17.alpha.-cyanomethylestra-4,9-dien derivatives and pharmaceutic

Details 17.alpha.-cyanomethylestra-4,9-dien derivatives and pharmaceutic 17.alpha.-cyanomethylestra-4,9-dien derivatives and pharmaceutic

1996-12-20

1999-02-02

Dees, Jose G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

550598, A61K 3157, C07J 700

Patent

active

058665595

ABSTRACT:
The 17.alpha.-cyanomethylestra-4,9-diene derivative compounds are of formula I: ##STR1## wherein R.sub.1 is an alkyl group having from 1 to 2 carbon atoms; R.sub.2 is an alkyl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or a trialkylsilyl group; and R.sub.3 is an oxygen atom or a R--O--N group, wherein R is a hydrogen atom, an acyl group with 1 to 10 carbon atoms, an alkyl group with 1 to 10 carbon atoms, a sulfamoyl group, an alkylsilyl group or a trialkylsilyl group. These compounds, particularly in combination with at least one suitable estrogen, are suitable for treatment of endometrioses or gestagen-dependent tumors and for hormonal contraception and climacteric hormone replacement therapy (HRT). Processes for making the new steroids are described as well as methods of making the pharmaceutical compositions containing them.

REFERENCES:
Croxatto, H. B. et al., "Female contraception and male fertility Regulation", ed. by Runnebaum, Rabe & Kiesel, vol. 2, Advances in Gynecological and Obstetric Research Series, p. 241, 1991.

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