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1. 发明申请

WO02064557A2 NEW CRYSTAL FORMS OF OXCARBAZEPINE AND PROCESSES FOR THEIR PREPARATION 审中-公开
公开(公告)号：WO02064557A2
公开(公告)日：2002-08-22
申请号：PCT/US0204065
申请日：2002-02-12
申请人： TEVA PHARMA , TEVA PHARMA , ARONHIME JUDITH , DOLITZKY BEN-ZION , BERKOVICH YANA , GARTH NISSIM
发明人： ARONHIME JUDITH , DOLITZKY BEN-ZION , BERKOVICH YANA , GARTH NISSIM
IPC分类号： A61K9/10 , A61K9/20 , A61K9/44 , A61K31/55 , A61P25/08 , A61P25/16 , A61P43/00 , C07D223/22 , C07D
CPC分类号： C07D223/22
摘要： The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling th same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art. These conversions may occur by storage at ambient temperature, by heating one particular Form or treatment with a protic solvent.

2. 发明申请

WO02064557A9 NEW CRYSTAL FORMS OF OXCARBAZEPINE AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：氧化腈的新晶体形式及其制备方法
公开(公告)号：WO02064557A9
公开(公告)日：2002-11-28
申请号：PCT/US0204065
申请日：2002-02-12
申请人： TEVA PHARMA , TEVA PHARMA , ARONHIME JUDITH , DOLITZKY BEN-ZION , BERKOVICH YANA , GARTH NISSIM
发明人： ARONHIME JUDITH , DOLITZKY BEN-ZION , BERKOVICH YANA , GARTH NISSIM
IPC分类号： A61K9/10 , A61K9/20 , A61K9/44 , A61K31/55 , A61P25/08 , A61P25/16 , A61P43/00 , C07D223/22 , C07D223/18
CPC分类号： C07D223/22
摘要： The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling th same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art. These conversions may occur by storage at ambient temperature, by heating one particular Form or treatment with a protic solvent.
摘要翻译：本发明提供了奥卡西平，更特别是奥卡西平形式B，C，D和E的新结晶形式。本发明还提供了这些形式的制备方法。通过从奥卡西平溶于甲苯和二氯甲烷的溶液中蒸发溶剂制备形式B. 通过立即冷却奥卡西平和甲苯的溶液也可获得形式B. 以较慢的速率冷却相同的溶液，但仍然相当快速地导致奥卡西平形式C.以更慢的速率冷却相同的溶液导致另一种形式奥卡西平形式D.奥卡西平E型氯仿溶剂化物通过沉淀奥卡西平和氯仿溶液。本发明还提供了将新发现的奥卡西平晶体之一转化为另一种晶体形式的方法，包括现有技术中的形式A. 这些转化可以通过在环境温度下储存，通过加热一种特定形式或用质子溶剂处理来进行。

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