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    • 4. 发明申请
    • NEW CO CRYSTALS USEFUL IN THE PREPARATION OF PHARMACEUTICAL COMPOSITIONS
    • 新的CO晶体可用于制备药物组合物
    • WO2013054146A1
    • 2013-04-18
    • PCT/HU2012/000101
    • 2012-10-09
    • EGIS GYÓGYSZERGYÁR NYILVÁNOSAN MÜKÖDÖ RÉSZVÉNYTÁRSASÁG
    • SIPOS, ÉvaKOVÁNYINÉ LAX, GyörgyiVOLK, BalázsBARKÓCZY, JózsefMEZÖVÁRI, MónikaVARGA, ZoltánDANCSÓ, András
    • A61K31/5377C07D413/14A61P7/02
    • C07D413/14
    • The invention relates to the new co crystals of 5-chloro-N-///5S/-2-oxo-3-/4-/3- oxo-moφholine-4-yl/-phenyl/-l,3-oxazolidine-5-yl/-methyl/-thiophen-2- carboxamide having the INN rivaroxaban formed with oxalic acid and gamma- cyclodextrine. The invention also relates to a process for the preparation of the co crystal of rivaroxaban and oxalic acid of the Formula 2. According to said process amorphous or crystalline rovaroxaban or a hydrate, solvate or co crystal of rivaroxaban is dissolved in an organic solvent, water or a mixture of an organic solvent and water, to the solution oxalic acid is added and the solvent is removed. According to the invention there is also provided a process for the preparation of the co crystal of rivaroxaban and gamma-cyclodextrin of the Formula 3 /wherein n is 0.9-1.1, preferably n=l/. According to said process amorphous or crystalline rivaroxaban or a hydrate, solvate or co crystal of rivaroxaban is dissolved in an organic solvent, water or a mixture of an organic solvent and water, to the solution gamma-cyclodextrine is added and the solvent is removed.
    • 本发明涉及5-氯-N-// / 5S / -2-氧代-3- / 4- / 3-氧代 - 吗啉-4-基/苯基/ -1,3-恶唑烷的新共晶体 -5-基 - 甲基 - 噻吩-2-甲酰胺,其用草酸和γ-环糊精形成INN利伐沙班。 本发明还涉及制备式2的利伐沙班和草酸的共晶的方法。根据所述方法,将无定形或结晶的罗伐卡班或水合物,利伐沙班的溶剂合物或共晶溶于有机溶剂,水 或有机溶剂和水的混合物加入到溶液中,并除去溶剂。 根据本发明,还提供了制备式3的rivaroaxaban和γ-环糊精的共晶的方法,其中n为0.9-1.1,优选n = 1 /。 根据所述方法,加入无定形或结晶的利伐沙班或利伐沙班的水合物,溶剂合物或共晶体溶解在有机溶剂中,将水或有机溶剂和水的混合物加入到γ-环糊精溶液中并除去溶剂。