公开(公告)号：EP1497277A1

公开(公告)日：2005-01-19

申请号：EP03733871.2

申请日：2003-04-18

申请人： Signal Pharmaceuticals, Inc. ,  Novartis AG

发明人： MCKIE, Jeffrey, A. ,  BHAGWAT, Shripad, S. ,  RENAUD, Johanne ,  MISSBACH, Martin

IPC分类号： C07D311/16 ,  A61K31/352

CPC分类号： C07D311/16 ,  C07D311/58

摘要： Benzopyranone compounds having the structure of formula (I), are disclosed. The compounds of formula (I), wherein R1 is H, can be prepared by demethylation of the corresponding phenolic methyl ether. The compounds are useful for treating a bone-resorbing disease, cancer, arthritis or an estrogen-related condition such as 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：EP1246814B1

公开(公告)日：2005-02-16

申请号：EP00990966.4

申请日：2000-12-29

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： BHAGWAT, Shripad, S. ,  MCKIE, Jeffrey, A. ,  KHAMMUNGKHUNE, Sak

IPC分类号： C07D311/16 ,  C07D405/12 ,  A61K31/32 ,  A61P35/00

CPC分类号： C07D405/12 ,  C07D311/16

摘要： Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having formula (I), as well as pharmaceutical compositions containing the same wherein R1, R2, R3, n and p are as defined here. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are also disclosed for modulating ER-β in cells and/or tissues expressing the same, including cells and/or tissues that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

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.

公开(公告)号：EP1246814A2

公开(公告)日：2002-10-09

申请号：EP00990966.4

申请日：2000-12-29

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： BHAGWAT, Shripad, S. ,  MCKIE, Jeffrey, A. ,  KHAMMUNGKHUNE, Sak

IPC分类号： C07D311/16 ,  C07D405/12 ,  A61K31/32 ,  A61P35/00

CPC分类号： C07D405/12 ,  C07D311/16

摘要： Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having formula (I), as well as pharmaceutical compositions containing the same wherein R1, R2, R3, n and p are as defined here. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are also disclosed for modulating ER-β in cells and/or tissues expressing the same, including cells and/or tissues that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

公开(公告)号：EP1322617A1

公开(公告)日：2003-07-02

申请号：EP01975252.6

申请日：2001-09-18

申请人： SIGNAL PHARMACEUTICALS, INC. ,  AXYS PHARMACEUTICALS, INC.

发明人： BHAGWAT, Shripad, S. ,  GAYO-FUNG, Leah, M. ,  STEIN, Bernd, M. ,  CHAO, Qi ,  GANGLOFF, Anthony, R. ,  MCKIE, Jeffrey, A. ,  RICE, Kenneth, D.

IPC分类号： C07D217/20 ,  C07D217/18 ,  C07D209/44 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D417/12 ,  C07D405/12 ,  C07D413/10 ,  C07D401/10 ,  C07D401/06 ,  A61K31/472 ,  A61P35/00

CPC分类号： C07D223/16 ,  C07D209/44 ,  C07D217/04 ,  C07D217/16 ,  C07D217/18 ,  C07D217/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/10 ,  C07D417/12

摘要： Compounds have the structure: including srereoisomers and pharmaceutically acceptable salts thereof; wherein a is 0, 1 or 2; A, B and C are independently CH, CR or N, wherein R is C1-6 alkyl; D is-(CH2)nC(=O)(CH2)m-; R1, R2, R3 are substituents modulate the estrogen receptor (ER) and methods for treating estrogen-related conditions, including conditions such as breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

公开(公告)号：EP1667999A1

公开(公告)日：2006-06-14

申请号：EP04784110.1

申请日：2004-09-13

申请人： Signal Pharmaceuticals LLC ,  Novartis AG

发明人： MCKIE, Jeffrey, A. ,  BHAGWAT, Shripad, S. ,  RENAUD, Johanne ,  MISSBACH, Martin

IPC分类号： C07D405/12 ,  A61K31/4025

CPC分类号： C07D311/16 ,  C07D311/14

摘要： Benzopyranone Compounds having the following structure: (I) wherein R1, R2, X, Y and n are as defined herein, are disclosed. The Benzopyranone Compounds are useful for treating or preventing a bone-resorbing disease, a neoplastic disease, arthritis, a disease exacerbated by the presence of estrogen or a disease improved by the presence of estrogen, comprising administering an effective amount of a Benzopyranone Compound to a patient in need of the treating or preventing; activating the function of estrogen receptor ('ER') in a bone cell; inhibiting the function of ER in a cancer cell; inhibiting the expression of interleukin-6 ('IL-6') in a cell; and inhibiting the growth of a neoplastic cell, comprising contacting the cell with an effective amount of a Benzopyranone Compound.