PROCESS FOR CABAZITAXEL
    32.
    发明申请
    PROCESS FOR CABAZITAXEL 有权
    CABAZITAXEL的方法

    公开(公告)号:US20170029392A1

    公开(公告)日:2017-02-02

    申请号:US14968034

    申请日:2015-12-14

    CPC classification number: C07D305/14

    Abstract: The present invention provides an improved process for the preparation of 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β,13α-dihydroxy-7β,10β-dimethoxy-9-oxo-11-taxene (7β,10β-dimethoxy-10-deacetoxybaccatin III). The present invention also provides a novel process for the preparation of cabazitaxel.

    Abstract translation: 本发明提供了制备4α-乙酰氧基-2α-苯甲酰氧基-5β,20-环氧-1β,13α-二羟基-7β,10β-二甲氧基-9-氧代-11-紫杉醇(7β,10β-二甲氧基 -10-脱乙酰氧基浆果赤霉素III)。 本发明还提供了一种制备卡巴他赛的新方法。

    ELVITEGRAVIR SOLID DISPERSION
    35.
    发明申请
    ELVITEGRAVIR SOLID DISPERSION 审中-公开
    ELVITEGRAVIR固体分散体

    公开(公告)号:US20150141457A1

    公开(公告)日:2015-05-21

    申请号:US14402234

    申请日:2013-05-21

    CPC classification number: A61K31/47 A61K9/146

    Abstract: The present invention provides a novel amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In a preferred embodiment the process for the preparation of amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier comprises: preparing a solution comprising a mixture of elvitegravir and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol, span 20 or soluplus in a solvent; and removing the solvent from the solution obtained; adding hydrocarbon solvent to the residual solid; and isolating amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier.

    Abstract translation: 本发明提供了一种新颖的Elvitegravir的无定形固体分散体与药学上可接受的载体,其制备方法和包含它的药物组合物。 在优选的实施方案中,将Elvitegravir的无定形固体分散体与药学上可接受的载体组合的方法包括:制备包含选自共聚维酮,乙基纤维素,羟丙基甲基纤维素,聚乙烯的一种或多种药学上可接受的载体的混合物的溶液 乙二醇,20或溶剂中的溶剂; 并从所得溶液中除去溶剂; 向残余固体中加入烃溶剂; 并将Elvitegravir的无定形固体分散体与药学上可接受的载体组合。

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