公开(公告)号：EP1841767A1

公开(公告)日：2007-10-10

申请号：EP06701504.0

申请日：2006-01-20

申请人： Bayer Schering Pharma AG

发明人： BRIEM, Hans ,  THIERAUCH, Karl-Heinz ,  KETTSCHAU, Georg ,  SCHAEFER, Martina ,  SCHWEDE, Wolfgang ,  HUSEMANN, Manfred ,  TER LAAK, Antonius ,  KUENZER, Hermann ,  INCE ,Stuart ,James

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00 ,  A61P27/00 ,  A61P17/00 ,  C07D213/85

CPC分类号： C07D471/04 ,  C07D213/85

摘要： The invention relates to pyrazolopyridines according to the general formula (I), and salts thereof, to pharmaceutical compositions comprising said pyrazolopyridines and to a method of preparing said pyrazolopyridines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with angiopoietin and therefore influence Tie2 signalling.

公开(公告)号：EP1226155B1

公开(公告)日：2007-05-02

申请号：EP00981233.0

申请日：2000-11-02

申请人： Bayer Schering Pharma AG

发明人： HILLISCH, Alexander ,  BOIDOL, Werner ,  SCHWEDE, Wolfgang ,  ESPERLING, Peter ,  SAUER, Gerhard ,  HEGELE-HARTUNG, Christa ,  KOLLENKIRCHEN, Uwe ,  FRITZEMEIER, Karl-Heinrich

IPC分类号： C07J1/00 ,  A61K31/565

CPC分类号： C07J1/0062 ,  A61K31/565 ,  A61K31/566 ,  A61K31/567 ,  C07J1/007 ,  C07J1/0088 ,  C07J1/0096

摘要： The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R , R , R , R , R , R , R , R , R , R , R , R , R , R and R have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention. The invention also relates to utilization of steroids based on the gonatriene molecular skeleton in order to treat estrogen deficiency-induced diseases and disorders, in addition to the use of said gonatriene structural component in the total structure of compounds which dissociate to produce enhanced estrogen activity in bone as compared to the uterus.