiazepine derivatives
AU2019205542B2 (en) 2018-01-08 2025-10-23 Regeneron Pharmaceuticals, Inc. Steroids and antibody-conjugates thereof
CA3087993A1 (en) * 2018-01-12 2019-07-18 Immunogen, Inc. Methods for antibody drug conjugation, purification, and formulation
AU2019262953B2 (en) 2018-04-30 2025-12-04 Regeneron Pharmaceuticals, Inc. Antibodies, and bispecific antigen-binding molecules that bind HER2 and/or APLP2, conjugates, and uses thereof
SG11202010909RA (en) 2018-05-09 2020-12-30 Regeneron Pharma Anti-msr1 antibodies and methods of use thereof
US12252544B2 (en) 2018-05-17 2025-03-18 Regeneron Pharmaceuticals, Inc. Anti-CD63 antibodies, conjugates, and uses thereof
US20210275685A1 (en) 2018-06-26 2021-09-09 Immunogen, Inc. Immunoconjugates targeting adam9 and methods of use thereof
WO2020014306A1 (en) 2018-07-10 2020-01-16 Immunogen, Inc. Met antibodies and immunoconjugates and uses thereof
TW202024133A (zh) 2018-09-20 2020-07-01 日商第一三共股份有限公司 利用投予抗her3抗體-藥物結合物之her3突變癌之治療
CN109350748B (zh) * 2018-10-24 2021-06-11 沈阳药科大学 氧化还原双敏感键桥连小分子前药及其自组装纳米粒
TWI897855B (zh) 2018-10-26 2025-09-21 美商免疫遺傳股份有限公司 Ｅ ｐ Ｃ Ａ Ｍ 抗體、可活化抗體及免疫偶聯物以及其用途
MA53455B1 (fr) 2018-11-20 2022-11-30 Regeneron Pharma Dérivés de bis-octahydrophénanthrène carboxamide et leurs conjugués protéiques destinés à être utilisés en tant qu'agonistes de lxr
SG11202106658XA (en) 2018-12-21 2021-07-29 Regeneron Pharma Rifamycin analogs and antibody-drug conjugates thereof
EA202191769A1 (ru) 2018-12-21 2021-12-08 Регенерон Фармасьютикалз, Инк. Тубулизины и конъюгаты белок-тубулизин
KR20250156850A (ko) 2019-01-08 2025-11-03 리제너론 파마슈티칼스 인코포레이티드 흔적이 없는 링커 및 이의 단백질-접합체
MX2021010114A (es) 2019-02-21 2021-12-10 Regeneron Pharma Métodos para tratar el cáncer ocular mediante el uso de anticuerpos anti-met y moléculas de unión a antígeno bispecíficas que se unen a met.
JP7682798B2 (ja) 2019-03-20 2025-05-26 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア クローディン６抗体及び薬物複合体
JP7682797B2 (ja) 2019-03-20 2025-05-26 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア クローディン６二重特異性抗体
TW202102506A (zh) 2019-03-29 2021-01-16 美商伊繆諾金公司 苯二氮平衍生物
EP4316524A3 (en) 2019-04-26 2024-04-24 ImmunoGen, Inc. Camptothecin derivatives
US11535634B2 (en) 2019-06-05 2022-12-27 Massachusetts Institute Of Technology Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
PE20220485A1 (es) 2019-07-10 2022-04-04 Cybrexa 3 Inc Conjugados peptidicos de agentes dirigidos a microtubulos como terapeuticos
PE20220563A1 (es) 2019-07-10 2022-04-13 Cybrexa 2 Inc Conjugados peptidicos de citotoxinas como terapeuticos
MX2022002886A (es) 2019-09-16 2022-04-06 Regeneron Pharma Proteinas de union met radiomarcadas para la obtencion de imagenes por inmuno-pet.
US11814428B2 (en) 2019-09-19 2023-11-14 Regeneron Pharmaceuticals, Inc. Anti-PTCRA antibody-drug conjugates and uses thereof
CN115348874A (zh) 2020-01-24 2022-11-15 里珍纳龙药品有限公司 蛋白质-抗病毒化合物偶联物
BR112022017064A2 (pt) 2020-02-25 2022-11-16 Mediboston Inc Derivados da camptotecina e seus conjugados
KR20220148200A (ko) 2020-02-28 2022-11-04 리제너론 파마슈티칼스 인코포레이티드 Her2에 결합하는 이중특이적 항원 결합 분자 및 이의 사용 방법
US11701427B2 (en) 2020-04-16 2023-07-18 Regeneron Pharmaceuticals, Inc. Diels-alder conjugation methods
EP4171653A2 (en) 2020-06-24 2023-05-03 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
EP4178624A2 (en) 2020-07-07 2023-05-17 Bionecure Therapeutics, Inc. Maytansinoids as adc payloads and their use for the treatment of cancer
AU2021308190A1 (en) 2020-07-13 2023-02-02 Regeneron Pharmaceuticals, Inc. Camptothecin analogs conjugated to a glutamine residue in a protein, and their use
BR112023000711A2 (pt) 2020-07-17 2023-01-31 Daiichi Sankyo Co Ltd Método para produzir uma composição de conjugado de anticorpo-fármaco, e, composição de conjugado de anticorpo-fármaco
KR20230070337A (ko) 2020-09-14 2023-05-22 리제너론 파마슈티칼스 인코포레이티드 Glp1 펩티도미메틱을 포함하는 항체-약물 접합체 및 이의 용도
CN116406379A (zh) 2020-10-22 2023-07-07 瑞泽恩制药公司 抗fgfr2抗体和其使用方法
AR124681A1 (es) 2021-01-20 2023-04-26 Abbvie Inc Conjugados anticuerpo-fármaco anti-egfr
US12030888B2 (en) 2021-02-24 2024-07-09 Massachusetts Institute Of Technology Himastatin derivatives, and processes of preparation thereof, and uses thereof
US20220378929A1 (en) 2021-02-25 2022-12-01 MediBoston Limted Anti-her2 antibody-drug conjugates and uses thereof
EP4304658A4 (en) 2021-03-08 2025-03-12 Genequantum Healthcare (Suzhou) Co., Ltd. Antibody-immunagonist conjugate and applications thereof
WO2022218331A1 (en) 2021-04-14 2022-10-20 Genequantum Healthcare (Suzhou) Co., Ltd. Linkers, conjugates and applications thereof
JP2024529960A (ja) 2021-07-28 2024-08-14 レゲネロン ファーマシューティカルス，インコーポレーテッド タンパク質－抗ウイルス化合物コンジュゲート
JP2024534101A (ja) * 2021-08-20 2024-09-18 プサン ナショナル ユニバーシティ インダストリー － ユニバーシティ コーポレイション ファンデーション オブジェクトが固定された膨潤性高分子の製造方法
US12377157B2 (en) 2021-12-15 2025-08-05 The Administrators Of The Tulane Educational Fund Conjugates, their compositions, and their related methods
WO2023129518A1 (en) 2021-12-29 2023-07-06 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
MX2024008640A (es) 2022-01-12 2024-07-24 Regeneron Pharma Analogos de camptotecina conjugados a un residuo de glutamina en una proteina y su uso.
MX2024008361A (es) 2022-01-14 2024-09-10 Regeneron Pharma Derivados de verrucarina a y conjugados anticuerpo-fármaco de los mismos.
JP2025512735A (ja) 2022-03-11 2025-04-22 リジェネロン ファーマシューティカルズ，インク． Ｇｌｐ１ペプチド模倣体を含む抗ｇｌｐ１ｒ抗体係留型薬物コンジュゲートおよびその使用
CN120239705A (zh) 2022-07-21 2025-07-01 萤火虫生物股份有限公司 糖皮质激素受体激动剂和其缀合物
US20240108744A1 (en) 2022-07-27 2024-04-04 Mediboston Limited Auristatin derivatives and conjugates thereof
KR20250128394A (ko) 2022-11-30 2025-08-27 리제너론 파마슈티칼스 인코포레이티드 Tlr7 작용제 및 이의 항체-약물-접합체
AU2023407365A1 (en) 2022-12-21 2025-07-31 Regeneron Pharmaceuticals, Inc. Prodrugs of topoisomerase i inhibitor for adc conjugations and methods of use thereof
CN121001751A (zh) 2023-02-09 2025-11-21 里珍纳龙药品有限公司 借助逆电子需求狄尔斯-阿尔德反应的抗体-药物缀合物
WO2024220628A1 (en) * 2023-04-18 2024-10-24 The Regents Of The University Of Colorado, A Body Corporate Target for combatting the foreign body response to implantable biomaterials
WO2024229105A1 (en) 2023-05-02 2024-11-07 Regeneron Pharmaceuticals, Inc. Anti-human m-cadherin (cdh15) antibodies, conjugates, and uses thereof for delivery of genetic payloads to muscle cells
CN121219016A (zh) 2023-06-02 2025-12-26 第一三共株式会社 抗-her3抗体-药物缀合物和rasg12c抑制剂的组合
WO2025014533A1 (en) 2023-07-10 2025-01-16 Regeneron Pharmaceuticals, Inc. Anti-human cacng1 antibody-drug conjugates and uses thereof
WO2025094146A1 (en) 2023-11-02 2025-05-08 Immunogen Switzerland Gmbh Vasconstrictors for reducing ocular toxicity of antibody-maytansinoid conjugates
WO2025096921A1 (en) 2023-11-03 2025-05-08 Regeneron Pharmaceuticals, Inc. Peptide acids as a glp1r agonist and antibody-drug conjugates thereof
WO2025117727A1 (en) 2023-11-29 2025-06-05 Regeneron Pharmaceuticals, Inc. Analogs of quinoxaline/quinoline cytotoxins, linker- payloads, protein-drug conjugates, and uses thereof
CN118580194A (zh) * 2024-05-21 2024-09-03 南方科技大学 一种双功能分子探针的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030220245A1 (en) * 2000-06-02 2003-11-27 Hubbell Jeffrey A Conjugate addition reactions for the controlled delivery of pharmaceutical active compounds
US20050169933A1 (en) * 2003-10-10 2005-08-04 Immunogen, Inc. Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
US20060127352A1 (en) * 1999-02-01 2006-06-15 Eidgenossische Technische Hochschule Zurich Conjugate addition reactions for the controlled delivery of pharmaceutically active compounds
RU2404810C2 (ru) * 2004-06-01 2010-11-27 Дженентек, Инк. Конъюгаты антитело-лекарственное средство и способы

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7157458B2 (en) * 2001-04-17 2007-01-02 Cryolife, Inc. Bifunctional energy-reversible acyl-compositions
WO2002087497A2 (en) * 2001-04-26 2002-11-07 Board Of Regents, The University Of Texas System Therapeutic agent/ligand conjugate compositions, their methods of synthesis and use
US6441163B1 (en) 2001-05-31 2002-08-27 Immunogen, Inc. Methods for preparation of cytotoxic conjugates of maytansinoids and cell binding agents
US6716821B2 (en) 2001-12-21 2004-04-06 Immunogen Inc. Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same
US8877901B2 (en) * 2002-12-13 2014-11-04 Immunomedics, Inc. Camptothecin-binding moiety conjugates
US6596757B1 (en) * 2002-05-14 2003-07-22 Immunogen Inc. Cytotoxic agents comprising polyethylene glycol-containing taxanes and their therapeutic use
US7276497B2 (en) 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
AU2004240541B2 (en) 2003-05-20 2009-08-20 Immunogen, Inc. Improved cytotoxic agents comprising new maytansinoids
US9005625B2 (en) * 2003-07-25 2015-04-14 Novo Nordisk A/S Antibody toxin conjugates
ZA200601182B (en) * 2003-10-10 2007-04-25 Immunogen Inc Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
CN104447992A (zh) 2004-09-23 2015-03-25 健泰科生物技术公司 半胱氨酸改造的抗体和偶联物
JP2008518023A (ja) * 2004-10-27 2008-05-29 メディミューン，インコーポレーテッド 同族抗原に対する親和性を改変することによる抗体特異性の調節
EP1853322B1 (en) * 2005-02-11 2014-06-25 ImmunoGen, Inc. Process for preparing maytansinoid antibody conjugates
US20090226465A1 (en) * 2005-10-31 2009-09-10 Jackson David Y Macrocyclic depsipeptide antibody-drug conjugates and methods
PT2032606E (pt) * 2006-05-30 2014-02-05 Genentech Inc Anticorpos e imunoconjugados e respetivas utilizações
US20080311040A1 (en) * 2007-03-06 2008-12-18 Flagship Ventures METHODS AND COMPOSITIONS FOR IMPROVED THERAPEUTIC EFFECTS WITH siRNA
EP2176295B1 (en) * 2007-07-16 2014-11-19 Genentech, Inc. Humanized anti-cd79b antibodies and immunoconjugates and methods of use
SG189817A1 (en) 2008-04-30 2013-05-31 Immunogen Inc Potent conjugates and hydrophilic linkers

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060127352A1 (en) * 1999-02-01 2006-06-15 Eidgenossische Technische Hochschule Zurich Conjugate addition reactions for the controlled delivery of pharmaceutically active compounds
US20030220245A1 (en) * 2000-06-02 2003-11-27 Hubbell Jeffrey A Conjugate addition reactions for the controlled delivery of pharmaceutical active compounds
US20050169933A1 (en) * 2003-10-10 2005-08-04 Immunogen, Inc. Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
RU2404810C2 (ru) * 2004-06-01 2010-11-27 Дженентек, Инк. Конъюгаты антитело-лекарственное средство и способы

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2754369C2 (ru) * 2016-03-02 2021-09-01 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конъюгаты антитело-лекарственное средство на основе эрибулина и способы применения
RU2844753C2 (ru) * 2016-03-02 2025-08-05 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конъюгаты антитело-лекарственное средство на основе эрибулина и способы применения
RU2653443C2 (ru) * 2016-07-15 2018-05-08 Закрытое Акционерное Общество "Биокад" Биспецифичные анти-her2/анти-her3 антитела

Also Published As

Publication number Publication date
CN102083461A (zh) 2011-06-01
ZA201007806B (en) 2013-01-30
RU2010148740A (ru) 2012-06-10
US20100129314A1 (en) 2010-05-27
CN104258413A (zh) 2015-01-07
JP2011523628A (ja) 2011-08-18
WO2009134952A3 (en) 2010-01-07
AU2009243009A1 (en) 2009-11-05
JP2015163622A (ja) 2015-09-10
MX2010011808A (es) 2011-03-04
KR20100137585A (ko) 2010-12-30
AU2009243009B2 (en) 2014-09-11
EP2276506A4 (en) 2014-05-07
IL208937A0 (en) 2011-01-31
US20160114052A1 (en) 2016-04-28
CN102083461B (zh) 2014-09-17
US20120226026A1 (en) 2012-09-06
US9150649B2 (en) 2015-10-06
UA108598C2 (xx) 2015-05-25
WO2009134952A2 (en) 2009-11-05
BRPI0911442A2 (pt) 2019-03-12
SG189817A1 (en) 2013-05-31
NZ588851A (en) 2013-05-31
WO2009134976A1 (en) 2009-11-05
CA2722109A1 (en) 2009-11-05
EP2276506A1 (en) 2011-01-26
JP5980989B2 (ja) 2016-08-31

Similar Documents

Publication Publication Date Title
RU2487877C2 (ru) Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры)
JP2011523628A5 (cg-RX-API-DMAC7.html)
JP2011519864A5 (cg-RX-API-DMAC7.html)
JP2021113210A5 (cg-RX-API-DMAC7.html)
JP6598821B2 (ja) ペプチドリンカーを有する新規メイタンシノイド誘導体およびその結合体
JP6462591B2 (ja) 新規抗体コンジュゲートおよびその使用
RU2503687C2 (ru) Сшивающие реагенты и их применение
CY1122302T1 (el) Νεα anti-cd38 αντισωματα για τη θεραπευτικη αγωγη καρκινου
JP2019532056A5 (cg-RX-API-DMAC7.html)
BR112021004656A2 (pt) conjugado fármaco-ligante de análogo exatecano, método para preparar o mesmo e aplicação do mesmo
JP2018523471A5 (cg-RX-API-DMAC7.html)
JP2012006928A5 (cg-RX-API-DMAC7.html)
JP7791843B2 (ja) 抗ｂｃｍａ抗体－薬物コンジュゲート及び使用方法
CN110831976A (zh) 用于制备抗体-药物缀合物的双重缀合方法
JP2018523471A (ja) システイン置換免疫グロブリン
CA2833477A1 (en) Novel binder-drug conjugates (adcs) and their use
JP2013506709A (ja) 有効なコンジュゲートおよび親水性リンカー
RU2016145445A (ru) Конъюгат антитела и лекарственного средства и его применение для лечения рака
RU2012135395A (ru) Антитела против рецептора фолиевой кислоты 1, их иммуноконъюгаты и использование
RU2016133846A (ru) Конъюгат лиганд - цитотоксическое лекарственное средство, способ его получения и его применения
US20190290775A1 (en) Use of Antibody Drug Conjugates Comprising Tubulin Disrupting Agents to Treat Solid Tumor
JP2013506709A5 (cg-RX-API-DMAC7.html)
IL278574B1 (en) Compounds acting on glycans and methods of using them
EA039757B1 (ru) Конъюгат антитела против erbb2 и лекарственного средства и его композиция, способ его получения и его применение
EA034138B1 (ru) Цитотоксические бензодиазепиновые производные

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20170501