Substituted 16,17-annellated steroid compounds for use in womens healthcare
View Patent ↗The present invention relates to substituted steroid compounds having the formula Wherein R 1 is H or halogen; R 2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R 3 is H or halogen; R 4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R 5 is methyl or ethyl; R 6 is H or methyl; R 7 is H or methyl; R 8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
1. A compound of the formula
wherein
R 1 is H or halogen;
R 2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl;
R 3 is H or halogen;
R 4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl;
R 5 is methyl or ethyl;
R 6 is H or methyl;
R 7 is H or methyl;
R 8 is H or acyl.
2. The compound according to claim 1 , wherein R 8 is H.
3. The compound according to claim 1 or 2 , wherein R 1 is H or F and R 3 is H or F.
4. The compound according to claim 1 or 2 , wherein R 6 is H or α-methyl.
5. The compound according to claim 1 or 2 , wherein R 5 is methyl.
6. The compound according to claim 1 or 2 , wherein R 4 is (1C-4C)alkyl.
7. The compound according to claim 6 , wherein R 4 is propyl.
8. The compound according to claim 5 , wherein R 6 is H and R 7 is H.
9. The compound according to claim 3 , wherein R 5 is methyl; R 6 is H and R 7 is H.
10. The compound according to claim 9 , wherein R 4 is propyl.
11. The compound according to claim 1 , wherein R 2 is H or (1C-4C) acyl.
12. The compound according to claim 11 , wherein R 1 is H; R 3 is H; R 4 is propyl; R 5 is methyl; R 6 is H and R 7 is H.
13. A compound of the formula
14. A pharmaceutical composition comprising a compound according to claim 1 and one Or more pharmaceutical excipients.
15. A pharmaceutical composition comprising the compound according to claim 13 and one or more pharmaceutical excipients.
16. A method of treatment for endometriosis comprising administering a compound of the formula
in a pharmaceutical formulation at a therapeutically effective dose.
17. A method of contraception comprising administration to a woman of a compound according to claim 1 .
18. A method of treatment for endometriosis in a woman by administration of the compound according to claim 1 in a pharmaceutical formulation at a therapeutically effective dose.