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    Preparation method of azithromycin hydrates
    7.
    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。

    Preparation of gabapentin
    8.
    发明授权
    Preparation of gabapentin 失效
    加巴喷丁的制备

    公开(公告)号：US06255526B1

    公开(公告)日：2001-07-03

    申请号：US09331555

    申请日：1999-06-22

    申请人： Michael Pesachovich ,  Claude Singer ,  Gideon Pilarski

    发明人： Michael Pesachovich ,  Claude Singer ,  Gideon Pilarski

    IPC分类号： C07C6106

    CPC分类号： C07C227/42 ,  C07C229/28 ,  C07C2601/14

    摘要： There is disclosed a method of converting gabapenting hydrochloride substantially free of inorganic salts to gabapenting form II. The method comprises the steps of: (1) obtaining gabapentin hydrochloride that is substantially free of inorganic salts; (2) mixing a solution of the gabapenting hydrochloride with an additional amine in a first solvent so as to obtain a precipitate comprising gabapenting; and then (3) recovering gabapentin form II from the precipitate. The precipitated gabapentin is a novel polymorphic form of gabapentin possessing a crystalline structure characterized by novel sets of peaks in the powder X-ray diffraction pattern and in the FTIR spectra. This newly disclosed polymorph of gabapentin is characterized herein as gabapentin form III. The recovery step may comprise, for example, one of two alternative methods, slurrying the gabapentin form II in methanol, and then filtering the suspension to obtain gabapentin form II, or solubilizing the gabapentin form III in methanol with heating by reflux, and then cooling the solution to obtain gabapentin form II by crystallization.

    摘要翻译： 公开了一种将基本上不含无机盐的盐酸氢化盐转化为耙状II的方法。 该方法包括以下步骤：（1）获得基本上不含无机盐的盐酸加巴喷丁; （2）在第一溶剂中将加巴喷丁盐酸盐溶液与另外的胺混合，以获得包含加砂的沉淀物; 然后（3）从沉淀物中回收加巴喷丁II型。 沉淀的加巴喷丁是一种具有特征在于粉末X射线衍射图和FTIR光谱中新颖的峰组的加巴喷丁的新型多晶型物。 这种新公开的加巴喷丁多晶型物在本文中被表征为加巴喷丁形式III。 回收步骤可以包括例如两种替代方法之一，将加巴喷丁II型在甲醇中制浆，然后过滤悬浮液以获得形式II的加巴喷丁，或者通过回流加热将加巴喷丁形式III溶解在甲醇中，然后冷却 通过结晶获得形式II的加巴喷丁的溶液。

    Methods for preparation of sertraline hydrochloride polymorphs
    9.
    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
    10.
    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。