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    POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3-YL) BUTYL] PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE AND PROCESS FOR PREPARING THEREOF
    1.
    发明申请
    POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3-YL) BUTYL] PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE AND PROCESS FOR PREPARING THEREOF 审中-公开
    5-（4- [4-（5-氰基-1H-吲哚-3-基）丁基]哌嗪-1-基）苯并呋喃-2-羧酰胺的多晶型及其制备方法

    公开(公告)号：US20140179713A1

    公开(公告)日：2014-06-26

    申请号：US14071930

    申请日：2013-11-05

    申请人： CADILA HEALTHCARE LIMITED

    发明人： Shriprakash Dhar DWIVEDI ,  Ramesh Chandra Singh ,  Sachin Ashokrao Patil

    IPC分类号： C07D405/12

    CPC分类号： C07D405/12

    摘要： The present invention provides a solid state Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide. The present invention also provides a process for preparing Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide comprising the steps of i) reacting solid state form of 5-(1-piperazinyl)benzofuran-2-carboxamide or its salts with 3-(4-chlorobutyl)-1H-indole-5-carbonitrile an organic solvent in presence of a base to obtain crude vilazodone free base; ii) purifying the crude vilazodone free base of step (i) in an organic solvent; iii) treating the purified vilazodone free base of step (ii) with an organic solvent to obtain solid state form-Z of vilazodone. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of an amorphous form of vilazodone hydrochloride and use of solid state Form-Z of vilazodone for the treatment of major depressive disorders.

    摘要翻译： 本发明提供5-（4- [4-（5-氰基-1H-吲哚-3-基）丁基]哌嗪-1-基）苯并呋喃-2-甲酰胺的固体形式Z。 本发明还提供了制备5-（4- [4-（5-氰基-1H-吲哚-3-基）丁基]哌嗪-1-基）苯并呋喃-2-甲酰胺的形式Z的方法，包括步骤 的i）使固体形式的5-（1-哌嗪基）苯并呋喃-2-甲酰胺或其盐与3-（4-氯丁基）-1H-吲哚-5-甲腈在有机溶剂的存在下反应，得到粗品 维拉佐酮游离碱 ii）在有机溶剂中纯化步骤（i）的游离原始维拉唑酮碱; iii）用有机溶剂处理纯化的步骤（ⅱ）维拉唑酮碱，得到维拉唑酮固体形式-Z。 本发明还提供了一种药物组合物，其包含治疗有效量的无定形形式的盐酸维拉唑酮，并且使用维拉唑酮的固态形式Z用于治疗重度抑郁症。