Estra-1,3,5(10)-trien derivatives, processes for their preparation and pharmaceutical compositions containing these compounds

US6080735A · kind A · utility

Assignee

• Jenapharm GmbH & Co. KG · DE

Inventors

• Sigfrid Schwarz · Jena, DE
• Walter Elger · Berlin, DE
• Hans-Joachim Siemann · Jena, DE
• by Margit Lucas, heir · Mettmann, DE
• by Frank Siemann, heir · Geringswalde, DE
• Gudrun Reddersen · Jena, DE
• Birgitt Schneider · Jena, DE

Key dates

• Filing date: Feb 2, 1998
• Grant date: Jun 27, 2000
• Expiry date: Feb 2, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J53/004
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention is relating to new estra-1,3,5(10)-trien-sulfamates carrying at the 3-position an R--SO.sub.2 --O--group, with R being an R.sup.1 R.sup.2 N--group in which R.sup.1 and R.sup.2, independently of each other, represent a hydrogen atom, an alkyl residue with 1-5 C atoms or, together with the N atom, a polymethylene-imino residue with 4-6 C atoms or a morpholino residue. The compounds, according to this invention, are suitable for hormonal contraception and climacteric hormone replacement therapy (HRT) as well as for treatment of gynecological and andrological diseases. Hence, only low hepatic estrogenicity is exhibited by the compounds according to this invention. Also described are processes for preparation of the compounds according to this invention and for preparation of pharmaceutical compositions.