Steroids having a mixed androgenic and progestagenic profile
View Patent ↗The invention provides 19-nor-D-homosteroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R 1 is O, or NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl, R 2 is methyl or ethyl, and R 3 is hydrogen or (C 1-15 )acyl.
1. A compound of formula I,
wherein,
R 1 is O, or NOR, with R being hydrogen, (C 1-6 ) alkyl or (C 1-6 ) acyl,
R 2 is methyl or ethyl, and
R 3 is hydrogen or (C 1-15 ) acyl.
2. A compound according to claim 1 , wherein R 1 is O.
3. A compound according to claim 1 , wherein R 1 O and R 3 is hydrogen.
4. The compound (7α,17aβ)-17a-hydroxy-7,17a-dimethyl-D-homoestr-4-en-3 -one.
5. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable excipient.
6. The compound according to claim 2 , wherein R 1 is O and R 3 is hydrogen.
7. A pharmaceutical composition comprising a compound according to claim 2 and a pharmaceutically acceptable excipient.
8. A pharmaceutical composition comprising a compound according to claim 3 and a pharmaceutically acceptable excipient.
9. A pharmaceutical composition comprising a compound according to claim 4 and a pharmaceutically acceptable excipient.
10. A pharmaceutical composition comprising a compound according to claim 6 and a pharmaceutically acceptable excipient.
11. A method of contraception, comprising administering to a male patient an effective amount of a compound according to claim 1 .
12. A method of treating androgen insufficiency, comprising administering to a male patient suffering from androgen insufficiency an effective amount of a compound according to claim 1 .