Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives
AssigneeCassiopea S.P.A.
InventorsMauro Ajani, Luigi Moro
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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.
Claims34
Crystalline form I of cortexolone-17α-propionate characterized by:
- a DRX as shown in FIG. 1;
- or
- a DRX with at least peaks at about:
- 7.6, 8.4, 14.3, 14.8, 15.7, 17.0, and 20.1 degrees 2theta.
A pharmaceutical composition comprising at least one physiologically acceptable excipient and crystalline form I of cortexolone-17α-propionate, wherein crystalline form I of cortexolone-17α-propionate is characterized by:
- a DRX as shown in FIG. 1;
- or
- a DRX with at least peaks at about:
- 7.6, 8.4, 14.3, 14.8, 15.7, 17.0, and 20.1 degrees 2theta.
A process for preparing crystalline form I of cortexolone-17α-propionate, the process comprising crystallizing cortexolone-17α-propionate from tert-butylmethylether.
A method of treating a pathology affecting the skin and/or the cutaneous appendages, wherein the pathology affecting the skin and/or the cutaneous appendages is acne, androgenetic alopecia, hirsutism, or seborrheic dermatitis, the method comprising administering to a subject in need thereof an effective amount of crystalline form I of cortexolone-17α-propionate, wherein crystalline form I of cortexolone-17α-propionate is characterized by:
- a DRX as shown in FIG. 1;
- or
- a DRX with at least peaks at about:
- 7.6, 8.4, 14.3, 14.8, 15.7, 17.0, and 20.1 degrees 2theta.
Dependencies are inferred from the claim text.