8β-hydrocarbyl-substituted estratrienes for use as selective estrogens

US7378404B2 · kind B2 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Olaf Peters · Bad Tabarz, DE
• Alexander Hillisch · Solingen, DE
• Ina Thieme · Graitschen, DE
• Walter Elger · Berlin, DE
• Christa Hegele-Hartung · Neheim, DE
• Uwe Kollenkirchen · Berlin, DE
• Karl-Heinrich Fritzemeier · Berlin, DE
• Vladimir Patchev · Jena, DE

Key dates

• Filing date: Apr 12, 2001
• Grant date: May 27, 2008
• Expiry date: Apr 12, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J41/0072
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention describes the new 8β-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17 and R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8β-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rathe…