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KINASE INHIBITOR POLYMORPHES
专利权人:
ЭлЭлСи (US);ИНТЕЛЛАЙКИН
发明人:
ЖЭНЬ Пинда (US),МАРТИН Майкл (US)
申请号:
RU2014109023/04
公开号:
RU2014109023A
申请日:
2012.08.10
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. A method of obtaining a polymorphic Form C of the compound of Formula I, wherein said method comprises (i) exposing the composition containing one or more polymorphs other than Form C of the compound of Formula I to a solvent system for a period of time sufficient to convert at least about 50% from the total number of polymorphs other than Form C to Form C of the compound of Formula I; and (ii) isolation of said polymorphic Form C.2. The method according to claim 1. characterized in that said solvent system contains water. 3. The method according to claim 1, characterized in that said solvent system contains THF or dioxane. The method according to claim 1, characterized in that said solvent system comprises a double crystallization system containing an organic solvent and liquid water. The method according to claim 4, characterized in that said liquid water is present in an amount selected from about 1%, about 5%, about 10%, about 15%, about 20%, about 25%, about 30%, about 35% approximately 40%, approximately 45%, approximately 50%, approximately 55%, approximately 60%, approximately 65%, approximately 70%, approximately 75%, approximately 80%, approximately 85%, approximately 90%, approximately 95 and 100% on the volume of the solvent system. 6. The method according to claim 4, characterized in that said liquid water is present in an amount of from about 85 to about 95% by volume of the solvent system. The method according to claim 1, characterized in that said one or more polymorphs other than Form C are selected from the group consisting of Form A, Form B, Form D, Form E, Form F, amorphous φ1. Способ получения полиморфной Формы C соединения Формулы Iпричем указанный способ включает(i) подвергание композиции, содержащей один или более полиморфов, отличных от Формы C соединения Формулы I, воздействию системы растворителей в течение периода времени, достаточного для превращения по меньшей мере приблизительно 50% от общего количества полиморфов, отличных от Формы
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