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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Canada
Prior art keywords
oeg
compound
lys
cleavable linker
cleavable
Prior art date
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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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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • 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
    • A61K51/0474Organic 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
    • A61K51/0482Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/26Glucagons
    • 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
    • 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
    • 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
    • A61K51/0402Organic compounds carboxylic acid carriers, fatty acids
    • 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
    • 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
    • A61K51/06Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
    • 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
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • C07D257/00Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other 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
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • 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
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/081Peptides, 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (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 (10)

Country Link
US (2) US12214059B2 (https=)
EP (1) EP4436979A1 (https=)
JP (1) JP2024542592A (https=)
KR (1) KR20240121775A (https=)
CN (1) CN118451091A (https=)
AU (1) AU2022397307A1 (https=)
CA (1) CA3238734A1 (https=)
CL (1) CL2024001560A1 (https=)
MX (1) MX2024005950A (https=)
WO (1) WO2023097038A1 (https=)

Families Citing this family (9)

* 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
AU2022397307A1 (en) 2021-11-26 2024-06-06 Full-Life Technologies Uk Limited Cleavable radioligands for targeting cell surface receptors and uses thereof
WO2024126687A1 (en) * 2022-12-16 2024-06-20 Silence Therapeutics Gmbh Nucleic acids conjugated to an albumin binding moiety
CN121219017A (zh) * 2023-05-31 2025-12-26 辐联科技香港有限公司 缀合物及其用途
AU2024282578A1 (en) * 2023-05-31 2025-12-04 Full-Life Technologies Uk Limited Radioligands for targeting cell surface receptors and uses thereof
TW202540073A (zh) * 2023-11-30 2025-10-16 大陸商輻聯科技香港有限公司 靶向sstr受體的放射性化合物及其用途
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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2721183C (en) * 2008-04-11 2019-07-16 Alnylam Pharmaceuticals, Inc. Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components
EP3609541A4 (en) * 2017-04-05 2021-04-07 Cornell University Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies
CA3060143A1 (en) * 2017-05-24 2018-11-29 Itm Isotopen Technologien Munchen Ag Novel psma-binding agents and uses thereof
AU2022397307A1 (en) 2021-11-26 2024-06-06 Full-Life Technologies Uk Limited Cleavable radioligands for targeting cell surface receptors and uses thereof

Also Published As

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

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