NEW CRYSTALLINE FORMS OF PERINDOPRIL ERBUMINE

Disclosed are two new crystalline forms, .delta. and .epsilon., of perindopril erbumine. Perindopril (2S,3aS,7aS)-1-[2-(1-ethoxycarbonyl-(S)-butylamino)-(S)-propionyl] -octahydroindole-2-carboxylic acid) has the following formula (I): (See Above Formula) Those forms are suitable as therapeutic activ...

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Hauptverfasser:	LELLEK, VIT, FAESSLER, ROGER, STRAESSLER, CHRISTOPH
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Zusammenfassung:	Disclosed are two new crystalline forms, .delta. and .epsilon., of perindopril erbumine. Perindopril (2S,3aS,7aS)-1-[2-(1-ethoxycarbonyl-(S)-butylamino)-(S)-propionyl] -octahydroindole-2-carboxylic acid) has the following formula (I): (See Above Formula) Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardiovascular diseases, especially high blood pressure and heart failure. The .epsilon. crystalline form is obtained in the crystallisation of perindopril erbumine. If water is then removed, and stirring is continued, the .epsilon. crystalline form is converted to the .delta. crystalline form. The .delta. crystalline form can also be obtained by stirring the a or .beta. crystalline with seeding with the .delta. crystalline form. The .epsilon. crystalline form can also be obtained by stirring the a or .beta. crystalline form with seeding with the .epsilon. crystalline form; or by stirring the a or .beta. crystalline form in tert.-butyl methyl ether and water.