Crystal forms of oxcarbazepine and processes for their...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C540S589000

Reexamination Certificate

active

10074181

ABSTRACT:
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 the 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.

REFERENCES:
patent: 3716640 (1973-02-01), Schindler
patent: 4452738 (1984-06-01), Aufderhaar
patent: 4559174 (1985-12-01), Aufderhaar
patent: 5658900 (1997-08-01), Boireau et al.
patent: 5808058 (1998-09-01), Milanese
patent: 6670472 (2003-12-01), Ansari et al.
patent: WO 03/106414 (2003-12-01), None

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