公开(公告)号：EP1515964A1

公开(公告)日：2005-03-23

申请号：EP03735581.5

申请日：2003-06-07

申请人： ALTANA Pharma AG ,  Signal Pharmaceuticals, Inc.

发明人： BAUDLER, Monika ,  BHAGWAT, Shripad, S. ,  ERDMAN, Paul, E. ,  GANTNER, Florian ,  PALANKI, Moorthy S., S. ,  SCHUDT, Christian ,  STADLWIESER, Josef ,  ZAPF, James

IPC分类号： C07D401/14 ,  C07D409/14 ,  A61K31/506 ,  A61P11/00 ,  C07D405/14

CPC分类号： C07D409/14 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14

摘要： The invention relates to substituted diaminopyrimidine compounds, which are effective therapeutic compounds for treating diseases and disorders associated with those commonly treated by Protein Kinase C theta (PKCtheta) inhibitors.

摘要翻译： 本发明涉及取代的二氨基嘧啶化合物，其是治疗与通常由蛋白激酶Cθ（PKCθ）抑制剂治疗的疾病和病症有关的疾病和病症的有效治疗性化合物。

公开(公告)号：EP1349841A2

公开(公告)日：2003-10-08

申请号：EP01999564.6

申请日：2001-12-05

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： KOIS, Adam ,  MACFARLANE, Karen, J. ,  SATOH, Yoshitaka ,  BHAGWAT, Shripad, S. ,  PARNES, Jason, S. ,  PALANKI, Moorthy, S., S. ,  ERDMAN, Paul, E.

IPC分类号： C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D403/12 ,  A61K31/505 ,  A61P29/00

CPC分类号： C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: (A) wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods or treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

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：EP1349840A2

公开(公告)日：2003-10-08

申请号：EP01996103.6

申请日：2001-12-05

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： KOIS, Adam ,  MACFARLANE, Karen, J. ,  SATOH, Yoshitaka ,  BHAGWAT, Shripad, S. ,  PARNES, Jason, S. ,  PALANKI, Moorthy, S., S. ,  ERDMAN, Paul, E.

IPC分类号： C07D239/00

CPC分类号： C07D239/42 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D487/08 ,  C07D491/10 ,  A61K2300/00

摘要： Compounds having activity as inhibitors of the JNK pathway are disclosed. The compounds of this invention are anilinopyrimidine derivatives having the following structure: (I) wherein R1 through R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to inhibition of the JNK pathway. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

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：EP1608363A1

公开(公告)日：2005-12-28

申请号：EP04758139.2

申请日：2004-03-24

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： BENNETT, Brydon, L. ,  BHAGWAT, Shripad, S. ,  MANNING, Anthony, M. ,  MURRAY, Brion, W. ,  O'LEARY, Eoin, C. ,  SATOH, Yoshitaka

IPC分类号： A61K31/416 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/10 ,  A61P29/00 ,  A61P1/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/00 ,  A61P27/00 ,  A61P37/00

CPC分类号： C07D409/12 ,  A61K31/416 ,  C07D231/54 ,  C07D401/12

摘要： This invention generally relates to methods for treating or preventing an inflammatory disease or disorder comprising administering to a patient in need thereof an effective amount of a Pyrazoloanthrone Derivative having the following structure: Formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined herein.

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：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：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.