16-hydroxyestratrienes as selectively active estrogens

US7109360B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Hermann Kuenzer · Berlin, DE
• Rudolf Knauthe · Berlin, DE
• Monika Lessl · Berlin, DE
• Karl-Heinrich Fritzemeier · Berlin, DE
• Christa Hegele-Hartung · Neheim, DE
• Ulf Boemer · Berlin, DE
• Gerd Mueller · Hamburg, DE
• Dirk Kosemund · Berlin, DE

Key dates

• Filing date: Feb 4, 2000
• Grant date: Sep 19, 2006
• Expiry date: Feb 4, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J41/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.The new compounds are 16α- and 16β-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.