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    Aztreonam β polymorph with very low residual solvent content
    41.
    发明授权
    Aztreonam β polymorph with very low residual solvent content 有权
    氨丁宁β多晶型物，残留溶剂含量非常低

    公开(公告)号：US07452991B2

    公开(公告)日：2008-11-18

    申请号：US10847123

    申请日：2004-05-17

    申请人： Viktor Gyollai ,  Csaba Szabo ,  Claude Singer ,  Ehud Amir

    发明人： Viktor Gyollai ,  Csaba Szabo ,  Claude Singer ,  Ehud Amir

    IPC分类号： C07D205/085

    CPC分类号： C07D417/12

    摘要： The invention relates to the β polymorph of Aztreonam, which contains less than 2.5% by weight residual solvent and to a process of making said polymorph. In the process of the invention, a polymorph of Aztreonam is dissolved in an absolute C1-6 alcohol in the presence of a base to form a solution, an acid is added to the solution, and the solution is stirred efficiently.

    摘要翻译： 本发明涉及氨曲南的β多晶型物，其含有小于2.5％（重量）的残留溶剂和制备所述多晶型物的方法。 在本发明的方法中，在碱的存在下将氨丁三醇的多晶型物溶解在绝对的C 1-6醇中以形成溶液，向溶液中加入酸，并将溶液 被有效地搅拌。

    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole
    42.
    发明申请
    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole 审中-公开
    制备2 - [（吡啶基）甲基]亚磺酰基取代的苯并咪唑和泮托拉唑的新氯化衍生物的方法

    公开(公告)号：US20080004319A1

    公开(公告)日：2008-01-03

    申请号：US11881465

    申请日：2007-07-27

    申请人： Viviana Braude ,  Nina Finkelstein ,  Kobi Chen ,  Gideon Pilarsky ,  Anita Liberman ,  Claude Singer ,  Yuriy Raizi

    发明人： Viviana Braude ,  Nina Finkelstein ,  Kobi Chen ,  Gideon Pilarsky ,  Anita Liberman ,  Claude Singer ,  Yuriy Raizi

    IPC分类号： A61K31/4439 ,  C07D401/12 ,  G01N30/00

    CPC分类号： C07D401/12

    摘要： The present invention provides a process comprising admixing a thioether with about 1.05 to about 1.6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorite, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide that is preferably pantoprazole, lansoprazole, omeprazole, or rabeprazole. The process may further comprise contacting the sulfoxide with a source of sodium ions, preferably sodium hydroxide, to produce the sodium salt of the sulfoxide. The invention also relates to novel chlorinated derivatives of pantoprazole including 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H-benzimidazole and 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chlorohydroxymethyl]sulfinyl]-1H-benzimidazole and processes for making them. The invention also relates to processes of quantifying and identifying a compound other than pantoprazole in a mixture of pantoprazole and at least one other compound.

    摘要翻译： 本发明提供了一种方法，其包括将硫醚与约1.05至约1.6摩尔当量的活性氯氧化剂，优选次氯酸钠和约2.5至约5.0摩尔当量碱金属碱混合; 并回收优选泮托拉唑，兰索拉唑，奥美拉唑或雷贝拉唑的亚砜。 该方法可以进一步包括使亚砜与钠离子源（优选氢氧化钠）接触以产生亚砜的钠盐。 本发明还涉及泮托拉新的氯化衍生物，包括5-（二氟甲氧基）-2 - [[（3,4-二甲氧基-2-吡啶基） - 氯甲基]亚磺酰基] -1H-苯并咪唑和5-（二氟甲氧基）-2- [[（3,4-二甲氧基-2-吡啶基） - 氯羟甲基]亚磺酰基] -1H-苯并咪唑及其制备方法。 本发明还涉及在泮托拉唑和至少一种其它化合物的混合物中量化和鉴定泮托拉唑以外的化合物的方法。

    Crystalline forms of ibandronic acid and processes for the preparation thereof
    44.
    发明申请
    Crystalline forms of ibandronic acid and processes for the preparation thereof 审中-公开
    伊班膦酸的结晶形式及其制备方法

    公开(公告)号：US20090099390A1

    公开(公告)日：2009-04-16

    申请号：US12284811

    申请日：2008-09-24

    申请人： Claude Singer ,  Sharon W. Avhar-Maydan ,  Tamas Koltai ,  Amir Gold

    发明人： Claude Singer ,  Sharon W. Avhar-Maydan ,  Tamas Koltai ,  Amir Gold

    IPC分类号： C07F9/38

    CPC分类号： C07F9/386 ,  C07F9/3873

    摘要： A crystalline ibandronic acid characterized by data selected from the group consisting of at least one of a powder x-ray diffraction pattern having peaks at about 4.1, 12.3 and 13.4±0.2 degrees two-theta and at least two more peaks selected from the group consisting of: 8.2, 11.3, 16.2 and 16.9 and 20.8±0.2 degrees two-theta, and by a powder X-ray diffraction pattern depicted in FIG. 1 is provided. Also provided is a crystalline ibandronic acid characterized by data selected from the group consisting of at least one of a powder x-ray diffraction pattern having peaks at about peaks at about 5.2, 11.7, and 18.7±0.2 degrees two-theta and at least two more peaks selected from the group consisting of: 5.8, 10.1, 12.0, 17.1, and 20.0±0.2 degrees two-theta and a powder X-ray diffraction pattern as depicted in FIG. 2. Methods of preparing the crystalline forms are also provided.

    摘要翻译： 一种结晶伊班膦酸，其特征在于选自以下的数据：至少一种粉末X射线衍射图，其具有在约4.1,12.3和13.4±0.2度2-θ以及至少两个以上的峰，所述峰选自 ：8.2,11.3,16.2和16.9和20.8±0.2度2-θ，以及图1中所示的粉末X射线衍射图。 1。 还提供了结晶伊班膦酸，其特征在于选自以下的数据：粉末x射线衍射图中的至少一种，其峰值在约5.2,11.7和18.7±0.2度2θ和至少两个 选自由5.8，10.1，12.0,17.1和20.0±0.2度2-θ组成的组的更多峰和如图1所示的粉末X射线衍射图。 还提供了制备结晶形式的方法。