SUBSTITUTED 16,17-ANNELLATED STEROID COMPOUNDS FOR USE IN WOMENS HEALTH
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 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.
2 . The compound according to claim 1 , wherein R 8 is H.
3 . The compound according to claim 1 , wherein R 1 is H or F and R 3 is H or F.
4 . The compound according to claim 1 , wherein R 6 is H or α-methyl.
5 . The compound according to claim 1 , wherein R 5 is methyl.
6 . The compound according to claim 1 , 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 having the formula
14 . A pharmaceutical composition comprising a compound according to any one of claims 1 - 12 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 of a human or an animal in need of treatment with the compound according to any one of claims 1 - 12 by administration of the compound in a pharmaceutical formulation and in a therapeutically effective dose.
17 . The method according to claim 16 , whereby the human is a woman and the need for treatment is for therapy of endometriosis.
18 . A method of treatment for endometriosis comprising administering a compound having the formula
in a pharmaceutical formulation at a therapeutically effective dose.
19 . A method of contraception comprising administration to a woman of a compound according to claim 1 .