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    Method of stabilizing lansoprazole
    1.
    发明授权
    Method of stabilizing lansoprazole 失效
    兰索拉唑稳定方法

    公开(公告)号：US07678816B2

    公开(公告)日：2010-03-16

    申请号：US10773535

    申请日：2004-02-05

    申请人： Claude Singer ,  Anita Liberman ,  Irena Veinberg

    发明人： Claude Singer ,  Anita Liberman ,  Irena Veinberg

    IPC分类号： A61K31/4439 ,  C07D401/12

    CPC分类号： C07D401/12

    摘要： The present invention provides a stable 2-(2-pyridylmethyl)sulfinyl-1H-benzimidazole (lansoprazole) and a method for stabilizing lansoprazole by use of a weakly basic material. The present invention also provides a method for the preparation of a stable lansoprazole.

    摘要翻译： 本发明提供稳定的2-（2-吡啶基甲基）亚磺酰基-1H-苯并咪唑（兰索拉唑）和通过使用弱碱性物质来稳定兰索拉唑的方法。 本发明还提供了制备稳定的兰索拉唑的方法。

    POLYMORPHS OF ESZOPICLONE MALATE
    2.
    发明申请
    POLYMORPHS OF ESZOPICLONE MALATE 审中-公开
    异黄酮黄酮的多聚体

    公开(公告)号：US20080027223A1

    公开(公告)日：2008-01-31

    申请号：US11690580

    申请日：2007-03-23

    申请人： Alex Mainfeld ,  Shlomit Wizel ,  Marioara Mendelovici ,  Anita Liberman ,  Tamas Koltai

    发明人： Alex Mainfeld ,  Shlomit Wizel ,  Marioara Mendelovici ,  Anita Liberman ,  Tamas Koltai

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention provides crystalline Eszopiclone malate form II, crystalline Eszopiclone form V, processes from preparing the crystalline Eszopiclone malate form II or V, pharmaceutical compositions comprising the crystalline Eszopiclone malate form II or V and methods of treating insomnia comprising administering the crystalline Eszopiclone malate form II or V.

    摘要翻译： 本发明提供结晶埃索替普罗苹果酸盐形式II，结晶埃索普洛尔形式V，从制备结晶依佐匹克隆苹果酸盐形式II或V的方法，包含结晶异山梨酸丙酮酸形式II或V的药物组合物和治疗失眠症的方法，包括施用结晶埃索普洛尔苹果酸盐形式 II或V.

    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 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。

    METHODS FOR PREPARING ESZOPICLONE CRYSTALLINE FORM A, SUBSTANTIALLY PURE ESZOPICLONE AND OPTICALLY ENRICHED ESZOPICLONE
    4.
    发明申请
    METHODS FOR PREPARING ESZOPICLONE CRYSTALLINE FORM A, SUBSTANTIALLY PURE ESZOPICLONE AND OPTICALLY ENRICHED ESZOPICLONE 审中-公开
    方法制备环磷酰胺形式A，物质纯度和光学强化剂

    公开(公告)号：US20070270590A1

    公开(公告)日：2007-11-22

    申请号：US11738115

    申请日：2007-04-20

    申请人： Marioara MENDELOVICI ,  Anita LIBERMAN ,  Alex MAINFELD ,  Nina FINKELSTEIN

    发明人： Marioara MENDELOVICI ,  Anita LIBERMAN ,  Alex MAINFELD ,  Nina FINKELSTEIN

    IPC分类号： C07D487/02

    CPC分类号： C07D487/04

    摘要： The present invention provides methods for preparing eszopiclone Form A, substantially chemically pure eszopiclone, or eszopiclone with low level(s) of residual solvent(s). The present invention also provides eszopiclone with low level(s) of residual solvent(s). The present invention also provides a process for optical enrichment of eszopiclone free base. For instance, one of the embodiments of the invention is directed to a method of preparing eszopiclone Form A, wherein the method comprises crystallizing eszopiclone free base from a solvent selected from the group consisting of isopropanol (IPA), methyl isobutyl ketone (MIBK), acetone, n-butanol, i-butanolisobutanol, 2-butanol, tetrahydrofuran (THF), dimethyl carbonate, methanol, ethanol, ethyl lactate, dimethylformamide (DMF), carbon tetrachloride, toluene, iso-butyl acetate and mixtures thereof.

    摘要翻译： 本发明提供了制备具有低水平的残留溶剂的依佐匹克A型，基本上化学纯的右佐佐普隆或舍佐匹克隆的方法。 本发明还提供了具有低水平的残留溶剂的依佐匹克隆。 本发明还提供了一种用于自由基佐佐匹克的光学富集的方法。 例如，本发明的一个实施方案涉及一种制备替佐氟曲霉A型的方法，其中所述方法包括从选自异丙醇（IPA），甲基异丁基酮（MIBK）， 丙酮，正丁醇，异丁醇异丁醇，2-丁醇，四氢呋喃（THF），碳酸二甲酯，甲醇，乙醇，乳酸乙酯，二甲基甲酰胺（DMF），四氯化碳，甲苯，乙酸异丁酯及其混合物。

    Methods for preparation of sertraline hydrochloride polymorphs
    6.
    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。

    DNT-maleate and methods of preparation thereof
    7.
    发明授权
    DNT-maleate and methods of preparation thereof 有权
    DNT-马来酸盐及其制备方法

    公开(公告)号：US07842717B2

    公开(公告)日：2010-11-30

    申请号：US11525336

    申请日：2006-09-21

    申请人： Santiago Ini ,  Anita Liberman ,  Mili Abramov ,  Tamas Koltai

    发明人： Santiago Ini ,  Anita Liberman ,  Mili Abramov ,  Tamas Koltai

    IPC分类号： A61K31/381 ,  C07D333/20

    CPC分类号： C07D333/20 ,  A61K31/38

    摘要： (S)-N,N-Dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine maleate (DNT-maleate) and polymorphs of DNT-maleate, compositions of DNT-maleate and its polymorphs, processes for the preparation of DNT-maleate and its polymorphs, and processes for the preparation of duloxetine hydrochloride from DNT-maleate are provided.

    摘要翻译： （S）-N，N-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺马来酸盐（DNT-马来酸盐）和DNT-马来酸盐的多晶型物，DNT-马来酸盐的组成及其多晶型物， 提供了DNT-马来酸盐及其多晶型物的制备，以及从DNT-马来酸盐制备盐酸度洛西汀的方法。

    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole
    8.
    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。

    Stable iansoprazole containing more than 500 ppm, up to about 3,000 ppm water and more than 200 ppm, up to about 5,000 ppm alcohol
    9.
    发明授权
    Stable iansoprazole containing more than 500 ppm, up to about 3,000 ppm water and more than 200 ppm, up to about 5,000 ppm alcohol 失效
    含有超过500ppm，高达约3,000ppm水和超过200ppm，高达约5,000ppm酒精的稳定的索非唑

    公开(公告)号：US07683080B2

    公开(公告)日：2010-03-23

    申请号：US10717325

    申请日：2003-11-18

    申请人： Anita Liberman ,  Claude Singer ,  Irena Veinberg

    发明人： Anita Liberman ,  Claude Singer ,  Irena Veinberg

    IPC分类号： A61K31/4439 ,  C07D401/12

    CPC分类号： C07D401/12

    摘要： The present invention provides a stable 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazole (lansoprazole) comprising either greater than 500 ppm and not more than about 3,000 ppm water or greater than 200 ppm and not more than about 5,000 ppm alcohol, or both. The present invention provides a method of preparing a stable lansoprozole as well as a pharmaceutical composition containing same. The present invention further provides a method of purifying lansoprazole that is substantially free of sulfone and sulfide derivatives.

    摘要翻译： 本发明提供包含大于500ppm且不大于约3,000ppm水或大于200ppm且不超过约5,000ppm的醇的稳定的2-（2-吡啶基甲基）亚磺酰基-1H-苯并咪唑（兰索拉唑），或 都。 本发明提供了制备稳定的兰索佐唑以及含有它的药物组合物的方法。 本发明还提供了一种纯化基本上不含砜和硫化物衍生物的兰索拉唑的方法。

    METHODS FOR PREPARING ESZOPICLONE CRYSTALLINE FORM A, SUBSTANTIALLY PURE ESZOPICLONE AND OPTICALLY ENRICHED ESZOPICLONE
    10.
    发明申请
    METHODS FOR PREPARING ESZOPICLONE CRYSTALLINE FORM A, SUBSTANTIALLY PURE ESZOPICLONE AND OPTICALLY ENRICHED ESZOPICLONE 审中-公开
    方法制备环磷酰胺形式A，物质纯度和光学强化剂

    公开(公告)号：US20100029943A1

    公开(公告)日：2010-02-04

    申请号：US12565971

    申请日：2009-09-24

    申请人： Marioara MENDELOVICI ,  Anita LIBERMAN ,  Alex MAINFELD ,  Nina FINKELSTEIN

    发明人： Marioara MENDELOVICI ,  Anita LIBERMAN ,  Alex MAINFELD ,  Nina FINKELSTEIN

    IPC分类号： C07D471/04

    CPC分类号： C07D487/04

    摘要： The present invention provides methods for preparing eszopiclone Form A, substantially chemically pure eszopiclone, or eszopiclone with low level(s) of residual solvent(s). The present invention also provides eszopiclone with low level(s) of residual solvent(s). The present invention also provides a process for optical enrichment of eszopiclone free base. For instance, one of the embodiments of the invention is directed to a method of preparing eszopiclone Form A, wherein the method comprises crystallizing eszopiclone free base from a solvent selected from the group consisting of isopropanol (IPA), methyl isobutyl ketone (MIBK), acetone, n-butanol, i-butanolisobutanol, 2-butanol, tetrahydrofuran (THF), dimethyl carbonate, methanol, ethanol, ethyl lactate, dimethylformamide (DMF), carbon tetrachloride, toluene, iso-butyl acetate and mixtures thereof.

    摘要翻译： 本发明提供了制备具有低水平的残留溶剂的依佐匹克A型，基本上化学纯的右佐佐普隆或舍佐匹克隆的方法。 本发明还提供了具有低水平的残留溶剂的依佐匹克隆。 本发明还提供了一种用于自由基佐佐匹克的光学富集的方法。 例如，本发明的一个实施方案涉及一种制备替佐氟曲霉A型的方法，其中所述方法包括从选自异丙醇（IPA），甲基异丁基酮（MIBK）， 丙酮，正丁醇，异丁醇异丁醇，2-丁醇，四氢呋喃（THF），碳酸二甲酯，甲醇，乙醇，乳酸乙酯，二甲基甲酰胺（DMF），四氯化碳，甲苯，乙酸异丁酯及其混合物。