BR112023015831A2 - Ligantes de proteína de ativação de fibroblastos bivalentes para aplicações de liberação direcionada - Google Patents

Ligantes de proteína de ativação de fibroblastos bivalentes para aplicações de liberação direcionada

Info

Publication number
BR112023015831A2
BR112023015831A2 BR112023015831A BR112023015831A BR112023015831A2 BR 112023015831 A2 BR112023015831 A2 BR 112023015831A2 BR 112023015831 A BR112023015831 A BR 112023015831A BR 112023015831 A BR112023015831 A BR 112023015831A BR 112023015831 A2 BR112023015831 A2 BR 112023015831A2
Authority
BR
Brazil
Prior art keywords
bivalent
linders
targeted release
activating protein
fap
Prior art date
Application number
BR112023015831A
Other languages
English (en)
Inventor
Andrea Galbiati
Aureliano Zana
Jacopo Millul
Samuele Cazzamalli
Original Assignee
Philochem Ag
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
Priority claimed from PCT/EP2021/053494 external-priority patent/WO2021160825A1/en
Priority claimed from EP21190665.6A external-priority patent/EP4043452A1/en
Application filed by Philochem Ag filed Critical Philochem Ag
Publication of BR112023015831A2 publication Critical patent/BR112023015831A2/pt

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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
    • C07D401/02—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
    • 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
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/55—Medicinal 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/62—Medicinal 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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K51/0446—Heterocyclic 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

ligantes de proteína de ativação de fibroblastos bivalentes para aplicações de liberação direcionada. a presente invenção refere-se a ligantes da proteína de ativação de fibroblastos (fap) para a liberação ativa de várias cargas úteis (por exemplo, fármacos citotóxicos, radionuclídeos, fluoróforos, proteínas e imunomoduladores) no sítio da doença. em particular, a presente invenção refere-se ao desenvolvimento de ligantes de fap bivalentes para aplicações de direcionamento, em particular métodos de diagnóstico e/ou métodos para terapia ou cirurgia em relação a uma doença ou distúrbio, como câncer, inflamação ou outra doença caracterizada pela superexpressão de fap.
BR112023015831A 2021-02-12 2022-02-11 Ligantes de proteína de ativação de fibroblastos bivalentes para aplicações de liberação direcionada BR112023015831A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/EP2021/053494 WO2021160825A1 (en) 2020-02-12 2021-02-12 Fibroblast activation protein ligands for targeted delivery applications
EP21190665.6A EP4043452A1 (en) 2021-02-12 2021-08-10 Bivalent fibroblast activation protein ligands for targeted delivery applications
PCT/EP2022/053404 WO2022171811A1 (en) 2021-02-12 2022-02-11 Bivalent fibroblast activation protein ligands for targeted delivery applications

Publications (1)

Publication Number Publication Date
BR112023015831A2 true BR112023015831A2 (pt) 2023-10-10

Family

ID=80685200

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112023015831A BR112023015831A2 (pt) 2021-02-12 2022-02-11 Ligantes de proteína de ativação de fibroblastos bivalentes para aplicações de liberação direcionada

Country Status (9)

Country Link
US (1) US20240148916A1 (pt)
EP (1) EP4291554A1 (pt)
JP (1) JP2024506644A (pt)
KR (1) KR20230145162A (pt)
AU (1) AU2022219525A1 (pt)
BR (1) BR112023015831A2 (pt)
CA (1) CA3207999A1 (pt)
IL (1) IL304960A (pt)
WO (1) WO2022171811A1 (pt)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102021133942A1 (de) * 2021-12-20 2023-06-22 Atoms for Cure GmbH FAP-adressierendes Pharmazeutikum für die Therapie und Diagnose von Krebserkrankungen
CN116554146A (zh) * 2022-01-29 2023-08-08 中国科学院生物物理研究所 一种FAP-α特异性放射性药物及其应用
CN115368342B (zh) * 2022-08-24 2024-01-23 西南医科大学附属医院 成纤维细胞活性蛋白抑制剂、其放射性核素标记物及制备方法和应用
WO2024052333A1 (en) 2022-09-06 2024-03-14 Philochem Ag Multivalent fibroblast activation protein ligands for targeted delivery applications

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7375078B2 (en) 2004-02-23 2008-05-20 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
EP1729774A4 (en) 2004-03-09 2009-05-06 Nat Health Research Institutes PYRROLIDINE COMPOUNDS
WO2013107820A1 (en) 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
WO2018111989A1 (en) 2016-12-14 2018-06-21 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
US20200330624A1 (en) 2017-10-23 2020-10-22 The Johns Hopkins University Imaging and radiotherapeutics agents targeting fibroblast-activation protein-alpha (fap-alpha)
JP2021506972A (ja) 2017-12-15 2021-02-22 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
WO2019154859A1 (en) 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
IL276594B2 (en) 2018-02-06 2023-11-01 Univ Heidelberg FAP inhibitors

Also Published As

Publication number Publication date
CA3207999A1 (en) 2022-08-18
JP2024506644A (ja) 2024-02-14
KR20230145162A (ko) 2023-10-17
WO2022171811A1 (en) 2022-08-18
AU2022219525A1 (en) 2023-09-21
EP4291554A1 (en) 2023-12-20
US20240148916A1 (en) 2024-05-09
IL304960A (en) 2023-10-01

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