公开(公告)号：EP1272504B1

公开(公告)日：2007-05-30

申请号：EP01931609.0

申请日：2001-04-12

申请人： Bayer Schering Pharma Aktiengesellschaft

发明人： PETERS, Olaf ,  HILLISCH, Alexander ,  THIEME, Ina ,  ELGER, Walter ,  HEGELE-HARTUNG, Christa ,  KOLLENKIRCHEN, Uwe ,  FRITZEMEIER, Karl-Heinrich ,  PATCHEV, Vladimir

IPC分类号： C07J1/00 ,  A61K31/565 ,  C07J41/00 ,  A61P5/30

CPC分类号： C07J1/007 ,  C07J1/0059 ,  C07J1/0062 ,  C07J1/0074 ,  C07J41/0072

摘要： The invention relates to novel 8ß-substituted estratrienes of the general formula (I), wherein R?2, 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 8ß-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.

公开(公告)号：EP2176282A2

公开(公告)日：2010-04-21

申请号：EP08775031.1

申请日：2008-07-11

申请人： Bayer Schering Pharma Aktiengesellschaft

发明人： PETERS, Olaf ,  BRAEUER, Nico ,  THIEME, Ina ,  PRELLE, Katja ,  MUHN, Hans-Peter ,  FRITZEMEIER, Karl-Heinrich

IPC分类号： C07J1/00 ,  A61K31/565 ,  A61P5/30

CPC分类号： C07J1/007 ,  C07J1/0062

摘要： The invention refers to 8β-substituted estra-1,3,5(10)-triene derivatives of general formula (I), their use 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 in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.