JP6946342B2 - エバンスブルー誘導体の化学的コンジュゲート、ならびに放射線治療剤およびイメージング剤としてのそれらの使用 - Google Patents

エバンスブルー誘導体の化学的コンジュゲート、ならびに放射線治療剤およびイメージング剤としてのそれらの使用 Download PDF

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JP6946342B2
JP6946342B2 JP2018558662A JP2018558662A JP6946342B2 JP 6946342 B2 JP6946342 B2 JP 6946342B2 JP 2018558662 A JP2018558662 A JP 2018558662A JP 2018558662 A JP2018558662 A JP 2018558662A JP 6946342 B2 JP6946342 B2 JP 6946342B2
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シァオユェン チェン
シァオユェン チェン
オリト ジェイコブソン ワイス
オリト ジェイコブソン ワイス
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
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    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/082—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the peptide being a RGD-containing peptide
    • 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
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
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    • C09B29/00—Monoazo dyes prepared by diazotising and coupling
    • C09B29/24—Monoazo dyes prepared by diazotising and coupling from coupling components containing both hydroxyl and amino directing groups
    • C09B29/28—Amino naphthols
    • C09B29/30—Amino naphtholsulfonic acid
    • 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
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2018558662A 2016-05-09 2017-05-09 エバンスブルー誘導体の化学的コンジュゲート、ならびに放射線治療剤およびイメージング剤としてのそれらの使用 Active JP6946342B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662333427P 2016-05-09 2016-05-09
US62/333,427 2016-05-09
PCT/US2017/031696 WO2017196806A1 (en) 2016-05-09 2017-05-09 Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents

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JP2019519491A JP2019519491A (ja) 2019-07-11
JP2019519491A5 JP2019519491A5 (https=) 2020-05-28
JP6946342B2 true JP6946342B2 (ja) 2021-10-06

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US (1) US10696631B2 (https=)
EP (1) EP3455206B1 (https=)
JP (1) JP6946342B2 (https=)
CN (1) CN109153641B (https=)
SG (1) SG11201809982RA (https=)
WO (1) WO2017196806A1 (https=)

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US10709790B2 (en) 2015-06-22 2020-07-14 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chemical conjugates of Evans Blue derivatives and their use in the production of long-acting therapeutics
SG11202002882VA (en) 2017-10-03 2020-04-29 The United States Of America As Represented By The Secretary Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents
AU2019225154B2 (en) * 2018-02-22 2024-10-24 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents for targeting prostate cancer
TWI745616B (zh) * 2018-09-10 2021-11-11 行政院原子能委員會核能研究所 放射線標誌長效型靶向性胜肽藥物及其生產方法
CN109485642A (zh) * 2018-11-21 2019-03-19 希施生物科技（上海）有限公司 一种制备伊文氏蓝衍生物的方法
WO2020160222A2 (en) 2019-01-30 2020-08-06 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Conjugates of bivalent evans blue dye derivatives and methods of use
US12357712B2 (en) * 2019-05-24 2025-07-15 Beijing Giluntide Pharmaceutical Co., Ltd. Targeted radiopharmaceutical for tumor and its use in the imaging-guided combination therapy of targeted radiotherapy and immunotherapy
CA3174082A1 (en) * 2020-03-04 2021-09-10 Nihon Medi-Physics Co., Ltd. Compound and radioactive labeling compound
MX2022013783A (es) * 2020-05-06 2023-04-19 Univ Cornell Compuestos tratanosticos que contienen cobre y metodos de uso.
CN114790193B (zh) * 2020-12-21 2024-05-10 苏州药明博锐生物科技有限公司 成纤维细胞活化蛋白抑制剂
CN114369084B (zh) * 2021-02-10 2023-02-03 烟台蓝纳成生物技术有限公司 一种截短型伊文思蓝修饰的成纤维细胞活化蛋白抑制剂及其制备方法和应用
NZ803235A (en) 2021-02-10 2026-01-30 Yantai Lannacheng Biotechnology Co Ltd Truncated evans blue modified fibroblast activation protein inhibitor, preparation method therefor, and application thereof
CN113004371A (zh) 2021-03-01 2021-06-22 上海蓝纳成生物技术有限公司 一种长循环半衰期的前列腺特异性膜抗原靶向化合物及其制备方法和应用
CN114796532A (zh) * 2022-04-20 2022-07-29 北京先通国际医药科技股份有限公司 放射性标记的伊文思蓝衍生物药物水溶液及其用途
WO2023236778A1 (zh) * 2022-06-10 2023-12-14 北京大学 一种三功能化合物及其用途
CN115433261B (zh) * 2022-11-07 2023-01-13 烟台蓝纳成生物技术有限公司 一种rgd二聚体化合物及其制备方法和应用
CN115583989B (zh) * 2022-12-09 2023-02-28 烟台蓝纳成生物技术有限公司 一种靶向sstr2的化合物及其制备方法和应用
CN115611779A (zh) * 2022-12-21 2023-01-17 北京先通国际医药科技股份有限公司 一种放射性药物前体的中间体的制备方法及其用途
CN115838393B (zh) * 2023-02-16 2023-05-05 烟台蓝纳成生物技术有限公司 用于fapi合成的中间体及其制备方法和应用
CN115850367B (zh) * 2023-03-02 2023-05-23 北京先通国际医药科技股份有限公司 Psma抑制剂的纯化方法及其用途
CN115947775B (zh) * 2023-03-13 2023-06-09 北京先通国际医药科技股份有限公司 一种制备化合物（i）的方法和化合物（i）及其用途
KR20260009883A (ko) * 2023-05-24 2026-01-20 베이징 창핑 래보러토리 신규 삼관능 화합물 및 이의 용도

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SG11202002882VA (en) 2017-10-03 2020-04-29 The United States Of America As Represented By The Secretary Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents
AU2019225154B2 (en) 2018-02-22 2024-10-24 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents for targeting prostate cancer

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CN109153641B (zh) 2022-10-18
EP3455206A4 (en) 2019-11-27
EP3455206B1 (en) 2020-11-04
US20190084931A1 (en) 2019-03-21
US10696631B2 (en) 2020-06-30
WO2017196806A1 (en) 2017-11-16
JP2019519491A (ja) 2019-07-11
CN109153641A (zh) 2019-01-04
EP3455206A1 (en) 2019-03-20
SG11201809982RA (en) 2018-12-28

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