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    Polymorphs of darunavir
    1.
    发明授权
    Polymorphs of darunavir 有权
    地瑞那韦的多晶型物

    公开(公告)号：US09580440B2

    公开(公告)日：2017-02-28

    申请号：US14047243

    申请日：2013-10-07

    Applicant: Hetero Research Foundation

    Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Rapolu Raji Reddy ,  Kesireddy Subash Chander Reddy ,  Bandi Vamsi Krishna

    IPC: A01N43/08 ,  A61K31/34 ,  C07D493/00 ,  C07D493/04 ,  A61K9/20

    CPC classification number: C07D493/04 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/34

    Abstract: The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.

    Abstract translation: 本发明提供了地瑞那韦的新型溶剂化形式及其制备方法。 本发明还提供了制备地瑞那韦非晶形式的新方法和包含它的药物组合物。 因此，例如，将地瑞那韦2-甲基-2-丁醇溶剂合物溶解在二氯甲烷中，在45℃下真空蒸馏，得到残留物，将环己烷加入残留物中，在20〜25℃下搅拌30小时 将分离出的固体过滤，用环己烷洗涤，在50℃下真空干燥12小时，得到地瑞那韦非晶形式。

    POLYMORPHS OF DARUNAVIR
    3.
    发明申请
    POLYMORPHS OF DARUNAVIR 有权
    DARUNAVIR的POLYMORPHS

    公开(公告)号：US20140200356A1

    公开(公告)日：2014-07-17

    申请号：US14047243

    申请日：2013-10-07

    Applicant: Hetero Research Foundation

    Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Rapolu Raji Reddy ,  Kesireddy Subash Chander Reddy ,  Bandi Vamsi Krishna

    IPC: C07D493/04

    CPC classification number: C07D493/04 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/34

    Abstract: The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.

    Abstract translation: 本发明提供了地瑞那韦的新型溶剂化形式及其制备方法。 本发明还提供了制备地瑞那韦非晶形式的新方法和包含它的药物组合物。 因此，例如，将地瑞那韦2-甲基-2-丁醇溶剂合物溶解在二氯甲烷中，在45℃下真空蒸馏，得到残留物，将环己烷加入残留物中，在20〜25℃下搅拌30小时 将分离出的固体过滤，用环己烷洗涤，在50℃下真空干燥12小时，得到地瑞那韦非晶形式。

    ELVITEGRAVIR SOLID DISPERSION
    7.
    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

    Applicant: HETERO RESEARCH FOUNDATION

    Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy ,  Bandi Vamsi Krishna

    IPC: A61K31/47 ,  A61K9/14

    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。

    NOVEL POLYMORPHS OF FOSAMPRENAVIR CALCIUM
    8.
    发明申请
    NOVEL POLYMORPHS OF FOSAMPRENAVIR CALCIUM 审中-公开
    FOSAMPRENAVIR钙的新型聚合物

    公开(公告)号：US20150025040A1

    公开(公告)日：2015-01-22

    申请号：US14125386

    申请日：2012-05-21

    Applicant: HETERO RESEARCH FOUNDATION

    Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy ,  Bandi Vamsi Krishna

    IPC: C07F9/655

    CPC classification number: C07F9/65515 ,  C07B2200/13

    Abstract: Crystalline Forms of fosamprenavir calcium are disclosed, processes for its preparation and pharmaceutical compositions therefrom. The process for the preparation of fosamprenavir calcium crystalline Form H1, comprises: a) suspending fosamprenavir calcium in a nitrile solvent; b) heating the suspension obtained in step (a) at reflux; c) optionally adding a solvent to the reaction mass obtained in step (b); d) cooling the reaction mass at below 35 degrees Centigrade; and e) isolating fosamprenavir calcium crystalline Form H1. Another process for the preparation of substantially pure amorphous fosamprenavir calcium, which comprises: a) dissolving fosamprenavir calcium in an ester solvent; b) a portion of solvent from the solution obtained in step (a) until at least separation of fosamprenavir calcium as solid occurs; and c) isolating substantially pure amorphous fosamprenavir calcium. The pharmaceutical composition may comprse substantially pure amorphous fosamprenavir calcium and pharmaceutically acceptable excipients.

    Abstract translation: 披露了福沙那韦钙的结晶形式，其制备方法及其药物组合物。 制备福沙那韦钙晶体形式H1的方法包括：a）将福沙那韦钙悬浮在腈溶剂中; b）将在步骤（a）中获得的悬浮液加热回流; c）任选地向步骤（b）中获得的反应物料中加入溶剂; d）将反应物料冷却至35摄氏度以下; 和e）分离福桑那韦钙晶体形式H1。 制备基本上纯的无定形福桑那韦钙的另一种方法，其包括：a）将福沙那韦钙溶于酯溶剂中; b）将来自步骤（a）中获得的溶液的一部分溶剂直至至少分离作为固体的福沙那韦钙; 和c）分离基本上纯的无定形福桑那韦。 药物组合物可以包括基本上纯的无定形福桑那韦钙和药学上可接受的赋形剂。

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