JP6280103B2 - 薬物コンジュゲート、コンジュゲーション方法およびその使用 - Google Patents

薬物コンジュゲート、コンジュゲーション方法およびその使用 Download PDF

Info

Publication number
JP6280103B2
JP6280103B2 JP2015512771A JP2015512771A JP6280103B2 JP 6280103 B2 JP6280103 B2 JP 6280103B2 JP 2015512771 A JP2015512771 A JP 2015512771A JP 2015512771 A JP2015512771 A JP 2015512771A JP 6280103 B2 JP6280103 B2 JP 6280103B2
Authority
JP
Japan
Prior art keywords
optionally substituted
alkyl
compound
group
aryl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2015512771A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015518833A5 (enExample
JP2015518833A (ja
Inventor
ジェンウェイ・ミャオ
ユーフォン・ホン
トン・ジュウ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sorrento Therapeutics Inc
Original Assignee
Sorrento Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sorrento Therapeutics Inc filed Critical Sorrento Therapeutics Inc
Publication of JP2015518833A publication Critical patent/JP2015518833A/ja
Publication of JP2015518833A5 publication Critical patent/JP2015518833A5/ja
Application granted granted Critical
Publication of JP6280103B2 publication Critical patent/JP6280103B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K47/6855Medicinal 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 breast cancer cell
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • 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
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • 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
    • A61K47/6849Medicinal 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/587Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with aliphatic hydrocarbon radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms, said aliphatic radicals being substituted in the alpha-position to the ring by a hetero atom, e.g. with m >= 0, Z being a singly or a doubly bound hetero atom
    • C07D277/593Z being doubly bound oxygen or doubly bound nitrogen, which nitrogen is part of a possibly substituted oximino radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cell Biology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2015512771A 2012-05-15 2013-05-14 薬物コンジュゲート、コンジュゲーション方法およびその使用 Expired - Fee Related JP6280103B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201261647300P 2012-05-15 2012-05-15
US61/647,300 2012-05-15
US201261648532P 2012-05-17 2012-05-17
US201261648406P 2012-05-17 2012-05-17
US61/648,532 2012-05-17
US61/648,406 2012-05-17
US201261652512P 2012-05-29 2012-05-29
US61/652,512 2012-05-29
PCT/US2013/041028 WO2013173393A1 (en) 2012-05-15 2013-05-14 Drug-conjugates, conjugation methods, and uses thereof

Publications (3)

Publication Number Publication Date
JP2015518833A JP2015518833A (ja) 2015-07-06
JP2015518833A5 JP2015518833A5 (enExample) 2016-06-30
JP6280103B2 true JP6280103B2 (ja) 2018-02-14

Family

ID=49584226

Family Applications (5)

Application Number Title Priority Date Filing Date
JP2015512771A Expired - Fee Related JP6280103B2 (ja) 2012-05-15 2013-05-14 薬物コンジュゲート、コンジュゲーション方法およびその使用
JP2015512770A Active JP6239598B2 (ja) 2012-05-15 2013-05-14 薬物複合体、複合体形成方法、およびその使用
JP2015512769A Active JP6239597B2 (ja) 2012-05-15 2013-05-14 薬物コンジュゲート、コンジュゲーション方法およびその使用
JP2017212167A Pending JP2018052951A (ja) 2012-05-15 2017-11-01 薬物複合体、複合体形成方法、およびその使用
JP2017212053A Pending JP2018058851A (ja) 2012-05-15 2017-11-01 薬物コンジュゲート、コンジュゲーション方法およびその使用

Family Applications After (4)

Application Number Title Priority Date Filing Date
JP2015512770A Active JP6239598B2 (ja) 2012-05-15 2013-05-14 薬物複合体、複合体形成方法、およびその使用
JP2015512769A Active JP6239597B2 (ja) 2012-05-15 2013-05-14 薬物コンジュゲート、コンジュゲーション方法およびその使用
JP2017212167A Pending JP2018052951A (ja) 2012-05-15 2017-11-01 薬物複合体、複合体形成方法、およびその使用
JP2017212053A Pending JP2018058851A (ja) 2012-05-15 2017-11-01 薬物コンジュゲート、コンジュゲーション方法およびその使用

Country Status (7)

Country Link
US (7) US9981046B2 (enExample)
EP (6) EP2849797B1 (enExample)
JP (5) JP6280103B2 (enExample)
CN (4) CN104662000B (enExample)
ES (2) ES2887208T3 (enExample)
HK (1) HK1208216A1 (enExample)
WO (3) WO2013173393A1 (enExample)

Families Citing this family (142)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1789391B1 (en) 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
JP5829793B2 (ja) 2007-03-14 2015-12-09 エンドサイト・インコーポレイテッドEndocyte, Inc. 結合性リガンドが結合したツブリシンの薬剤送達結合体
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
WO2009002993A1 (en) 2007-06-25 2008-12-31 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
WO2013126797A1 (en) 2012-02-24 2013-08-29 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
US20140079636A1 (en) 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
US9981046B2 (en) 2012-05-15 2018-05-29 Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. Drug-conjugates, conjugation methods, and uses thereof
EP2908818A4 (en) 2012-10-16 2016-07-13 Endocyte Inc CONJUGATES OF DRUG DELIVERY CONTAINING ARTIFICIAL AMINO ACIDS AND METHODS OF USE
AU2013364065B2 (en) 2012-12-21 2018-10-04 Altrubio Inc. Hydrophilic self-immolative linkers and conjugates thereof
MY174813A (en) 2013-03-15 2020-05-16 Zymeworks Inc Cytotoxic and anti-mitotic compounds, and methods of using the same
WO2014197991A1 (en) 2013-06-12 2014-12-18 Muhammad Yousaf Compounds for promoting liposomal and cellular adhesion and compositions and methods of use thereof
AU2014318826B2 (en) 2013-09-10 2019-10-10 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
CA2934030A1 (en) 2013-10-15 2015-04-23 Sorrento Therapeutics Inc. Drug-conjugates with a targeting molecule and two different drugs
KR102538993B1 (ko) 2013-10-15 2023-06-02 씨젠 인크. 개선된 리간드-약물 컨쥬게이트 약물동력학을 위한 peg화된 약물-링커
WO2015066053A2 (en) 2013-10-28 2015-05-07 Synta Pharmaceuticals Corp. Targeted therapeutics
AU2014373640B2 (en) 2013-12-27 2018-08-30 Var2 Pharmaceuticals Aps VAR2CSA-drug conjugates
CA2935077C (en) 2013-12-27 2022-03-15 Geoffrey C. Winters Sulfonamide-containing linkage systems for drug conjugates
US10183970B2 (en) 2014-01-28 2019-01-22 Tube Pharmaceuticals Gmbh Cytotoxic tubulysin compounds for conjugation
WO2015116774A1 (en) 2014-01-29 2015-08-06 Synta Pharmaceuticals Corp. Targeted therapeutics
GB201402006D0 (en) * 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
AU2015224576A1 (en) 2014-03-03 2016-09-22 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
MA39483A (fr) 2014-03-18 2015-09-24 Synta Pharmaceuticals Corp Agents thérapeutiques cibles
CN107041139A (zh) 2014-05-28 2017-08-11 艾更斯司股份有限公司 海兔脯氨酸‑海兔异亮氨酸肽的衍生物
CA2952876A1 (en) 2014-06-20 2015-12-23 Bioalliance C.V. Anti-folate receptor alpha (fra) antibody-drug conjugates and methods of using thereof
HRP20200283T1 (hr) 2014-07-11 2020-05-29 Genmab A/S Protutijela koja se vežu na axl
JP6473226B2 (ja) * 2014-09-11 2019-02-20 シアトル ジェネティックス, インコーポレイテッド 第3級アミン含有薬物物質の標的送達
CA2960899C (en) * 2014-09-17 2021-08-17 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
ES2885854T3 (es) 2014-10-14 2021-12-15 Polytherics Ltd Proceso para la conjugación de un péptido o proteína con un reactivo que comprende un grupo saliente que incluye una porción de PEG
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
US20180280531A1 (en) * 2014-12-08 2018-10-04 Sorrento Therapeutics, Inc. C-met antibody drug conjugate
US9968683B2 (en) 2014-12-17 2018-05-15 Organolinx Corp. Method for conjugating molecules
ES2918425T3 (es) * 2015-01-28 2022-07-15 Sorrento Therapeutics Inc Conjugados de anticuerpo-fármaco
US20170224835A1 (en) * 2015-02-06 2017-08-10 Sorrento Therapeutics, Inc. Antibody Drug Conjugates
CN106794258B (zh) * 2015-02-15 2019-07-12 江苏恒瑞医药股份有限公司 配体-细胞毒性药物偶联物、其制备方法及其应用
CN106279352B (zh) 2015-05-29 2020-05-22 上海新理念生物医药科技有限公司 海兔毒素10的衍生物及其应用
EP3308801A4 (en) 2015-06-09 2019-02-27 XDCExplorer (Shanghai) Co., Ltd. ANTIBODY-ACTIVE CONJUGATE, INTERMEDIATE PRODUCT, METHOD OF MANUFACTURE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
SMT202000359T1 (it) 2015-07-10 2020-09-10 Genmab As Coniugati anticorpo-farmaco specifici per axl per il trattamento del cancro
AU2015242213A1 (en) 2015-07-12 2018-03-08 Hangzhou Dac Biotech Co., Ltd Bridge linkers for conjugation of cell-binding molecules
US9839687B2 (en) 2015-07-15 2017-12-12 Suzhou M-Conj Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
WO2017054080A1 (en) * 2015-09-29 2017-04-06 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
WO2017058808A1 (en) * 2015-10-02 2017-04-06 Sirenas Llc Anti-cancer compounds and conjugates thereof
EP3165237B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Antibody-drug conjugate (adc) and method for forming the same
CN106729743B (zh) * 2015-11-23 2021-09-21 四川科伦博泰生物医药股份有限公司 抗ErbB2抗体-药物偶联物及其组合物、制备方法和应用
CN108367043A (zh) 2015-12-04 2018-08-03 西雅图基因公司 季铵化的微管溶素化合物的缀合物
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
TWI753875B (zh) 2016-01-08 2022-02-01 美商美國全心醫藥生技股份有限公司 四價抗psgl-1抗體及其用途
CN107029244B (zh) * 2016-02-04 2021-04-27 浙江昭华生物医药有限公司 抗her2抗体-药物偶联物及其应用
SMT202100416T1 (it) 2016-03-02 2021-09-14 Eisai R&D Man Co Ltd Coniugati anticorpo-farmaco a base di eribulina e metodi di uso
EP3433278A4 (en) 2016-03-25 2019-11-06 Seattle Genetics, Inc. METHOD FOR THE PRODUCTION OF PEGYLATED ACTIVE LINKERS AND INTERMEDIATE PRODUCTS THEREOF
US20170281758A1 (en) * 2016-03-29 2017-10-05 Sorrento Therapeutics, Inc. Calicheamicin antibody drug conjugates linking an amidoacetyl group to a sugar moiety on calicheamicin
CN108779146B (zh) * 2016-03-29 2022-03-18 东丽株式会社 肽衍生物及其用途
MA45328A (fr) 2016-04-01 2019-02-06 Avidity Biosciences Llc Compositions acide nucléique-polypeptide et utilisations de celles-ci
CA3025931A1 (en) * 2016-05-31 2017-12-07 Sorrento Therapeutics, Inc. Antibody drug conjugates having derivatives of amatoxin as the drug
IL263744B2 (en) 2016-06-17 2023-11-01 Magenta Therapeutics Inc Compositions and methods for the depletion of cd117 plus cells
WO2018036438A1 (zh) * 2016-08-23 2018-03-01 四川科伦博泰生物医药股份有限公司 一种抗体-药物偶联物及其制备方法和应用
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
CN109810039B (zh) * 2017-11-22 2021-11-12 迈威(上海)生物科技股份有限公司 一种用于抗体-药物偶联的双取代马来酰胺类连接子及其制备方法和用途
CN110088086B (zh) * 2016-11-25 2022-12-16 迈威(上海)生物科技股份有限公司 用于抗体-药物偶联的双取代马来酰胺类连接子及其制备方法和用途
CN108101825B (zh) * 2016-11-25 2022-02-22 迈威(上海)生物科技股份有限公司 用于抗体-药物偶联的双取代马来酰胺类连接子及其制备方法和用途
US10864279B2 (en) 2016-12-16 2020-12-15 Industrial Technology Research Institute Linker-drug and antibody-drug conjugate (ADC) employing the same
KR20190104381A (ko) 2017-01-06 2019-09-09 어비디티 바이오사이언시스 엘엘씨 핵산-폴리펩티드 조성물 및 엑손 스키핑을 유도하는 방법
CA3049501A1 (en) 2017-01-20 2018-07-26 Magenta Therapeutics, Inc. Compositions and methods for the depletion of cd137+ cells
JP7527787B2 (ja) 2017-03-24 2024-08-05 シージェン インコーポレイテッド グルクロニド薬物-リンカーの調製のためのプロセスおよびその中間体
MX2019011957A (es) * 2017-04-06 2019-11-07 Hangzhou Dac Biotech Co Ltd Conjugacion de un farmaco citotoxico con enlace bis.
US11207420B2 (en) 2017-04-19 2021-12-28 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Cytotoxin and conjugate, uses of same and preparation method therefor
KR102771835B1 (ko) * 2017-06-20 2025-02-26 비바솔, 인코포레이티드. Cd38 항체 약물 접합체
AU2018289349A1 (en) 2017-06-20 2020-01-02 Madrigal Pharmaceuticals, Inc. Combination therapies comprising targeted therapeutics
KR20200016875A (ko) 2017-06-20 2020-02-17 마드리갈 파마슈티칼스 인코포레이티드 표적화 치료제
GB201711809D0 (en) 2017-07-21 2017-09-06 Governors Of The Univ Of Alberta Antisense oligonucleotide
JP7368856B2 (ja) 2017-07-25 2023-10-25 トゥルーバインディング,インコーポレイテッド Tim-3とそのリガンドとの相互作用の遮断によるがん治療
US10799598B2 (en) 2017-08-01 2020-10-13 Sorrento Therapeutics, Inc. Disulfide bridging conjugates
CA3072500A1 (en) 2017-08-10 2019-02-14 Sumitomo Dainippon Pharma Co., Ltd. Hemiasterlin derivatives and antibody-drug conjugates including same
IL272837B2 (en) 2017-09-08 2024-06-01 Seagen Inc Process for the preparation of tubulysins and intermediates thereof
MX2020003596A (es) 2017-10-04 2020-07-22 Avidity Biosciences Inc Composiciones de acido nucleico-polipeptido y usos de las mismos.
BR112020010503A2 (pt) * 2017-11-30 2020-10-20 Seattle Genetics, Inc. processo para a preparação de compostos ligantes a fármacos
JP7506601B2 (ja) 2017-12-06 2024-06-26 アビディティー バイオサイエンシーズ,インク. 筋萎縮症と筋緊張性ジストロフィーを処置するための組成物および方法
CN113683622B (zh) 2017-12-15 2025-02-18 四川科伦博泰生物医药股份有限公司 生物活性物偶联物及其制备方法和用途
WO2019149116A1 (zh) * 2018-01-30 2019-08-08 四川科伦博泰生物医药股份有限公司 制备偶联物的方法
TWI838358B (zh) * 2018-02-20 2024-04-11 美商思進公司 疏水性奧瑞他汀(auristatin)f化合物及其結合物
MX2020012940A (es) 2018-06-01 2021-03-25 Eisai R&D Man Co Ltd Metodos de uso de moduladores de empalme.
IL316090A (en) 2018-06-01 2024-12-01 Eisai R&D Man Co Ltd Antibody-drug conjugates of splicing modulators and methods of use
US20210276971A1 (en) 2018-06-20 2021-09-09 The Research Foundation For The State University Of New York Triazamacrocycle-derived chelator compositions for coordination of imaging and therapy metal ions and methods of using same
MY195368A (en) * 2018-10-12 2023-01-16 Hangzhou Dac Biotech Co Ltd A Conjugation Linker Containing 2,3-Diaminosuccinyl Group
WO2020081493A1 (en) 2018-10-16 2020-04-23 Molecular Templates, Inc. Pd-l1 binding proteins
PH12021551389A1 (en) 2018-12-13 2022-05-16 Eisai R&D Man Co Ltd Herboxidiene antibody-drug conjugates and methods of use
CA3122316A1 (en) * 2018-12-21 2020-06-25 Seagen Inc. Adcs with thiol multiplex linkers
IL319265A (en) 2018-12-21 2025-04-01 Avidity Biosciences Inc Anti-transferrin receptor antibodies and their uses
CN116063505B (zh) 2019-01-30 2024-05-03 真和制药有限公司 抗gal3抗体及其用途
JP7479302B2 (ja) 2019-02-13 2024-05-08 住友ファーマ株式会社 ヘミアスタリン誘導体とその抗体薬物複合体
CA3127312A1 (en) 2019-02-13 2020-08-20 Sumitomo Dainippon Pharma Co., Ltd. Hemiasterlin derivative having cysteine residue
CN109824759A (zh) * 2019-03-08 2019-05-31 联宁(苏州)生物制药有限公司 一种用于抗体药物偶联物的药物-连接子mc-mmaf的制备方法及其中间体
AU2020263487A1 (en) 2019-04-25 2021-12-16 Avidity Biosciences, Inc. Nucleic acid compositions and methods of multi-exon skipping
CA3142283A1 (en) 2019-06-06 2020-12-10 Avidity Biosciences, Inc. Nucleic acid-polypeptide compositions and uses thereof
WO2020247818A1 (en) 2019-06-06 2020-12-10 Avidity Biosciences, Inc. Una amidites and uses thereof
US11918649B2 (en) 2019-09-18 2024-03-05 Molecular Templates, Inc. PD-L1-binding molecules comprising Shiga toxin a subunit scaffolds
JP2023509991A (ja) 2020-01-13 2023-03-10 シンアフィックス ビー.ブイ. 抗体及び免疫細胞エンゲージャーのコンジュゲート
CN115666656A (zh) 2020-01-13 2023-01-31 西纳福克斯股份有限公司 通过环加成双侧功能化抗体
WO2021144314A1 (en) 2020-01-13 2021-07-22 Synaffix B.V. Via cycloaddition bilaterally functionalized antibodies
CN115485300A (zh) 2020-02-26 2022-12-16 索伦托药业有限公司 具有通用掩蔽部分的可活化的抗原结合蛋白
CA3170633A1 (en) * 2020-03-09 2021-09-16 David Goeddel Efficient preparation of dolastatin and auristatin analogs through a common intermediate
CA3172111A1 (en) 2020-03-19 2021-09-23 Barbora MALECOVA Compositions and methods of treating facioscapulohumeral muscular dystrophy
EP4656242A2 (en) 2020-03-27 2025-12-03 Avidity Biosciences, Inc. Compositions and methods of treating muscle dystrophy
US10987487B1 (en) 2020-04-29 2021-04-27 Cure Medical Llc Gripper sleeve for urinary catheter
US12281166B2 (en) 2020-05-26 2025-04-22 Truebinding, Inc. Methods of treating inflammatory diseases by blocking Galectin-3
MX2022015374A (es) 2020-06-05 2023-01-16 Eisai R&D Man Co Ltd Conjugados de anticuerpo anti antigeno de maduracion de linfocitos b (bcma)-farmaco y metodos de uso.
EP4172141A1 (en) 2020-06-26 2023-05-03 Synaffix B.V. Methods for the preparation of linker payload constructs
NL2026400B1 (en) 2020-09-02 2022-05-04 Synaffix Bv Methods for the preparation of bioconjugates
JP2023540526A (ja) 2020-09-04 2023-09-25 ノヴァロック バイオセラピューティクス, リミテッド ネクチン-4抗体およびそれの使用
WO2022058395A1 (en) 2020-09-15 2022-03-24 Synaffix B.V. Antibody-exatecan conjugates
NL2026947B1 (en) 2020-11-20 2022-07-01 Synaffix Bv Tyrosine-based antibody conjugates
AR124475A1 (es) 2020-12-23 2023-03-29 Univ Muenchen Ludwig Maximilians Conjugados anticuerpo-droga mejorados dirigidos contra cd30 y usos de los mismos
JP2024504475A (ja) * 2021-01-28 2024-01-31 南京▲樺▼冠生物技▲術▼有限公司 複合体およびその使用
CN117157107A (zh) 2021-02-08 2023-12-01 西纳福克斯股份有限公司 多功能抗体
US20240181073A1 (en) 2021-03-03 2024-06-06 Sorrento Therapeutics, Inc. Antibody-Drug Conjugates Comprising an Anti-BCMA Antibody
WO2022197945A1 (en) 2021-03-17 2022-09-22 Molecular Templates, Inc. Pd-l1 binding proteins comprising shiga toxin a subunit scaffolds and cd8+ t cell antigens
WO2022204947A1 (zh) * 2021-03-30 2022-10-06 上海复旦张江生物医药股份有限公司 一种连接基药物偶联物的制备方法及其中间体
EP4370555A4 (en) 2021-07-13 2025-11-12 Truebinding Inc METHODS FOR PREVENTING PROTEIN AGGREGATION
CN118265544A (zh) 2021-09-16 2024-06-28 艾维迪提生物科学公司 治疗面肩肱型肌营养不良的组合物和方法
CN118524852A (zh) 2021-11-09 2024-08-20 真和制药有限公司 治疗或抑制心血管疾病的方法
KR20240125036A (ko) 2021-12-23 2024-08-19 마이레큘, 인크. 폴리뉴클레오타이드의 전달을 위한 조성물
JP2025509286A (ja) 2022-03-10 2025-04-11 ビバソル, インコーポレイテッド 抗体-薬物コンジュゲートおよびその使用
US12071621B2 (en) 2022-04-05 2024-08-27 Avidity Biosciences, Inc. Anti-transferrin receptor antibody-PMO conjugates for inducing DMD exon 44 skipping
WO2024026474A1 (en) 2022-07-29 2024-02-01 Regeneron Pharmaceuticals, Inc. Compositions and methods for transferrin receptor (tfr)-mediated delivery to the brain and muscle
CN119997985A (zh) 2022-08-15 2025-05-13 西纳福克斯股份有限公司 蒽环类药物及其缀合物
AU2023350248A1 (en) 2022-09-30 2025-04-17 Shanghai De Novo Pharmatech Co., Ltd. Benzazepine derivative, conjugate containing same, and use thereof
AU2023379457A1 (en) 2022-11-14 2025-05-15 Regeneron Pharmaceuticals, Inc. Compositions and methods for fibroblast growth factor receptor 3-mediated delivery to astrocytes
EP4389152A1 (en) 2022-12-23 2024-06-26 Synaffix B.V. Conjugates of pbd prodrugs
CN116621927B (zh) * 2023-01-09 2024-03-26 联宁(苏州)生物制药有限公司 带有伊喜替康和C-lock定点偶联基团的抗体偶联中间体、偶联方法及抗体偶联药物
EP4410313A1 (en) 2023-01-31 2024-08-07 Synaffix B.V. Homogeneous antibody-conjugates with high payload loading
AU2024229817A1 (en) 2023-02-28 2025-08-14 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Chemical coupling linker and use thereof
WO2024211234A1 (en) 2023-04-05 2024-10-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
WO2024211236A2 (en) 2023-04-05 2024-10-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
WO2024211235A1 (en) 2023-04-05 2024-10-10 Sorrento Therapeutics, Inc. Antibody-drug conjugates and uses thereof
EP4450093A1 (en) 2023-04-17 2024-10-23 Synaffix B.V. Cleavable immune cell engagers
WO2024218164A1 (en) 2023-04-17 2024-10-24 Synaffix B.V. Stable 4-isoxazoline conjugates
US12491257B2 (en) 2023-06-27 2025-12-09 Avidity Biosciences, Inc. Compositions and methods of using PRKAG2-targeting antibody-oligonucleotide conjugates
WO2025007063A1 (en) 2023-06-30 2025-01-02 Avidity Biosciences, Inc. Compositions and methods of using pln-targeting antibody-oligonucleotide conjugates
WO2025027529A1 (en) 2023-07-31 2025-02-06 Advesya Anti-il-1rap antibody drug conjugates and methods of use thereof
TW202530255A (zh) 2023-12-15 2025-08-01 法商亞維西亞有限公司 抗il-1rap結合結構域及其抗體-藥物偶聯物
CN117964682A (zh) * 2024-01-12 2024-05-03 杭州爱科瑞思生物医药有限公司 Dolastatin衍生物及其制备方法和应用
WO2025238253A1 (en) 2024-05-16 2025-11-20 Synaffix B.V. Antibody-oligonucleotide conjugates

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
US6569834B1 (en) 1992-12-03 2003-05-27 George R. Pettit Elucidation and synthesis of antineoplastic tetrapeptide w-aminoalkyl-amides
US5780588A (en) 1993-01-26 1998-07-14 Arizona Board Of Regents Elucidation and synthesis of selected pentapeptides
US6214345B1 (en) * 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
KR100332254B1 (ko) 1993-10-01 2002-09-27 데이꼬꾸 조끼 세이야꾸 가부시키가이샤 신규인펩티드유도체
US5525474A (en) * 1994-01-31 1996-06-11 Boehringer Mannheim Corporation Piperidine analogs and conjugates of procainamide and NAPA
AU2002243438A1 (en) 2000-10-25 2002-07-24 Mayo Foundation For Medical Education And Research Transcobalamin binding conjugates useful for treating abnormal cellular proliferation
JP4477881B2 (ja) 2002-03-01 2010-06-09 ジ アドミニストレイターズ オブ ザ チューレン エデュケイショナル ファンド 治療剤または細胞毒性剤と生物活性ペプチドとの抱合体
US20090068178A1 (en) 2002-05-08 2009-03-12 Genentech, Inc. Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin
AU2003266233A1 (en) 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie Novel tubulysin analogues
PT2357006E (pt) 2002-07-31 2016-01-22 Seattle Genetics Inc Conjugados de fármacos e sua utilização para tratamento do cancro, de uma doença autoimune ou de uma doença infeciosa
DE10254439A1 (de) 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
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
US7276497B2 (en) 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
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
SG149815A1 (en) 2003-11-06 2009-02-27 Seattle Genetics Inc Monomethylvaline compounds capable of conjugation to ligands
TR201808537T4 (tr) 2004-09-23 2018-07-23 Genentech Inc Sistein değiştirilmiş antikorlar ve konjugatlar.
WO2006060533A2 (en) 2004-12-01 2006-06-08 Genentech, Inc. Conjugates of 1, 8-bis-naphthalimides with an antibody
US20070134243A1 (en) 2004-12-01 2007-06-14 Gazzard Lewis J Antibody drug conjugates and methods
EP1844076A2 (en) 2005-01-31 2007-10-17 Genentech, Inc. Anti-ephb2 antibodies and methods using same
LT1912671T (lt) * 2005-07-18 2017-12-11 Seattle Genetics, Inc. Vaisto konjugatai, turintys gliukoronido linkerį
NZ566982A (en) * 2005-09-26 2011-06-30 Medarex Inc Duocarmycin drug conjugates
AR059900A1 (es) 2006-03-17 2008-05-07 Genentech Inc Anticuerpos anti-tat226 e inmunoconjugados
AR063942A1 (es) 2006-06-06 2009-03-04 Enanta Pharm Inc Compuestos de oximilo aciclico inhibidores de proteasa del virus de hepatitis c
CA2660572C (en) * 2006-08-11 2014-07-22 University Of Medicine And Dentistry Of New Jersey Dual-sensitizer-containing luminescent compounds, conjugates, and uses thereof
CN101500548A (zh) * 2006-08-18 2009-08-05 弗·哈夫曼-拉罗切有限公司 用于体内递送多核苷酸的多缀合物
JP5829793B2 (ja) 2007-03-14 2015-12-09 エンドサイト・インコーポレイテッドEndocyte, Inc. 結合性リガンドが結合したツブリシンの薬剤送達結合体
WO2008128164A1 (en) 2007-04-12 2008-10-23 The Penn State Research Foundation Accumulation field effect microelectronic device and process for the formation thereof
WO2009002993A1 (en) * 2007-06-25 2008-12-31 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
WO2009012958A2 (en) 2007-07-20 2009-01-29 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
KR101667062B1 (ko) 2008-07-15 2016-10-17 제넨테크, 인크. 안트라시클린 유도체 접합체, 그의 제조 방법 및 항-종양 화합물로서의 그의 용도
JP5675619B2 (ja) * 2008-09-17 2015-02-25 エンドサイト, インク.Endocyte, Inc. 葉酸拮抗薬の葉酸受容体結合性コンジュゲート
EP2174947A1 (en) 2008-09-25 2010-04-14 Universität des Saarlandes Bioactive pre-tubulysins and use thereof
CA3150199C (en) * 2009-01-09 2025-07-22 Seagen Inc. WEEKLY DOSING REGIMEN FOR ANTI-CD30 ANTIBODY CONJUGATIONS VC-PAB-MMAE - MEDICINE
WO2010100430A1 (en) 2009-03-04 2010-09-10 Polytherics Limited Conjugated proteins and peptides
US8394922B2 (en) * 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
TWI504410B (zh) * 2010-02-08 2015-10-21 Agensys Inc 結合至161p2f10b蛋白之抗體藥物結合物(adc)
NZ602840A (en) * 2010-06-03 2014-11-28 Genentech Inc Immuno-pet imaging of antibodies and immunoconjugates and uses therefor
AU2011265054B2 (en) 2010-06-08 2016-09-15 Genentech, Inc. Cysteine engineered antibodies and conjugates
EP2409983A1 (en) 2010-07-19 2012-01-25 Leibniz-Institut für Pflanzenbiochemie (IPB) Tubulysin analogues
CN103379912B (zh) 2010-09-29 2016-03-16 西雅图基因公司 正羧烷基耳他汀及其应用
BR112013013127B1 (pt) 2010-12-02 2021-06-22 Nerviano Medical Sciences S.R.L. Processo para a preparação de derivados de morfolinil antraciclina, compostos derivados de morfolinil antraciclina e composição farmacêutica compreendendo estes compostos
ES2690993T3 (es) 2011-05-27 2018-11-23 Ambrx, Inc. Composiciones que contienen y métodos que implican derivados de dolastatina enlazados con aminoácidos no naturales y usos de los mismos
MX345538B (es) 2011-05-27 2017-02-03 Ambrx Inc Composiciones que contienen, metodos que incluyen, y usos de derivados de dolastatina enlazados a aminoacidos no naturales.
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
JP6209159B2 (ja) 2011-06-21 2017-10-04 イミュノジェン・インコーポレーテッド 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
CA2857398A1 (en) * 2011-12-05 2013-06-13 Igenica Biotherapeutics, Inc. Antibody-drug conjugates and related compounds, compositions, and methods
US9981046B2 (en) 2012-05-15 2018-05-29 Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. Drug-conjugates, conjugation methods, and uses thereof
MX363116B (es) 2012-06-07 2019-03-11 Ambrx Inc Conjugados anticuerpo-farmaco de antigeno de membrana especifico de prostata.
CN104619351B (zh) 2012-06-19 2020-01-21 Ambrx公司 抗cd70抗体药物结合物
HK1207972A1 (en) 2012-07-09 2016-02-19 基因泰克公司 Immunoconjugates comprising anti - cd79b antibodies
CA2934030A1 (en) 2013-10-15 2015-04-23 Sorrento Therapeutics Inc. Drug-conjugates with a targeting molecule and two different drugs
ES2918425T3 (es) 2015-01-28 2022-07-15 Sorrento Therapeutics Inc Conjugados de anticuerpo-fármaco
US20170224835A1 (en) 2015-02-06 2017-08-10 Sorrento Therapeutics, Inc. Antibody Drug Conjugates

Also Published As

Publication number Publication date
US20180243438A1 (en) 2018-08-30
EP2849790A4 (en) 2016-04-13
JP2018052951A (ja) 2018-04-05
EP2850059A4 (en) 2016-06-29
EP3520817A1 (en) 2019-08-07
EP3925627A1 (en) 2021-12-22
US20150105539A1 (en) 2015-04-16
EP2849797A1 (en) 2015-03-25
EP3590541A1 (en) 2020-01-08
JP2015518832A (ja) 2015-07-06
JP6239597B2 (ja) 2017-11-29
EP2849797A4 (en) 2016-04-27
WO2013173392A1 (en) 2013-11-21
EP2849790A1 (en) 2015-03-25
HK1208163A1 (en) 2016-02-26
US9801951B2 (en) 2017-10-31
US20250135024A1 (en) 2025-05-01
JP2015518833A (ja) 2015-07-06
EP2849797B1 (en) 2019-12-18
US12115228B2 (en) 2024-10-15
CN107982545A (zh) 2018-05-04
WO2013173393A1 (en) 2013-11-21
JP6239598B2 (ja) 2017-11-29
ES2887208T3 (es) 2021-12-22
CN107982545B (zh) 2021-04-09
US20160067350A1 (en) 2016-03-10
CN104640572B (zh) 2018-04-27
JP2015518831A (ja) 2015-07-06
US20210187119A1 (en) 2021-06-24
US9981046B2 (en) 2018-05-29
US9884127B2 (en) 2018-02-06
ES2734259T3 (es) 2019-12-05
US10967071B2 (en) 2021-04-06
EP3590541B1 (en) 2021-08-11
CN104379168A (zh) 2015-02-25
EP2849790B1 (en) 2019-04-10
CN104640572A (zh) 2015-05-20
CN104662000A (zh) 2015-05-27
HK1208216A1 (en) 2016-02-26
CN104379168B (zh) 2017-08-15
WO2013173391A1 (en) 2013-11-21
US20180085471A1 (en) 2018-03-29
EP2850059A1 (en) 2015-03-25
JP2018058851A (ja) 2018-04-12
CN104662000B (zh) 2018-08-17
HK1208165A1 (en) 2016-04-01
US20150141646A1 (en) 2015-05-21

Similar Documents

Publication Publication Date Title
JP6280103B2 (ja) 薬物コンジュゲート、コンジュゲーション方法およびその使用
US10722593B2 (en) Anti-cancer compounds and conjugates thereof
HK40064991A (en) Drug-conjugates and uses thereof
HK40012657A (en) Drug-conjugates, conjugation methods, and uses thereof
HK1208163B (en) Drug-conjugates, conjugation methods, and uses thereof
HK40011591B (en) Drug-conjugates and uses thereof
HK40011591A (en) Drug-conjugates and uses thereof
HK1208165B (en) Drug-conjugates, conjugation methods, and uses thereof

Legal Events

Date Code Title Description
A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20150203

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160511

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160511

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170316

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170411

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170710

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170711

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20171128

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171206

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20171219

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20180118

R150 Certificate of patent or registration of utility model

Ref document number: 6280103

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

LAPS Cancellation because of no payment of annual fees