发明公开
EP1368322A2 NEW CRYSTAL FORMS OF OXCARBAZEPINE AND PROCESSES FOR THEIR PREPARATION
审中-公开
奥卡西平与方法新的晶体形态及其
- 专利标题: NEW CRYSTAL FORMS OF OXCARBAZEPINE AND PROCESSES FOR THEIR PREPARATION
- 专利标题(中): 奥卡西平与方法新的晶体形态及其
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申请号: EP02718948.9申请日: 2002-02-12
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公开(公告)号: EP1368322A2公开(公告)日: 2003-12-10
- 发明人: ARONHIME, Judith , DOLITZKY, Ben-Zion , BERKOVICH, Yana , GARTH, Nissim
- 申请人: TEVA PHARMACEUTICAL INDUSTRIES LTD.
- 申请人地址: 5 Basel Street,P.O. Box 3190 49131 Petah Tiqva IL
- 专利权人: TEVA PHARMACEUTICAL INDUSTRIES LTD.
- 当前专利权人: TEVA PHARMACEUTICAL INDUSTRIES LTD.
- 当前专利权人地址: 5 Basel Street,P.O. Box 3190 49131 Petah Tiqva IL
- 代理机构: Nachshen, Neil Jacob
- 优先权: US268314P 20010212
- 国际公布: WO02064557 20020822
- 主分类号: C07D223/18
- IPC分类号: C07D223/18 ; A61K31/55 ; A61P25/08
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.
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