Enzymatic process for obtaining 17 α-monoesters of cortexolone and/or its 9,11-dehydroderivatives
AssigneeCassiopea S.P.A.
InventorsMauro Ajani, Luigi Moro
Life of this patent
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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.
Claims20
A composition comprising:
- a) crystalline form III of cortexolone-17α-propionate characterized by a DRX spectrum as represented in FIG. 7, 10, or 13, or a DRX spectrum with at least peaks at about:
- 6.2, 12.6, 14.1, 14.3, 16.0, 22.4, and 23.7 degrees 2theta, or a DSC spectrum as represented in FIG. 8, 11, or 14, or an IR spectrum as shown in FIG. 9, 12, or 15;
- and
- b) crystalline form IV of cortexolone-17α-propionate characterized by a DRX spectrum as represented in FIG. 28, or a DRX spectrum with at least peaks at about:
- 4.8, 12.9, 14.4, 15.8, 16, 19.3, and 19.5 degrees 2theta.
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 a composition comprising
- a) crystalline form III of cortexolone-17α-propionate characterized by a DRX spectrum as represented in FIG. 7, 10, or 13, or a DRX spectrum with at least peaks at about:
- 6.2, 12.6, 14.1, 14.3, 16.0, 22.4, and 23.7 degrees 2theta, or a DSC spectrum as represented in FIG. 8, 11, or 14, or an IR spectrum as shown in FIG. 9, 12, or 15;
- and;
- b) crystalline form IV of cortexolone-17α-propionate characterized by a DRX spectrum as represented in FIG. 28, or a DRX spectrum with at least peaks at about:
- 4.8, 12.9, 14.4, 15.8, 16, 19.3, and 19.5 degrees 2theta.
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 a composition comprising:
- a) water;
- b) at least one physiologically acceptable excipient;
- c) crystalline form III of cortexolone-17α-propionate characterized by a DRX spectrum as represented in FIG. 7, 10, or 13, or a DRX spectrum with at least peaks at about:
- 6.2, 12.6, 14.1, 14.3, 16.0, 22.4, and 23.7 degrees 2theta, or a DSC spectrum as represented in FIG. 8, 11, or 14, or an IR spectrum as shown in FIG. 9, 12, or 15;
- and
- d) crystalline form IV of cortexolone-17α-propionate characterized by a DRX spectrum as represented in FIG. 28, or a DRX spectrum with at least peaks at about:
- 4.8, 12.9, 14.4, 15.8, 16, 19.3, and 19.5 degrees 2theta.
Dependencies are inferred from the claim text.