CA2745495C - Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals - Google Patents
Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals Download PDFInfo
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- CA2745495C CA2745495C CA2745495A CA2745495A CA2745495C CA 2745495 C CA2745495 C CA 2745495C CA 2745495 A CA2745495 A CA 2745495A CA 2745495 A CA2745495 A CA 2745495A CA 2745495 C CA2745495 C CA 2745495C
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- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 title claims description 29
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- 239000003446 ligand Substances 0.000 claims abstract description 73
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- 238000000034 method Methods 0.000 claims abstract description 38
- -1 activated dicarbonyl compound Chemical class 0.000 claims description 67
- 229910052739 hydrogen Inorganic materials 0.000 claims description 35
- 229910021645 metal ion Inorganic materials 0.000 claims description 22
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 15
- 229910052736 halogen Inorganic materials 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 15
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims description 13
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 12
- 125000006850 spacer group Chemical group 0.000 claims description 12
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 9
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- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- BSYVTEYKTMYBMK-UHFFFAOYSA-N tetrahydrofurfuryl alcohol Chemical compound OCC1CCCO1 BSYVTEYKTMYBMK-UHFFFAOYSA-N 0.000 description 1
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- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
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- JBWKIWSBJXDJDT-UHFFFAOYSA-N triphenylmethyl chloride Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(Cl)C1=CC=CC=C1 JBWKIWSBJXDJDT-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D521/00—Heterocyclic compounds containing unspecified hetero rings
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- 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
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- A61K51/04—Organic compounds
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/082—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the peptide being a RGD-containing peptide
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61K49/00—Preparations for testing in vivo
- A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
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- A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
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- A61K49/101—Organic compounds the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals
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- 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
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- 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
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- 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
- A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K51/04—Organic compounds
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
- A61K51/1045—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody against animal or human tumor cells or tumor cell determinants
- A61K51/106—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody against animal or human tumor cells or tumor cell determinants the tumor cell being from kidney or bladder
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
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| AU2008906239A AU2008906239A0 (en) | 2008-12-02 | Radiopharmaceuticals | |
| PCT/AU2009/001572 WO2010063069A1 (en) | 2008-12-02 | 2009-12-02 | Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals |
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| US9422286B2 (en) | 2014-01-27 | 2016-08-23 | Washington University | Metal-binding bifunctional compounds as diagnostic agents for Alzheimer's disease |
| GB201417067D0 (en) | 2014-09-26 | 2014-11-12 | South African Nuclear Energy | Radiopharmaceutical conjugate |
| BR112019009172A2 (pt) * | 2016-11-04 | 2019-07-16 | Clarity Pharmaceuticals Pty Ltd | formulações para radioterapia e diagnóstico por imagem. |
| CA3066525A1 (en) * | 2017-06-06 | 2018-12-13 | The University Of Melbourne | Radiopharmaceuticals, radioimaging agents, and uses thereof |
| WO2019195890A1 (en) * | 2018-04-11 | 2019-10-17 | Clarity Pharmaceuticals Pty Ltd | Formulations and kits for radiotherapy and diagnostic imaging |
| CN120365276A (zh) * | 2018-04-11 | 2025-07-25 | 透明医药有限公司 | 靶向化合物及其生产方法 |
| US20220313600A1 (en) * | 2019-05-24 | 2022-10-06 | Clarity Pharmaceuticals Limited | Formulations of psma imaging agents |
| CN115175910A (zh) * | 2019-11-08 | 2022-10-11 | 昆士兰大学 | 放射性标记的靶向配体 |
| WO2021150258A1 (en) * | 2020-01-26 | 2021-07-29 | Mainline Biosciences Llc | Isotopically labelled selective cxcr4 binding peptide conjugate and methods for making and using the same |
| WO2021225760A1 (en) * | 2020-05-06 | 2021-11-11 | Cornell University | Copper-containing theragnostic compounds and methods of use |
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| PT90959B (pt) * | 1988-06-24 | 1995-05-04 | Dow Chemical Co | Processo para a preparacao de quelantes macrociclicos bifuncionais, de seus complexos e seus conjugados com anticorpos |
| US5245055A (en) * | 1990-12-18 | 1993-09-14 | E. R. Squibb & Sons, Inc. | Process for preparing a cis oxabicyclo olefinic acid and ester from an oxabicyclo pyranol |
| JPH04244085A (ja) | 1990-12-21 | 1992-09-01 | Doujin Kagaku Kenkyusho:Kk | 蛍光性化合物、錯体、試薬および該試薬を用いる特異的結合アッセイ |
| CN1152880A (zh) * | 1994-04-22 | 1997-06-25 | 孟山都公司 | 使用含氮大环配拉体的金属络合物的诊断图像分析的方法 |
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| AUPP803899A0 (en) * | 1999-01-05 | 1999-01-28 | Australian National University, The | Cryptate compounds and methods for diagnosis and therapy. |
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| GB0116815D0 (en) | 2001-07-10 | 2001-08-29 | Nycomed Amersham Plc | Improved chelator conjugates |
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| US9056129B2 (en) * | 2007-02-09 | 2015-06-16 | Northeastern University | Precision-guided nanoparticle systems for drug delivery |
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| US11905301B2 (en) | 2024-02-20 |
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| EP3098225B1 (en) | 2018-11-28 |
| JP2012510477A (ja) | 2012-05-10 |
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