Claims for Patent: 9,486,458

Summary for Patent: 9,486,458

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:	14/886,774
Patent Claims:	1. 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 seborrhoeic dermatitis, the method comprising administering to a subject in need thereof an effective amount of crystalline form IV of cortexolone-17.alpha.-propionate, wherein crystalline form IV of cortexolone-17.alpha.-propionate is characterized by a DRX as shown in FIG. 28. 2. The method of claim 1, wherein crystalline form IV of cortexolone-17.alpha.-propionate is applied topically. 3. The method of claim 2, wherein the pathology affecting the skin and/or the cutaneous appendages is acne. 4. The method of claim 2, wherein the pathology affecting the skin and/or the cutaneous appendages is androgenetic alopecia. 5. The method of claim 2, wherein the pathology affecting the skin and/or the cutaneous appendages is hirsutism. 6. The method of claim 2, wherein the pathology affecting the skin and/or the cutaneous appendages is seborrhoeic dermatitis. 7. 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 seborrhoeic dermatitis, the method comprising administering to a subject in need thereof an effective amount of a composition comprising water, at least one physiologically acceptable excipient, and crystalline form IV of cortexolone-17.alpha.-propionate, wherein crystalline form IV of cortexolone-17.alpha.-propionate is characterized by a DRX as shown in FIG. 28. 8. The method of claim 7, wherein the administering comprises topically applying the composition. 9. The method of claim 8, wherein the pathology affecting the skin and/or the cutaneous appendages is acne. 10. The method of claim 8, wherein the pathology affecting the skin and/or the cutaneous appendages is androgenetic alopecia. 11. The method of claim 8, wherein the pathology affecting the skin and/or the cutaneous appendages is hirsutism. 12. The method of claim 8, wherein the pathology affecting the skin and/or the cutaneous appendages is seborrhoeic dermatitis. 13. The method of claim 8, 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. 14. 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 seborrhoeic dermatitis, the method comprising administering to a subject in need thereof an effective amount of crystalline form IV of cortexolone-17.alpha.-propionate, wherein crystalline form IV of cortexolone-17.alpha.-propionate is characterized by XRPD peaks at about 4.8, 12.9, 14.4, 15.8, 16, 19.3, and 19.5 degrees 2theta. 15. The method of claim 14, wherein the administering comprises topically applying crystalline form IV of cortexolone-17.alpha.-propionate. 16. The method of claim 15, wherein the pathology affecting the skin and/or the cutaneous appendages is acne. 17. The method of claim 15, wherein the pathology affecting the skin and/or the cutaneous appendages is androgenetic alopecia. 18. The method of claim 15, wherein the pathology affecting the skin and/or the cutaneous appendages is hirsutism. 19. The method of claim 15, wherein the pathology affecting the skin and/or the cutaneous appendages is seborrhoeic dermatitis. 20. The method of claim 14, wherein crystalline form IV of cortexolone-17.alpha.-propionate is formulated in a composition comprising at least one pharmaceutically acceptable excipient selected from the group consisting of propylene glycol, cetylic alcohol, glyceryl monostearate, liquid paraffin, and combinations of any of the foregoing. 21. The method of claim 20, wherein the composition is in the form of a tablet, capsule, powder, pellet, suspension, emulsion, cream, gel, ointment, lotion, or paste. 22. The method of claim 7, wherein the composition is in the form of a tablet, capsule, powder, pellet, suspension, emulsion, cream, gel, ointment, lotion, or paste. 23. The method of claim 21, wherein the composition is applied topically. 24. The method of claim 22, wherein the composition is applied topically.