EA201791024A1 - Конъюгаты биомолекул - Google Patents

Конъюгаты биомолекул

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Publication number
EA201791024A1
EA201791024A1 EA201791024A EA201791024A EA201791024A1 EA 201791024 A1 EA201791024 A1 EA 201791024A1 EA 201791024 A EA201791024 A EA 201791024A EA 201791024 A EA201791024 A EA 201791024A EA 201791024 A1 EA201791024 A1 EA 201791024A1
Authority
EA
Eurasian Patent Office
Prior art keywords
conjugates
biomolecule
nnaa
methods
relates
Prior art date
Application number
EA201791024A
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English (en)
Other versions
EA039794B1 (ru
Inventor
Эрик Шварц
Лаура Акуллиан Д'Агостино
Эрнан Куэрво
Уэсли Остин
Original Assignee
Селджин Корпорейшн
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Publication date
Application filed by Селджин Корпорейшн filed Critical Селджин Корпорейшн
Publication of EA201791024A1 publication Critical patent/EA201791024A1/ru
Publication of EA039794B1 publication Critical patent/EA039794B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
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    • 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
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    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
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    • 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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    • 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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
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    • 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
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    • 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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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Настоящее изобретение относится к конъюгатам биомолекул, которые содержат биомолекулу, в которой по меньшей мере одна аминокислота неприродного происхождения (NNAA) является встроенной в структуру биомолекулы и в которой NNAA представляет собой точку присоединения линкера, к которой присоединяется полезная нагрузка, в частности цитотоксическое средство. В частности, настоящее изобретение относится к конъюгатам клеточно-связывающих средств и продуктам активного высвобождения, состоящих из цитотоксических средств, где конъюгаты получены посредством реакции циклоприсоединения. Предусматриваются способы получения, фармацевтические композиции и способы применения.
EA201791024A 2014-12-04 2015-12-03 Конъюгаты биомолекул EA039794B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462087369P 2014-12-04 2014-12-04
PCT/US2015/063774 WO2016090157A1 (en) 2014-12-04 2015-12-03 Biomolecule conjugates

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EA201791024A1 true EA201791024A1 (ru) 2017-11-30
EA039794B1 EA039794B1 (ru) 2022-03-15

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US (1) US10335495B2 (ru)
EP (3) EP3903826B1 (ru)
JP (1) JP2018502067A (ru)
KR (2) KR20170125799A (ru)
CN (2) CN114656483A (ru)
AU (1) AU2015358367B2 (ru)
BR (1) BR112017011773A2 (ru)
CA (2) CA2969584C (ru)
EA (1) EA039794B1 (ru)
IL (2) IL252618B (ru)
MX (2) MX2017007218A (ru)
NZ (2) NZ732624A (ru)
SG (2) SG11201704487XA (ru)
WO (1) WO2016090157A1 (ru)

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EP3595729A4 (en) * 2017-02-10 2022-01-12 The Board of Trustees of the University of Illinois TRIGGER-ACTIVATED SUGAR CONJUGATES FOR CANCER SELECTIVE LABELING AND TARGETING
CN107080751A (zh) * 2017-04-27 2017-08-22 皖西学院 一种治疗增生性骨关节病的西药组合物及其应用
WO2019118314A2 (en) * 2017-12-13 2019-06-20 Merck Sharp & Dohme Corp. Scintillation proximity assay system comprising mutant dehalogenase
WO2020245229A1 (en) * 2019-06-03 2020-12-10 Synaffix B.V. Acetal-based cleavable linkers
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