KR20240093543A - 방사성 표지된 섬유모세포 활성화 단백질 리간드 - Google Patents

방사성 표지된 섬유모세포 활성화 단백질 리간드 Download PDF

Info

Publication number
KR20240093543A
KR20240093543A KR1020247015053A KR20247015053A KR20240093543A KR 20240093543 A KR20240093543 A KR 20240093543A KR 1020247015053 A KR1020247015053 A KR 1020247015053A KR 20247015053 A KR20247015053 A KR 20247015053A KR 20240093543 A KR20240093543 A KR 20240093543A
Authority
KR
South Korea
Prior art keywords
cancer
independently
alkylene
cooh
aryl
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
KR1020247015053A
Other languages
English (en)
Korean (ko)
Inventor
아우렐리아노 자나
안드레아 갈비아티
야코포 밀룰
에토레 길라르도니
리카르도 스투키
사무엘 카자말리
Original Assignee
필로켐 아게
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 필로켐 아게 filed Critical 필로켐 아게
Publication of KR20240093543A publication Critical patent/KR20240093543A/ko
Pending legal-status Critical Current

Links

Classifications

    • 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)
KR1020247015053A 2021-10-04 2022-10-04 방사성 표지된 섬유모세포 활성화 단백질 리간드 Pending KR20240093543A (ko)

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
KR20240093543A true KR20240093543A (ko) 2024-06-24

Family

ID=84330437

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020247015053A Pending KR20240093543A (ko) 2021-10-04 2022-10-04 방사성 표지된 섬유모세포 활성화 단백질 리간드

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
WO2023057457A1 (en) 2023-04-13
JP2024536362A (ja) 2024-10-04
CA3234394A1 (en) 2023-04-13
AU2022358921A1 (en) 2024-05-02

Similar Documents

Publication Publication Date Title
EP3891138B1 (en) Fibroblast activation protein ligands for targeted delivery applications
AU2022358921A1 (en) Radiolabelled fibroblast activation protein ligands
US20240148916A1 (en) Bivalent fibroblast activation protein ligands for targeted delivery applications
TWI657827B (zh) 用於正子斷層掃描之化合物
US20250177582A1 (en) High-affinity ligands of fibroblast activation protein for targeted delivery applications
CN118234720A (zh) 放射性标记的成纤维细胞激活蛋白配体
CN118955616B (zh) 一种靶向结合成纤维细胞活化蛋白化合物及应用
KR20230118160A (ko) 섬유아세포 활성화 단백질 억제제
JP7646637B2 (ja) 画像化及び治療用組成物
CN119192214B (zh) 一种靶向结合成纤维细胞活化蛋白多聚化合物及其应用
EP4678642A1 (en) Nitrogen-containing heterocyclic compound, preparation method therefor, and use thereof
EP4043452A1 (en) Bivalent fibroblast activation protein ligands for targeted delivery applications
CN120957982A (zh) 靶向成纤维细胞活化蛋白的配体
AU2013254326A1 (en) Labelled quinoxaline derivatives as multimodal radiopharmaceuticals and their precursors
JP2025540658A (ja) 神経ペプチドy1受容体(npy1r)を標的とした治療薬およびその使用
HK40077413A (en) Fibroblast activation protein ligands for targeted delivery applications
HK40053369A (en) Fibroblast activation protein ligands for targeted delivery applications
HK40053369B (en) Fibroblast activation protein ligands for targeted delivery applications
WO2026007968A1 (zh) 一种靶向结合成纤维细胞活化蛋白的化合物及应用
BR112023015831B1 (pt) Ligantes de proteína de ativação de fibroblastos bivalentes para aplicações de liberação direcionada, composições farmacêuticas, seus usos e métodos para preparar um conjugado
CN117813121A (zh) 二膦化合物和复合物
WO2011124713A1 (en) Labelled huprine derivatives and their use in medical imaging

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20240503

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application