AU2020213892B2 - Silicon-fluoride acceptor substituted radiopharmaceuticals and precursors thereof - Google Patents

Silicon-fluoride acceptor substituted radiopharmaceuticals and precursors thereof Download PDF

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Publication number
AU2020213892B2
AU2020213892B2 AU2020213892A AU2020213892A AU2020213892B2 AU 2020213892 B2 AU2020213892 B2 AU 2020213892B2 AU 2020213892 A AU2020213892 A AU 2020213892A AU 2020213892 A AU2020213892 A AU 2020213892A AU 2020213892 B2 AU2020213892 B2 AU 2020213892B2
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bond
group
amino acid
hydrophilic
moiety
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AU2020213892A1 (en
Inventor
Daniel Di Carlo
Hans-Jürgen Wester
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Technische Universitaet Muenchen
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Technische Universitaet Muenchen
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    • 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
    • A61K51/088Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • 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
    • A61K51/0489Phosphates or phosphonates, e.g. bone-seeking phosphonates
    • 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
    • A61K51/0402Organic compounds carboxylic acid carriers, fatty acids
    • 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
    • A61K51/0497Organic compounds conjugates with a carrier being an organic compounds
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Physics & Mathematics (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
AU2020213892A 2019-01-30 2020-01-29 Silicon-fluoride acceptor substituted radiopharmaceuticals and precursors thereof Active AU2020213892B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19154636 2019-01-30
EP19154636.5 2019-01-30
PCT/EP2020/052159 WO2020157128A1 (en) 2019-01-30 2020-01-29 Silicon-fluoride acceptor substituted radiopharmaceuticals and precursors thereof

Publications (2)

Publication Number Publication Date
AU2020213892A1 AU2020213892A1 (en) 2021-07-22
AU2020213892B2 true AU2020213892B2 (en) 2025-04-10

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AU2020213892A Active AU2020213892B2 (en) 2019-01-30 2020-01-29 Silicon-fluoride acceptor substituted radiopharmaceuticals and precursors thereof

Country Status (7)

Country Link
US (1) US12576169B2 (https=)
EP (1) EP3917581A1 (https=)
JP (1) JP7421232B2 (https=)
CN (1) CN113677375B (https=)
AU (1) AU2020213892B2 (https=)
BR (1) BR112021012110A2 (https=)
WO (1) WO2020157128A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB202005282D0 (en) 2020-04-09 2020-05-27 Blue Earth Diagnostics Ltd Pharmaceutical Formulations
WO2022018264A1 (en) * 2020-07-23 2022-01-27 Technische Universität München Silicon-containing ligand compounds
JP2024544153A (ja) 2021-11-16 2024-11-28 テクニシェ ユニバーシタット ミュンヘン 溶解した[18f]フッ化物を含む組成物の調製方法およびその方法によって得ることができる組成物
GB202207372D0 (en) 2022-05-19 2022-07-06 Blue Earth Diagnostics Ltd Synthesis of fluorosilyl compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170246327A1 (en) * 2014-10-20 2017-08-31 Deutsches Krebsforschungszentrum 18f-tagged inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
WO2019020831A1 (en) * 2017-07-28 2019-01-31 Technische Universität München AGENTS WITH TWO RADIOTRATIVE AND THERAPEUTIC MODES

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR057023A1 (es) 2005-05-16 2007-11-14 Gilead Sciences Inc Compuestos heterociclicos con propiedades inhibidoras de hiv-integrasa
PL2187965T3 (pl) 2007-08-17 2020-05-18 Purdue Research Foundation Koniugaty wiążący psma ligand-łącznik i sposoby ich zastosowania
US10800797B2 (en) 2015-05-26 2020-10-13 California Institute Of Technology Heteroaromatic silicon-fluoride-acceptors useful for 18F labeling of molecules and biomolecules, and methods of preparing same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170246327A1 (en) * 2014-10-20 2017-08-31 Deutsches Krebsforschungszentrum 18f-tagged inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
WO2019020831A1 (en) * 2017-07-28 2019-01-31 Technische Universität München AGENTS WITH TWO RADIOTRATIVE AND THERAPEUTIC MODES

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
LUKAS O. DIALER ET AL: "Studies toward the Development of New Silicon-Containing Building Blocks for the Direct 18 F-Labeling of Peptides", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 19, 10 October 2013 (2013-10-10), pages 7552 - 7563. *
S. LITAU ET AL: "Next Generation of SiFA lin -Based TATE Derivatives for PET Imaging of SSTR-Positive Tumors:...", BIOCONJUGATE CHEMISTRY, vol. 26, no. 12, 2015-12-16, pages 2350 - 2359. *
SIMON LINDNER ET AL: "Synthesis and in Vitro and in Vivo Evaluation of SiFA-Tagged Bombesin and RGD Peptides as Tumor Imaging Probes for Positron Emission Tomography", BIOCONJUGATE CHEMISTRY, vol. 25, no. 4, 2014-04-16, US, pages 738 - 749. *

Also Published As

Publication number Publication date
JP2022518598A (ja) 2022-03-15
EP3917581A1 (en) 2021-12-08
CN113677375B (zh) 2024-07-23
WO2020157128A1 (en) 2020-08-06
CA3123738A1 (en) 2020-08-06
JP7421232B2 (ja) 2024-01-24
AU2020213892A1 (en) 2021-07-22
BR112021012110A2 (pt) 2021-09-08
US20220096669A1 (en) 2022-03-31
CN113677375A (zh) 2021-11-19
US12576169B2 (en) 2026-03-17

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