17.alpha.-cyanomethylestra-4,9-dien derivatives and pharmaceutical compositions containing same

US5866559A · kind A · utility

Assignee

• Jenapharm GmbH · DE

Inventors

• Gerhard Teichmuller · Jena, DE
• Gerd Muller · Jena, DE
• Sigfrid Schwarz · Jena, DE
• Bernd Undeutsch · Jena, DE
• Harry Henkel · Dayton, US
• Ronald Gebuhr · Jena, DE
• Gunter Kaufmann · Jena, DE
• Doris Hubler · Jena, DE
• Michael Oettel · Jena, DE

Key dates

• Filing date: Dec 20, 1996
• Grant date: Feb 2, 1999
• Expiry date: Dec 20, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J41/0094
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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.