DE102021114711B4 - Trislinker-konjugierte dimere Markierungsvorläufer und daraus abgeleitete Radiotracer - Google Patents

Trislinker-konjugierte dimere Markierungsvorläufer und daraus abgeleitete Radiotracer Download PDF

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Publication number
DE102021114711B4
DE102021114711B4 DE102021114711.5A DE102021114711A DE102021114711B4 DE 102021114711 B4 DE102021114711 B4 DE 102021114711B4 DE 102021114711 A DE102021114711 A DE 102021114711A DE 102021114711 B4 DE102021114711 B4 DE 102021114711B4
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acid
amino
marking
precursors
group
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DE102021114711A1 (de
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Frank Rösch
Martin Marcel
Tilmann Grus
Euy Sung Moon
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Medianezia De GmbH
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Medianezia GmbH
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Priority to DE102021114711.5A priority Critical patent/DE102021114711B4/de
Application filed by Medianezia GmbH filed Critical Medianezia GmbH
Priority to US18/567,891 priority patent/US20250235566A1/en
Priority to AU2022288744A priority patent/AU2022288744A1/en
Priority to PCT/EP2022/065440 priority patent/WO2022258637A1/de
Priority to EP22734235.9A priority patent/EP4351663A1/de
Priority to CN202280040063.2A priority patent/CN117642190A/zh
Priority to BR112023023149A priority patent/BR112023023149A2/pt
Priority to KR1020247000764A priority patent/KR20240019301A/ko
Priority to JP2023576067A priority patent/JP2024522200A/ja
Priority to CA3222226A priority patent/CA3222226A1/en
Publication of DE102021114711A1 publication Critical patent/DE102021114711A1/de
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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
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0455Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61K51/0491Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00Preparations for testing in vivo

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical & Material Sciences (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)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Paints Or Removers (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Treatment And Processing Of Natural Fur Or Leather (AREA)
  • Medicinal Preparation (AREA)
DE102021114711.5A 2021-06-08 2021-06-08 Trislinker-konjugierte dimere Markierungsvorläufer und daraus abgeleitete Radiotracer Active DE102021114711B4 (de)

Priority Applications (10)

Application Number Priority Date Filing Date Title
DE102021114711.5A DE102021114711B4 (de) 2021-06-08 2021-06-08 Trislinker-konjugierte dimere Markierungsvorläufer und daraus abgeleitete Radiotracer
JP2023576067A JP2024522200A (ja) 2021-06-08 2022-06-07 トリスリンカー結合二量体化標識前駆体およびそれに由来する放射性トレーサー
PCT/EP2022/065440 WO2022258637A1 (de) 2021-06-08 2022-06-07 Trislinker-konjugierte dimere markierungsvorläufer und daraus abgeleitete radiotracer
EP22734235.9A EP4351663A1 (de) 2021-06-08 2022-06-07 Trislinker-konjugierte dimere markierungsvorläufer und daraus abgeleitete radiotracer
CN202280040063.2A CN117642190A (zh) 2021-06-08 2022-06-07 缀合有三接头的二聚体标记前体和由其衍生的放射性示踪剂
BR112023023149A BR112023023149A2 (pt) 2021-06-08 2022-06-07 Precursores de marcação diméricos conjugados via um trislinker e radiotraçadores derivados dos mesmos
US18/567,891 US20250235566A1 (en) 2021-06-08 2022-06-07 Trislinker-conjugated dimeric labeling precursors and radiotracers derived therefrom
AU2022288744A AU2022288744A1 (en) 2021-06-08 2022-06-07 Trislinker-conjugated dimeric labelling precursors and radiotracers derived therefrom
CA3222226A CA3222226A1 (en) 2021-06-08 2022-06-07 Trislinker-conjugated dimeric labeling precursors and radiotracers derived therefrom
KR1020247000764A KR20240019301A (ko) 2021-06-08 2022-06-07 트리스링커-접합된 이량체 표지 전구체 및 이로부터 유도되는 방사성 추적자

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102021114711.5A DE102021114711B4 (de) 2021-06-08 2021-06-08 Trislinker-konjugierte dimere Markierungsvorläufer und daraus abgeleitete Radiotracer

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DE102021114711A1 DE102021114711A1 (de) 2022-12-08
DE102021114711B4 true DE102021114711B4 (de) 2023-11-02

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Country Status (10)

Country Link
US (1) US20250235566A1 (https=)
EP (1) EP4351663A1 (https=)
JP (1) JP2024522200A (https=)
KR (1) KR20240019301A (https=)
CN (1) CN117642190A (https=)
AU (1) AU2022288744A1 (https=)
BR (1) BR112023023149A2 (https=)
CA (1) CA3222226A1 (https=)
DE (1) DE102021114711B4 (https=)
WO (1) WO2022258637A1 (https=)

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CA3248367A1 (en) * 2022-01-14 2023-07-20 Provincial Health Services Authority Radiolabeled compounds for imaging fibroblast-activating protein (FAP) and treating FAP-related disorders
WO2023222558A1 (en) 2022-05-14 2023-11-23 Zounek Alexis Nikolai Precursor and theranostic radiotracer with improved tumor retention
DE102022116009A1 (de) * 2022-06-28 2023-12-28 Positron Precision GmbH Fibroblasten-Aktivierungsprotein adressierender Präkursor und Radiotracer
CN115947775B (zh) * 2023-03-13 2023-06-09 北京先通国际医药科技股份有限公司 一种制备化合物(i)的方法和化合物(i)及其用途
CN117304125A (zh) * 2023-09-12 2023-12-29 北京师范大学 靶向PSMA的EuK二聚体化合物及其药用盐和应用
WO2025063849A2 (en) * 2023-09-21 2025-03-27 Erasmus University Medical Center Rotterdam Dimeric fap targeting agents
WO2025087229A1 (zh) * 2023-10-27 2025-05-01 四川科伦博泰生物医药股份有限公司 一类喹啉结构的配体化合物及其放射性或非放射性标记物以及应用
WO2025125335A1 (en) 2023-12-13 2025-06-19 Radiovaxx Gmbh Cytotoxic or radiopharmaceutical compound with sulfur fluoride exchange group
CN120136958A (zh) * 2023-12-13 2025-06-13 无锡诺宇医药科技有限公司 Fap靶向放射性药物
WO2025125621A1 (en) 2023-12-14 2025-06-19 Radiovaxx Gmbh Cancer-associated protein-targeted strong or covalently binding precursor compounds and radiotracers
WO2025146433A1 (en) 2024-01-05 2025-07-10 Radiovaxx Gmbh Precursor and theranostic radiotracer with prolonged tumor retention
TW202535358A (zh) * 2024-01-11 2025-09-16 大陸商上海復星醫藥產業發展有限公司 一種fap結合化合物、金屬錯合物及其用途
CN118271393B (zh) * 2024-05-31 2024-09-03 中国药科大学 一种靶向fap的二聚化合物及其探针和应用
EP4696686A1 (en) * 2024-08-15 2026-02-18 Tetrakit Technologies ApS Fapi theranostic compounds assembled with tetrazine ligation
CN119060093B (zh) * 2024-08-26 2025-09-05 广州医科大学附属第一医院(广州呼吸中心) 一种靶向成纤维细胞激活蛋白的抑制剂类放射性探针及其制备方法和应用
CN119060094B (zh) * 2024-08-26 2025-09-05 广州医科大学附属第一医院(广州呼吸中心) 一种靶向成纤维细胞激活蛋白的抑制剂类放射性探针及其制备方法和应用
CN118955353A (zh) * 2024-10-14 2024-11-15 南京恒远科技开发有限公司 一种(s)-4,4-二氟-1-甘氨酰吡咯烷-2-氰基的合成方法
CN119679977B (zh) * 2024-12-16 2025-09-05 山东第一医科大学附属肿瘤医院(山东省肿瘤防治研究院、山东省肿瘤医院) 一种Al18F示踪剂一体化冻干粉的制备方法、试剂盒及其应用
CN119409613B (zh) * 2025-01-03 2025-04-11 南京恒远科技开发有限公司 (s)-[2-(2-氰基-4,4-二氟吡咯烷-1-基)-2-氧代-乙基]氨基甲酸叔丁酯的合成方法

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WO2015055318A1 (en) 2013-10-18 2015-04-23 Deutsches Krebsforschungszentrum Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

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US11167048B2 (en) * 2018-12-14 2021-11-09 The Curators Of The University Of Missouri Dual targeting ligand for cancer diagnosis and treatment
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DE102021101216A1 (de) * 2021-01-21 2022-07-21 Johannes Gutenberg-Universität Mainz, Körperschaft des öffentlichen Rechts Markierungsvorläufer und Radiotracer zur nuklearmedizinischen Diagnose und Therapie von Prostatakrebs induzierten Knochenmetastasen
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Amide bond formation: beyond the myth of coupling reagents; E. Valeur, M. Bradley; Chem. Soc. Rev., 2009, 38, 606-631
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Also Published As

Publication number Publication date
CA3222226A1 (en) 2022-12-15
DE102021114711A1 (de) 2022-12-08
WO2022258637A1 (de) 2022-12-15
CN117642190A (zh) 2024-03-01
AU2022288744A9 (en) 2023-12-21
JP2024522200A (ja) 2024-06-11
AU2022288744A1 (en) 2023-12-14
KR20240019301A (ko) 2024-02-14
BR112023023149A2 (pt) 2024-01-23
EP4351663A1 (de) 2024-04-17
US20250235566A1 (en) 2025-07-24

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