JP7266365B2 - 分子および生体分子の18f標識化に有用な新規な複素芳香環フッ化ケイ素アクセプタおよびその調製方法 - Google Patents

分子および生体分子の18f標識化に有用な新規な複素芳香環フッ化ケイ素アクセプタおよびその調製方法 Download PDF

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JP7266365B2
JP7266365B2 JP2017548194A JP2017548194A JP7266365B2 JP 7266365 B2 JP7266365 B2 JP 7266365B2 JP 2017548194 A JP2017548194 A JP 2017548194A JP 2017548194 A JP2017548194 A JP 2017548194A JP 7266365 B2 JP7266365 B2 JP 7266365B2
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マーティン ヴァルドマン クリストファー
エイ トゥトヴ アントン
マリー マーフィー ジェニファー
エイチ グラブス ロバート
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University of California San Diego UCSD
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/004Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/12Organo silicon halides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies 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
    • A61K51/1027Antibodies 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies 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
    • A61K51/1045Antibodies 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 animal or human tumor cells or tumor cell determinants
    • A61K51/1072Antibodies 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 animal or human tumor cells or tumor cell determinants the tumor cell being from the reproductive system, e.g. ovaria, uterus, testes or prostate
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
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  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Reproductive Health (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2017548194A 2015-05-26 2016-05-24 分子および生体分子の18f標識化に有用な新規な複素芳香環フッ化ケイ素アクセプタおよびその調製方法 Active JP7266365B2 (ja)

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US201562166240P 2015-05-26 2015-05-26
US62/166,240 2015-05-26
PCT/US2016/033923 WO2016191424A2 (en) 2015-05-26 2016-05-24 Novel heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same

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JP2021017722A Withdrawn JP2021073293A (ja) 2015-05-26 2021-02-05 分子および生体分子の18f標識化に有用な新規な複素芳香環フッ化ケイ素アクセプタおよびその調製方法

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EP (1) EP3303349B1 (enExample)
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CN (1) CN107667109B (enExample)
CA (1) CA2982269C (enExample)
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JP7266365B2 (ja) 2015-05-26 2023-04-28 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 分子および生体分子の18f標識化に有用な新規な複素芳香環フッ化ケイ素アクセプタおよびその調製方法
US11413360B2 (en) * 2017-07-28 2022-08-16 Technische Universität München Dual mode radiotracer and—therapeutics
WO2019055825A1 (en) 2017-09-15 2019-03-21 The Regents Of The University Of California INHIBITION OF AMINOACYLASE 3 (AA3) IN THE TREATMENT OF CANCER
EP3917581A1 (en) * 2019-01-30 2021-12-08 Technische Universität München Silicon-fluoride acceptor substituted radiopharmaceuticals and precursors thereof
WO2020220020A1 (en) * 2019-04-26 2020-10-29 The Regents Of The University Of California Silicon-fluoride heteroaromatic systems for applications in positron emission tomography (pet) molecular imaging
EP3976562A1 (en) * 2019-05-24 2022-04-06 Duke University 18 f-radiolabeled biomolecules
US20230202944A1 (en) * 2020-05-29 2023-06-29 Fuzionaire, Inc. Methods for Rapid Formation of Chemicals Including Positron Emission Tomography Biomarkers
CN119301134A (zh) * 2022-04-20 2025-01-10 富齐奥奈尔治疗诊断股份有限公司 治疗诊断用的氟化硅杂芳族系统及其方法

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US6972336B2 (en) * 2002-07-18 2005-12-06 Novartis Ag N-alkylation of indole derivatives
WO2008040441A2 (en) 2006-10-02 2008-04-10 Bayer Schering Pharma Aktiengesellschaft Silicon derivatives for pet imaging
WO2010075286A1 (en) * 2008-12-24 2010-07-01 University Of Washington MOLECULAR ACTIVATORS OF THE Wnt/β-CATENIN PATHWAY
AU2011349482A1 (en) * 2010-12-22 2013-07-25 Ge Healthcare Limited HER2 binding peptides labeled with aluminium-(18) fluoride complexed by NOTA
JP7266365B2 (ja) 2015-05-26 2023-04-28 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 分子および生体分子の18f標識化に有用な新規な複素芳香環フッ化ケイ素アクセプタおよびその調製方法

Non-Patent Citations (9)

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A.Frenzel 外4名、Z.Natureforsch.、1995年、50b、p.1658~1664
Bjorn Wangler 10名、Bioconjugate Chem.、2009年、20、p.317~321
C.Baum 外3名、Z.Anorg.Allg.Chem.、1999年、625、p.1969~1978
L.O.Dialer 外10名、Journal of Medicinal Chemistry、2013年、Vol.56、p.7552~7563
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Uwe Klingebiel 外2名、Journal of Organometallic Chemistry、1993年、455、p.51~55

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EP3303349B1 (en) 2022-07-06
JP2021073293A (ja) 2021-05-13
US20180346491A1 (en) 2018-12-06
EP3303349A4 (en) 2019-03-13
CN107667109A (zh) 2018-02-06
WO2016191424A2 (en) 2016-12-01
US20230114064A1 (en) 2023-04-13
US12371445B2 (en) 2025-07-29
US10800797B2 (en) 2020-10-13
CA2982269C (en) 2023-12-05
WO2016191424A3 (en) 2016-12-29
US20200377529A1 (en) 2020-12-03
JP2018521956A (ja) 2018-08-09
CN107667109B (zh) 2021-08-03
US20250333425A1 (en) 2025-10-30
CA2982269A1 (en) 2016-12-01
EP3303349A2 (en) 2018-04-11
US11447508B2 (en) 2022-09-20

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