EA201990470A1 - Конъюгаты лекарственного средства с самостабилизирующимися линкерами, имеющие улучшенные физико-химические свойства - Google Patents

Конъюгаты лекарственного средства с самостабилизирующимися линкерами, имеющие улучшенные физико-химические свойства

Info

Publication number
EA201990470A1
EA201990470A1 EA201990470A EA201990470A EA201990470A1 EA 201990470 A1 EA201990470 A1 EA 201990470A1 EA 201990470 A EA201990470 A EA 201990470A EA 201990470 A EA201990470 A EA 201990470A EA 201990470 A1 EA201990470 A1 EA 201990470A1
Authority
EA
Eurasian Patent Office
Prior art keywords
self
chemical properties
improved physical
stabilizing linkers
conjugates
Prior art date
Application number
EA201990470A
Other languages
English (en)
Russian (ru)
Inventor
Филип Моквист
Original Assignee
Сиэтл Дженетикс, 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 Сиэтл Дженетикс, Инк. filed Critical Сиэтл Дженетикс, Инк.
Publication of EA201990470A1 publication Critical patent/EA201990470A1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/549Sugars, nucleosides, nucleotides or nucleic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68031Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68035Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a pyrrolobenzodiazepine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • A61K47/6867Medicinal 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 a cell of a blood cancer
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6873Medicinal 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 an immunoglobulin; the antibody being an anti-idiotypic antibody
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6889Conjugates 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IG], 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2878Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cell Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Toxicology (AREA)
  • Dermatology (AREA)
EA201990470A 2016-08-09 2017-08-09 Конъюгаты лекарственного средства с самостабилизирующимися линкерами, имеющие улучшенные физико-химические свойства EA201990470A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662372455P 2016-08-09 2016-08-09
PCT/US2017/046157 WO2018031690A1 (en) 2016-08-09 2017-08-09 Drug conjugates with self-stabilizing linkers having improved physiochemical properties

Publications (1)

Publication Number Publication Date
EA201990470A1 true EA201990470A1 (ru) 2019-09-30

Family

ID=61162990

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201990470A EA201990470A1 (ru) 2016-08-09 2017-08-09 Конъюгаты лекарственного средства с самостабилизирующимися линкерами, имеющие улучшенные физико-химические свойства

Country Status (14)

Country Link
US (2) US11944689B2 (https=)
EP (1) EP3496747A4 (https=)
JP (2) JP7257951B2 (https=)
KR (2) KR20190038579A (https=)
CN (1) CN109562152B (https=)
AU (2) AU2017310436B2 (https=)
BR (1) BR112019001945A2 (https=)
EA (1) EA201990470A1 (https=)
IL (1) IL264453A (https=)
MA (1) MA45945A (https=)
MX (2) MX2019001302A (https=)
SG (1) SG11201900699QA (https=)
TW (2) TWI851531B (https=)
WO (1) WO2018031690A1 (https=)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20180134351A (ko) 2016-03-25 2018-12-18 시애틀 지네틱스, 인크. 페길화된 약물-링커 및 그의 중간체의 제조를 위한 공정
MX2019001302A (es) 2016-08-09 2019-06-12 Seattle Genetics Inc Conjugados de farmaco con enlazadores autoestabilizantes que tienen propiedades fisioquimicas mejoradas.
AU2018237683A1 (en) 2017-03-24 2019-10-31 Seagen Inc. Process for the preparation of glucuronide drug-linkers and intermediates thereof
TWI851577B (zh) 2018-06-07 2024-08-11 美商思進公司 喜樹鹼結合物
GB201820864D0 (en) * 2018-12-20 2019-02-06 J A Kemp Antibody-drug conjugates
MA53765B2 (fr) 2018-12-21 2025-04-30 Regeneron Pharmaceuticals, Inc. Tubulysines et conjugués tubulysines-protéines
JP2022530482A (ja) * 2019-05-02 2022-06-29 レゴケム バイオサイエンシズ, インク. トリス構造を有するリンカーを含むリガンド―薬物複合体
CN113727734A (zh) * 2019-05-02 2021-11-30 乐高化学生物科学股份有限公司 包含具有tris结构的连接子的配体-药物偶联物
AU2020296295B2 (en) * 2019-06-21 2025-05-29 Ascendis Pharma A/S Conjugates of an electron-donating nitrogen or tertiary amine comprising compounds
AU2020482800B2 (en) * 2020-12-23 2025-08-21 Genequantum Healthcare (Suzhou) Co., Ltd. Novel isomeric compounds comprising a ring-opened thiosuccinimide group, an oligopeptide fragment and a chiral moiety
JP7717832B2 (ja) 2021-04-10 2025-08-04 ジェンマブ エー/エス Folr1結合剤、そのコンジュゲートおよびこれを使用する方法
WO2022226317A1 (en) 2021-04-23 2022-10-27 Profoundbio Us Co. Anti-cd70 antibodies, conjugates thereof and methods of using the same
TW202320857A (zh) 2021-07-06 2023-06-01 美商普方生物製藥美國公司 連接子、藥物連接子及其結合物及其使用方法
MX2024002571A (es) 2021-09-03 2024-03-20 Toray Industries Composicion farmaceutica para tratamiento y/o prevencion de cancer.
WO2023092099A1 (en) 2021-11-19 2023-05-25 Ardeagen Corporation Gpc3 binding agents, conjugates thereof and methods of using the same
KR20250031149A (ko) 2022-06-30 2025-03-06 도레이 카부시키가이샤 암의 치료 및/또는 예방용 의약 조성물
CN118684724A (zh) 2023-03-22 2024-09-24 映恩生物制药(苏州)有限公司 连接子及其在配体药物偶联物中的应用
AR132368A1 (es) 2023-04-18 2025-06-18 Astrazeneca Ab Conjugados que comprenden enlazadores escindibles
KR20250074353A (ko) 2023-11-20 2025-05-27 주식회사 에이비켐바이오 높은 dar를 갖는 신규한 항체-약물 중합체, 이의 제조방법 및 이의 용도
KR20240159448A (ko) 2023-04-28 2024-11-05 주식회사 에이비켐바이오 균일한 dar를 갖는 신규한 항체-약물 중합체의 제조방법
KR20240159447A (ko) 2023-04-28 2024-11-05 주식회사 에이비켐바이오 말레이미드 함유 링커-페이로드 접합체
CN121568721A (zh) * 2023-06-29 2026-02-24 广州百济神州生物制药有限公司 生物活性缀合物、其制备方法和其用途
TW202525851A (zh) * 2023-08-15 2025-07-01 瑞典商阿斯特捷利康公司 包含可切割連接子的軛合物
AU2024339683A1 (en) 2023-09-13 2026-03-26 Toray Industries, Inc. Pharmaceutical composition for treating, preventing and/or diagnosing cancer
AU2024353316A1 (en) 2023-09-26 2026-03-26 Genmab A/S Ptk7 binding agents, conjugates thereof and methods of using the same
WO2025149661A1 (en) 2024-01-10 2025-07-17 Genmab A/S Slitrk6 binding agents, conjugates thereof and methods of using the same
WO2025181219A1 (en) 2024-02-29 2025-09-04 Genmab A/S Egfr and c-met bispecific binding agents, conjugates thereof and methods of using the same
WO2026039642A1 (en) 2024-08-16 2026-02-19 Ardeagen Corporation Anti-mesothelin antibody conjugates and methods of use thereof

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2036891B (en) 1978-12-05 1983-05-05 Windsor Smith C Change speed gear
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
JPS6147500A (ja) 1984-08-15 1986-03-07 Res Dev Corp Of Japan キメラモノクロ−ナル抗体及びその製造法
EP0173494A3 (en) 1984-08-27 1987-11-25 The Board Of Trustees Of The Leland Stanford Junior University Chimeric receptors by dna splicing and expression
GB8422238D0 (en) 1984-09-03 1984-10-10 Neuberger M S Chimeric proteins
JPS61134325A (ja) 1984-12-04 1986-06-21 Teijin Ltd ハイブリツド抗体遺伝子の発現方法
JPS63501765A (ja) 1985-11-01 1988-07-21 インタ−ナショナル、ジェネティック、エンジニアリング インコ−ポレ−テッド 抗体遺伝子のモジュ−ル組立体、それにより産生された抗体及び用途
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
US4880935A (en) 1986-07-11 1989-11-14 Icrf (Patents) Limited Heterobifunctional linking agents derived from N-succinimido-dithio-alpha methyl-methylene-benzoates
JPS6423340U (https=) 1987-08-03 1989-02-07
IL106992A (en) 1988-02-11 1994-06-24 Bristol Myers Squibb Co Acylhydrazone derivatives of anthracycline and methods for their preparation
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
US5091542A (en) 1990-03-09 1992-02-25 Hybritech Incorporated Tris-maleimido compounds as intermediates in trifunctional antibody synthesis
US5622929A (en) 1992-01-23 1997-04-22 Bristol-Myers Squibb Company Thioether conjugates
WO1994001485A1 (en) 1992-07-01 1994-01-20 Akzo Nobel N.V. Process for the modification of polyphenylene ether resin compositions
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
ATE234635T1 (de) 1995-12-22 2003-04-15 Bristol Myers Squibb Co Verzweigte hydrazongruppen enthaltende kuppler
JP4046354B2 (ja) 1996-03-18 2008-02-13 ボード オブ リージェンツ,ザ ユニバーシティ オブ テキサス システム 増大した半減期を有する免疫グロブリン様ドメイン
US6130237A (en) 1996-09-12 2000-10-10 Cancer Research Campaign Technology Limited Condensed N-aclyindoles as antitumor agents
US5973166A (en) 1998-03-02 1999-10-26 The Dexter Corporation Method for the preparation of maleimides
US6884869B2 (en) 2001-04-30 2005-04-26 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
US7256257B2 (en) 2001-04-30 2007-08-14 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
US20030083263A1 (en) 2001-04-30 2003-05-01 Svetlana Doronina Pentapeptide compounds and uses related thereto
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
US7125844B2 (en) 2002-01-03 2006-10-24 Migenix Inc. Dab9 derivatives of lipopeptide antibiotics and methods of making and using the same
US8877901B2 (en) 2002-12-13 2014-11-04 Immunomedics, Inc. Camptothecin-binding moiety conjugates
SI1545613T1 (sl) 2002-07-31 2011-11-30 Seattle Genetics Inc Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni
US7432331B2 (en) 2002-12-31 2008-10-07 Nektar Therapeutics Al, Corporation Hydrolytically stable maleimide-terminated polymers
EP1578841B2 (en) * 2002-12-31 2016-10-12 Nektar Therapeutics AL, Corporation Maleamic acid polymer derivatives and their bioconjugates
US8088387B2 (en) 2003-10-10 2012-01-03 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
RU2448117C2 (ru) 2003-11-06 2012-04-20 Сиэтл Дженетикс, Инк. Монометилвалиновые соединения, способные образовывать конъюгаты с лигандами
US7498298B2 (en) 2003-11-06 2009-03-03 Seattle Genetics, Inc. Monomethylvaline compounds capable of conjugation to ligands
EP1718667B1 (en) 2004-02-23 2013-01-09 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
CN1997402B (zh) * 2004-05-19 2014-04-02 梅达雷克斯有限责任公司 化学连接基团及其缀合物
JP4806680B2 (ja) 2004-05-19 2011-11-02 メダレックス インコーポレイテッド 自己犠牲リンカー及び薬剤複合体
KR20120064120A (ko) 2004-06-01 2012-06-18 제넨테크, 인크. 항체 약물 접합체 및 방법
US20060292616A1 (en) * 2005-06-23 2006-12-28 U.S. Genomics, Inc. Single molecule miRNA-based disease diagnostic methods
US8871720B2 (en) 2005-07-07 2014-10-28 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus
JP5171621B2 (ja) 2005-07-07 2013-03-27 シアトル ジェネティックス, インコーポレイテッド フェニルアラニン側鎖修飾をc末端に有するモノメチルバリン化合物
HUE035853T2 (en) 2005-07-18 2018-05-28 Seattle Genetics Inc Beta-glucuronide-linker-drug conjugates
BRPI0617546A2 (pt) 2005-09-26 2011-07-26 Medarex Inc conjugado de fÁrmaco-anticorpo, formulaÇço farmacÊutica, mÉtodo para matar uma cÉlula de tumor, mÉtodo para retardar ou interromper o crescimento de um tumor em um sujeito mamÍfero e composto
SI1813614T1 (sl) 2006-01-25 2012-01-31 Sanofi 174 Citotoksična sredstva, ki obsegajo nove tomajmicinske derivate
US8257706B2 (en) 2006-08-25 2012-09-04 Seattle Genetics, Inc. CD30 binding agents and uses thereof
BRPI0812970A2 (pt) 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
RU2476441C2 (ru) 2007-10-19 2013-02-27 Сиэтл Дженетикс, Инк. Cd19-связывающие средства и их применение
EP2265283B1 (en) 2008-03-18 2014-09-03 Seattle Genetics, Inc. Auristatin drug linker conjugates
KR20200058590A (ko) 2008-04-30 2020-05-27 이뮤노젠 아이엔씨 가교제 및 그 용도
BRPI0923283A2 (pt) 2008-12-05 2017-06-06 Angiochem Inc conjugados terapêuticos de peptídeo e usos dos mesmos
CN102365021B (zh) 2009-02-05 2015-07-15 伊缪诺金公司 新型苯并二氮杂*衍生物
EP3912643B8 (en) 2009-02-13 2023-08-23 Immunomedics, Inc. Immunoconjugates with an intracellularly-cleavable linkage
FR2949469A1 (fr) 2009-08-25 2011-03-04 Sanofi Aventis Derives anticancereux, leur preparation et leur application en therapeutique
DK2528625T3 (da) 2010-04-15 2013-10-14 Spirogen Sarl Pyrrolobenzodiazepiner og konjugater deraf
AU2011316917B2 (en) 2010-10-22 2016-02-25 Seagen Inc. Synergistic effects between auristatin-based antibody drug conjugates and inhibitors of the PI3K-AKT mTOR pathway
JP6105481B2 (ja) 2010-12-06 2017-03-29 シアトル ジェネティクス,インコーポレーテッド Liv−1に対するヒト化抗体および癌治療のためのその使用
JP6049642B2 (ja) 2011-02-15 2016-12-21 イミュノジェン・インコーポレーテッド 複合体の調製方法
CH706603B1 (de) 2011-08-03 2016-08-31 Ophthametrics Ag Hrm Man & Treuhand Ag Aufnahmevorrichtung zur Aufnahme einer Netzhaut eines Auges sowie Aufnahmeverfahren.
CN104244718A (zh) 2011-12-05 2014-12-24 伊格尼卡生物治疗公司 抗体-药物缀合物以及相关化合物、组合物和方法
CN104220094A (zh) 2012-02-17 2014-12-17 西雅图基因公司 针对整联蛋白αvβ6的抗体和使用该抗体治疗癌症
CA2864872C (en) * 2012-02-24 2022-07-05 Alteogen Inc. Modified antibody in which motif comprising cysteine residue is bound
KR102557309B1 (ko) 2012-05-15 2023-07-20 씨젠 인크. 자가-안정화 링커 접합체
US9504756B2 (en) * 2012-05-15 2016-11-29 Seattle Genetics, Inc. Self-stabilizing linker conjugates
US20130309223A1 (en) 2012-05-18 2013-11-21 Seattle Genetics, Inc. CD33 Antibodies And Use Of Same To Treat Cancer
EP2968591A1 (en) 2013-03-15 2016-01-20 Novartis AG Cell proliferation inhibitors and conjugates thereof
ES2826398T3 (es) 2013-10-15 2021-05-18 Seagen Inc Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco
JP6701077B2 (ja) 2013-12-19 2020-05-27 シアトル ジェネティックス, インコーポレイテッド 標的化薬物結合体と使用するためのメチレンカルバメートリンカー
SG10202001468UA (en) 2014-02-17 2020-04-29 Seattle Genetics Inc Hydrophilic antibody-drug conjugates
SI3900742T1 (sl) 2014-09-11 2024-10-30 Seagen Inc. Ciljana dostava zdravilnih snovi, ki vsebujejo terciarne amine
MX2019001302A (es) 2016-08-09 2019-06-12 Seattle Genetics Inc Conjugados de farmaco con enlazadores autoestabilizantes que tienen propiedades fisioquimicas mejoradas.
JP7337698B2 (ja) 2017-02-28 2023-09-04 シージェン インコーポレイテッド コンジュゲート化のためのシステイン突然変異抗体
WO2018201087A1 (en) 2017-04-27 2018-11-01 Seattle Genetics, Inc. Quaternized nicotinamide adenine dinucleotide salvage pathway inhibitor conjugates
AR114112A1 (es) 2018-02-15 2020-07-22 Seattle Genetics Inc Anticuerpos de glipicano 3 y conjugados de los mismos

Also Published As

Publication number Publication date
CN109562152B (zh) 2024-04-02
KR20240010534A (ko) 2024-01-23
SG11201900699QA (en) 2019-02-27
TW201808343A (zh) 2018-03-16
WO2018031690A1 (en) 2018-02-15
AU2017310436A1 (en) 2019-03-21
TWI851531B (zh) 2024-08-11
MX2019001302A (es) 2019-06-12
JP2019524759A (ja) 2019-09-05
MA45945A (fr) 2019-06-19
JP7257951B2 (ja) 2023-04-14
CA3032147A1 (en) 2018-02-15
EP3496747A1 (en) 2019-06-19
US20240226320A1 (en) 2024-07-11
AU2022275478B2 (en) 2024-08-29
US11944689B2 (en) 2024-04-02
US20190167806A1 (en) 2019-06-06
AU2022275478A1 (en) 2023-01-05
JP2023082171A (ja) 2023-06-13
KR20190038579A (ko) 2019-04-08
IL264453A (en) 2019-02-28
AU2017310436B2 (en) 2022-08-25
JP7573679B2 (ja) 2024-10-25
BR112019001945A2 (pt) 2019-05-07
EP3496747A4 (en) 2020-04-15
CN109562152A (zh) 2019-04-02
MX2023013592A (es) 2023-12-15
TW202500191A (zh) 2025-01-01

Similar Documents

Publication Publication Date Title
EA201990470A1 (ru) Конъюгаты лекарственного средства с самостабилизирующимися линкерами, имеющие улучшенные физико-химические свойства
CY1124606T1 (el) Στοχευμενη χορηγηση φαρμακευτικων ουσiων που περιεχουν τριτοταγη αμινη
EA201990890A1 (ru) Целевая доставка ингибиторов реутилизационного пути никотинамидадениндинуклеотида
MX2023002599A (es) Conjugados de compuestos de tubulisina cuaternizada.
CY1123983T1 (el) Ειδικα σε axl συζευγματα αντισωματος-φαρμακου για τη θεραπεια καρκινου
PH12019500214A1 (en) Substituted thiazolo-pyridine compounds as malt1 inhibitors
CY1122707T1 (el) Ετεροκυκλικοι αναστολεις γλουταμινασης
EA201201400A1 (ru) Композиции и способы лечения аутоиммунных и других заболеваний
EA201790404A1 (ru) Макропиноцитозирующие человеческие анти-cd46 антитела и таргетная терапия рака
MX2022000449A (es) Conjugados peptídicos de citotoxinas como terapéuticos.
EA201992350A1 (ru) Комбинированные лекарственные средства, нацеленные на pd-1, tim-3 и lag-3
EA201791050A1 (ru) Конъюгаты антител и лекарственных средств
CY1125150T1 (el) Ενωσεις φαινυλο-2-υδροξυ-ακετυλαμινο-2-μεθυλο-φαινυλιου
PE20151180A1 (es) Anticuerpos anti-ceacam5 y usos de estos
EA201791867A1 (ru) Бициклические гетероциклы как ингибиторы fgfr4
BR112016029916A2 (pt) inibidores mnk e métodos correlatos
EA201890530A1 (ru) Конъюгаты антитела к dll3 и лекарственного средства и способы их применения
NZ710729A (en) Amatoxin derivatives
MX386616B (es) Compuestos de carfilzomib pegilados.
EA201791535A1 (ru) Новое соединение 4'-тионуклеозида, а также способ его получения, его фармацевтическая композиция и применение
EA202092518A1 (ru) Композиции и способы лечения рака
EA201990949A1 (ru) Сульфоксиалкильные органические нитросоединения и родственные соединения и фармацевтические композиции для применения в медицине
EA201790773A1 (ru) Композиции и способы для ингибирования биологической активности растворимых биомолекул
EA202091112A1 (ru) Сокристаллы, фармацевтические композиции на их основе и способы лечения, предусматривающие их применение
MX386761B (es) Compuestos de indenilo, composiciones farmacéuticas y usos médicos del mismo.