Кристаллическая β-модификация 3-(4-амино-1-оксо-1,3-дигидро-2Н-изоиндол-2-ил)-пиперидин-2,6-диона, способ её получения и фармацевтическая композиция на её основе
Mikhajlov Oleg Rostislavovich,Михайлов Олег Ростиславович,Uvarov Nikolaj Aleksandrovich,Уваров Николай Александрович,Malin Aleksandr Aleksandrovich,Малин Александр Александрович
申请号：
RU2016113305
公开号：
RU0002616976C1
申请日:
2016.04.07
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: pharmacology.SUBSTANCE: invention relates to a new crystalline modification of 3-(4-amino-1-oxo-1,3-dihydro-2H-isoindol-2-yl)-piperidine-2,6-dione (lenalidomide is an international non-proprietary name) - β-modification, characterized by the following set of interplanar distances (d, Å) and corresponding intensities (Irel., %): 12.358 - 8.39% 11.893 - 29.79% 11.551 - 100.00% 8.606 - 8.39% 7.641 - 4.62% 7.024 - 8.05% 5.927 - 8.05% 5.811 - 19.86% 5.262 - 28.42% 5.117 - 9.42% 4.850 - 5.99% 4.595 - 5.99% 4.215 - 10.45% 4.011 - 6.68% 3.948 - 11.47% 3.877 - 51.88% 3.843 - 39.73% 3.698 - 16.44% 3.426 - 6.51% 3.316 - 4.97% 3.201 - 5.14% 3.103 - 4.45% 3.025 - 3.42% 2.989 - 2.91% 2.905 - 9.93% 2.846 - 5.99% 2.826-5.65% 2.702 - 10.27% 2.640 - 7.88% 2.555 - 10.27% 2.478 - 7.19% 2.339 - 6.51% 2.647 - 23.12% 2.282 - 11.82% 2.243 - 9.93% 2.168 - 5.82% 2.107 - 9.08% 2.081 - 7.36% 2.066 - 10.96% 2.027 - 9.76% 1.943 - 5.65% 1.912 - 24.83% 1.795 - 4.45% 1.719 - 4.62% 1.694 - 5.72% 1.659 - 7.19% 1.634 - 3.94% and DSC curve with two thermal effects: exothermic effect at temperature (174.9±0.5)°C and endothermic effect at a temperature of (267.7±0.5)°C. As well as to a method for its preparation and use in the pharmaceutical industry and medicine as a representative of a new class of immunomodulators possessing both immunomodulatory and anti-angiogenic properties for multiple myeloma treatment.EFFECT: increased efficiency of composition application.4 cl, 4 tbl, 6 dwg, 4 exИзобретение касается новой кристаллической модификации 3-(4-амино-1-оксо-1,3-дигидро-2Н-изоиндол-2-ил)-пиперидин-2,6-диона (леналидомид - международное непатентованное название), названной β-модификацией, характеризующейся следующим набором межплоскостных расстояний (d, Å) и соответствующих им интенсивностей (Iотн., %): 12,358 - 8,39% 11,893 - 29,79% 11,551 - 100,00% 8,606 - 8,39% 7,641 - 4,62% 7,024 - 8,05% 5,927 - 8,05% 5,811 - 19,86% 5,262 - 28,42% 5,117 - 9,42% 4,850 - 5,99% 4,595 - 5,99% 4,215 - 10,45% 4,011
