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    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole
    2.
    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。

    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole
    3.
    发明申请
    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole 失效
    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：US20050075370A1

    公开(公告)日：2005-04-07

    申请号：US10866261

    申请日：2004-06-10

    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： C07D401/12 ,  C07D43/02 ,  A61K31/4439

    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。

    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole
    4.
    发明授权
    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole 失效
    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：US07683177B2

    公开(公告)日：2010-03-23

    申请号：US10866261

    申请日：2004-06-10

    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： C07D401/12

    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。

    Processes for preparing crystalline and amorphous mupirocin calcium
    5.
    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。