JP2024520283A - 化学的カップリングリンカー及びその使用 - Google Patents
化学的カップリングリンカー及びその使用 Download PDFInfo
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- JP2024520283A JP2024520283A JP2023567997A JP2023567997A JP2024520283A JP 2024520283 A JP2024520283 A JP 2024520283A JP 2023567997 A JP2023567997 A JP 2023567997A JP 2023567997 A JP2023567997 A JP 2023567997A JP 2024520283 A JP2024520283 A JP 2024520283A
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- antibody
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68037—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6849—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic 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
- C07D207/44—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members
- C07D207/444—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic 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
- C07D207/44—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members
- C07D207/444—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
- C07D207/448—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
- C07D207/452—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/38—One sulfur atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/58—Two sulfur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
- C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
- C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
- C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
- C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
- C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
- C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
- C07D251/20—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with no nitrogen atoms directly attached to a ring carbon atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
- C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
- C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
- C07D251/40—Nitrogen atoms
- C07D251/42—One nitrogen atom
- C07D251/46—One nitrogen atom with oxygen or sulfur atoms attached to the two other ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/12—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Cell Biology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (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)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110615166 | 2021-06-02 | ||
| CN202110615166.4 | 2021-06-02 | ||
| CN202111225483 | 2021-10-21 | ||
| CN202111225483.1 | 2021-10-21 | ||
| PCT/CN2022/094540 WO2022253033A1 (zh) | 2021-06-02 | 2022-05-23 | 一类化学偶联连接子及其用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2024520283A true JP2024520283A (ja) | 2024-05-24 |
| JP2024520283A5 JP2024520283A5 (enExample) | 2025-04-24 |
Family
ID=84323890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023567997A Pending JP2024520283A (ja) | 2021-06-02 | 2022-05-23 | 化学的カップリングリンカー及びその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20240252665A1 (enExample) |
| EP (1) | EP4349832A1 (enExample) |
| JP (1) | JP2024520283A (enExample) |
| KR (1) | KR20240017343A (enExample) |
| CN (1) | CN117255790A (enExample) |
| WO (1) | WO2022253033A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2022216696A1 (en) * | 2021-02-05 | 2023-08-17 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Camptothecin compound, preparation method therefor, and application thereof |
| WO2024114318A1 (zh) * | 2022-11-29 | 2024-06-06 | 四川科伦博泰生物医药股份有限公司 | 药物连接子化合物及其制备方法和用途 |
| KR20250113394A (ko) * | 2022-11-29 | 2025-07-25 | 쓰촨 케룬-바이오테크 바이오파마수티컬 컴퍼니 리미티드 | 접합 반응에 사용할 수 있는 화합물 및 이의 접합체 |
| KR20250153767A (ko) * | 2023-02-28 | 2025-10-27 | 쓰촨 케룬-바이오테크 바이오파마수티컬 컴퍼니 리미티드 | 화학적 접합 링커 및 이의 용도 |
| CN122080121A (zh) * | 2023-03-22 | 2026-05-26 | 映恩生物科技(上海)有限公司 | 连接子及其在配体药物偶联物中的应用 |
| WO2024235131A1 (zh) * | 2023-05-12 | 2024-11-21 | 四川科伦博泰生物医药股份有限公司 | 大环类药物偶联物及其制备方法和用途 |
| WO2024235133A1 (zh) * | 2023-05-12 | 2024-11-21 | 四川科伦博泰生物医药股份有限公司 | 多环类药物偶联物及其制备方法和用途 |
| CN120981249A (zh) * | 2023-05-12 | 2025-11-18 | 四川科伦博泰生物医药股份有限公司 | 多环化合物及其制备方法和用途 |
| WO2024235136A1 (zh) * | 2023-05-12 | 2024-11-21 | 四川科伦博泰生物医药股份有限公司 | 杂环类化合物及其制备方法和用途 |
| WO2024235134A1 (zh) * | 2023-05-12 | 2024-11-21 | 四川科伦博泰生物医药股份有限公司 | 具有靶向作用的偶联物及其制备方法和用途 |
| WO2024235135A1 (zh) * | 2023-05-12 | 2024-11-21 | 四川科伦博泰生物医药股份有限公司 | 大环化合物及其制备方法和用途 |
| KR20260115591A (ko) * | 2023-10-19 | 2026-07-24 | 유노벨(상하이) 바이오파마 씨오 엘티디 | 폴리펩타이드, 생리활성 접합체, 이의 제조방법 및 용도 |
| AU2024369355A1 (en) * | 2023-10-23 | 2026-05-07 | Shanghai Qilu Pharmaceutical Research And Development Centre Ltd. | Camptothecin drug conjugate, and preparation method therefor and use thereof |
| CN122249237A (zh) * | 2023-11-14 | 2026-06-19 | 先声再明医药股份有限公司 | 配体-药物偶联物、偶联连接子及其用途 |
| CN122161833A (zh) * | 2023-11-15 | 2026-06-05 | 四川科伦博泰生物医药股份有限公司 | 靶向EGFR/c-MET的抗体-药物缀合物及其制备方法和用途 |
| WO2025149667A1 (en) * | 2024-01-12 | 2025-07-17 | Pheon Therapeutics Ltd | Antibody drug conjugates and uses thereof |
| WO2025232688A1 (zh) * | 2024-05-10 | 2025-11-13 | 四川科伦博泰生物医药股份有限公司 | 并环类药物偶联物及其制备方法和用途 |
| WO2025232843A1 (zh) * | 2024-05-10 | 2025-11-13 | 四川科伦博泰生物医药股份有限公司 | 稠环类化合物及其制备方法和用途 |
| WO2025232118A1 (zh) * | 2024-05-10 | 2025-11-13 | 四川科伦博泰生物医药股份有限公司 | 稠环类化合物及其制备方法和用途 |
| WO2025232845A1 (zh) * | 2024-05-10 | 2025-11-13 | 四川科伦博泰生物医药股份有限公司 | 具有靶向作用的偶联物及其制备方法和用途 |
| WO2026067713A1 (zh) * | 2024-09-29 | 2026-04-02 | 四川科伦博泰生物医药股份有限公司 | 抗体药物偶联物,及其制备方法和用途 |
Citations (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2993901A (en) * | 1953-06-08 | 1961-07-25 | American Cyanamid Co | Benzanthrone anthraquinone acridines as dyestuffs |
| JPH04194847A (ja) * | 1990-11-22 | 1992-07-14 | Fuji Photo Film Co Ltd | ハロゲン化銀カラー写真感光材料 |
| JPH05222043A (ja) * | 1991-10-17 | 1993-08-31 | Merck & Co Inc | Mrsa活性2−フェニル−カルバペネム |
| WO2000029404A1 (en) * | 1998-11-17 | 2000-05-25 | Kumiai Chemical Industry Co., Ltd. | Pyrimidinylbenzimidazole and triazinylbenzimidazole derivatives and agricultura/horticultural bactericides |
| JP2002193710A (ja) * | 2000-12-25 | 2002-07-10 | Kumiai Chem Ind Co Ltd | ピリミジン又はトリアジン誘導体及び農園芸用殺菌剤 |
| JP2007502267A (ja) * | 2003-08-14 | 2007-02-08 | ディ − ファーム リミテッド | 癲癇発生の危険性の低減用および/または発作性疾患の治療用の組成物および方法 |
| JP2007509043A (ja) * | 2003-10-07 | 2007-04-12 | レノビス, インコーポレイテッド | イオンチャネルリガンドとしてのアミド誘導体および薬学的組成物、ならびにこれらを使用する方法 |
| WO2007056215A2 (en) * | 2005-11-02 | 2007-05-18 | Cytovia, Inc. | N-aryl-thienopyrimidin-4-amines and the use thereof |
| JP2008500943A (ja) * | 2003-05-06 | 2008-01-17 | プロテオジス アクチェンゲゼルシャフト | リン酸化ペプチドおよび/またはタンパク質のアフィニティに基づく濃縮 |
| JP2009518442A (ja) * | 2005-12-05 | 2009-05-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 可溶性エポキシド加水分解酵素インヒビターとして有益な置換ピラゾール化合物 |
| JP2010517957A (ja) * | 2007-02-01 | 2010-05-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Pi3−キナーゼインヒビターとしてのプテリジノン誘導体 |
| JP2010537981A (ja) * | 2007-08-29 | 2010-12-09 | シェーリング コーポレイション | 置換インドール誘導体およびその使用の方法 |
| JP2011506600A (ja) * | 2007-12-18 | 2011-03-03 | アリーナ ファーマシューティカルズ, インコーポレイテッド | 自己免疫性障害および炎症性障害の治療において有用なテトラヒドロシクロペンタ[b]インドール−3−イルカルボン酸誘導体 |
| US20110178134A1 (en) * | 2008-02-07 | 2011-07-21 | Sanofi-Aventis | Novel phenyl-substituted imidazolidines, process for preparation thereof, medicaments comprising said compounds and use thereof |
| WO2012109164A1 (en) * | 2011-02-07 | 2012-08-16 | Rempex Pharmaceuticals, Inc. | Boron containing polybasic bacterial efflux pump inhibitors and therapeutics uses thereof |
| JP2012529535A (ja) * | 2009-06-12 | 2012-11-22 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼモジュレーターとして有用なニコチンアミド化合物 |
| JP2013523658A (ja) * | 2010-03-26 | 2013-06-17 | グラクソ グループ リミテッド | キナーゼ阻害剤としてのピラゾリル‐ピリミジン |
| CN103274989A (zh) * | 2013-06-08 | 2013-09-04 | 南京正荣医药化学有限公司 | 八氢环戊并[c]吡咯衍生物及其盐的制备方法 |
| WO2015057876A1 (en) * | 2013-10-15 | 2015-04-23 | Sorrento Therapeutics Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| JP2015518831A (ja) * | 2012-05-15 | 2015-07-06 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 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 |
| WO2015175855A1 (en) * | 2014-05-16 | 2015-11-19 | Emory University | Chemokine cxcr4 and ccr5 receptor modulators and used related thereto |
| JP2016534105A (ja) * | 2013-08-14 | 2016-11-04 | ウィリアム マーシュ ライス ユニバーシティWilliam Marsh Rice University | ウンシアラマイシン誘導体、合成方法、および抗腫瘍薬としてのそれらの使用 |
| WO2017172907A1 (en) * | 2016-03-29 | 2017-10-05 | Sorrento Therapeutics, Inc. | Calicheamicin antibody drug conjugates linking an amidoacetyl group to a sugar moiety on calicheamicin |
| JP2018507844A (ja) * | 2015-02-06 | 2018-03-22 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 抗体薬物コンジュゲート |
| JP2018512376A (ja) * | 2015-01-28 | 2018-05-17 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 抗体薬物コンジュゲート |
| WO2019011078A1 (en) * | 2017-07-10 | 2019-01-17 | Newbio Therapeutics, Inc. | OXADIAZOLE LINKS AND ASSOCIATED USE |
| JP2019508495A (ja) * | 2016-02-04 | 2019-03-28 | 浙江昭華生物医薬有限公司 | 抗her2抗体−薬物抱合体およびその使用 |
| JP2019523761A (ja) * | 2016-05-31 | 2019-08-29 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 薬物としてアマトキシンの誘導体を有する抗体薬物コンジュゲート |
| WO2019220101A1 (en) * | 2018-05-15 | 2019-11-21 | The University Of Manchester | Kinase inhibitors |
| JP2020514302A (ja) * | 2017-01-08 | 2020-05-21 | 浙江昭華生物医薬有限公司 | 抗5t4抗体−薬物複合体およびその使用 |
| US20200179529A1 (en) * | 2017-04-19 | 2020-06-11 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Cytotoxin and conjugate, uses of same and preparation method therefor |
| JP2020524675A (ja) * | 2017-06-20 | 2020-08-20 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | Cd38抗体薬物コンジュゲート |
| CN113264900A (zh) * | 2021-06-07 | 2021-08-17 | 南京中医药大学 | 一种苯并异噻唑和苯并噻吩的制备方法及其医药用途 |
| CN113549127A (zh) * | 2020-04-24 | 2021-10-26 | 上海翰森生物医药科技有限公司 | 长春新碱及其抗体偶联物、其制备方法和医药用途 |
| CN113816990A (zh) * | 2021-03-22 | 2021-12-21 | 联宁(苏州)生物制药有限公司 | 修饰的氨基酸及其在adc中的应用 |
| US20220024904A1 (en) * | 2020-07-06 | 2022-01-27 | Research Foundation Of The City University Of New York | Reagent for bioconjugation via irreversible rebridging of disulfide linkages |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR3008408B1 (fr) * | 2013-07-11 | 2018-03-09 | Mc Saf | Nouveaux conjugues anticorps-medicament et leur utilisation en therapie |
| WO2019057964A1 (en) | 2017-09-22 | 2019-03-28 | Heidelberg Pharma Research Gmbh | AMANITINE CONJUGATES TARGETING PSMA |
| FR3096259B1 (fr) * | 2019-05-20 | 2023-12-15 | Mc Saf | conjugués anticorps-médicament et leur utilisation en thérapie |
-
2022
- 2022-05-23 US US18/559,039 patent/US20240252665A1/en active Pending
- 2022-05-23 CN CN202280032554.2A patent/CN117255790A/zh active Pending
- 2022-05-23 JP JP2023567997A patent/JP2024520283A/ja active Pending
- 2022-05-23 EP EP22815080.1A patent/EP4349832A1/en active Pending
- 2022-05-23 KR KR1020237037967A patent/KR20240017343A/ko active Pending
- 2022-05-23 WO PCT/CN2022/094540 patent/WO2022253033A1/zh not_active Ceased
Patent Citations (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2993901A (en) * | 1953-06-08 | 1961-07-25 | American Cyanamid Co | Benzanthrone anthraquinone acridines as dyestuffs |
| JPH04194847A (ja) * | 1990-11-22 | 1992-07-14 | Fuji Photo Film Co Ltd | ハロゲン化銀カラー写真感光材料 |
| JPH05222043A (ja) * | 1991-10-17 | 1993-08-31 | Merck & Co Inc | Mrsa活性2−フェニル−カルバペネム |
| WO2000029404A1 (en) * | 1998-11-17 | 2000-05-25 | Kumiai Chemical Industry Co., Ltd. | Pyrimidinylbenzimidazole and triazinylbenzimidazole derivatives and agricultura/horticultural bactericides |
| JP2002193710A (ja) * | 2000-12-25 | 2002-07-10 | Kumiai Chem Ind Co Ltd | ピリミジン又はトリアジン誘導体及び農園芸用殺菌剤 |
| JP2008500943A (ja) * | 2003-05-06 | 2008-01-17 | プロテオジス アクチェンゲゼルシャフト | リン酸化ペプチドおよび/またはタンパク質のアフィニティに基づく濃縮 |
| JP2007502267A (ja) * | 2003-08-14 | 2007-02-08 | ディ − ファーム リミテッド | 癲癇発生の危険性の低減用および/または発作性疾患の治療用の組成物および方法 |
| JP2007509043A (ja) * | 2003-10-07 | 2007-04-12 | レノビス, インコーポレイテッド | イオンチャネルリガンドとしてのアミド誘導体および薬学的組成物、ならびにこれらを使用する方法 |
| WO2007056215A2 (en) * | 2005-11-02 | 2007-05-18 | Cytovia, Inc. | N-aryl-thienopyrimidin-4-amines and the use thereof |
| JP2009518442A (ja) * | 2005-12-05 | 2009-05-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 可溶性エポキシド加水分解酵素インヒビターとして有益な置換ピラゾール化合物 |
| JP2010517957A (ja) * | 2007-02-01 | 2010-05-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Pi3−キナーゼインヒビターとしてのプテリジノン誘導体 |
| JP2010537981A (ja) * | 2007-08-29 | 2010-12-09 | シェーリング コーポレイション | 置換インドール誘導体およびその使用の方法 |
| JP2011506600A (ja) * | 2007-12-18 | 2011-03-03 | アリーナ ファーマシューティカルズ, インコーポレイテッド | 自己免疫性障害および炎症性障害の治療において有用なテトラヒドロシクロペンタ[b]インドール−3−イルカルボン酸誘導体 |
| US20110178134A1 (en) * | 2008-02-07 | 2011-07-21 | Sanofi-Aventis | Novel phenyl-substituted imidazolidines, process for preparation thereof, medicaments comprising said compounds and use thereof |
| JP2012529535A (ja) * | 2009-06-12 | 2012-11-22 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼモジュレーターとして有用なニコチンアミド化合物 |
| JP2013523658A (ja) * | 2010-03-26 | 2013-06-17 | グラクソ グループ リミテッド | キナーゼ阻害剤としてのピラゾリル‐ピリミジン |
| WO2012109164A1 (en) * | 2011-02-07 | 2012-08-16 | Rempex Pharmaceuticals, Inc. | Boron containing polybasic bacterial efflux pump inhibitors and therapeutics uses thereof |
| JP2015518831A (ja) * | 2012-05-15 | 2015-07-06 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 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 |
| JP2015518833A (ja) * | 2012-05-15 | 2015-07-06 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 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 |
| CN103274989A (zh) * | 2013-06-08 | 2013-09-04 | 南京正荣医药化学有限公司 | 八氢环戊并[c]吡咯衍生物及其盐的制备方法 |
| JP2016534105A (ja) * | 2013-08-14 | 2016-11-04 | ウィリアム マーシュ ライス ユニバーシティWilliam Marsh Rice University | ウンシアラマイシン誘導体、合成方法、および抗腫瘍薬としてのそれらの使用 |
| WO2015057876A1 (en) * | 2013-10-15 | 2015-04-23 | Sorrento Therapeutics Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| WO2015175855A1 (en) * | 2014-05-16 | 2015-11-19 | Emory University | Chemokine cxcr4 and ccr5 receptor modulators and used related thereto |
| JP2018512376A (ja) * | 2015-01-28 | 2018-05-17 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 抗体薬物コンジュゲート |
| JP2018507844A (ja) * | 2015-02-06 | 2018-03-22 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 抗体薬物コンジュゲート |
| JP2019508495A (ja) * | 2016-02-04 | 2019-03-28 | 浙江昭華生物医薬有限公司 | 抗her2抗体−薬物抱合体およびその使用 |
| WO2017172907A1 (en) * | 2016-03-29 | 2017-10-05 | Sorrento Therapeutics, Inc. | Calicheamicin antibody drug conjugates linking an amidoacetyl group to a sugar moiety on calicheamicin |
| JP2019523761A (ja) * | 2016-05-31 | 2019-08-29 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | 薬物としてアマトキシンの誘導体を有する抗体薬物コンジュゲート |
| JP2020514302A (ja) * | 2017-01-08 | 2020-05-21 | 浙江昭華生物医薬有限公司 | 抗5t4抗体−薬物複合体およびその使用 |
| US20200179529A1 (en) * | 2017-04-19 | 2020-06-11 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Cytotoxin and conjugate, uses of same and preparation method therefor |
| JP2020524675A (ja) * | 2017-06-20 | 2020-08-20 | ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. | Cd38抗体薬物コンジュゲート |
| WO2019011078A1 (en) * | 2017-07-10 | 2019-01-17 | Newbio Therapeutics, Inc. | OXADIAZOLE LINKS AND ASSOCIATED USE |
| WO2019220101A1 (en) * | 2018-05-15 | 2019-11-21 | The University Of Manchester | Kinase inhibitors |
| CN113549127A (zh) * | 2020-04-24 | 2021-10-26 | 上海翰森生物医药科技有限公司 | 长春新碱及其抗体偶联物、其制备方法和医药用途 |
| US20220024904A1 (en) * | 2020-07-06 | 2022-01-27 | Research Foundation Of The City University Of New York | Reagent for bioconjugation via irreversible rebridging of disulfide linkages |
| CN113816990A (zh) * | 2021-03-22 | 2021-12-21 | 联宁(苏州)生物制药有限公司 | 修饰的氨基酸及其在adc中的应用 |
| CN113264900A (zh) * | 2021-06-07 | 2021-08-17 | 南京中医药大学 | 一种苯并异噻唑和苯并噻吩的制备方法及其医药用途 |
Non-Patent Citations (8)
| Title |
|---|
| BARDELLE, CATHERINE ET AL.: "Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-b", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 18(21), JPN7026001729, 2008, NL, pages 5717 - 5721, ISSN: 0005849617 * |
| BOOTHE, J. H. ET AL.: "7-Methylpteroylglutamic acid and some related compounds", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 74, JPN7026001734, 1952, US, pages 5407 - 5409, ISSN: 0005849612 * |
| DATABASE REGISTRY [ONLINE] RETRIEVED FROM STN, JPN7026001727, 29 October 2004 (2004-10-29), ISSN: 0005849619 * |
| DATABASE REGISTRY [ONLINE] RETRIEVED FROM STN, JPN7026001732, 1 November 2004 (2004-11-01), ISSN: 0005849614 * |
| DE MACEDO PAYAU, P. ET AL.: "Synthesis of substrate analogs and inhibitors for the phosphoglycerate mutase enzyme", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS, vol. 129, JPN7026001733, 1997, UK, pages 13 - 45, ISSN: 0005849613 * |
| ELAHEH KHOZEIMEH SARBISHEH ET AL.: "DiPODS: A Reagent for Site-Specific Bioconjugation via the Irreversible Rebridging of Disulfide Link", BIOCONJUGATE CHEMISTRY, vol. 31, JPN7026001731, 2020, US, pages 2789 - 2806, ISSN: 0005849615 * |
| HARNDEN, MICHAEL R. ET AL.: "The chemistry of pyrimidinethiols. III. The synthesis of some substituted pyrimidinethiols and som", AUSTRALIAN JOURNAL OF CHEMISTRY, vol. 43(1), JPN7026001728, 1990, AU, pages 55 - 62, ISSN: 0005849618 * |
| VOLKOV, OLEG A. ET AL.: "Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylas", JOURNAL OF MEDICINAL CHEMISTRY, vol. 61(3), JPN7026001730, 2018, US, pages 1182 - 1203, ISSN: 0005849616 * |
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| US20240252665A1 (en) | 2024-08-01 |
| WO2022253033A1 (zh) | 2022-12-08 |
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