KR20150085808A - 약물 단백질 결합체 - Google Patents

약물 단백질 결합체 Download PDF

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Publication number
KR20150085808A
KR20150085808A KR1020157009803A KR20157009803A KR20150085808A KR 20150085808 A KR20150085808 A KR 20150085808A KR 1020157009803 A KR1020157009803 A KR 1020157009803A KR 20157009803 A KR20157009803 A KR 20157009803A KR 20150085808 A KR20150085808 A KR 20150085808A
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South Korea
Prior art keywords
group
conjugate
binding
linker
antibody
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KR1020157009803A
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English (en)
Korean (ko)
Inventor
존 버트
안토니 갓윈
마크 프리게리오
조지 바데스쿠
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폴리테릭스 리미티드
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    • A61K47/48384
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K47/48569
    • A61K47/48715
    • 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
    • A61K47/68033Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889Conjugates 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • 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
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged systems

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020157009803A 2012-10-24 2013-10-11 약물 단백질 결합체 Withdrawn KR20150085808A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261717743P 2012-10-24 2012-10-24
US61/717,743 2012-10-24

Publications (1)

Publication Number Publication Date
KR20150085808A true KR20150085808A (ko) 2015-07-24

Family

ID=49488609

Family Applications (1)

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KR1020157009803A Withdrawn KR20150085808A (ko) 2012-10-24 2013-10-11 약물 단백질 결합체

Country Status (19)

Country Link
US (1) US20150283259A1 (enExample)
EP (1) EP2911696B1 (enExample)
JP (1) JP6328649B2 (enExample)
KR (1) KR20150085808A (enExample)
CN (1) CN104755106B (enExample)
AU (1) AU2013336410B2 (enExample)
BR (1) BR112015008311A2 (enExample)
CA (1) CA2884359A1 (enExample)
DK (1) DK2911696T3 (enExample)
ES (1) ES2652513T3 (enExample)
HU (1) HUE037604T2 (enExample)
IL (1) IL237673A0 (enExample)
IN (1) IN2015DN02577A (enExample)
MX (1) MX2015005124A (enExample)
NO (1) NO2789793T3 (enExample)
RU (1) RU2015119557A (enExample)
SG (1) SG11201501955VA (enExample)
WO (1) WO2014064424A1 (enExample)
ZA (1) ZA201501996B (enExample)

Families Citing this family (29)

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KR102306490B1 (ko) 2013-03-15 2021-09-28 리제너론 파아마슈티컬스, 인크. 생물학적 활성 분자, 그의 접합체 및 치료 용도
WO2014194030A2 (en) * 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
SG11201601230RA (en) 2013-08-26 2016-03-30 Regeneron Pharma Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
EP3145552B1 (en) * 2014-05-23 2020-03-04 Novartis AG Methods for making conjugates from disulfide-containing proteins
JP6800021B2 (ja) * 2014-06-02 2020-12-16 レゲネロン ファーマシューティカルス,インコーポレーテッド 抗体−薬物コンジュゲート、それらの製造、及びそれらの治療用途
GB2531715A (en) * 2014-10-24 2016-05-04 Polytherics Ltd Novel drug conjugates
EP3218009B1 (en) 2014-10-14 2021-04-07 Polytherics Limited Process for the conjugation of a peptide or protein with a reagent comprising a leaving group including a portion of peg
EP3220956B1 (en) * 2014-10-24 2023-08-09 Abzena (UK) Limited Conjugates and conjugating reagents
CN107995912A (zh) 2015-03-27 2018-05-04 里珍纳龙药品有限公司 美登素类衍生物、其偶联物和使用方法
NZ739830A (en) 2015-07-12 2021-12-24 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
EP3331569A1 (en) * 2015-08-07 2018-06-13 Gamamabs Pharma Antibodies, antibody drug conjugates and methods of use
MX390630B (es) 2016-01-25 2025-03-21 Regeneron Pharma Derivados de maitansinoide, conjugados de los mismos y metodos de uso.
WO2017161206A1 (en) 2016-03-16 2017-09-21 Halozyme, Inc. Conjugates containing conditionally active antibodies or antigen-binding fragments thereof, and methods of use
US11273224B2 (en) 2016-04-14 2022-03-15 Polytherics Limited Conjugates and conjugating reagents comprising a linker that includes at least two (-CH2—CH2—O-) units in a ring
GB201608936D0 (en) 2016-05-20 2016-07-06 Polytherics Ltd Novel conjugates and novel conjugating reagents
CN109311996B (zh) 2016-06-06 2023-11-28 阿布泽纳(英国)有限公司 抗体、其用途及其缀合物
GB201614162D0 (en) 2016-08-18 2016-10-05 Polytherics Ltd Antibodies, uses thereof and conjugates thereof
GB201615725D0 (en) * 2016-09-15 2016-11-02 Polytherics Ltd Novel cytotoxic agents and conjugates thereof
KR102345175B1 (ko) 2016-11-14 2021-12-31 항저우 디에이씨 바이오테크 씨오, 엘티디 결합 링커, 그러한 결합 링커를 함유하는 세포 결합 분자-약물 결합체, 링커를 갖는 그러한 결합체의 제조 및 사용
US10864279B2 (en) 2016-12-16 2020-12-15 Industrial Technology Research Institute Linker-drug and antibody-drug conjugate (ADC) employing the same
WO2020081493A1 (en) 2018-10-16 2020-04-23 Molecular Templates, Inc. Pd-l1 binding proteins
CA3145050A1 (en) 2019-06-29 2021-01-07 Robert Zhao Conjugates of tubulysin derivatives and cell binding molecules and methods of making
WO2021055816A1 (en) 2019-09-18 2021-03-25 Molecular Templates, Inc. Pd-l1 binding molecules comprising shiga toxin a subunit scaffolds
EP4208259A2 (en) 2020-09-04 2023-07-12 NovaRock Biotherapeutics, Ltd. Nectin-4 antibodies and uses thereof
US20220306700A1 (en) 2021-03-17 2022-09-29 Molecular Templates, Inc. Pd-l1 binding proteins comprising shiga toxin a subunit scaffolds and cd8+ t cell antigens
CA3236930A1 (en) 2021-11-03 2022-04-21 Hangzhou Dac Biotech Co., Ltd. Specific conjugation of an antibody
CN117147824A (zh) * 2022-05-29 2023-12-01 菲鹏生物股份有限公司 一种抗体缀合物及其应用
WO2024260217A1 (zh) * 2023-06-19 2024-12-26 广东菲鹏生物有限公司 标记Fab抗体

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GB0316294D0 (en) 2003-07-11 2003-08-13 Polytherics Ltd Conjugated biological molecules and their preparation
NZ583292A (en) * 2003-11-06 2012-03-30 Seattle Genetics Inc Monomethylvaline compounds capable of conjugation to ligands
JP5290756B2 (ja) * 2005-09-26 2013-09-18 メダレックス インコーポレイテッド 抗体−薬剤コンジュゲート及びその使用
CN101903403B (zh) * 2007-10-19 2016-03-16 西雅图基因公司 Cd19结合剂及其应用
BRPI0911442A2 (pt) * 2008-04-30 2019-03-12 Immunogen, Inc. conjugados potentes e ligantes hidrofílicos
EP2403538B1 (en) 2009-03-04 2017-10-04 Polytherics Limited Conjugated proteins and peptides
UY32913A (es) * 2009-10-02 2011-04-29 Sanofi Aventis Nuevos maitansinoides y el uso de dichos maitansinoides para preparar conjugados con un anticuero
EP2861261A2 (en) * 2012-06-19 2015-04-22 Polytherics Limited Process for preparation of antibody conjugates and antibody conjugates

Also Published As

Publication number Publication date
HUE037604T2 (hu) 2018-09-28
JP2015536329A (ja) 2015-12-21
HK1208186A1 (en) 2016-02-26
BR112015008311A2 (pt) 2017-07-04
CN104755106A (zh) 2015-07-01
EP2911696A1 (en) 2015-09-02
MX2015005124A (es) 2015-10-29
AU2013336410B2 (en) 2017-08-03
ZA201501996B (en) 2016-01-27
AU2013336410A1 (en) 2015-04-09
WO2014064424A1 (en) 2014-05-01
JP6328649B2 (ja) 2018-05-23
IL237673A0 (en) 2015-04-30
CN104755106B (zh) 2018-03-13
ES2652513T3 (es) 2018-02-02
RU2015119557A (ru) 2016-12-20
SG11201501955VA (en) 2015-04-29
EP2911696B1 (en) 2017-09-20
NO2789793T3 (enExample) 2018-01-27
IN2015DN02577A (enExample) 2015-09-11
CA2884359A1 (en) 2014-05-01
DK2911696T3 (en) 2018-01-08
US20150283259A1 (en) 2015-10-08

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