CA3238734A1 - Cleavable radioligands for targeting cell surface receptors and uses thereof - Google Patents

Cleavable radioligands for targeting cell surface receptors and uses thereof Download PDF

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Publication number
CA3238734A1
CA3238734A1 CA3238734A CA3238734A CA3238734A1 CA 3238734 A1 CA3238734 A1 CA 3238734A1 CA 3238734 A CA3238734 A CA 3238734A CA 3238734 A CA3238734 A CA 3238734A CA 3238734 A1 CA3238734 A1 CA 3238734A1
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CA
Canada
Prior art keywords
oeg
compound
lys
cleavable linker
cleavable
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3238734A
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English (en)
French (fr)
Inventor
Fa Liu
Alla Darwish
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Full Life Technologies Hk Ltd
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Full Life Technologies Hk Ltd
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Filing date
Publication date
Application filed by Full Life Technologies Hk Ltd filed Critical Full Life Technologies Hk Ltd
Publication of CA3238734A1 publication Critical patent/CA3238734A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • 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
    • 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
    • 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
    • A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
    • 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
    • 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
    • A61K51/06—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
    • 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
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/081—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the protein being an albumin, e.g. human serum albumin [HSA], bovine serum albumin [BSA], ovalbumin

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (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)
CA3238734A 2021-11-26 2022-11-23 Cleavable radioligands for targeting cell surface receptors and uses thereof Pending CA3238734A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163283361P 2021-11-26 2021-11-26
US63/283,361 2021-11-26
PCT/US2022/050952 WO2023097038A1 (en) 2021-11-26 2022-11-23 Cleavable radioligands for targeting cell surface receptors and uses thereof

Publications (1)

Publication Number Publication Date
CA3238734A1 true CA3238734A1 (en) 2023-06-01

Family

ID=86540347

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3238734A Pending CA3238734A1 (en) 2021-11-26 2022-11-23 Cleavable radioligands for targeting cell surface receptors and uses thereof

Country Status (9)

Country Link
US (2) US12214059B2 (enExample)
EP (1) EP4436979A4 (enExample)
JP (1) JP2024542592A (enExample)
KR (1) KR20240121775A (enExample)
CN (1) CN118451091A (enExample)
CA (1) CA3238734A1 (enExample)
CL (1) CL2024001560A1 (enExample)
MX (1) MX2024005950A (enExample)
WO (1) WO2023097038A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018204872A2 (en) * 2017-05-05 2018-11-08 Fusion Pharmaceuticals Inc. Igf-1r monoclonal antibodies and uses thereof
EP4436979A4 (en) 2021-11-26 2026-06-10 Full Life Tech Uk Limited Cleftable radioligands for targeting cell surface receptors and their uses
WO2024126687A1 (en) * 2022-12-16 2024-06-20 Silence Therapeutics Gmbh Nucleic acids conjugated to an albumin binding moiety
EP4719486A1 (en) * 2023-05-31 2026-04-08 Full-Life Technologies UK Limited Conjugates and uses thereof
EP4719498A1 (en) * 2023-05-31 2026-04-08 Full-Life Technologies UK Limited Radioligands for targeting cell surface receptors and uses thereof
WO2025113628A1 (en) * 2023-11-30 2025-06-05 Full-Life Technologies Hk Limited Sstr receptor targeting radio compounds and uses thereof
CN118240015B (zh) * 2024-03-21 2025-03-21 中国科学院近代物理研究所 一种针对脑胶质瘤的靶向多肽及放射性示踪剂
WO2026002208A1 (zh) * 2024-06-28 2026-01-02 思路迪生物医药(上海)有限公司 前列腺特异性膜抗原小分子抑制剂及其放射性核素配合物的制备及应用
WO2026080432A1 (en) * 2024-10-07 2026-04-16 Beth Israel Deaconess Medical Center, Inc. Dimeric p-selectin inhibitors and uses thereof
CN121991166A (zh) * 2024-11-05 2026-05-08 成都纽瑞特医疗科技股份有限公司 放射性配体化合物及其用途
WO2026119233A1 (en) * 2024-12-04 2026-06-11 Full-Life Technologies Uk Limited Conjugates and uses thereof

Family Cites Families (23)

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US5021556A (en) 1987-07-22 1991-06-04 Neorx Corporation Method of radiolabeling chelating compounds comprising sulfur atoms with metal radionuclides
US5075099A (en) 1988-05-31 1991-12-24 Neorx Corporation Metal radionuclide chelating compounds for improved chelation kinetics
US5364613A (en) 1989-04-07 1994-11-15 Sieving Paul F Polychelants containing macrocyclic chelant moieties
US5367080A (en) 1990-11-08 1994-11-22 Sterling Winthrop Inc. Complexing agents and targeting radioactive immunoreagents useful in therapeutic and diagnostic imaging compositions and methods
US5886142A (en) 1997-05-20 1999-03-23 Thomas Jefferson University Radiolabeled thrombus imaging agents
US8575123B2 (en) * 2008-04-11 2013-11-05 Tekmira Pharmaceuticals Corporation Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components
EP4420730A3 (en) 2009-03-19 2024-11-13 The Johns Hopkins University Psma-targeting compounds and uses thereof
ES2743482T3 (es) * 2014-05-06 2020-02-19 Univ Johns Hopkins Inhibidores de PSMA marcados con metal/radiometal para obtención de imágenes dirigidas a PSMA y radioterapia
MX392700B (es) 2016-08-10 2025-03-11 Cancer Targeted Tech Llc Inhibidores de antígeno de la membrana específico para la próstata (psma) quelados.
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WO2019246311A1 (en) 2018-06-19 2019-12-26 Lumiphore, Inc. Macrocycle conjugates
ES3038393T3 (en) * 2018-08-09 2025-10-13 Hoffmann La Roche Cleavable linker for peptide synthesis
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JP7894086B2 (ja) 2020-05-06 2026-07-23 コーネル ユニヴァーシティー 銅含有セラグノスティック化合物及びその使用の方法
EP4436979A4 (en) 2021-11-26 2026-06-10 Full Life Tech Uk Limited Cleftable radioligands for targeting cell surface receptors and their uses

Also Published As

Publication number Publication date
CL2024001560A1 (es) 2025-03-28
CN118451091A (zh) 2024-08-06
US12214059B2 (en) 2025-02-04
EP4436979A1 (en) 2024-10-02
MX2024005950A (es) 2024-08-06
AU2022397307A1 (en) 2024-06-06
US20240382630A1 (en) 2024-11-21
JP2024542592A (ja) 2024-11-15
EP4436979A4 (en) 2026-06-10
KR20240121775A (ko) 2024-08-09
WO2023097038A1 (en) 2023-06-01
US20250099632A1 (en) 2025-03-27
US12673122B2 (en) 2026-07-07

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