AU2022358921A1 - Radiolabelled fibroblast activation protein ligands - Google Patents

Radiolabelled fibroblast activation protein ligands Download PDF

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Publication number
AU2022358921A1
AU2022358921A1 AU2022358921A AU2022358921A AU2022358921A1 AU 2022358921 A1 AU2022358921 A1 AU 2022358921A1 AU 2022358921 A AU2022358921 A AU 2022358921A AU 2022358921 A AU2022358921 A AU 2022358921A AU 2022358921 A1 AU2022358921 A1 AU 2022358921A1
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Prior art keywords
cancer
independently
compound
alkylene
cooh
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AU2022358921A
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Inventor
Samuele CAZZAMALLI
Andrea Galbiati
Ettore GILARDONI
Jacopo MILLUL
Riccardo STUCCHI
Aureliano ZANA
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Philochem AG
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Philochem AG
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Publication of AU2022358921A1 publication Critical patent/AU2022358921A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F1/00Compounds containing elements of Groups 1 or 11 of the Periodic Table
    • C07F1/005Compounds containing elements of Groups 1 or 11 of the Periodic Table without C-Metal linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/003Compounds containing elements of Groups 3 or 13 of the Periodic Table without C-Metal linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/06Aluminium compounds
    • C07F5/069Aluminium compounds without C-aluminium linkages
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
AU2022358921A 2021-10-04 2022-10-04 Radiolabelled fibroblast activation protein ligands Pending AU2022358921A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP21200719 2021-10-04
EP21200719.9 2021-10-04
EP22151771.7 2022-01-17
EP22151771 2022-01-17
PCT/EP2022/077598 WO2023057457A1 (en) 2021-10-04 2022-10-04 Radiolabelled fibroblast activation protein ligands

Publications (1)

Publication Number Publication Date
AU2022358921A1 true AU2022358921A1 (en) 2024-05-02

Family

ID=84330437

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2022358921A Pending AU2022358921A1 (en) 2021-10-04 2022-10-04 Radiolabelled fibroblast activation protein ligands

Country Status (8)

Country Link
EP (1) EP4412996A1 (https=)
JP (1) JP2024536362A (https=)
KR (1) KR20240093543A (https=)
AU (1) AU2022358921A1 (https=)
CA (1) CA3234394A1 (https=)
IL (1) IL311694A (https=)
MX (1) MX2024004077A (https=)
WO (1) WO2023057457A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202426433A (zh) 2022-09-23 2024-07-01 瑞士商紐利迪姆股份公司 成纖維細胞活化蛋白(fap)抑制劑、fap結合物及其診斷與治療用途
KR20250073273A (ko) * 2022-09-23 2025-05-27 누클리디움 아게 고순도 구리 방사성 의약 조성물 및 이의 진단 및 치료 용도
CN120957982A (zh) 2023-05-08 2025-11-14 江苏恒瑞医药股份有限公司 靶向成纤维细胞活化蛋白的配体
CN116925041B (zh) * 2023-06-12 2024-12-24 上海交通大学医学院附属仁济医院 靶向成纤维细胞激活蛋白的氟标记放射性药物前体、放射性标记化合物及其应用
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
WO2025167951A1 (zh) * 2024-02-07 2025-08-14 苏州博锐创合医药有限公司 一种成纤维细胞活化蛋白抑制剂
TW202600606A (zh) * 2024-02-21 2026-01-01 美商雅博得樂醫療公司 抗體連接子結合物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005087235A1 (en) 2004-03-09 2005-09-22 National Health Research Institutes Pyrrolidine compounds
WO2013107820A1 (en) 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
CN116474108A (zh) 2016-12-14 2023-07-25 普渡研究基金会 成纤维细胞活化蛋白(fap)-靶向成像和治疗
EA202090776A1 (ru) 2017-10-23 2020-07-27 Дзе Джонс Хопкинс Юниверсити Визуализирующие и радиотерапевтические агенты, нацеленные на фибробласт-активирующий белок-альфа (fapalpha)
US11780821B2 (en) 2017-12-15 2023-10-10 Praxis Biotech LLC Inhibitors of fibroblast activation protein
EP3749663A1 (en) 2018-02-06 2020-12-16 Universität Heidelberg Fap inhibitor
WO2019154859A1 (en) 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
EP4019507A1 (en) * 2020-02-12 2022-06-29 Philochem AG Fibroblast activation protein ligands for targeted delivery applications

Also Published As

Publication number Publication date
KR20240093543A (ko) 2024-06-24
IL311694A (en) 2024-05-01
CA3234394A1 (en) 2023-04-13
JP2024536362A (ja) 2024-10-04
EP4412996A1 (en) 2024-08-14
MX2024004077A (es) 2024-04-18
WO2023057457A1 (en) 2023-04-13

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