| abstract |
The present invention describes novel 8GG-substituted Estratrien of general formula I wherein R2, R3, R6, R6 ', R7, R7', R9, R11, R11 ', R12, R14, R15, R15', R16, R16 ', R17 and R17 'has the meaning given thereto and R8 means branched or straight-chain, optionally partially or fully halogenated alkyl or alkenyl residue with up to 5 carbon atoms ethinyl or prop-1-inyl, as pharmaceutically active substances, which have a greater affinity in vitro estrogen receptor preparations of rat prostate than estrogen receptor preparations of rat uterus and in vivo particularly preferential effect on bone in comparison with uterus and / or pronounced effect as regards stimulation of 5HT2a receptor and transporter expression, their preparation, their therapeutic use and pharmaceutical forms administrations, containing new compounds. The invention further describes the use of these compounds for the treatment of hormone-induced diseases and conditions, as well as the application of the 8Gj-substituted estratriene portion of the structure to total structures of the compounds exhibiting dissociation in favor of their estrogenic action on bone compared to the uterus. -substituted estratrienes of the general formula (I), wherein R2, R3, R6, R6 ', R7, R7', R9, R11, R11 ', R12, R14, R15, R15', R16, R16 ', R17 and R17 R8 is a straight or branched-chained, optionally partially or completely halogenated alkyl or alkenyl group having 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 for estrogen receptor preparations of rat prostate than for estrogen receptor preparations of rat uterus and which in vivo prefer to have a preferential effect on bone material as compared to uterus and / or a pronounced effect with respect to stimulation of the expression of the 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 the use of an 8Gj-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. |