公开(公告)号：US20060122271A1

公开(公告)日：2006-06-08

申请号：US11336552

申请日：2006-01-20

申请人： Claude Singer ,  Gideon Pilarski ,  Michael Pesachovich ,  Eduard Schwartz

发明人： Claude Singer ,  Gideon Pilarski ,  Michael Pesachovich ,  Eduard Schwartz

IPC分类号： A61K31/195 ,  A61K9/20

CPC分类号： A61K31/195 ,  A61K9/145 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2059 ,  C07C227/40 ,  C07C227/44 ,  C07C2601/14 ,  C07D209/96 ,  C07C229/28

摘要： A pharmaceutical composition containing substantially pure and stable gabapentin are disclosed wherein gabapentin has a pH of between 6.8 to 7.3.

公开(公告)号：US20070199856A1

公开(公告)日：2007-08-30

申请号：US11521594

申请日：2006-09-14

申请人： Michael Pesachovich ,  Sarah Isaacs ,  Claude Singer ,  Eduard Schwartz ,  Edit Berger ,  Ruth Tenengauzer ,  Joseph Schwarz ,  Julia Hrakovsky ,  Tania Lessen ,  Lev Khondo ,  Mathi Mathivanan

发明人： Michael Pesachovich ,  Sarah Isaacs ,  Claude Singer ,  Eduard Schwartz ,  Edit Berger ,  Ruth Tenengauzer ,  Joseph Schwarz ,  Julia Hrakovsky ,  Tania Lessen ,  Lev Khondo ,  Mathi Mathivanan

IPC分类号： B65D85/84

CPC分类号： A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054

摘要： A method of packaging of azithromycin which provides improved stability of azithromycin upon storage. Additionally, compositions and methods of stabilizing azithromycin compositions are described. Stabilized azithromycin compositions comprise an intimate admixture of azithromycin and a stabilizing-effective amount of an antioxidant to improve the resistance of the azithromycin to degradation. Coprecipitation or co-milling of azithromycin and an antioxidant are particularly preferred means of achieving an intimate admixture. Pharmaceutical formulations comprising a stabilized azithromycin composition and methods of making such formulations are also described.

摘要翻译： 包装阿奇霉素的方法，其提供阿奇霉素在储存时的改善的稳定性。 另外，描述了稳定阿奇霉素组合物的组合物和方法。 稳定的阿奇霉素组合物包含阿奇霉素和稳定有效量的抗氧化剂的紧密混合物，以改善阿奇霉素降解的抗性。 阿奇霉素和抗氧化剂的共沉淀或共研磨是特别优选的实现紧密混合的方法。 还描述了包含稳定的阿奇霉素组合物的药物制剂和制备这些制剂的方法。

公开(公告)号：US20080149521A9

公开(公告)日：2008-06-26

申请号：US11521594

申请日：2006-09-13

申请人： Michael Pesachovich ,  Sarah Isaacs ,  Claude Singer ,  Eduard Schwartz ,  Edit Berger ,  Ruth Tenengauzer ,  Joseph Schwarz ,  Julia Hrakovsky ,  Tania Lessen ,  Lev Khondo ,  Mathi Mathivanan

发明人： Michael Pesachovich ,  Sarah Isaacs ,  Claude Singer ,  Eduard Schwartz ,  Edit Berger ,  Ruth Tenengauzer ,  Joseph Schwarz ,  Julia Hrakovsky ,  Tania Lessen ,  Lev Khondo ,  Mathi Mathivanan

IPC分类号： B65D85/84

CPC分类号： A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054

摘要： A method of packaging of azithromycin which provides improved stability of azithromycin upon storage. Additionally, compositions and methods of stabilizing azithromycin compositions are described. Stabilized azithromycin compositions comprise an intimate admixture of azithromycin and a stabilizing-effective amount of an antioxidant to improve the resistance of the azithromycin to degradation. Coprecipitation or co-milling of azithromycin and an antioxidant are particularly preferred means of achieving an intimate admixture. Pharmaceutical formulations comprising a stabilized azithromycin composition and methods of making such formulations are also described.

摘要翻译： 包装阿奇霉素的方法，其提供阿奇霉素在储存时的改善的稳定性。 另外，描述了稳定阿奇霉素组合物的组合物和方法。 稳定的阿奇霉素组合物包含阿奇霉素和稳定有效量的抗氧化剂的紧密混合物，以改善阿奇霉素降解的抗性。 阿奇霉素和抗氧化剂的共沉淀或共研磨是特别优选的实现紧密混合的方法。 还描述了包含稳定的阿奇霉素组合物的药物制剂和制备这些制剂的方法。

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。

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。

公开(公告)号：US20060241189A1

公开(公告)日：2006-10-26

申请号：US11415830

申请日：2006-05-01

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 ,  C07C211/42

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.

公开(公告)号：US07022881B2

公开(公告)日：2006-04-04

申请号：US10861274

申请日：2004-06-04

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： C07C211/00

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可以通过将盐酸舍曲林多晶型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。

公开(公告)号：US06500987B1

公开(公告)日：2002-12-31

申请号：US09448985

申请日：1999-11-24

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： 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。

公开(公告)号：US20060069267A1

公开(公告)日：2006-03-30

申请号：US11271839

申请日：2005-11-14

申请人： Tamar Nidam ,  Marioara Mendelovici ,  Eduard Schwartz ,  Shlomit Wizel

发明人： Tamar Nidam ,  Marioara Mendelovici ,  Eduard Schwartz ,  Shlomit Wizel

IPC分类号： C07D261/20

CPC分类号： C07D261/20

摘要： The present invention relates to a novel sulfonation of an intermediate of zonisamide. The sulfonation processes using chlorosulfonic acid as well as acetic anhydride and sulfuric acid in an organic solvent are disclosed. Crystalline forms of benzisoxazole methane sulfonic acid (BOS-H) and its salts (BOS-Na, BOS-Ca, and BOS-Ba) and their novel preparation processes are disclosed.

公开(公告)号：US20050124629A1

公开(公告)日：2005-06-09

申请号：US11037152

申请日：2005-01-19

申请人： Valerie Niddam-Hildesheim ,  Neomi Gershon ,  Eduard Schwartz

发明人： Valerie Niddam-Hildesheim ,  Neomi Gershon ,  Eduard Schwartz

IPC分类号： C07D498/06 ,  A61K31/496 ,  C07D43/02

CPC分类号： C07D498/06

摘要： Levofloxacin has been purified by dissolving levofloxacin in a polar solvent at an elevated temperature and crystallizing purified levofloxacin. Preferably, an antioxidant is added to increase the purity.

摘要翻译： 左氧氟沙星已经通过在升高的温度下将左氧氟沙星溶解在极性溶剂中并使纯化的左氧氟沙星结晶来纯化。 优选地，加入抗氧化剂以提高纯度。