EA202193076A1 - Макроциклические хелаторы и способы их применения - Google Patents

Макроциклические хелаторы и способы их применения

Info

Publication number
EA202193076A1
EA202193076A1 EA202193076A EA202193076A EA202193076A1 EA 202193076 A1 EA202193076 A1 EA 202193076A1 EA 202193076 A EA202193076 A EA 202193076A EA 202193076 A EA202193076 A EA 202193076A EA 202193076 A1 EA202193076 A1 EA 202193076A1
Authority
EA
Eurasian Patent Office
Prior art keywords
radioactive
immunoconjugates
methods
radioactive metal
alpha
Prior art date
Application number
EA202193076A
Other languages
English (en)
Inventor
Рис Салтер
Вадим Дудкин
Фынбинь Сун
Вэй Чжан
Шалом Голдберг
Джон Кейт
Original Assignee
Янссен Байотек, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Янссен Байотек, Инк. filed Critical Янссен Байотек, Инк.
Publication of EA202193076A1 publication Critical patent/EA202193076A1/ru

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/025—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus inorganic Tc complexes or compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1027—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody against receptors, cell-surface antigens or cell-surface determinants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Предложены макроциклические хелаторы (I) для хелатирования ионов альфа-излучающих радиоактивных металлов, таких как актиний-225. Также предложены комплексы радиоактивных металлов, содержащие ион альфа-излучающего радиоактивного металла, связанный с макроциклическим хелатором посредством координационного связывания, и радиоактивные иммуноконъюгаты, содержащие комплексы радиоактивных металлов, ковалентно связанные с нацеливающим лигандом, таким как антитело или его антигенсвязывающий фрагмент. Радиоактивные иммуноконъюгаты могут быть получены с помощью клик-химических реакций. Также описаны способы применения радиоактивных комплексов и радиоактивных иммуноконъюгатов для селективного нацеливания на неопластические клетки для лучевой терапии и лечения неопластических заболеваний и расстройств.
EA202193076A 2019-05-10 2020-05-08 Макроциклические хелаторы и способы их применения EA202193076A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962846044P 2019-05-10 2019-05-10
PCT/IB2020/054381 WO2020229974A1 (en) 2019-05-10 2020-05-08 Macrocyclic chelators and methods of use thereof

Publications (1)

Publication Number Publication Date
EA202193076A1 true EA202193076A1 (ru) 2022-02-16

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA202193076A EA202193076A1 (ru) 2019-05-10 2020-05-08 Макроциклические хелаторы и способы их применения

Country Status (20)

Country Link
US (2) US11576986B2 (ru)
EP (1) EP3966211A1 (ru)
JP (1) JP2022532157A (ru)
KR (1) KR20220006613A (ru)
CN (1) CN114127059A (ru)
AU (1) AU2020273654A1 (ru)
BR (1) BR112021022237A2 (ru)
CA (1) CA3139806A1 (ru)
CL (1) CL2021002960A1 (ru)
CO (1) CO2021015713A2 (ru)
CR (1) CR20210556A (ru)
DO (1) DOP2021000233A (ru)
EA (1) EA202193076A1 (ru)
EC (1) ECSP21089217A (ru)
IL (1) IL287909A (ru)
MA (1) MA55885A (ru)
MX (1) MX2021013667A (ru)
PE (1) PE20220935A1 (ru)
SG (1) SG11202112100PA (ru)
WO (1) WO2020229974A1 (ru)

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DK3966207T3 (da) 2019-05-10 2023-12-18 Deciphera Pharmaceuticals Llc Phenylaminopyrimidinamid-autophagi-hæmmere og fremgangsmåder til anvendelse deraf
WO2021250240A1 (en) * 2020-06-12 2021-12-16 Orano Diaza-18-crown-6 derivative useful for chelating radium, conjugate and radium chelate comprising the same, and uses thereof
EP4243935A1 (en) * 2020-11-10 2023-09-20 Janssen Biotech, Inc. Macrocyclic compounds and methods of use thereof
CA3205707A1 (en) 2021-01-27 2022-08-04 Fei Shen Immunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses
WO2022203082A1 (ja) * 2021-03-26 2022-09-29 日本メジフィジックス株式会社 化合物、化合物の製造方法及び保管方法、ターゲッティング剤の製造方法、並びに組成物
US20240207463A1 (en) * 2021-03-31 2024-06-27 Nihon Medi-Physics Co., Ltd. Radioactive complex of anti-egfr antibody, and radiopharmaceutical
CA3219934A1 (en) 2021-05-27 2022-12-01 Rhys Salter Compositions and methods for the treatment of prostate cancer
MX2024001620A (es) * 2021-08-02 2024-02-28 Rayzebio Inc Composiciones estabilizadas de radionucleidos y sus usos.
WO2023013589A1 (ja) * 2021-08-03 2023-02-09 住友化学株式会社 放射性金属錯体及びその製造方法、並びに放射性金属捕捉剤
EP4392081A1 (en) * 2021-08-27 2024-07-03 Janssen Biotech, Inc. Anti-psma radioconjugates and uses thereof
EP4392454A1 (en) 2021-08-27 2024-07-03 Janssen Biotech, Inc. Anti-psma antibodies and uses thereof
CA3233458A1 (en) * 2021-09-29 2023-04-06 Katherine Anne MORGAN Macrocycle containing compounds and radiolabelled complexes thereof, as ligands in targeted radiotherapy applications
WO2023084396A1 (en) * 2021-11-09 2023-05-19 Janssen Biotech, Inc. Macrocyclic compounds and methods of making the same
WO2023084397A1 (en) * 2021-11-09 2023-05-19 Janssen Biotech, Inc. Macrocyclic compounds and diagnostic uses thereof
WO2023144723A1 (en) 2022-01-26 2023-08-03 Janssen Biotech, Inc. Immunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses
CN114656422B (zh) * 2022-04-22 2023-05-23 重庆理工大学 一种新型氮杂冠醚化合物及其阳离子脂质体、制备方法与应用
CN114874214B (zh) * 2022-05-31 2023-03-21 南京航空航天大学 可偶联巯基的双功能大环螯合剂衍生物及其制备方法
CN114949259B (zh) * 2022-07-11 2023-09-19 重庆理工大学 一种氮杂冠醚结构的基因递送载体及其制备方法和应用

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CN103221398B (zh) 2010-07-23 2016-03-23 特拉华大学 用于快速构建放射性核素标记探针的四嗪-反式环辛烯连接反应
WO2015073746A2 (en) 2013-11-13 2015-05-21 Whitehead Institute For Biomedical Research 18f labeling of proteins using sortases
KR20230132599A (ko) 2013-11-19 2023-09-15 프레닥스 에이비 인간화된 안티 칼리크레인-2 항체
KR20240093912A (ko) 2017-03-30 2024-06-24 코넬 유니버시티 알파-방출 방사선핵종의 거대고리형 복합체 및 암의 표적화된 방사선요법에서의 이의 용도
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Also Published As

Publication number Publication date
SG11202112100PA (en) 2021-11-29
ECSP21089217A (es) 2022-01-31
AU2020273654A1 (en) 2021-11-25
CR20210556A (es) 2021-12-17
MX2021013667A (es) 2022-01-31
US20230110178A1 (en) 2023-04-13
CN114127059A (zh) 2022-03-01
BR112021022237A2 (pt) 2022-03-29
KR20220006613A (ko) 2022-01-17
EP3966211A1 (en) 2022-03-16
PE20220935A1 (es) 2022-05-31
JP2022532157A (ja) 2022-07-13
CO2021015713A2 (es) 2021-11-30
IL287909A (en) 2022-01-01
CL2021002960A1 (es) 2022-06-24
DOP2021000233A (es) 2022-07-31
MA55885A (fr) 2022-03-16
CA3139806A1 (en) 2020-11-19
WO2020229974A1 (en) 2020-11-19
US11576986B2 (en) 2023-02-14
US20200353105A1 (en) 2020-11-12

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