abstract |
The invention relates to novel 8th substituted estratrians of the general formula (I), wherein R2, R3, R6, R6 ', R7, R7', R9, R11, R11 ', R12, R14, R15, R15' , R16, R16 ', R17 and R17' are as defined in the description, and R8 represents a linear or branched chain alkyl or alkenyl group, optional, partially or completely halogenated with up to 5 carbon atoms, an ethynyl or prop group -1-inilo. The estranges of the invention are used as pharmaceutically active substances that have a higher affinity in vitro for rat prostate estrogen receptor preparations compared to rat third-estrogen receptor preparations and which preferably have an effect. preferential in vivo on bone material, in comparison with the third, or a pronounced effect with respect to the stimulation of the expression of the 5HT2a receptor and transporter. The invention also relates to the production of these novel compounds, their use in therapy and pharmaceutical administration forms containing novel compounds. The invention further describes the use of such compounds to treat diseases and conditions related to estrogen deficiency, and with the use of a structural part of estratriene substituted at 8 °, in the total structures of compounds that are characterized by dissociation in favor of its estrogenic effect on the bone, in comparison with the third. |