CL2020002026A1 - Inhibidor de fap. - Google Patents

Inhibidor de fap.

Info

Publication number
CL2020002026A1
CL2020002026A1 CL2020002026A CL2020002026A CL2020002026A1 CL 2020002026 A1 CL2020002026 A1 CL 2020002026A1 CL 2020002026 A CL2020002026 A CL 2020002026A CL 2020002026 A CL2020002026 A CL 2020002026A CL 2020002026 A1 CL2020002026 A1 CL 2020002026A1
Authority
CL
Chile
Prior art keywords
compound
pharmaceutical composition
fap
fap inhibitor
inhibitor
Prior art date
Application number
CL2020002026A
Other languages
English (en)
Inventor
Uwe Haberkorn
Anastasia Loktev
Thomas Lindner
Walter Mier
Frederik Giesel
Clemens Kratochwil
Original Assignee
Univ Heidelberg
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 filed Critical Univ Heidelberg
Publication of CL2020002026A1 publication Critical patent/CL2020002026A1/es

Links

Classifications

    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
    • 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
    • A61K51/0497—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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Radiology & Medical Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

La presente invención se refiere a un compuesto de fórmula I, una composición farmacéutica que comprende o consiste en dicho compuesto, un kit que comprende o consiste en dicho compuesto o composición farmacéutica y el uso del compuesto o composición farmacéutica en el diagnóstico o tratamiento de una enfermedad caracterizada por la sobreexpresión de proteína activadora de fibroblastos (FAP, por sus siglas en inglés).
CL2020002026A 2018-02-06 2020-08-04 Inhibidor de fap. CL2020002026A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18155420 2018-02-06
EP18155419 2018-02-06
EP18199641 2018-10-10

Publications (1)

Publication Number Publication Date
CL2020002026A1 true CL2020002026A1 (es) 2020-11-27

Family

ID=67548792

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2020002026A CL2020002026A1 (es) 2018-02-06 2020-08-04 Inhibidor de fap.

Country Status (14)

Country Link
US (2) US20210038749A1 (es)
EP (1) EP3749663A1 (es)
JP (1) JP2021512949A (es)
KR (1) KR20200123148A (es)
CN (2) CN118146196A (es)
AU (2) AU2019219057B2 (es)
BR (1) BR112020015985A2 (es)
CA (1) CA3088326A1 (es)
CL (1) CL2020002026A1 (es)
CO (1) CO2020009625A2 (es)
IL (1) IL276594B2 (es)
MX (1) MX2020008271A (es)
SG (1) SG11202007180QA (es)
WO (1) WO2019154886A1 (es)

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MX2020004807A (es) 2017-10-23 2020-10-05 Univ Johns Hopkins Agentes radioterapeuticos y de imagenologia que se dirigen a proteina-alfa de activacion fibroblastos (fap-alfa).
WO2019118932A1 (en) 2017-12-15 2019-06-20 Praxis Biotech LLC Inhibitors of fibroblast activation protein
DE102018126558A1 (de) * 2018-10-24 2020-04-30 Helmholtz-Zentrum Dresden - Rossendorf E.V. Markierungsvorläufer mit Quadratsäure-Kopplung
JP2022514352A (ja) 2018-12-21 2022-02-10 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤
EP3891138B1 (en) 2020-02-12 2022-01-12 Philochem AG Fibroblast activation protein ligands for targeted delivery applications
JP2023514275A (ja) * 2020-02-12 2023-04-05 フィロケム・アーゲー 標的化された送達の用途のための線維芽細胞活性化タンパク質リガンド
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
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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
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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
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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
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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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CN115505032A (zh) * 2022-09-29 2022-12-23 烟台蓝纳成生物技术有限公司 一种成纤维细胞活化蛋白FAP和整合素αvβ3双重靶向化合物及其制备方法和应用
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
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Also Published As

Publication number Publication date
IL276594A (en) 2020-09-30
EP3749663A1 (en) 2020-12-16
US20210038749A1 (en) 2021-02-11
KR20200123148A (ko) 2020-10-28
AU2023201120A1 (en) 2023-03-30
IL276594B2 (en) 2023-11-01
AU2019219057A1 (en) 2020-07-09
WO2019154886A1 (en) 2019-08-15
CN118146196A (zh) 2024-06-07
RU2020126278A3 (es) 2022-03-09
IL276594B1 (en) 2023-07-01
US20230112012A1 (en) 2023-04-13
RU2020126278A (ru) 2022-03-09
CO2020009625A2 (es) 2020-08-21
CN111699181A (zh) 2020-09-22
CA3088326A1 (en) 2019-08-15
JP2021512949A (ja) 2021-05-20
AU2019219057B2 (en) 2022-11-24
SG11202007180QA (en) 2020-08-28
BR112020015985A2 (pt) 2020-12-15
MX2020008271A (es) 2020-11-09

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