CA3234394A1 - Radiolabelled fibroblast activation protein ligands - Google Patents

Radiolabelled fibroblast activation protein ligands Download PDF

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Publication number
CA3234394A1
CA3234394A1 CA3234394A CA3234394A CA3234394A1 CA 3234394 A1 CA3234394 A1 CA 3234394A1 CA 3234394 A CA3234394 A CA 3234394A CA 3234394 A CA3234394 A CA 3234394A CA 3234394 A1 CA3234394 A1 CA 3234394A1
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CA
Canada
Prior art keywords
cancer
independently
cooh
compound
alkylene
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
CA3234394A
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English (en)
French (fr)
Inventor
Aureliano ZANA
Andrea Galbiati
Jacopo MILLUL
Ettore GILARDONI
Riccardo STUCCHI
Samuele CAZZAMALLI
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.)
Philochem AG
Original Assignee
Philochem AG
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 Philochem AG filed Critical Philochem AG
Publication of CA3234394A1 publication Critical patent/CA3234394A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459—Heterocyclic 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • C07F1/00—Compounds containing elements of Groups 1 or 11 of the Periodic Table
    • C07F1/005—Compounds containing elements of Groups 1 or 11 of the Periodic Table without C-Metal linkages
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/003—Compounds containing elements of Groups 3 or 13 of the Periodic Table without C-Metal linkages
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/06—Aluminium compounds
    • C07F5/069—Aluminium compounds without C-aluminium linkages
    • 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

Landscapes

  • 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)
CA3234394A 2021-10-04 2022-10-04 Radiolabelled fibroblast activation protein ligands Pending CA3234394A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP21200719.9 2021-10-04
EP21200719 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
CA3234394A1 true CA3234394A1 (en) 2023-04-13

Family

ID=84330437

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3234394A Pending CA3234394A1 (en) 2021-10-04 2022-10-04 Radiolabelled fibroblast activation protein ligands

Country Status (8)

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

Families Citing this family (8)

* 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
IL319722A (en) 2022-09-23 2025-05-01 Nuclidium Ag High purity radionuclides and their diagnostic and medical uses
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
CN122319156A (zh) * 2024-10-31 2026-06-30 无锡诺宇医药科技有限公司 成纤维细胞活化蛋白靶向的放射性药物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100844593B1 (ko) 2004-03-09 2008-07-07 내셔날 헬스 리서치 인스티튜트 피롤리딘 화합물
WO2013107820A1 (en) 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
WO2015073678A1 (en) * 2013-11-14 2015-05-21 Endocyte, Inc. Compounds for positron emission tomography
JP7162592B2 (ja) 2016-12-14 2022-10-28 パーデュー・リサーチ・ファウンデイション 線維芽細胞活性化タンパク質(fap)標的イメージングおよび治療
JP2021500373A (ja) 2017-10-23 2021-01-07 ザ・ジョンズ・ホプキンス・ユニバーシティ 線維芽細胞活性化タンパク質α(FAP−α)を標的とする撮像剤および放射線療法用薬剤
AU2018386298B2 (en) 2017-12-15 2023-09-07 Praxis Biotech LLC Inhibitors of fibroblast activation protein
PH12020551205A1 (en) * 2018-02-06 2021-04-19 Univ Heidelberg Fap inhibitors
WO2019154859A1 (en) 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
KR20220154111A (ko) * 2020-02-12 2022-11-21 필로켐 아게 표적 전달 적용들을 위한 섬유아세포 활성화 단백질 리간드들

Also Published As

Publication number Publication date
MX2024004077A (es) 2024-04-18
IL311694A (en) 2024-05-01
EP4412996A1 (en) 2024-08-14
KR20240093543A (ko) 2024-06-24
WO2023057457A1 (en) 2023-04-13
JP2024536362A (ja) 2024-10-04
AU2022358921A1 (en) 2024-05-02

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