RU2012116880A - Обработка нерастворимых в воде наночастиц гидрофильными конъюгатами альфа-гидроксифосфоновой кислоты, модифицированные таким образом наночастицы и их применение в качестве контрастных агентов - Google Patents

Обработка нерастворимых в воде наночастиц гидрофильными конъюгатами альфа-гидроксифосфоновой кислоты, модифицированные таким образом наночастицы и их применение в качестве контрастных агентов Download PDF

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RU2012116880A
RU2012116880A RU2012116880/15A RU2012116880A RU2012116880A RU 2012116880 A RU2012116880 A RU 2012116880A RU 2012116880/15 A RU2012116880/15 A RU 2012116880/15A RU 2012116880 A RU2012116880 A RU 2012116880A RU 2012116880 A RU2012116880 A RU 2012116880A
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alpha
ethylene oxide
nanoparticle
hydroxyphosphonate
nanoparticles
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Брайан К. БЭЙЛС
Брюс Алан ХЭЙ
Бинил Айтти Айпе КАНДАПАЛЛИЛ
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Дженерал Электрик Компани
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Abstract

1. Композиция, содержащая:нерастворимую в воде наночастицу, к которой присоединена по меньшей мере одна альфа-гидроксифосфонатная группировка, имеющая формулу:где S представляет собой спейсер, L представляет собой связь между S и R, R представляет собой полимерную гидрофильную группировку, m и p равны 1-5, и n и o равны 0-5.2. Композиция по п.1, где R представляет собой полимерную гидрофильную группировку на основе этиленоксидных единиц.3. Композиция по п.1 или 2, где полимерные гидрофильные группировки основаны на этиленоксиде, и где поли(этиленоксид) имеет молекулярную массу, равную или меньше 5000 Да.4. Композиция по п.1, где наночастица представляет собой суперпарамагнитную наночастицу на основе оксида железа.5. Композиция по п.1, дополнительно содержащая фармацевтически приемлемый носитель или эксципиент.6. Композиция по п.5 для применения в качестве контрастного агента МРВ (магнитно-резонансная визуализация), подходящего для инъецирования субъекту-человеку.7. Способ использования нерастворимых в воде наночастиц, к которым присоединены альфа-гидроксифосфонатные группировки, в диагностической визуализации, включающийа) введение указанных наночастиц субъекту; иб) подвергание указанного субъекта диагностической визуализации, при которой указанные наночастицы действуют в качестве контрастного агента.8. Способ по п.7, где альфа-гидроксифосфонатные группировки имеют формулу:где S представляет собой спейсер, L представляет собой связь между S и R, R представляет собой полимерную гидрофильную группировку, m и p равны 1-5, и n и o равны 0-5.9. Способ по п.8, где R представляет собой полимерную гидрофильную группировку на основе этиленок�

Claims (15)

1. Композиция, содержащая:
нерастворимую в воде наночастицу, к которой присоединена по меньшей мере одна альфа-гидроксифосфонатная группировка, имеющая формулу:
Figure 00000001
где S представляет собой спейсер, L представляет собой связь между S и R, R представляет собой полимерную гидрофильную группировку, m и p равны 1-5, и n и o равны 0-5.
2. Композиция по п.1, где R представляет собой полимерную гидрофильную группировку на основе этиленоксидных единиц.
3. Композиция по п.1 или 2, где полимерные гидрофильные группировки основаны на этиленоксиде, и где поли(этиленоксид) имеет молекулярную массу, равную или меньше 5000 Да.
4. Композиция по п.1, где наночастица представляет собой суперпарамагнитную наночастицу на основе оксида железа.
5. Композиция по п.1, дополнительно содержащая фармацевтически приемлемый носитель или эксципиент.
6. Композиция по п.5 для применения в качестве контрастного агента МРВ (магнитно-резонансная визуализация), подходящего для инъецирования субъекту-человеку.
7. Способ использования нерастворимых в воде наночастиц, к которым присоединены альфа-гидроксифосфонатные группировки, в диагностической визуализации, включающий
а) введение указанных наночастиц субъекту; и
б) подвергание указанного субъекта диагностической визуализации, при которой указанные наночастицы действуют в качестве контрастного агента.
8. Способ по п.7, где альфа-гидроксифосфонатные группировки имеют формулу:
Figure 00000002
где S представляет собой спейсер, L представляет собой связь между S и R, R представляет собой полимерную гидрофильную группировку, m и p равны 1-5, и n и o равны 0-5.
9. Способ по п.8, где R представляет собой полимерную гидрофильную группировку на основе этиленоксидных единиц.
10. Способ по п.9, где полимерные гидрофильные группировки основаны на этиленоксиде, и где поли(этиленоксид) имеет молекулярную массу, равную или меньше 5000 Да.
11. Способ по любому из пп.7-10, где наночастица представляет собой суперпарамагнитную наночастицу на основе оксида железа.
12. Способ изготовления нерастворимых в воде наночастиц, к которым присоединены альфа-гидроксифосфонатные группировки, включающий:
а) получение суспензии наночастицы в суспензионном агенте; и
б) приведение указанной суспензии в контакт с указанными альфа-гидроксифосфонатными группировками.
13. Способ по п.12, где альфа-гидроксифосфонатные группировки имеют формулу:
Figure 00000003
где S представляет собой спейсер, L представляет собой связь между S и R, R представляет собой полимерную гидрофильную группировку, m и p равны 1-5, и n и o равны 0-5.
14. Способ по п.13, где R представляет собой гидрофильную группировку на основе этиленоксидных единиц.
15. Способ по п.14, где полимерные гидрофильные группировки основаны на этиленоксиде, и где поли(этиленоксид) имеет молекулярную массу, равную или меньше 5000 Да.
RU2012116880/15A 2009-10-30 2010-10-29 Обработка нерастворимых в воде наночастиц гидрофильными конъюгатами альфа-гидроксифосфоновой кислоты, модифицированные таким образом наночастицы и их применение в качестве контрастных агентов RU2012116880A (ru)

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PCT/EP2010/066429 WO2011051422A2 (en) 2009-10-30 2010-10-29 Treating water insoluble nanoparticles with hydrophilic alpha-hydroxyphosphonic acid conjugates, the so modified nanoparticles and their use as contrast agents

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US9827335B2 (en) 2017-11-28
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