CRYSTALLINE FORMS OF 11 ÿ-(4-ACETYLPHENYL)-20,20,21,21,21-PENTAF LUOR-17- HYDROXY-19-NOR-17α-PREGNA-4,9-DIEN-3-ONE

CRYSTALLINE FORMS OF 11 ÿ-(4-ACETYLPHENYL)-20,20,21,21,21-PENTAF LUOR-17- HYDROXY-19-NOR-17α-PREGNA-4,9-DIEN-3-ONE

The present invention relates to crystalline forms of 11 ÿ-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor -17α-pregna-4,9-dien-3-one. In particular, the invention relates to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present inventio...

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Bibliographische Detailangaben
Hauptverfasser: WOLFGANG BECKMANN, ARWED CLEVE, EVELIN AMOULONG, GABRIELE WINTER, EDDA KRAEMER, THOMAS GINKO
Format: Patent
Sprache:eng ; spa
Schlagworte:
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
STEROIDS
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Zusammenfassung:The present invention relates to crystalline forms of 11 ÿ-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor -17α-pregna-4,9-dien-3-one. In particular, the invention relates to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example, methanol and ethanol solvates of 11 ÿ-(4-acetylphenyl)- 20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17α-pregna-4,9-die n-3-one, as precursors for the preparation of these two polymorphs I and II. Processes are described for the preparation of polymorph I by means of displacement crystallization or by means of extraction. The choice of the last solvent, before the ansolvate formation can take place, on the basis of the differences in the purification ratios of the individual solvates of 11 ÿ-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor -17α-pregna-4,9-dien-3-one is described. Polymorph I, according to the invention, is particularly suitable for the preparation of drugs. Formas cristalinas de 11ß-(4-acetilfenil)-20,20,21,21,21-pentafluo ro-17-hidroxi-19-nor-17a-pregna-4,9-dien-3-ona. En particular, dos formas cristalinas de ansolvato/anhidrato de este compuesto, las formas polimórficas l y II. Solvatos cristalinos, por ejemplo, los solvatos de metanol y etanol de 11ß -(4-acetilifenil)-2O,2O,21,21,21-pentafluoro-17-hidroxi-19-nor-17 a-pregna-4,9-dien-3-ona, como precursores para la preparación de ambas formas polimórficas I y II. Se describen procesos para la preparación de la forma polimórfica I, por medio de cristalización con desplazamiento o remoción por agitación. La elección del solvente se realiza en función de las diferencias en el comportamiento de purificación de los solvatos individuales de la 11ß-(4-acetilfenil)-20,20,21,21,21-pentafluoro-17-hidroxi-19-no r-17a-pregna-4,9-dien-3-ona. La forma polimórfica I de acuerdo con la invención es apropiada para preparar medicamentos.