Dihydrospirorenone as an antiandrogen

• US 5,569,652 A
• Filed: 12/07/1993
• Issued: 10/29/1996
• Est. Priority Date: 05/16/1989
• Status: Expired due to Term

• Current Assignee: Bayer Pharma AG (Bayer AG)
• Original Assignee: Schering Ag (Merck & Co., Inc.)
• Inventors: Elger, Walter, Nishino, Yukishige, Beier, Sybille, Wiechert, Rudolf
• Primary Examiner(s): Criares, Theodore J.
• Application Number:
  US08/162,387
• Time in Patent Office: 1,057 Days
• Field of Search: 514/173, 514/172, 540/11, 540/8
• US Class Current: 514/173
• CPC Class Codes: A61K 31/585 containing lactone rings, e.g. oxandrolone, bufalin

Abstract

Dihydrospirorenone, ##STR1## preferably together with an estrogen, can be used for the production of a pharmaceutical agent suitable for treatment of hormonal irregularities during premenopause (menstruation stabilization), for hormonal substitution therapy during menopause, for treatment of androgen-induced disorders and/or for contraception.

Claims

1. A method of simultaneously achieving, during premenopause or menopause a gestagenic effect, antiandrogenic effect, and an antialdosterone effect in a female patient in need thereof comprising administering an amount of dihydrospirorenone to said female patient, wherein said amount of dihydrospirorenone is effective to simultaneously achieve a gestagenic effect, antiandrogenic effect and antialdosterone effect in said patient.

2. A method according to claim 1, wherein said patient is in premenopause.

3. A method of claim 2, wherein stabilization of menstruation is achieved.

4. A method according to claim 1, wherein said female is of age 35-55.

5. A method according to claim 1, wherein said patient is in menopause.

6. A method according to claim 1, wherein said effective amount of dihydrospirorenone is 0.5-50 mg per day.

7. A method according to claim 6, wherein said effective amount of dihydrospirorenone is 1-10 mg per day.

8. A method of claim 1, wherein said patient is predisposed to androgenization symptoms.

9. A method of claim 1, wherein said patient suffers from or is predisposed to high blood pressure.

10. A method of claim 2, wherein said patient suffers from or is predisposed to high blood pressure.

11. A method of simultaneously achieving, during premenopause or menopause, a contraceptive effect, an anti-androgenic effect, and an anti-aldosterone effect in a female patient in need thereof comprising administering an effective amount of dihydrospirorenone and an effective amount of an estrogenic compound, wherein said effective amount of dihydrospirorenone is effective to simultaneously achieve a gestagenic effect, anti-androgenic effect, and an anti-aldosterone effect in said female patient.

12. A method according to claim 11, wherein said effective amount of dihydrospirorenone is 0.5-50 mg per day and said effective amount of an estrogenic compound is an amount equivalent to 0.5-4.0 mg of estradiol valerate per day.

13. A method of claim 11, wherein said patient suffers from symptoms of androgenization.

14. A method of claim 11, wherein said patient suffers from or is predisposed to high blood pressure.

15. A method of claim 13, wherein said patient is in premenopause.

16. A method of claim 13, wherein said patient suffers from or is predisposed to high blood pressure.

17. A method of claim 11, wherein said estrogenic compound is a synthetic estrogen.

18. A method of claim 11, wherein said estrogenic compound is a natural estrogen.

19. A method according to claim 11, wherein said female is of age 35-55.

20. A method of claim 11, wherein said estrogenic compound is a synthetic estrogen.

21. A method of claim 12, wherein said estrogenic compound is a natural estrogen.

22. A method of claim 11, wherein the estrogenic compound is 17α

-ethynylestradiol.

23. A method of claim 11, wherein said patient is in menopause.

24. A method according to claim 11, wherein said effective amount of dihydrospirorenone is 1-10 mg per day.

25. A method of claim 11, wherein said patient is predisposed to androgenization symptoms.

26. A method of claim 15, wherein stabilization of menstruation is achieved.

27. A method according to claim 11, wherein said effective amount of dihydrospirorenone is 0.5-50 mg per day and said effective amount of an estrogenic compound is an amount equivalent to 0.02-0.04 mg of 17α

-ethynylestradiol per day.