IL276594B2 - FAP inhibitors - Google Patents

FAP inhibitors

Info

Publication number
IL276594B2
IL276594B2 IL276594A IL27659420A IL276594B2 IL 276594 B2 IL276594 B2 IL 276594B2 IL 276594 A IL276594 A IL 276594A IL 27659420 A IL27659420 A IL 27659420A IL 276594 B2 IL276594 B2 IL 276594B2
Authority
IL
Israel
Prior art keywords
fapi
alkyl
group
cancer
compound
Prior art date
Application number
IL276594A
Other languages
English (en)
Hebrew (he)
Other versions
IL276594B1 (en
IL276594A (en
Inventor
Haberkorn Uwe
Loktev Anastasia
Lindner Thomas
Mier Walter
KRATOCHWIL Clemens
Giesel Fredenik
Original Assignee
Univ Heidelberg
Haberkorn Uwe
Loktev Anastasia
Lindner Thomas
Mier Walter
KRATOCHWIL Clemens
Giesel Fredenik
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Univ Heidelberg, Haberkorn Uwe, Loktev Anastasia, Lindner Thomas, Mier Walter, KRATOCHWIL Clemens, Giesel Fredenik filed Critical Univ Heidelberg
Publication of IL276594A publication Critical patent/IL276594A/en
Publication of IL276594B1 publication Critical patent/IL276594B1/en
Publication of IL276594B2 publication Critical patent/IL276594B2/en

Links

Classifications

    • 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

Landscapes

  • 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)
IL276594A 2018-02-06 2019-02-06 FAP inhibitors IL276594B2 (en)

Applications Claiming Priority (4)

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

Publications (3)

Publication Number Publication Date
IL276594A IL276594A (en) 2020-09-30
IL276594B1 IL276594B1 (en) 2023-07-01
IL276594B2 true IL276594B2 (en) 2023-11-01

Family

ID=67548792

Family Applications (1)

Application Number Title Priority Date Filing Date
IL276594A IL276594B2 (en) 2018-02-06 2019-02-06 FAP inhibitors

Country Status (14)

Country Link
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)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
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CN116617420A (zh) 2017-10-23 2023-08-22 约翰霍普金斯大学 靶向成纤维细胞活化蛋白α的化合物、药物组合物及用途
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
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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
GB202109922D0 (en) 2021-07-09 2021-08-25 Blue Earth Diagnostics Ltd Radiotracers and therapeutics binding to fibroblast activation protein (fap)
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
TW202320805A (zh) * 2021-08-18 2023-06-01 美商杜夫特學院信託管理公司 用於pet造影之選擇性靶向纖維母細胞活化蛋白之放射性氟標誌試劑
CN117460826A (zh) * 2021-09-14 2024-01-26 菲柏生物医学技术（广州）有限公司 靶向FAP阳性细胞的siRNA缀合物及其药物组合物和应用
CN113880810B (zh) * 2021-09-24 2023-02-28 厦门大学 一种核素标记的配合物及其制备方法和应用
CN113880811B (zh) * 2021-09-29 2022-09-02 厦门大学附属第一医院 Fapi二聚体化合物、基于fapi二聚体的肿瘤诊断pet显像剂及其制备方法和应用
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
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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
EP4537851A1 (en) 2022-06-10 2025-04-16 Peking University Trifunctional compound and use thereof
CN119562951A (zh) 2022-06-21 2025-03-04 阿斯利康(瑞典)有限公司 N-(2-(4-氰基噻唑烷-3-基)-2-氧代乙基)-喹啉-4-甲酰胺
CN115304582B (zh) * 2022-07-20 2023-05-12 北京法伯新天医药科技有限公司 FAP-α特异性肿瘤诊断显像剂
WO2024022332A1 (en) 2022-07-26 2024-02-01 Shanghai Sinotau Biotech. Co., Ltd Fap inhibitors
CA3266566A1 (en) 2022-09-06 2024-03-14 Philochem Ag MULTIVALENT FIBROBLAST ACTIVATING PROTEIN LIGANDS FOR TARGETED DELIVERY APPLICATIONS
JP2025532104A (ja) 2022-09-23 2025-09-29 ヌクリディウム アクチェンゲゼルシャフト 高純度銅放射性医薬組成物ならびにその診断および治療用途
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