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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/004—Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/12—Organo silicon halides
    • 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
    • A61K51/1045—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 animal or human tumor cells or tumor cell determinants
    • A61K51/1072—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 animal or human tumor cells or tumor cell determinants the tumor cell being from the reproductive system, e.g. ovaria, uterus, testes or prostate
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically 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)
  • Public Health (AREA)
  • 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)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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 Division 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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JP2018521956A JP2018521956A (ja) 2018-08-09
JP2018521956A5 JP2018521956A5 (enExample) 2019-06-27
JP7266365B2 true JP7266365B2 (ja) 2023-04-28

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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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US (4) US10800797B2 (enExample)
EP (1) EP3303349B1 (enExample)
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Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3303349B1 (en) 2015-05-26 2022-07-06 The Regents of the University of California Novel heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same
KR20240027896A (ko) * 2017-07-28 2024-03-04 테크니쉐 우니베르지테트 뮌헨 이중 모드 방사성 트레이서 및 치료법
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
BR112021012110A2 (pt) * 2019-01-30 2021-09-08 Technische Universität München Radiofarmacêuticos substituídos por aceptor de fluoreto de silício
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
KR102899941B1 (ko) * 2019-05-24 2025-12-16 듀크 유니버시티 18f-방사선 표지된 생체 분자
US20230202944A1 (en) * 2020-05-29 2023-06-29 Fuzionaire, Inc. Methods for Rapid Formation of Chemicals Including Positron Emission Tomography Biomarkers
WO2023205755A2 (en) * 2022-04-20 2023-10-26 Fuzionaire Diagnostics, Inc. Theranostic silicon-fluoride heteroaromatic systems and methods thereof

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US6972336B2 (en) * 2002-07-18 2005-12-06 Novartis Ag N-alkylation of indole derivatives
KR20090085599A (ko) 2006-10-02 2009-08-07 바이엘 쉐링 파마 악티엔게젤샤프트 Ｐｅｔ 영상화용 규소 유도체
US20120046242A1 (en) * 2008-12-24 2012-02-23 Massachusetts Institute Of Technology Molecular activators of the wnt/beta-catenin pathway
EP2654803B1 (en) 2010-12-22 2021-08-18 General Electric Company Radiolabeled her2-binding peptide conjugates
EP3303349B1 (en) * 2015-05-26 2022-07-06 The Regents of the University of California Novel heteroaromatic silicon-fluoride-acceptors useful for 18f labeling of molecules and biomolecules, and methods of preparing same

Non-Patent Citations (9)

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Title
Ａ．ＦＲＥＮＺＥＬ 外４名、Ｍａｉｎ Ｇｒｏｕｐ Ｃｈｅｍｉｓｔｒｙ、１９９６年、Ｖｏｌ．１、ｐ．３９９～４０８
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
Ｍａｒｉｏｌａ Ｃａｌｌｅ 外５名、Ｓｙｎｔｈｅｓｉｓ、２００１年、Ｎｏ．１３、ｐ．１９４９～１９５８
Ｓｕｋ－Ｋｕ Ｋａｎｇ 外４名、Ｔｅｔｒａｈｅｄｒｏｎ、１９９７年、Ｖｏｌ．５３、Ｎｏ．９、ｐ．３０２７～３０３４
Ｔｈｏｍａｓ Ｂｒａｕｎ 外４名、Ｄａｌｔｏｎ Ｔｒａｎｓ．、２００６年、ｐ．５１１８～５１２３
Ｕｗｅ Ｋｌｉｎｇｅｂｉｅｌ 外２名、Ｊｏｕｒｎａｌ ｏｆ Ｏｒｇａｎｏｍｅｔａｌｌｉｃ Ｃｈｅｍｉｓｔｒｙ、１９９３年、４５５、ｐ．５１～５５

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

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