TWI871182B - 用於fapi合成的中間體及其製備方法和應用 - Google Patents

用於fapi合成的中間體及其製備方法和應用 Download PDF

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Publication number
TWI871182B
TWI871182B TW113105190A TW113105190A TWI871182B TW I871182 B TWI871182 B TW I871182B TW 113105190 A TW113105190 A TW 113105190A TW 113105190 A TW113105190 A TW 113105190A TW I871182 B TWI871182 B TW I871182B
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Taiwan
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compound
acid
amino
application
organic
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TW113105190A
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English (en)
Chinese (zh)
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TW202434565A (zh
Inventor
吳曉明
王相玉
何田
楊清寶
成琳
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大陸商煙臺藍納成生物技術有限公司
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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
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C07K1/08—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents using activating agents
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW113105190A 2023-02-16 2024-02-15 用於fapi合成的中間體及其製備方法和應用 TWI871182B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN202310124318X 2023-02-16
CN202310124318.XA CN115838393B (zh) 2023-02-16 2023-02-16 用于fapi合成的中间体及其制备方法和应用

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TW202434565A TW202434565A (zh) 2024-09-01
TWI871182B true TWI871182B (zh) 2025-01-21

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TW113105190A TWI871182B (zh) 2023-02-16 2024-02-15 用於fapi合成的中間體及其製備方法和應用

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US (1) US20250382329A1 (https=)
EP (1) EP4585607A4 (https=)
JP (1) JP7838187B2 (https=)
KR (1) KR20250022067A (https=)
CN (1) CN115838393B (https=)
CA (1) CA3255143A1 (https=)
TW (1) TWI871182B (https=)
WO (1) WO2024169973A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2025091141A1 (zh) * 2023-10-30 2025-05-08 烟台蓝纳成生物技术有限公司 用放射性标记的截短型伊文思蓝修饰的成纤维细胞活化蛋白抑制剂治疗甲状腺癌的方法
CN118754875B (zh) * 2024-09-06 2024-12-13 烟台蓝纳成生物技术有限公司 一种fapi前体化合物的制备工艺及应用

Citations (2)

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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
CN113582975A (zh) * 2021-07-03 2021-11-02 上海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

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US10696631B2 (en) * 2016-05-09 2020-06-30 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
EP3749663A1 (en) * 2018-02-06 2020-12-16 Universität Heidelberg Fap inhibitor
EP4126053A4 (en) * 2020-03-24 2024-11-20 Trustees Of Tufts College IMAGING AGENTS AND RADIOPHARMACEUTICALS TARGETING FAP, AND USES THEREOF
WO2022170732A1 (zh) * 2021-02-10 2022-08-18 上海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
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
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
CN113603678A (zh) * 2021-08-10 2021-11-05 上海蓝纳成生物技术有限公司 一种靶向成纤维细胞活化蛋白的诊断药物及其制备方法
CN113621021A (zh) * 2021-08-10 2021-11-09 上海蓝纳成生物技术有限公司 一种靶向成纤维细胞活化蛋白的治疗药物及其制备方法
CN115677829A (zh) * 2022-10-19 2023-02-03 广州华复生物科技有限公司 一种糖基化靶向fap化合物、靶向fap标记配合物及其制备方法与应用
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN113582975A (zh) * 2021-07-03 2021-11-02 上海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

Non-Patent Citations (1)

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Title
期刊 Xuejun Wen ETAL., "Evans blue-modified radiolabeled fibroblast activation protein inhibitor as long-acting cancer therapeutics", Theranostics. 12(1) 2022 pages 422–433 *

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Publication number Publication date
WO2024169973A1 (zh) 2024-08-22
TW202434565A (zh) 2024-09-01
EP4585607A4 (en) 2026-03-25
CA3255143A1 (en) 2025-03-28
US20250382329A1 (en) 2025-12-18
JP7838187B2 (ja) 2026-03-31
EP4585607A1 (en) 2025-07-16
CN115838393B (zh) 2023-05-05
JP2025534068A (ja) 2025-10-09
CN115838393A (zh) 2023-03-24
KR20250022067A (ko) 2025-02-14

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