8- HYDROCARBYL-SUBSTITUTED ESTRATRIENES FOR USE AS SELECTIVE ESTROGENS, PHARMACEUTICAL COMPOSITION BASED THEREON

摘要

The invention relates to novel 8 -substituted estratrienes of the general formula (I), , (I) wherein R2, R3, R6, R6', R7, R7', R9, R11, R11', R12, R14, R15, R15', R16, R16', R17 and R17' are defined as in the description and R8 represents a straight - or branched-chained, optionally partially or completely halogenated alkyl or alkenyl group with up to 5 carbon atoms, an ethinyl or prop-1-inyl group. The inventive estratrienes are used as pharmaceutically active substances that have in vitro a higher affinity to estrogen receptor preparations of rat prostate than to estrogen receptor preparations of rat uterus and which in vivo preferably have a preferential effect on bone material as compared to uterus and/or a pronounced effect with respect to the stimulation of the expression of 5HT2a receptor and transporter. The invention further relates to the production of these novel compounds, to their use in therapy and to the pharmaceutical forms of administration that contain said novel compounds. The invention further describes the use of said compounds for treating estrogen-deficiency related diseases and conditions and to the use of an 8 -substituted estratriene structural part in the overall structures of compounds that are characterized by a dissociation in favor of their estrogen effect on the bone as compared to the uterus.