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11. 发明申请

US20060142564A1 Methods of preparing pimecrolimus 失效
标题翻译：吡美莫司的制备方法
公开(公告)号：US20060142564A1
公开(公告)日：2006-06-29
申请号：US11293353
申请日：2005-12-01
申请人： Viktor Gyollai , Csaba Szabo
发明人： Viktor Gyollai , Csaba Szabo
IPC分类号： C07D281/18
CPC分类号： C07D498/18 , A61K9/145 , A61K9/1688 , A61K31/4745 , C07D491/14 , C07H19/01
摘要： The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated derivative at C-32. The activated ascomycin is then reacted with chloride ion. The process of the invention requires fewer process steps than prior art processes, and does not require the protection of the ascomycin C-24 hydroxyl group or the purification of the activated ascomycin derivative.
摘要翻译：本发明提供了从子囊霉素制备吡美莫司的方法，其中子囊霉素与转化试剂反应，转化试剂在C-32将子囊霉转化为活化衍生物。然后将活化的子囊霉素与氯离子反应。本发明的方法比现有技术方法需要更少的方法步骤，并且不需要保护子囊霉素C-24羟基或活化的子囊霉素衍生物的纯化。

12. 发明授权

US06995277B2 Process for preparing simvastatin having controlled ranges of simvastatin dimer content 失效
标题翻译：制备具有辛伐他汀二聚体含量受控范围的辛伐他汀的方法
公开(公告)号：US06995277B2
公开(公告)日：2006-02-07
申请号：US10777535
申请日：2004-02-11
申请人： Ferenc Korodi , Csaba Szabo , Szabolcs Salyi , Istvan Bodi
发明人： Ferenc Korodi , Csaba Szabo , Szabolcs Salyi , Istvan Bodi
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： The present invention relates to a process for preparing simvastatin, wherein the simvastatin dimer content is controlled. More particularly, the present invention relates to a process for preparing simvastatin having a simvastatin dimer content of about 0.2 to about 0.4% wt. The present invention also relates to a process for preparing simvastatin having a simvastatin dimer content of less than about 0.2% wt. The present invention also discloses a commercial scale process of preparing simvastatin having a specified simvastatin dimer content which is reproducible.
摘要翻译：本发明涉及一种辛伐他汀的制备方法，其中辛伐他汀二聚体含量受到控制。更具体地，本发明涉及制备辛伐他汀二聚体含量为约0.2至约0.4重量％的辛伐他汀的方法。本发明还涉及制备辛伐他汀二聚体含量小于约0.2重量％的辛伐他汀的方法。本发明还公开了制备具有可重现的特定辛伐他汀二聚体含量的辛伐他汀的商业规模的方法。

13. 发明申请

US20050004215A1 Amorphous simvastatin calcium and methods for the preparation thereof 审中-公开
标题翻译：无定形辛伐他汀钙及其制备方法
公开(公告)号：US20050004215A1
公开(公告)日：2005-01-06
申请号：US10815362
申请日：2004-04-01
申请人： Ferenc Korodi , Erika Feher , Csaba Szabo , Istvan Bodi , Adrienne Kovacsne-Mezei
发明人： Ferenc Korodi , Erika Feher , Csaba Szabo , Istvan Bodi , Adrienne Kovacsne-Mezei
IPC分类号： C07C67/28 , C07C67/52 , C07C69/30 , C07D309/30 , C07C69/66 , A61K31/225
CPC分类号： C07D309/30 , C07C67/28 , C07C67/52 , C07C69/30 , C07C2602/28 , C07D309/20
摘要： An amorphous dihydroxy open acid simvastatin calcium and methods for preparing amorphous simvastatin calcium.
摘要翻译：无定形二羟基开放酸辛伐他汀钙及其制备方法辛伐他汀钙非晶体。

14. 发明授权

US07279571B2 Methods of preparing pimecrolimus 失效
公开(公告)号：US07279571B2
公开(公告)日：2007-10-09
申请号：US11293353
申请日：2005-12-01
申请人： Viktor Gyollai , Csaba Szabo
发明人： Viktor Gyollai , Csaba Szabo
IPC分类号： C07D498/18
CPC分类号： C07D498/18 , A61K9/145 , A61K9/1688 , A61K31/4745 , C07D491/14 , C07H19/01
摘要： The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated derivative at C-32. The activated ascomycin is then reacted with chloride ion. The process of the invention requires fewer process steps than prior art processes, and does not require the protection of the ascomycin C-24 hydroxyl group or the purification of the activated ascomycin derivative.

15. 发明申请

US20060041148A1 Process for preparing simvastatin having controlled ranges of simvastatin dimer content 审中-公开
标题翻译：制备具有辛伐他汀二聚体含量受控范围的辛伐他汀的方法
公开(公告)号：US20060041148A1
公开(公告)日：2006-02-23
申请号：US11255304
申请日：2005-10-20
申请人： Ferenc Korodi , Csaba Szabo , Szabolcs Salyi , Istvan Bodi
发明人： Ferenc Korodi , Csaba Szabo , Szabolcs Salyi , Istvan Bodi
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： The present invention relates to a process for preparing simvastatin, wherein the simvastatin dimer content is controlled. More particularly, the present invention relates to a process for preparing simvastatin having a simvastatin dimer content of about 0.2 to about 0.4 % wt. The present invention also relates to a process for preparing simvastatin having a simvastatin dimer content of less than about 0.2% wt. The present invention also discloses a commercial scale process of preparing simvastatin having a specified simvastatin dimer content which is reproducible.
摘要翻译：本发明涉及一种辛伐他汀的制备方法，其中辛伐他汀二聚体含量受到控制。更具体地，本发明涉及制备辛伐他汀二聚体含量为约0.2至约0.4重量％的辛伐他汀的方法。本发明还涉及制备辛伐他汀二聚体含量小于约0.2重量％的辛伐他汀的方法。本发明还公开了制备具有可重现的特定辛伐他汀二聚体含量的辛伐他汀的商业规模的方法。

16. 发明申请

US20090137821A1 Method of making dorzolamide hydrochloride 审中-公开
标题翻译：盐酸多佐胺的制备方法
公开(公告)号：US20090137821A1
公开(公告)日：2009-05-28
申请号：US12317438
申请日：2008-12-22
申请人： Laszlo Zsolt Kovacs , Csaba Szabo , Erika Magyar Molnarne , Adrienne Kovacsne-Mezei , Claude Singer , Judith Aronhime
发明人： Laszlo Zsolt Kovacs , Csaba Szabo , Erika Magyar Molnarne , Adrienne Kovacsne-Mezei , Claude Singer , Judith Aronhime
IPC分类号： C07D335/04
CPC分类号： C07D495/04
摘要： Processes for the preparation of dorzolamide hydrochloride and an intermediate of Formula IV, are provided.
摘要翻译：提供了制备盐酸多佐胺和式IV中间体的方法。

17. 发明申请

US20050272768A1 Process for preparation of amorphous form of a drug 失效
标题翻译：制备无定形形式药物的方法
公开(公告)号：US20050272768A1
公开(公告)日：2005-12-08
申请号：US11143312
申请日：2005-06-01
申请人： Csaba Szabo , Szabolcs Szoke , Lorant Gyuricza , Claude Singer
发明人： Csaba Szabo , Szabolcs Szoke , Lorant Gyuricza , Claude Singer
IPC分类号： A61K9/19 , A61K31/47 , C07D215/16 , C07D215/18 , C07D407/06 , C07D498/14 , F26B5/04 , F26B11/12
CPC分类号： C07D215/18 , C07D407/06 , F26B5/041 , F26B11/12
摘要： Provided is a process for preparation of amorphous form of an active pharmaceutical ingredient.
摘要翻译：提供了制备活性药物成分的无定形形式的方法。

18. 发明授权

US07737177B2 Processes for preparing crystalline and amorphous mupirocin calcium 失效
标题翻译：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。

19. 发明授权

US07589128B2 Process for preparation of amorphous form of a drug 失效
标题翻译：制备无定形形式药物的方法
公开(公告)号：US07589128B2
公开(公告)日：2009-09-15
申请号：US11143312
申请日：2005-06-01
申请人： Csaba Szabo , Szabolcs Szoke , Lorant Gyuricza , Claude Singer , Valerie Niddam-Hildesheim , Greta Sterimbaum
发明人： Csaba Szabo , Szabolcs Szoke , Lorant Gyuricza , Claude Singer , Valerie Niddam-Hildesheim , Greta Sterimbaum
IPC分类号： A61K47/00
CPC分类号： C07D215/18 , C07D407/06 , F26B5/041 , F26B11/12
摘要： Provided is a process for preparation of amorphous form of an active pharmaceutical ingredient.
摘要翻译：提供了制备活性药物成分的无定形形式的方法。

20. 发明申请

US20050250773A1 Process for preparation of mycophenolate mofetil and other esters of mycophenolic acid 审中-公开
标题翻译：霉酚酸酯和麦考酚酸的其他酯的制备方法
公开(公告)号：US20050250773A1
公开(公告)日：2005-11-10
申请号：US11115820
申请日：2005-04-26
申请人： Sandor Molnar , Csaba Szabo , Tivadar Tamas , Janos Hajko , Claude Singer , Beata Kosztya
发明人： Sandor Molnar , Csaba Szabo , Tivadar Tamas , Janos Hajko , Claude Singer , Beata Kosztya
IPC分类号： A61K31/365 , A61K31/5377 , C07B63/00 , C07D307/88 , C07D413/02 , C07D413/14
CPC分类号： C07D307/88 , Y10T436/141111
摘要： Provided are processes for the preparation of mycophenolate mofetil and other esters of mycophenolic acid.
摘要翻译：提供了制备霉酚酸酯和麦考酚酸的其它酯的方法。

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