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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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

ID=70804855

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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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
AU2021379306A1 (en) * 2020-11-10 2023-07-06 Janssen Biotech, Inc. Macrocyclic compounds and methods of use thereof
WO2022162549A2 (en) 2021-01-27 2022-08-04 Janssen Biotech, Inc. Immunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses
EP4317152A1 (en) * 2021-03-26 2024-02-07 Nihon Medi-Physics Co., Ltd. Compound, method for producing and method for storing compound, method for producing targeting agent, and composition
AU2022250323A1 (en) * 2021-03-31 2023-11-09 Nihon Medi-Physics Co., Ltd. Radioactive complex of anti-egfr antibody, and radiopharmaceutical
EP4346916A1 (en) 2021-05-27 2024-04-10 Janssen Biotech, Inc. Compositions and methods for the treatment of prostate cancer
PE20240917A1 (es) * 2021-08-02 2024-04-30 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
PE20240727A1 (es) 2021-08-27 2024-04-15 Janssen Biotech Inc Anticuerpos anti-psma y usos de estos
WO2023026236A1 (en) * 2021-08-27 2023-03-02 Janssen Biotech, Inc. Anti-psma radioconjugates and uses thereof
WO2023049963A1 (en) * 2021-09-29 2023-04-06 The University Of Melbourne Macrocycle containing compounds and radiolabelled complexes thereof, as ligands in targeted radiotherapy applications
WO2023084397A1 (en) * 2021-11-09 2023-05-19 Janssen Biotech, Inc. Macrocyclic compounds and diagnostic uses thereof
WO2023084396A1 (en) * 2021-11-09 2023-05-19 Janssen Biotech, Inc. Macrocyclic compounds and methods of making the same
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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WO2012012612A2 (en) 2010-07-23 2012-01-26 University Of Delaware Tetrazine-trans-cyclooctene ligation for the rapid construction of radionuclide labeled probes
WO2015073746A2 (en) 2013-11-13 2015-05-21 Whitehead Institute For Biomedical Research 18f labeling of proteins using sortases
KR102442738B1 (ko) 2013-11-19 2022-09-15 프레닥스 에이비 인간화된 안티 칼리크레인-2 항체
JP2020515596A (ja) * 2017-03-30 2020-05-28 コーネル ユニバーシティー α線放出放射線核種の大環状錯体およびがんの標的放射線療法におけるそれらの使用
AU2018249559A1 (en) 2017-04-05 2019-10-31 Cornell University Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies
EP3703676A4 (en) * 2017-11-04 2021-12-15 Advanced Proteome Therapeutics, Inc. COMPOSITION AND PROCESS FOR MODIFYING POLYPEPTIDES
AU2018388467A1 (en) 2017-12-18 2020-06-11 Janssen Biotech, Inc. Radiolabeling of polypeptides
JOP20200303A1 (ar) 2018-05-24 2020-11-23 Janssen Biotech Inc عوامل ربط psma واستخداماتها
MX2021005808A (es) 2018-11-20 2021-07-02 Univ Cornell Complejos macrociclicos de radionucleidos alfa-emisores y su uso en radioterapia focalizada de cancer.

Also Published As

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

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