Schering Aktiengesellschaft

Rudolf Knauthe

Christa Hegele-Hartung

Rolf Bohlmann

Dirk Kosemund

Karl-Heinrich Fritzemeier

Hermann Kuenzer

Monika Lessl

Ulf Boemer

Gerd Mueller

Karl Heinrich Fritzemeier

Karsten Parzcyk

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 16&#x3b1;- and 16&#x3b2;-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.

16-hydroxyestratrienes as selectively active estrogens

Combination preparation of estrogen and anti-estrogen

This invention describes 11&bgr;-aryl-substituted 14,17-ethanoestratrienes of general formula (I). The new compounds are selective estrogens whose action occurs in a tissue-selective manner. The estrogenic action occurs in particular on bone, in the cardiovascular system and in the CNS (central nervous system). Only a slight estrogenic action or no estrogenic action occurs in the uterus and in the liver, however. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example for hormone replacement therapy, prevention and treatment of osteoporosis).

11&bgr;-aryl substituted 14,17-ethanoestratriens, method for the production of these compounds and their use in the production of medicaments

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Berlin, Germany

Rudolf Knauthe