PROCESS FOR PREPARING AMORPHOUS CABAZITAXEL
    3.
    发明申请
    PROCESS FOR PREPARING AMORPHOUS CABAZITAXEL 有权
    制备无定形卡宾的方法

    公开(公告)号:US20140336246A1

    公开(公告)日:2014-11-13

    申请号:US14349332

    申请日:2012-12-26

    IPC分类号: C07D305/14

    CPC分类号: C07D305/14 C07D413/12

    摘要: The present invention provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I), and process for preparation thereof.The present application also provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I) having an XRPD pattern as per FIG. 1, and IR spectrum as per FIG. 3 and is useful as an active pharmaceutical in a pharmaceutical composition comprising thereof and has anti-cancer activity.

    摘要翻译: 本发明提供一种非溶剂化无定形形式的(2α,5α,b,10α,17α)-4-乙酸基 - 13 - ({(2R,3S)-3 [(叔丁氧基羰基)氨基] -2-羟基-3-苯基丙酰基}氧基)-1-羟基-7,10-二甲氧基-9-氧代-5,20-环氧基十二烷-1-烯-2-基苯甲酸酯或卡巴他赛(I),以及制备方法 其中。 本申请还提供非溶剂化无定形形式的(2α,5β,7α,b,10α,13α)-4-乙酸基 - 13 - ({(2R,3S)-3 [(叔丁氧基羰基)氨基 ] -2-羟基-3-苯基丙酰基}氧基)-1-羟基-7,10-二甲氧基-9-氧代-5,20-环氧塔塔-1-烯-2-基苯甲酸酯或具有XRPD图案的卡巴他赛(I) 根据图 1和IR光谱如图1所示。 并且可用作其包含其的药物组合物中的活性药物并具有抗癌活性。

    Echothiophate iodide process
    4.
    发明授权

    公开(公告)号:US09708352B2

    公开(公告)日:2017-07-18

    申请号:US15108790

    申请日:2015-01-01

    IPC分类号: C07F9/202 C07F9/17

    摘要: The present invention relates to a process for preparation of Echothiophate Iodide (I). Echothiophate Iodide (I) obtained by the process of the present invention is obtained as new crystalline form designated as Form-SET. The process for preparation of Echothiophate Iodide (I) according to present invention is an ecofriendly process that avoids the use of hazardous solvent systems and provides Echothiophate Iodide (I) of high purity. Pharmaceutical composition of the said crystalline Form-SET of Echothiophate Iodide (I) of high purity is useful in the treatment of ocular disorders like Glaucoma.