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Last Updated: May 4, 2024

Claims for Patent: 9,211,295


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Summary for Patent: 9,211,295
Title:17 alpha, 21-dihydroxypregnene esters as antiandrogenic agents
Abstract: 17.alpha.,21-Dihydroxypregna-4,9(11)-diene-3,20-dione and 17.alpha.,21-dihydroxypregna-4-ene-3,20-dione 17 and/or 21 esters having remarkable antiandrogenic activity are provided, along with methods of using these compounds and processes for their preparation.
Inventor(s): Ajani; Mauro (Lainate, IT), Moro; Luigi (Milan, IT)
Assignee: CASSIOPEA S.P.A. (Lainate (MI), IT)
Application Number:14/474,765
Patent Claims: 1. A pharmaceutical formulation for the treatment of acne, alopecia, hirsutism, or seborrhea, the formulation comprising an effective amount of 17.alpha.-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione, wherein the formulation is suitable for topical application, and wherein the formulation comprises a pharmaceutically acceptable carrier.

2. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is in the form of a cream.

3. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is in the form of a gel.

4. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is in the form of a liposomal emulsion or suspension.

5. The pharmaceutical formulation of claim 2, wherein the cream comprises at least one excipient selected from the group consisting of cetyl alcohol, glycerol monostearate, liquid paraffin, propylene glycol, disodium mono-oleo-amide sulfosuccinate, citric acid monohydrate, and water.

6. The pharmaceutical formulation of claim 5, wherein the cream comprises cetyl alcohol.

7. The pharmaceutical formulation of claim 6, wherein the cream further comprises glycerol monostearate.

8. The pharmaceutical formulation of claim 7, wherein the cream further comprises liquid paraffin.

9. The pharmaceutical formulation of claim 8, wherein the cream further comprises propylene glycol.

10. The pharmaceutical formulation of claim 9, wherein the cream further comprises disodium mono-oleo-amide sulfosuccinate.

11. The pharmaceutical formulation of claim 10, wherein the cream further comprises citric acid monohydrate.

12. The pharmaceutical formulation of claim 11, wherein the cream further comprises water.

13. A method of treating hirsutism, the method comprising administering to a patient in need thereof an effective amount of 17.alpha.-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione.

14. The method of claim 13, wherein the 17.alpha.-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione is applied topically.

15. The method of claim 13, wherein the 17.alpha.-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione is present in a pharmaceutical formulation suitable for topical application.

16. The method of claim 15, wherein the pharmaceutical formulation comprises a pharmaceutically acceptable carrier.

17. The method of claim 15, wherein the pharmaceutical formulation is in the form of a cream.

18. The method of claim 15, wherein the pharmaceutical formulation is in the form of a gel.

19. The method of claim 15, wherein the pharmaceutical formulation is in the form of a liposomal emulsion or suspension.

20. A method of treating seborrhea, the method comprising administering to a patient in need thereof an effective amount of 17.alpha.-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione.

21. The method of claim 20, wherein the 17.alpha.-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione is applied topically.

22. The method of claim 21, wherein the 17.alpha.-propionyloxy-21-hydroxy-pregna-4-ene-3,20-dione is present in a pharmaceutical formulation suitable for topical application.

23. The method of claim 22, wherein the pharmaceutical formulation comprises a pharmaceutically acceptable carrier.

24. The method of claim 22, wherein the pharmaceutical formulation is in the form of a cream.

25. The method of claim 22, wherein the pharmaceutical formulation is in the form of a gel.

26. The method of claim 22, wherein the pharmaceutical formulation is in the form of a liposomal emulsion or suspension.

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