CA3222226A1 - Trislinker-conjugated dimeric labeling precursors and radiotracers derived therefrom - Google Patents

Trislinker-conjugated dimeric labeling precursors and radiotracers derived therefrom Download PDF

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Publication number
CA3222226A1
CA3222226A1 CA3222226A CA3222226A CA3222226A1 CA 3222226 A1 CA3222226 A1 CA 3222226A1 CA 3222226 A CA3222226 A CA 3222226A CA 3222226 A CA3222226 A CA 3222226A CA 3222226 A1 CA3222226 A1 CA 3222226A1
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CA
Canada
Prior art keywords
fapi
derivatives
scheme
hooc
cooh
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3222226A
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English (en)
French (fr)
Inventor
Frank Rosch
Marcel Martin
Tilmann Grus
Euy Sung Moon
Chandra Sekhar Bal
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Medianezia GmbH
Original Assignee
Medianezia GmbH
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 Medianezia GmbH filed Critical Medianezia GmbH
Publication of CA3222226A1 publication Critical patent/CA3222226A1/en
Pending legal-status Critical Current

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    • 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
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • 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
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0455—Heterocyclic 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
    • 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
    • A61K51/0489—Phosphates or phosphonates, e.g. bone-seeking phosphonates
    • 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
    • A61K51/0491—Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo

Landscapes

  • 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)
CA3222226A 2021-06-08 2022-06-07 Trislinker-conjugated dimeric labeling precursors and radiotracers derived therefrom Pending CA3222226A1 (en)

Applications Claiming Priority (3)

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
DE102021114711.5 2021-06-08
PCT/EP2022/065440 WO2022258637A1 (de) 2021-06-08 2022-06-07 Trislinker-konjugierte dimere markierungsvorläufer und daraus abgeleitete radiotracer

Publications (1)

Publication Number Publication Date
CA3222226A1 true CA3222226A1 (en) 2022-12-15

Family

ID=82258261

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3222226A Pending CA3222226A1 (en) 2021-06-08 2022-06-07 Trislinker-conjugated dimeric labeling precursors and radiotracers derived therefrom

Country Status (10)

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

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3456700A1 (en) 2013-10-18 2019-03-20 Deutsches Krebsforschungszentrum Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
DE102018126558A1 (de) * 2018-10-24 2020-04-30 Helmholtz-Zentrum Dresden - Rossendorf E.V. Markierungsvorläufer mit Quadratsäure-Kopplung
US11167048B2 (en) * 2018-12-14 2021-11-09 The Curators Of The University Of Missouri Dual targeting ligand for cancer diagnosis and treatment
CN114502528B (zh) * 2019-09-20 2024-09-06 墨尔本大学 成像和治疗组合物
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
CN113880810B (zh) * 2021-09-24 2023-02-28 厦门大学 一种核素标记的配合物及其制备方法和应用

Also Published As

Publication number Publication date
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
DE102021114711B4 (de) 2023-11-02
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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