Claims for Patent: 9,433,628

Summary for Patent: 9,433,628

Title:	Enzymatic process for obtaining 17.alpha.-monoesters of cortexolone and/or its 9,11-dehydroderivatives
Abstract:	The present invention refers to a new enzymatic process for obtaining 17.alpha.-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17.alpha.,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone 17.alpha.-propionate and 9,11-dehydro-cortexolone 17.alpha.-butanoate.
Inventor(s):	Ajani; Mauro (Lainate, IT), Moro; Luigi (Cairate, IT)
Assignee:	Cassiopea SPA (Lainate, IT)
Application Number:	14/073,928
Patent Claims:	1. Crystalline form IV of cortexolone-17.alpha.-propionate characterized by a DRX as shown in FIG. 28. 2. Crystalline form IV of cortexolone-17.alpha.-propionate characterized by XRPD peaks at about 4.8, 12.9, 14.4, 15.8, 16, 19.3, and 19.5 degrees 2theta. 3. A process for preparing crystalline form IV of cortexolone-17.alpha.-propionate, the process comprising crystallizing cortexolone-17.alpha.-propionate from a propylene glycol/water or polyethylene glycol/water mixture. 4. The process of claim 3, wherein the propylene glycol/water mixture has a ratio of propylene glycol to water of from about 1/2 to about 2/1. 5. The process of claim 4, wherein the ratio of propylene glycol to water is about 1/1. 6. The process of claim 3, wherein the polyethylene glycol/water mixture has a ratio of polyethylene glycol to water of from about 1/2 to about 2/1. 7. The process of claim 6, wherein the ratio of polyethylene glycol to water is about 1/1. 8. The process of claim 3, wherein the propylene glycol/water mixture has a ratio of propylene glycol to water of from about 1/3 to about 3/1. 9. Crystalline form IV of cortexolone-17.alpha.-propionate prepared by the process of claim 3. 10. Crystalline form IV of cortexolone-17.alpha.-propionate prepared by the process of claim 4. 11. Crystalline form IV of cortexolone-17.alpha.-propionate prepared by the process of claim 5. 12. Crystalline form IV of cortexolone-17.alpha.-propionate prepared by the process of claim 6. 13. Crystalline form IV of cortexolone-17.alpha.-propionate prepared by the process of claim 7. 14. A pharmaceutical composition comprising crystalline form IV of cortexolone-17.alpha.-propionate, water, and at least one physiologically acceptable excipient. 15. The composition of claim 14, wherein the at least one physiologically acceptable excipient is propylene glycol, cetylic alcohol, glyceryl monostearate, liquid paraffin, or a combination of any of the foregoing. 16. The composition of claim 14, further comprising mixed tocopherols, polysorbate 80, or a combination thereof. 17. The composition of claim 14, wherein the composition is in the form of a cream. 18. The composition of claim 14, wherein the composition further comprises solubilized cortexolone-17.alpha.-propionate. 19. The composition of claim 18, wherein the solubilized cortexolone-17.alpha.-propionate and crystalline form IV of cortexolone-17.alpha.-propionate together comprise 0.1 to 2% by weight of the composition. 20. The composition of claim 19, wherein the solubilized cortexolone-17.alpha.-propionate and crystalline form IV of cortexolone-17.alpha.-propionate together comprise 0.2 to 1% by weight of the composition. 21. The composition of claim 14, wherein the crystalline form IV of cortexolone-17.alpha.-propionate is present at from about 0.1 to about 2% by weight of the composition. 22. A pharmaceutical composition comprising crystalline form IV of cortexolone-17.alpha.-propionate. 23. The composition of claim 22, wherein the composition is in the form of a tablet, capsule, powder, pellet, suspension, emulsion, cream, gel, ointment, lotion, or paste. 24. The composition of claim 22, wherein the composition is in the form of a solid, semi-solid, or a paste.