公开(公告)号：EP1140889B1

公开(公告)日：2003-08-27

申请号：EP99968578.7

申请日：1999-12-30

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： STEIN, Bernd, M. ,  ANDERSON, David, W. ,  GAYO, Leah, M. ,  SUTHERLAND, May, S. ,  DOUBLEDAY, Mary ,  SHEVLIN, Graziella, I. ,  KOIS, Adam ,  KHAMMUNGKHUNE, Sak ,  JALLURI, Ravi, Kumar ,  BHAGWAT, Shripad, S. ,  MCKIE, Jeffrey, A.

IPC分类号： C07D311/16 ,  C07D311/18 ,  A61K31/37 ,  A61P35/00

CPC分类号： C07D311/18 ,  C07D311/16

摘要： Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having structure I, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.

公开(公告)号：EP1140889A2

公开(公告)日：2001-10-10

申请号：EP99968578.7

申请日：1999-12-30

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： STEIN, Bernd, M. ,  ANDERSON, David, W. ,  GAYO, Leah, M. ,  SUTHERLAND, May, S. ,  DOUBLEDAY, Mary ,  SHEVLIN, Graziella, I. ,  KOIS, Adam ,  KHAMMUNGKHUNE, Sak ,  JALLURI, Ravi, Kumar ,  BHAGWAT, Shripad, S. ,  MCKIE, Jeffrey, A.

IPC分类号： C07D311/16 ,  C07D311/18 ,  A61K31/37 ,  A61P35/00

CPC分类号： C07D311/18 ,  C07D311/16

摘要： Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having structure I, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.