CA3214070A1 - Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen - Google Patents

Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen Download PDF

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Publication number
CA3214070A1
CA3214070A1 CA3214070A CA3214070A CA3214070A1 CA 3214070 A1 CA3214070 A1 CA 3214070A1 CA 3214070 A CA3214070 A CA 3214070A CA 3214070 A CA3214070 A CA 3214070A CA 3214070 A1 CA3214070 A1 CA 3214070A1
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Canada
Prior art keywords
co2h
group
compound
fap
independently
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Pending
Application number
CA3214070A
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English (en)
French (fr)
Inventor
Sangeeta Banerjee RAY
Srikanth BOINAPALLY
Martin Gilbert Pomper
Andrew Horti
Deepankar DAS
Il MINN
Laurence Carroll
Hyojin CHA
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Johns Hopkins University
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Johns Hopkins University
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Application filed by Johns Hopkins University filed Critical Johns Hopkins University
Publication of CA3214070A1 publication Critical patent/CA3214070A1/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
    • A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
    • 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
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0032—Methine dyes, e.g. cyanine dyes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0052—Small organic molecules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/22—Echographic preparations; Ultrasonic imaging preparations
    • A61K49/221—Echographic preparations; Ultrasonic imaging preparations characterised by the targeting agent or modifying agent linked to the acoustically-active agent
    • 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
    • A61K51/0446—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • 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
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Radiology & Medical Imaging (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Acoustics & Sound (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3214070A 2021-04-02 2022-04-04 Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen Pending CA3214070A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163170035P 2021-04-02 2021-04-02
US63/170,035 2021-04-02
PCT/US2022/023374 WO2022212958A1 (en) 2021-04-02 2022-04-04 Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen

Publications (1)

Publication Number Publication Date
CA3214070A1 true CA3214070A1 (en) 2022-10-06

Family

ID=83459940

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3214070A Pending CA3214070A1 (en) 2021-04-02 2022-04-04 Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen

Country Status (11)

Country Link
US (1) US20240382629A1 (enExample)
EP (1) EP4313049A4 (enExample)
JP (1) JP2024514528A (enExample)
KR (1) KR20230165818A (enExample)
CN (1) CN117255685A (enExample)
AU (1) AU2022252419A1 (enExample)
BR (1) BR112023020123A2 (enExample)
CA (1) CA3214070A1 (enExample)
IL (1) IL307405A (enExample)
MX (2) MX2023011599A (enExample)
WO (1) WO2022212958A1 (enExample)

Families Citing this family (14)

* 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
WO2024078592A1 (zh) * 2022-10-14 2024-04-18 无锡诺宇医药科技有限公司 靶向成纤维细胞活化蛋白的药物及其应用
CN118852122A (zh) * 2023-04-27 2024-10-29 中国科学院上海药物研究所 一种fap抑制剂和靶向fap核素探针及其应用
US12440585B2 (en) * 2023-09-12 2025-10-14 Curadel Surgical Innovations, Inc. Zwitterionic metal chelators
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
KR20250062978A (ko) * 2023-10-31 2025-05-08 서울대학교병원 신규한 전립선 특이적 막 항원 리간드 및 이의 용도
WO2025119908A1 (en) * 2023-12-06 2025-06-12 Bracco Imaging Spa Psma-targeting fluorescent probes
WO2025163029A1 (en) 2024-01-31 2025-08-07 Bracco Imaging Spa Psma-targeting bimodal and heterobivalent fluorescent agents
CN117700485B (zh) * 2024-02-04 2024-04-16 山东大学 一种同时靶向psma和fap的化合物及其制备方法与应用
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
US12086990B1 (en) * 2024-04-23 2024-09-10 MultiFunctional Imaging LLC Systems and methods for simultaneous imaging of multiple positron emission tomography (PET) tracers
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
CN119080743B (zh) * 2024-08-30 2026-01-06 北京师范大学 靶向psma和fap的双重靶向化合物及其应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
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
PH12020551205A1 (en) * 2018-02-06 2021-04-19 Univ Heidelberg Fap inhibitors
CN112088169A (zh) * 2018-03-12 2020-12-15 纪念斯隆凯特琳癌症中心 双特异性结合剂及其用途
KR20210116437A (ko) * 2018-11-20 2021-09-27 코넬 유니버시티 방사성핵종의 마크로사이클릭 복합체 및 암의 방사선 요법에서의 이의 용도
CN113292538A (zh) * 2021-05-10 2021-08-24 北京肿瘤医院(北京大学肿瘤医院) 靶向肿瘤相关成纤维细胞激活蛋白的化合物及其制备方法和应用与靶向fap的肿瘤显影剂

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Publication number Publication date
BR112023020123A2 (pt) 2024-01-23
JP2024514528A (ja) 2024-04-02
EP4313049A4 (en) 2026-01-21
KR20230165818A (ko) 2023-12-05
CN117255685A (zh) 2023-12-19
MX2023011599A (es) 2024-02-02
EP4313049A1 (en) 2024-02-07
IL307405A (en) 2023-12-01
MX2026000948A (es) 2026-03-02
US20240382629A1 (en) 2024-11-21
AU2022252419A1 (en) 2023-10-19
WO2022212958A1 (en) 2022-10-06

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