9-α-substituted estratrienes as selectively active estrogens

US7414043B2 · kind B2 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Dirk Kosemund · Berlin, DE
• Gerd Mueller · Hamburg, DE
• Alexander Hillisch · Solingen, DE
• Karl-Heinrich Fritzemeier · Berlin, DE
• Peter Muhn · Berlin, DE

Key dates

• Filing date: Jun 11, 2003
• Grant date: Aug 19, 2008
• Expiry date: Mar 4, 2024

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/28
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention describes the new 9α-substituted estratrienes of general formula Iin which R3, R7, R7′, R13, R16 as well as R17 and R17′ have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.