Claims for Patent: 12,337,002

Summary for Patent: 12,337,002

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 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.
Inventor(s):	Mauro Ajani, Luigi Moro
Assignee:	Cosmo SpA , Cassiopea SpA
Application Number:	US18/057,031
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,337,002
Patent Claims:	1. A pharmaceutical composition comprising cortexolone 17α-propionate in at least one of polymorphic forms I, III, or IV, propylene glycol, cetyl alcohol, glyceryl monostearate, liquid paraffin, tocopherol, polyoxyethylene (80) sorbitan monooleate, and water, wherein: a) polymorphic form I is characterized by a DRX with at least peaks at about: 7.6, 8.4, 17.0, and 20.1 degrees 2theta; b) polymorphic form III is characterized by a DRX with at least peaks at about: 6.2, 12.6, 22.4, and 23.7 degrees 2theta; and c) polymorphic form IV is characterized by DRX with at least peaks at about: 4.8, 12.9, and 19.5 degrees 2theta. 2. The pharmaceutical composition of claim 1, wherein the cortexolone 17α-propionate comprises solvate crystalline form IV of cortexolone 17α-propionate. 3. The pharmaceutical composition of claim 1, wherein the cortexolone 17α-propionate comprises cortexolone 17α-propionate of crystalline form III. 4. The pharmaceutical composition of claim 2, wherein the cortexolone 17α-propionate further comprises cortexolone 17α-propionate of crystalline form III. 5. The pharmaceutical composition of claim 1, wherein the cortexolone 17α-propionate is present in the composition in an amount of 0.1 to 2 wt %. 6. The pharmaceutical composition of claim 2, wherein the cortexolone 17α-propionate is present in the composition in an amount of 0.1 to 2 wt %. 7. The pharmaceutical composition of claim 1, wherein the cortexolone 17α-propionate is present in the composition in an amount of 0.2 to 1 wt %. 8. The pharmaceutical composition of claim 2, wherein the cortexolone 17α-propionate is present in the composition in an amount of 0.2 to 1 wt %. 9. The pharmaceutical composition of claim 1, wherein the cortexolone 17α-propionate is present in the composition in an amount of about 1 wt %. 10. The pharmaceutical composition of claim 2, wherein the cortexolone 17α-propionate is present in the composition in an amount of about 1 wt %. 11. The pharmaceutical composition of claim 1, wherein the tocopherol is mixed tocopherols. 12. The pharmaceutical composition of claim 1, wherein the composition is formulated for topical administration. 13. The pharmaceutical composition of claim 2, wherein the composition is formulated for topical administration. 14. The pharmaceutical composition of claim 1, wherein the composition is an emulsion. 15. The pharmaceutical composition of claim 2, wherein the composition is an emulsion. 16. The pharmaceutical composition of claim 1, wherein the composition is a cream. 17. The pharmaceutical composition of claim 2, wherein the composition is a cream. 18. The pharmaceutical composition of claim 14, wherein the composition is a cream. 19. The pharmaceutical composition of claim 1, wherein the composition comprises: about 1 wt % cortexolone 17α-propionate, about 24.7 wt % propylene glycol, about 2.5 wt % cetyl alcohol, about 14.8 wt % glyceryl monostearate, about 9.9 wt % liquid paraffin, about 1 wt % polyoxyethylene (80) sorbitan monooleate. 20. The pharmaceutical composition of claim 19 further comprising about 0.05 wt % tocopherol. 21. A method of treating acne in a subject in need thereof, the method comprising topically administering an effective amount of the pharmaceutical composition of claim 1 to an affected area on the subject.