RU2019105539A - Композиция, содержащая буфер - Google Patents

Композиция, содержащая буфер Download PDF

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RU2019105539A
RU2019105539A RU2019105539A RU2019105539A RU2019105539A RU 2019105539 A RU2019105539 A RU 2019105539A RU 2019105539 A RU2019105539 A RU 2019105539A RU 2019105539 A RU2019105539 A RU 2019105539A RU 2019105539 A RU2019105539 A RU 2019105539A
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targeting agent
acid
radioactive metal
chelated
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RU2757768C2 (ru
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Юити ФУНАСЕ
Масахиро КУРОКАВА
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ФУДЖИФИЛМ Тояма Кемикал Ко., Лтд.
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K51/0478Organic 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 complexes from non-cyclic ligands, e.g. EDTA, MAG3
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    • 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
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    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies 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
    • A61K51/1027Antibodies 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 receptors, cell-surface antigens or cell-surface determinants
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    • A61K51/04Organic compounds
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    • A61K51/1045Antibodies 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
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    • A61K51/1096Antibodies 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 conjugates with carriers being antibodies radioimmunotoxins, i.e. conjugates being structurally as defined in A61K51/1093, and including a radioactive nucleus for use in radiotherapeutic applications
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    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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Claims (23)

1. Композиция, включающая:
(a) хелатированный нацеливающий агент, который является конъюгатом хелатной группы и нацеливающей группы; и
(b) по меньшей мере один вид буфера, выбранного из группы, состоящей из бензойной кислоты, малеиновой кислоты, фумаровой кислоты, янтарной кислоты и их солей,
причем композиция используется для формирования комплекса между радиоактивным металлом, выбранным из группы, состоящей из 90Y, 153Sm, 165Dy, 165Er, 166Ho и 177Lu, и хелатированным нацеливающим агентом.
2. Композиция по п.1, в которой радиоактивный металл выбран из группы, состоящей из 90Y и 177Lu.
3. Композиция по п.1, в которой хелатная группа включает хелатную группу, имеющую структуру DOTA, структуру DTPA или структуру NETA.
4. Композиция по п.1, в которой хелатная группа выбрана из группы, состоящей из следующих хелатных групп:
Figure 00000001
.
5. Композиция по п.1, в которой нацеливающая группа выбрана из группы, состоящей из низкомолекулярного соединения, пептида, белка, антитела, фрагмента антитела и нуклеиновой кислоты.
6. Композиция по п.1, в которой хелатированный нацеливающий агент и буфер хранят в одном и том же сосуде.
7. Композиция по п.1, в которой буфер высушивают сублимацией.
8. Композиция по любому из пп. 1-7, дополнительно включающая радиоактивный металл, выбранный из группы, состоящей из 90Y, 153Sm, 165Dy, 165Er, 166Ho и 177Lu,
причем радиоактивный металл и хелатированный нацеливающий агент размещают в состоянии, в котором радиоактивный металл и хелатированный нацеливающий агент не могут контактировать друг с другом.
9. Способ получения меченного радиоактивным металлом хелатированного нацеливающего агента, включающий:
смешивание радиоактивного металла, выбранного из группы, состоящей из 90Y, 153Sm, 165Dy, 165Er, 166Ho и 177Lu, и хелатированного нацеливающего агента в присутствии по меньшей мере одного вида буфера, выбранного из группы, состоящей из бензойной кислоты, малеиновой кислоты, фумаровой кислоты, янтарной кислоты и их солей, с формированием комплекса между радиоактивным металлом и хелатированным нацеливающим агентом.
10. Лекарственное средство для диагностики или лечения заболевания, включающее комбинацию: (A) радиоактивного металла, выбранного из группы, состоящей из 90Y, 153Sm, 165Dy, 165Er, 166Ho и 177Lu; (B) хелатированного нацеливающего агента; и (C) по меньшей мере одного вида буфера, выбранного из группы, состоящей из бензойной кислоты, малеиновой кислоты, фумаровой кислоты, янтарной кислоты и их солей,
причем заболевание является мишенью хелатированного нацеливающего агента.
11. Применение комбинации: (A) радиоактивного металла, выбранного из группы, состоящей из 90Y, 153Sm, 165Dy, 165Er, 166Ho и 177Lu; (B) хелатированного нацеливающего агента; и (C) по меньшей мере одного вида буфера, выбранного из группы, состоящей из бензойной кислоты, малеиновой кислоты, фумаровой кислоты, янтарной кислоты и их солей, для получения лекарственного средства для диагностики или лечения заболевания,
причем заболевание является мишенью хелатированного нацеливающего агента.
12. Комбинация: (A) радиоактивного металла, выбранного из группы, состоящей из 90Y, 153Sm, 165Dy, 165Er, 166Ho и 177Lu; (B) хелатированного нацеливающего агента; и (C) по меньшей мере одного вида буфера, выбранного из группы, состоящей из бензойной кислоты, малеиновой кислоты, фумаровой кислоты, янтарной кислоты и их солей, для диагностики или лечения заболевания,
причем заболевание является мишенью хелатированного нацеливающего агента.
13. Способ диагностики или лечения заболевания, включающий введение комбинации: (A) радиоактивного металла, выбранного из группы, состоящей из 90Y, 153Sm, 165Dy, 165Er, 166Ho и 177Lu; (B) хелатированного нацеливающего агента; и (C) по меньшей мере одного вида буфера, выбранного из группы, состоящей из бензойной кислоты, малеиновой кислоты, фумаровой кислоты, янтарной кислоты и их солей,
причем заболевание является мишенью хелатированного нацеливающего агента.
RU2019105539A 2016-08-19 2017-08-21 Композиция, содержащая буфер RU2757768C2 (ru)

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WO2018034354A1 (ja) 2018-02-22

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