CN117255685A - 靶向成纤维细胞活化蛋白α和/或前列腺特异性膜抗原的异二价剂和同二价剂 - Google Patents

靶向成纤维细胞活化蛋白α和/或前列腺特异性膜抗原的异二价剂和同二价剂 Download PDF

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CN117255685A
CN117255685A CN202280032772.6A CN202280032772A CN117255685A CN 117255685 A CN117255685 A CN 117255685A CN 202280032772 A CN202280032772 A CN 202280032772A CN 117255685 A CN117255685 A CN 117255685A
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group
compound
fap
hydrocarbyl
independently
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桑吉塔·班纳吉·雷
斯里坎特·博伊纳帕利
马丁·吉尔伯特·波姆珀
安德鲁·霍尔蒂
迪潘卡尔·达斯
闵逸
劳伦斯·卡罗尔
车孝真
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Johns Hopkins University
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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)
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  • Pharmacology & Pharmacy (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
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  • 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)
CN202280032772.6A 2021-04-02 2022-04-04 靶向成纤维细胞活化蛋白α和/或前列腺特异性膜抗原的异二价剂和同二价剂 Pending CN117255685A (zh)

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
CN117255685A true CN117255685A (zh) 2023-12-19

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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)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117700485A (zh) * 2024-02-04 2024-03-15 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
WO2024222888A1 (zh) * 2023-04-27 2024-10-31 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
CN119080743A (zh) * 2024-08-30 2024-12-06 北京师范大学 靶向psma和fap的双重靶向化合物及其应用
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

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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
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
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

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US20140357650A1 (en) * 2012-01-17 2014-12-04 Fox Chase Cancer Center Novel fap inhibitors
US20200157087A1 (en) * 2018-11-20 2020-05-21 Cornell University Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer
CN111699181A (zh) * 2018-02-06 2020-09-22 海德堡大学 Fap抑制剂
US20200330624A1 (en) * 2017-10-23 2020-10-22 The Johns Hopkins University Imaging and radiotherapeutics agents targeting fibroblast-activation protein-alpha (fap-alpha)
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

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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

Patent Citations (5)

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US20140357650A1 (en) * 2012-01-17 2014-12-04 Fox Chase Cancer Center Novel fap inhibitors
US20200330624A1 (en) * 2017-10-23 2020-10-22 The Johns Hopkins University Imaging and radiotherapeutics agents targeting fibroblast-activation protein-alpha (fap-alpha)
CN111699181A (zh) * 2018-02-06 2020-09-22 海德堡大学 Fap抑制剂
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
US20200157087A1 (en) * 2018-11-20 2020-05-21 Cornell University Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

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顾莹莹, 曹慧晓, 唐立钧.: "PSMA小分子抑制剂在前列腺癌PET/CT成像中的应用", 《国际医学放射学杂志》, vol. 43, no. 5, 21 October 2020 (2020-10-21), pages 591 - 595 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024222888A1 (zh) * 2023-04-27 2024-10-31 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
CN117700485A (zh) * 2024-02-04 2024-03-15 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
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
CN119080743A (zh) * 2024-08-30 2024-12-06 北京师范大学 靶向psma和fap的双重靶向化合物及其应用

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BR112023020123A2 (pt) 2024-01-23
JP2024514528A (ja) 2024-04-02
CA3214070A1 (en) 2022-10-06
EP4313049A4 (en) 2026-01-21
KR20230165818A (ko) 2023-12-05
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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