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    Ethanolate of azithromycin, process for manufacture, and pharmaceutical compositions thereof
    3.
    发明授权
    Ethanolate of azithromycin, process for manufacture, and pharmaceutical compositions thereof 有权
    阿奇霉素的乙醇酸酯，制造方法及其药物组合物

    公开(公告)号：US06365574B2

    公开(公告)日：2002-04-02

    申请号：US09451738

    申请日：1999-11-30

    申请人： Claude Singer ,  Judith Aronhime

    发明人： Claude Singer ,  Judith Aronhime

    IPC分类号： A61K3170

    CPC分类号： C07H17/08 ,  C07H1/00 ,  C07H17/00

    摘要： A novel, non-hygroscopic form of azithromycin is disclosed, as well as a method for preparing it by the gradual crystallization of azithromycin from ethanol by the addition of a minimal amount of water to effect crystal formation. Pharmaceutical compositions containing this novel form of azithromycin are also disclosed.

    摘要翻译： 公开了一种新型的非吸湿形式的阿奇霉素，以及通过加入最少量的水以使阿奇霉素从乙醇中逐渐结晶以制备晶体形成的方法。 还公开了含有这种新型形式的阿奇霉素的药物组合物。

    Methods for preparation of sertraline hydrochloride polymorphs
    5.
    发明授权
    Methods for preparation of sertraline hydrochloride polymorphs 有权
    盐酸舍曲林多晶型物的制备方法

    公开(公告)号：US06600073B1

    公开(公告)日：2003-07-29

    申请号：US09586842

    申请日：2000-06-05

    申请人： Eduard Schwartz ,  Tamar Nidam ,  Anita Liberman ,  Marioara Mendelovici ,  Judith Aronhime ,  Claude Singer ,  Evgeni Valdman

    发明人： Eduard Schwartz ,  Tamar Nidam ,  Anita Liberman ,  Marioara Mendelovici ,  Judith Aronhime ,  Claude Singer ,  Evgeni Valdman

    IPC分类号： C07C21100

    CPC分类号： C07C209/84 ,  A61K31/135 ,  C07C211/42 ,  C07C2602/10

    摘要： Novel methods for the preparation of sertraline hydrochloride Forms III, V, VI, VII, VII, IX and X are disclosed. According to the present invention, sertraline hydrochloride Form III may be produced by heating sertraline hydrochloride Forms V and VI. Sertraline hydrochloride Forms V and VI may be produced from either sertraline hydrochloride or sertraline base by crystallization. Sertraline hydrochloride Form VII may be produced by suspending sertraline chloride polymorph V in water, followed by filtration. Sertraline hydrochloride Forms VIII and IX may be produced by suspending sertraline base in water followed by acidification and filtration. Sertraline hydrochloride Form X may be produced by suspending sertraline hydrochloride in benzyl alcohol with heating, followed by filtration.

    摘要翻译： 公开了制备盐酸舍曲林的新方法，形式III，V，VI，VII，VII，IX和X。 根据本发明，盐酸舍曲林盐酸盐形式III可以通过加热盐酸舍曲林形式V和VI来制备。 盐酸舍曲林形式V和VI可以通过结晶从舍曲林盐酸盐或舍曲林碱产生。 盐酸舍曲林形式VII可以通过将舍曲林氯化物多晶型V悬浮在水中，然后过滤来制备。 盐酸舍曲林形式VIII和IX可以通过将舍曲林碱悬浮在水中然后酸化和过滤来制备。 舍曲林盐酸盐形式X可以通过在加热下将舍曲林盐酸舍曲林悬浮在苄醇中，然后过滤来制备。

    Sertraline hydrochloride polymorphs
    6.
    发明申请
    Sertraline hydrochloride polymorphs 审中-公开
    舍曲林盐酸多晶型物

    公开(公告)号：US20080176949A1

    公开(公告)日：2008-07-24

    申请号：US12077993

    申请日：2008-03-21

    申请人： Eduard Schwartz ,  Tamar Nidam ,  Anita Liberman ,  Marioara Mendelovici ,  Judith Aronhime ,  Claude Singer ,  Evgeni Valdman

    发明人： Eduard Schwartz ,  Tamar Nidam ,  Anita Liberman ,  Marioara Mendelovici ,  Judith Aronhime ,  Claude Singer ,  Evgeni Valdman

    IPC分类号： A61K31/135 ,  A61P43/00 ,  C07C211/33

    CPC分类号： C07C209/84 ,  A61K31/135 ,  C07C211/42 ,  C07C2602/10

    摘要： The present invention is directed to forms II, III, V, VI, VII, VIII, IX and X of sertraline hydrochloride and novel methods for their preparation. According to the present invention, sertraline hydrochloride polymorph II may be produced by slurrying sertraline hydrochloride polymorph VI in aprotic organic solvent. Sertraline hydrochloride polymorphic form III may be produced by heating sertraline hydrochloride polymorphs V and VI. Sertraline hydrochloride forms V and VI may be produced from either sertraline hydrochloride or sertraline base by crystallization. Sertraline hydrochloride Form VII may be produced by suspending sertraline chloride polymorph V in water, followed by filtration. Sertraline hydrochloride Forms VIII and IX may be produced by suspending sertraline base in water followed by acidification and filtration. Sertraline hydrochloride Form X may be produced by suspending sertraline hydrochloride in benzyl alcohol with heating, followed by filtration.

    摘要翻译： 本发明涉及舍曲林盐酸盐的形式II，III，V，VI，VII，VIII，IX和X及其制备方法。 根据本发明，盐酸舍曲林多晶型II可以通过将盐酸舍曲林多晶型VI制成非质子有机溶剂来制备。 舍曲林盐酸盐多晶型III可以通过加热舍曲林盐酸盐多晶型物V和VI来制备。 舍曲林盐酸盐形成V和VI可以通过结晶从舍曲林盐酸盐或舍曲林碱产生。 盐酸舍曲林形式VII可以通过将舍曲林氯化物多晶型V悬浮在水中，然后过滤来制备。 盐酸舍曲林形式VIII和IX可以通过将舍曲林碱悬浮在水中然后酸化和过滤来制备。 舍曲林盐酸盐形式X可以通过在加热下将舍曲林盐酸舍曲林悬浮在苄醇中，然后过滤来制备。

    Preparation method of azithromycin hydrates
    8.
    发明授权
    Preparation method of azithromycin hydrates 失效
    阿奇霉素水合物的制备方法

    公开(公告)号：US06586576B2

    公开(公告)日：2003-07-01

    申请号：US09755829

    申请日：2001-01-04

    申请人： Judith Aronhime ,  Claude Singer ,  Michael Pesachovich

    发明人： Judith Aronhime ,  Claude Singer ,  Michael Pesachovich

    IPC分类号： C07H1708

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： This invention relates to a method for preparing azithromycin dihydrate from crude azithromycin by the gradual crystallization of azithromycin from acetone by the addition of a minimal amount of water to effect crystal formation is disclosed. This invention also relates to a method of making azithromycin from desmethyl-azithromycin by dissolving desmethyl-azithromycin in acetone, adding activated carbon, adding formaldehyde, adding formic acid; refluxing the desmethyl-azithromycin acetone solution, adding sodium hydroxide to induce precipitation of azithromycin, and isolating azithromycin.

    摘要翻译： 本发明涉及从阿奇霉素制备阿奇霉素二水合物的方法，其通过加入最少量的水来实现晶体形成，由阿奇霉素从丙酮中逐渐结晶。 本发明还涉及通过将去甲基 - 阿奇霉素溶解在丙酮中，加入活性炭，加入甲醛，加入甲酸，由去甲基 - 阿奇霉素制备阿奇霉素的方法。 回流脱甲基阿奇霉素丙酮溶液，加入氢氧化钠诱导阿奇霉素沉淀，分离阿奇霉素。

    Processes for preparing crystalline and amorphous mupirocin calcium
    9.
    发明授权
    Processes for preparing crystalline and amorphous mupirocin calcium 失效
    制备结晶和无定形莫匹罗星钙的方法

    公开(公告)号：US07737177B2

    公开(公告)日：2010-06-15

    申请号：US10289919

    申请日：2002-11-06

    申请人： Lorant Gyuricza ,  Erszebet Meszaros-Sos ,  Csaba Szabo ,  Claude Singer

    发明人： Lorant Gyuricza ,  Erszebet Meszaros-Sos ,  Csaba Szabo ,  Claude Singer

    IPC分类号： A61K31/335

    CPC分类号： C07D407/06

    摘要： Processes are provided for preparing mupirocin calcium dihydrate from pseudomonic acid in a two phase system by using an organic carboxylate. A highly pure composition of amorphous mupirocin calcium is provided, and processes for its preparation by solvent removal, lyophilization and precipitation with use of an anti-solvent. Pharmaceutical compositions of amorphous form, and methods of using them to treat infections are also provided. Also provided are combined processes for preparing mupirocin calcium dihydrate and amorphous, by producing amorphous form first, followed by conversion of amorphous form into the dihydrate through crystallization from an aqueous solution. Also provided are processes for removing the water of crystallization of the dihydrate to obtain mupirocin calcium anhydrate.

    摘要翻译： 提供了通过使用有机羧酸盐在两相体系中由假单胞菌酸制备莫匹罗星二水合钙的方法。 提供了一种高纯度非晶莫匹罗星钙组合物，以及通过溶剂去除，冻干和使用抗溶剂沉淀制备的方法。 还提供了无定形形式的药物组合物，以及使用它们治疗感染的方法。 还提供了通过首先产生无定形形式，然后通过从水溶液中结晶将无定形形式转化为二水合物，制备莫匹罗星二水合物和无定形物的组合方法。 还提供了去除二水合物结晶水以获得莫匹罗星钙无水物的方法。