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

摘要

This invention describes the new 8beta-substituted estratrienes of general formula I in which R², R³, R⁶, R^6', R⁷, R^7', R⁹, R¹¹, R^11', R¹², R¹⁴, R¹⁵, R^15', R¹⁶, R^16', R¹⁷, R^17' 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 8beta-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.