Enzymatic process for obtaining 17α-monoesters of cortexolone and/or its 9,11-dehydroderivatives
AssigneeCassiopea S.P.A.
InventorsMauro Ajani, Luigi Moro
Life of this patent
Estimating the term…
Abstract
The present invention refers to a new enzymatic process for obtaining 17α-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17α,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone 17α-propionate and 9,11-dehydro-cortexolone 17α-butanoate.
Claims24
Crystalline form IV of cortexolone-17α-propionate characterized by a DRX as shown in FIG. 28.
Crystalline form IV of cortexolone-17α-propionate characterized by XRPD peaks at about 4.8, 12.9, 14.4, 15.8, 16, 19.3, and 19.5 degrees 2theta.
A process for preparing crystalline form IV of cortexolone-17α-propionate, the process comprising crystallizing cortexolone-17α-propionate from a propylene glycol/water or polyethylene glycol/water mixture.
A pharmaceutical composition comprising crystalline form IV of cortexolone-17α-propionate, water, and at least one physiologically acceptable excipient.
A pharmaceutical composition comprising crystalline form IV of cortexolone-17α-propionate.
Dependencies are inferred from the claim text.