JP2021512949A - Ｆａｐ阻害物質 - Google Patents

Ｆａｐ阻害物質 Download PDF

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JP2021512949A
JP2021512949A JP2020563822A JP2020563822A JP2021512949A JP 2021512949 A JP2021512949 A JP 2021512949A JP 2020563822 A JP2020563822 A JP 2020563822A JP 2020563822 A JP2020563822 A JP 2020563822A JP 2021512949 A JP2021512949 A JP 2021512949A
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group
fapi
cancer
fap
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JP2021512949A5 (enExample
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ウーヴェ・ハーベルコルン
アナスタシア・ロクテフ
トーマス・リントナー
ヴァルター・ミアー
フレデリク・ギーゼル
クレメンス・クラトホヴィル
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ウニベルジテート ハイデルベルク
ウニベルジテート ハイデルベルク
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    • 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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • A61K49/101—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals
    • A61K49/106—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals the complex-forming compound being cyclic, e.g. DOTA
    • 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
    • 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
    • A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Radiology & Medical Imaging (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020563822A 2018-02-06 2019-02-06 Ｆａｐ阻害物質 Withdrawn JP2021512949A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2025121203A JP2025165981A (ja) 2018-02-06 2025-07-18 Ｆａｐ阻害物質

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP18155419.7 2018-02-06
EP18155419 2018-02-06
EP18155420.5 2018-02-06
EP18155420 2018-02-06
EP18199641.4 2018-10-10
EP18199641 2018-10-10
PCT/EP2019/052952 WO2019154886A1 (en) 2018-02-06 2019-02-06 Fap inhibitor

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JP2025121203A Division JP2025165981A (ja) 2018-02-06 2025-07-18 Ｆａｐ阻害物質

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JP2021512949A true JP2021512949A (ja) 2021-05-20
JP2021512949A5 JP2021512949A5 (enExample) 2021-07-01

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JP2025121203A Pending JP2025165981A (ja) 2018-02-06 2025-07-18 Ｆａｐ阻害物質

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US (3) US20210038749A1 (enExample)
EP (1) EP3749663A1 (enExample)
JP (2) JP2021512949A (enExample)
KR (3) KR20250021601A (enExample)
CN (2) CN118146196A (enExample)
AU (5) AU2019219057B2 (enExample)
CA (1) CA3088326A1 (enExample)
CL (1) CL2020002026A1 (enExample)
CO (1) CO2020009625A2 (enExample)
IL (1) IL276594B2 (enExample)
MX (1) MX2020008271A (enExample)
PH (1) PH12020551205A1 (enExample)
SG (1) SG11202007180QA (enExample)
WO (1) WO2019154886A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023162946A1 (ja) * 2022-02-22 2023-08-31 国立大学法人大阪大学 放射標識されたＦＡＰα親和性化合物およびその用途
US11938201B2 (en) 2017-10-23 2024-03-26 The Johns Hopkins University Imaging and radiotherapeutics agents targeting fibroblast-activation protein-alpha (FAP-alpha)
JP2025503541A (ja) * 2022-07-20 2025-02-04 嘉興法伯新天医薬科技有限公司 ＦＡＰ－α特異的腫瘍診断イメージング剤

Families Citing this family (90)

* Cited by examiner, † Cited by third party
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EP3723753A4 (en) 2017-12-15 2022-01-26 Praxis Biotech LLC FIBROBLAST ACTIVATION PROTEIN INHIBITORS
DE102018126558A1 (de) * 2018-10-24 2020-04-30 Helmholtz-Zentrum Dresden - Rossendorf E.V. Markierungsvorläufer mit Quadratsäure-Kopplung
CN113811529A (zh) 2018-12-21 2021-12-17 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂
JP2022548155A (ja) * 2019-09-17 2022-11-16 パーデュー・リサーチ・ファウンデーション 線維芽細胞活性化タンパク質（ｆａｐ）を標的とする、がんならびに他の線維性疾患および炎症性疾患の画像化および治療の方法
US20240002408A1 (en) * 2020-01-31 2024-01-04 Purdue Research Foundation Fibroblast activation protein (fap) - targeted antifibrotic therapy
CN118812631A (zh) * 2020-02-12 2024-10-22 菲洛谢姆股份公司 用于靶向递送应用的成纤维细胞激活蛋白配体
DK3891138T3 (da) 2020-02-12 2022-04-04 Philochem Ag Fibroblastaktiveringsproteinligander til målrettede indgivelsesanvendelser
TW202202150A (zh) * 2020-03-24 2022-01-16 美商杜夫特學院信託管理公司 靶向fap之放射性藥品及造影劑，與其相關用途
WO2021234181A1 (en) * 2020-05-22 2021-11-25 Universität Heidelberg Use of fap inhibitor in a method of diagnosis
CN111991570B (zh) * 2020-07-24 2021-05-18 北京大学 一种FAP-α特异性肿瘤诊断SPECT显像剂
CN114073781A (zh) * 2020-08-11 2022-02-22 上海健康医学院 一种肿瘤间质显像剂及其制备方法
CN112138175A (zh) * 2020-09-01 2020-12-29 上海市质子重离子临床技术研发中心 一种放射性核素99mTc标记FAPI的化合物的制备方法
CN112972707A (zh) * 2020-09-10 2021-06-18 广州呼吸健康研究院 18F-FDG和68Ga-FAPI的应用
CN112194651B (zh) * 2020-10-12 2021-11-09 南方医科大学南方医院 一种pet示踪剂的前体化合物及其应用
CN114380795A (zh) * 2020-10-22 2022-04-22 四川大学华西医院 氘代fap抑制剂及其应用
CN112023064A (zh) * 2020-11-03 2020-12-04 南京大为科创服务有限责任公司 用于标记核素211At的成纤维细胞活化蛋白抑制剂的锡基衍生物及其制备方法和应用
CN112933253A (zh) * 2020-11-13 2021-06-11 上海市质子重离子临床技术研发中心 一种放射性核素标记fapi的化合物及其合成工艺方法
CN112409414B (zh) * 2020-12-01 2021-10-26 北京师范大学 锝-99m标记含异腈的FAPI衍生物及制备方法和应用
PE20232046A1 (es) 2020-12-17 2023-12-27 Astrazeneca Ab N-(2-(4-cianotiazolidin-3-il)-2-oxoetil)-quinolin-4-carboxamidas
CN112522388A (zh) * 2020-12-18 2021-03-19 上海市东方医院（同济大学附属东方医院） 成纤维细胞激活蛋白作为药物靶点在治疗骨关节炎中的用途
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
CN114790194B (zh) * 2020-12-21 2024-03-26 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
CN114790195B (zh) * 2020-12-21 2024-05-17 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
US20240139350A1 (en) * 2021-02-01 2024-05-02 Five Eleven Pharma, Inc Radioactively labeled ligand for fibroblast activation protein-alpha imaging agent and preparation method therefor
CA3210863C (en) * 2021-02-10 2024-06-04 Yantai Lannacheng Biotechnology Co., Ltd. Truncated evans blue modified fibroblast activation protein inhibitor, preparation method and application thereof
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
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
CN116917278A (zh) * 2021-02-12 2023-10-20 菲罗化学股份公司 用于靶向递送应用的二价成纤维细胞活化蛋白配体
EP4043452A1 (en) 2021-02-12 2022-08-17 Philochem AG Bivalent fibroblast activation protein ligands for targeted delivery applications
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BR112023020123A2 (pt) * 2021-04-02 2024-01-23 Univ Johns Hopkins Agentes heterobivalentes e homobivalentes que alvejam proteína alfa de ativação de fibroblasto alfa e/ou antígeno de membrana específico da próstata
MX2021005089A (es) * 2021-04-30 2022-11-01 Instituto Nac De Investigaciones Nucleares Radiofarmacos basados en el acido ((r)-1-((6-hidrazinilnicotinoil) d-alanil)pirrolidin-2-il)boronico (hynic-ifap) para la deteccion de la sobreexpresion de la proteina de activacion de fibrolastos.
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
CN113444146B (zh) * 2021-06-01 2022-03-11 南方医科大学南方医院 靶向成纤维细胞活化蛋白探针、制备方法及其在制备pet显像剂中的应用
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CN114099717A (zh) * 2021-09-30 2022-03-01 同济大学 一种肿瘤成纤维细胞活化蛋白靶向磁共振造影剂及其制备和应用
MX2024004077A (es) 2021-10-04 2024-04-18 Philochem Ag Ligandos de proteina de activacion de fibroblastos radioetiquetados.
TW202317541A (zh) 2021-10-28 2023-05-01 行政院原子能委員會核能研究所 一種靶向成纖維細胞活化蛋白之化合物或其鹽，其製備方法及其用途
CN114315795B (zh) * 2021-11-30 2023-05-02 北京师范大学 68Ga标记的靶向成纤维细胞激活蛋白的抑制剂类放射性探针及其制备方法
DE102021133942A1 (de) 2021-12-20 2023-06-22 Atoms for Cure GmbH FAP-adressierendes Pharmazeutikum für die Therapie und Diagnose von Krebserkrankungen
CN114573558B (zh) * 2022-01-05 2022-11-08 四川大学华西医院 一种水溶性甲基苄醚衍生物、正电子核素探针、核素标记物及制备方法和应用
WO2023144379A1 (en) 2022-01-30 2023-08-03 Philochem Ag High-affinity ligands of fibroblast activation protein for targeted delivery applications
WO2023202655A1 (en) * 2022-04-21 2023-10-26 Shanghai Sinotau Biotech. Co., Ltd Fap inhibitors
WO2023222558A1 (en) 2022-05-14 2023-11-23 Zounek Alexis Nikolai Precursor and theranostic radiotracer with improved tumor retention
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