Claims for Patent: 10,159,682

Summary for Patent: 10,159,682

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 S.P.A. (Lainate (MI), IT)
Application Number:	15/211,094
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 seborrheic dermatitis, the method comprising administering to a subject in need thereof an effective amount of crystalline form III of cortexolone-17.alpha.-propionate, wherein crystalline form III of cortexolone-17.alpha.-propionate is characterized by: a DRX as shown in FIG. 7, 10, or 13; or a DRX with at least peaks at about: 6.2, 12.6, 14.1, 14.3, 16.0, 22.4, and 23.7 degrees 2theta. 2. The method of claim 1, wherein crystalline form III 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 seborrheic 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 seborrheic dermatitis, the method comprising administering to a subject in need thereof an effective amount of a composition comprising at least one physiologically acceptable excipient and crystalline form III of cortexolone-17.alpha.-propionate, wherein crystalline form III of cortexolone-17.alpha.-propionate is characterized by: a DRX as shown in FIG. 7, 10, or 13; or a DRX with at least peaks at about: 6.2, 12.6, 14.1, 14.3, 16.0, 22.4, and 23.7 degrees 2theta. 8. The method of claim 7, wherein the effective amount of the composition comprising at least one physiologically acceptable excipient and crystalline form III of cortexolone-17.alpha.-propionate is administered topically. 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 seborrheic 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. 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. 15. The method of claim 14, wherein the composition is a powder, suspension, emulsion, cream, gel, ointment, lotion, or past, and is applied topically. 16. The method of claim 7, wherein the composition further comprises solubilized cortexolone-17.alpha.-propionate. 17. The method of claim 16, wherein the solubilized cortexolone-17.alpha.-propionate is present in the composition in a concentration of from 0.1 to 2% by weight of the composition. 18. The method of claim 16, wherein the solubilized cortexolone-17.alpha.-propionate and crystalline form III of cortexolone-17.alpha.-propionate together comprise 0.1 to 2% by weight of the composition or comprise 0.2 to 1% by weight of the composition. 19. The method of claim 16, wherein the composition further comprises any of crystalline forms I, II, or IV of cortexolone-17.alpha.-propionate, or any combination thereof, and wherein the solubilized cortexolone-17.alpha.-propionate and crystalline form III of cortexolone-17.alpha.-propionate together with any of crystalline forms I, II, or IV of cortexolone-17.alpha.-propionate, or any combination thereof, comprise 0.1 to 2% by weight of the composition or 0.2 to 1% by weight of the composition. 20. The method of claim 16, wherein the composition further comprises any of crystalline forms I, II, or IV of cortexolone-17.alpha.-propionate, or any combination thereof, and wherein the solubilized cortexolone-17.alpha.-propionate and crystalline form III of cortexolone-17.alpha.-propionate together with any of crystalline forms I, II, or IV of cortexolone-17.alpha.-propionate, or any combination thereof, comprise 1% by weight of the composition.