JP2024514528A - 線維芽細胞活性化タンパク質アルファおよび／または前立腺特異的膜抗原を標的とするヘテロ二価およびホモ二価薬剤 - Google Patents

線維芽細胞活性化タンパク質アルファおよび／または前立腺特異的膜抗原を標的とするヘテロ二価およびホモ二価薬剤 Download PDF

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JP2024514528A
JP2024514528A JP2023560919A JP2023560919A JP2024514528A JP 2024514528 A JP2024514528 A JP 2024514528A JP 2023560919 A JP2023560919 A JP 2023560919A JP 2023560919 A JP2023560919 A JP 2023560919A JP 2024514528 A JP2024514528 A JP 2024514528A
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JPWO2022212958A5 (https=
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バネルジー レイ サンギータ
ボイナパリー スリカンス
ギルバート ポンパー マーティン
ホルティ アンドリュー
ダス ディーパンカー
ミン イル
キャロル ローレンス
チャ ヒョジン
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Johns Hopkins University
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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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)
  • Veterinary Medicine (AREA)
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  • 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)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2023560919A 2021-04-02 2022-04-04 線維芽細胞活性化タンパク質アルファおよび／または前立腺特異的膜抗原を標的とするヘテロ二価およびホモ二価薬剤 Pending JP2024514528A (ja)

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

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JP2024514528A true JP2024514528A (ja) 2024-04-02
JP2024514528A5 JP2024514528A5 (https=) 2025-04-14
JPWO2022212958A5 JPWO2022212958A5 (https=) 2025-04-14

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JP2023560919A Pending JP2024514528A (ja) 2021-04-02 2022-04-04 線維芽細胞活性化タンパク質アルファおよび／または前立腺特異的膜抗原を標的とするヘテロ二価およびホモ二価薬剤

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

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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
AU2023347470A1 (en) 2022-09-23 2025-04-10 Nuclidium Ag High-purity copper radiopharmaceutical compositions and diagnostic and therapeutic uses thereof
CN117883585A (zh) * 2022-10-14 2024-04-16 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
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
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
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

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Publication number Priority date Publication date Assignee Title
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
EA202090776A1 (ru) * 2017-10-23 2020-07-27 Дзе Джонс Хопкинс Юниверсити Визуализирующие и радиотерапевтические агенты, нацеленные на фибробласт-активирующий белок-альфа (fapalpha)
SG11202007180QA (en) * 2018-02-06 2020-08-28 Univ Heidelberg Fap inhibitor
CA3093694A1 (en) * 2018-03-12 2019-09-19 Memorial Sloan Kettering Cancer Center Bispecific binding agents and uses thereof
US11279698B2 (en) * 2018-11-20 2022-03-22 Cornell University Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer
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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CN117255685A (zh) 2023-12-19
US20240382629A1 (en) 2024-11-21
WO2022212958A1 (en) 2022-10-06
MX2023011599A (es) 2024-02-02
BR112023020123A2 (pt) 2024-01-23
MX2026000948A (es) 2026-03-02
EP4313049A1 (en) 2024-02-07
IL307405A (en) 2023-12-01
EP4313049A4 (en) 2026-01-21
CA3214070A1 (en) 2022-10-06
KR20230165818A (ko) 2023-12-05
AU2022252419A1 (en) 2023-10-19

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