AU2020348781B2 - Fibroblast activation protein (FAP)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases - Google Patents

Fibroblast activation protein (FAP)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases

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Publication number
AU2020348781B2
AU2020348781B2 AU2020348781A AU2020348781A AU2020348781B2 AU 2020348781 B2 AU2020348781 B2 AU 2020348781B2 AU 2020348781 A AU2020348781 A AU 2020348781A AU 2020348781 A AU2020348781 A AU 2020348781A AU 2020348781 B2 AU2020348781 B2 AU 2020348781B2
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AU2020348781A1 (en
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Philip Stewart Low
Ramesh Mukkamala
Madduri SRINIVASARAO
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Purdue Research Foundation
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/001Preparation for luminescence or biological staining
    • A61K49/0013Luminescence
    • A61K49/0017Fluorescence in vivo
    • A61K49/0019Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0032Methine dyes, e.g. cyanine dyes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/001Preparation for luminescence or biological staining
    • A61K49/0013Luminescence
    • A61K49/0017Fluorescence in vivo
    • A61K49/0019Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0041Xanthene dyes, used in vivo, e.g. administered to a mice, e.g. rhodamines, rose Bengal
    • A61K49/0043Fluorescein, used in vivo
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/001Preparation for luminescence or biological staining
    • A61K49/0013Luminescence
    • A61K49/0017Fluorescence in vivo
    • A61K49/005Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0052Small organic molecules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/085Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier conjugated systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0446Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0497Organic compounds conjugates with a carrier being an organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Radiology & Medical Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2020348781A 2019-09-17 2020-09-17 Fibroblast activation protein (FAP)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases Active AU2020348781B2 (en)

Priority Applications (1)

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AU2026200943A AU2026200943A1 (en) 2019-09-17 2026-02-10 Fibroblast activation protein (FAP)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases

Applications Claiming Priority (3)

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US201962901792P 2019-09-17 2019-09-17
US62/901,792 2019-09-17
PCT/US2020/051328 WO2021055641A1 (en) 2019-09-17 2020-09-17 Fibroblast activation protein (fap)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases

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AU2020348781A1 AU2020348781A1 (en) 2022-04-14
AU2020348781B2 true AU2020348781B2 (en) 2025-11-27

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AU2026200943A Abandoned AU2026200943A1 (en) 2019-09-17 2026-02-10 Fibroblast activation protein (FAP)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases

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US (1) US20220409747A1 (https=)
EP (1) EP4031184A4 (https=)
JP (2) JP2022548155A (https=)
KR (1) KR20220066098A (https=)
CN (1) CN114901315B (https=)
AU (2) AU2020348781B2 (https=)
BR (1) BR112022005013A2 (https=)
CA (1) CA3150890A1 (https=)
IL (1) IL291386A (https=)
MX (1) MX2022003215A (https=)
WO (1) WO2021055641A1 (https=)

Families Citing this family (10)

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Publication number Priority date Publication date Assignee Title
EP2934532B1 (en) 2012-12-20 2019-10-23 Purdue Research Foundation Chimeric antigen receptor-expressing t cells as anti-cancer therapeutics
JP7282521B2 (ja) 2016-04-08 2023-05-29 パーデュー・リサーチ・ファウンデイション Car t細胞療法のための方法および組成物
JP7178355B2 (ja) 2017-02-28 2022-11-25 エンドサイト・インコーポレイテッド Car t細胞療法のための組成物および方法
JP7549303B2 (ja) 2018-01-22 2024-09-11 エンドサイト・インコーポレイテッド Car t細胞の使用方法
CN112105382A (zh) 2018-02-23 2020-12-18 恩多塞特公司 用于car t细胞疗法的顺序方法
US20230147962A1 (en) * 2020-02-12 2023-05-11 Philochem Ag Fibroblast activation protein ligands for targeted delivery applications
EP4132921A4 (en) * 2020-04-09 2024-03-27 Purdue Research Foundation Pi3 kinase inhibitors and uses thereof
WO2023244828A1 (en) * 2022-06-17 2023-12-21 Purdue Research Foundation Fibroblast activation protein-targeted nanoparticle magnetic resonance imaging agents
AU2024235779A1 (en) * 2023-03-10 2025-10-23 Purdue Research Foundation Bi-specific adapters and their use with universal car-t cells in the treatment of tumors and the inhibition of cancer-associated fibroblasts
WO2026041108A1 (zh) * 2024-08-23 2026-02-26 苏州博锐创合医药有限公司 基于环肽和共价弹头的化合物及其用途

Citations (3)

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US20100234431A1 (en) * 2009-03-13 2010-09-16 National Health Research Institutes Pyrrolidine compounds
WO2018111989A1 (en) * 2016-12-14 2018-06-21 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
WO2020083853A1 (de) * 2018-10-24 2020-04-30 Johannes Gutenberg-Universität Mainz Markierungsvorläufer mit quadratsäure-kopplung

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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CN103788071A (zh) * 2012-11-01 2014-05-14 中国人民解放军第二军医大学 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
AU2017213404A1 (en) * 2016-01-29 2018-09-20 Kyowa Kirin Co., Ltd. Nucleic acid conjugate
EA202090776A1 (ru) * 2017-10-23 2020-07-27 Дзе Джонс Хопкинс Юниверсити Визуализирующие и радиотерапевтические агенты, нацеленные на фибробласт-активирующий белок-альфа (fapalpha)
US10966999B2 (en) * 2017-12-20 2021-04-06 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
WO2019154859A1 (en) * 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
SG11202007180QA (en) * 2018-02-06 2020-08-28 Univ Heidelberg Fap inhibitor

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100234431A1 (en) * 2009-03-13 2010-09-16 National Health Research Institutes Pyrrolidine compounds
WO2018111989A1 (en) * 2016-12-14 2018-06-21 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
WO2020083853A1 (de) * 2018-10-24 2020-04-30 Johannes Gutenberg-Universität Mainz Markierungsvorläufer mit quadratsäure-kopplung

Also Published As

Publication number Publication date
CN114901315B (zh) 2025-04-29
MX2022003215A (es) 2022-04-25
AU2020348781A1 (en) 2022-04-14
JP2022548155A (ja) 2022-11-16
BR112022005013A2 (pt) 2022-06-21
WO2021055641A1 (en) 2021-03-25
CN114901315A (zh) 2022-08-12
JP2025131780A (ja) 2025-09-09
EP4031184A4 (en) 2023-12-06
AU2026200943A1 (en) 2026-02-26
KR20220066098A (ko) 2022-05-23
CA3150890A1 (en) 2021-03-25
IL291386A (en) 2022-05-01
EP4031184A1 (en) 2022-07-27
US20220409747A1 (en) 2022-12-29

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