公开(公告)号：EP1838710A1

公开(公告)日：2007-10-03

申请号：EP06718361.6

申请日：2006-01-13

申请人： SIGNAL PHARMACEUTICALS, INC. ,  Pharmacopeia Drug Discovery, Inc.

发明人： ALBERS, Ronald ,  AYALA, Leticia ,  CLAREEN, Steven, S. ,  DELGADO MEDEROS, Maria, M. ,  HILGRAF, Robert ,  HEDGE, Sayee ,  HUGHES, Kevin ,  KOIS, Adam ,  PLANTEVIN-KRENITSKY, Veronique ,  MCCARRICK, Meg ,  NADOLNY, Lisa ,  PALANKI, Moorthy ,  SAHASRABUDHE, Kiran ,  SAPIENZA, John ,  SATOH, Yoshitaka ,  SLOSS, Marian ,  SUDBECK, Elise ,  WRIGHT, Jonathan

IPC分类号： C07D473/00 ,  C07D473/32 ,  A61K31/52 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D473/00 ,  A61K31/52 ,  C07D473/32

摘要： Provided herein are Aminopurine Compounds having the following structure: (I) wherein R1 , R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.

公开(公告)号：EP1556374A2

公开(公告)日：2005-07-27

申请号：EP03777639.0

申请日：2003-10-15

申请人： Signal Pharmaceuticals, Inc.

发明人： FRIEDMAN, Glenn ,  MCKIE, Jeffrey ,  WRIGHT, Jonathan

IPC分类号： C07D405/02 ,  A61K31/40

CPC分类号： C07D311/16 ,  A61K31/40

摘要： This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.

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：EP1212621A1

公开(公告)日：2002-06-12

申请号：EP00959571.1

申请日：2000-08-29

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： HOEKSTRA, Merl, F. ,  XIE, Weilin ,  MURRAY, Brion, W. ,  MERCURIO, Frank, M.

IPC分类号： G01N33/68 ,  C12Q1/25 ,  G01N33/50 ,  G01N33/566

CPC分类号： G01N33/74 ,  C12Q1/25 ,  G01N2333/495 ,  G01N2500/10

摘要： Methods are provided for identifying agents that modulate signaling mediated by transforming growth factor beta (TGF-β) and members of the TGF-β family, such as bone morphogenic protein (BMP). Such agents may be identified using screens that evaluate candidate agents for the ability to modulate Smad protein degradation. Agents identified as described herein may be used to augment or inhibit signaling mediated by one or more TGF-β family members in a variety of cell types and for therapeutic purposes.

公开(公告)号：EP1060245A2

公开(公告)日：2000-12-20

申请号：EP99912239.3

申请日：1999-03-02

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： LI, Ronghao ,  SAH, Dinah, W., Y.

IPC分类号： C12N5/10 ,  C12Q1/00

CPC分类号： C12N5/0623 ,  C12N2503/00 ,  C12N2510/04

摘要： Conditionally-immortalized human spinal cord cell lines are provided. Such cell lines, which may be clonal, may be used to generate neurons, including motoneurons. The cell lines and/or differentiated cells may be used for the development of therapeutic agents to prevent and treat a variety of spinal cord-related diseases and injuries. The cell lines and/or differentiated cells may also be used in assays and for the general study of spinal cord cell development and differentiation.

公开(公告)号：EP1009824A1

公开(公告)日：2000-06-21

申请号：EP98908593.1

申请日：1998-02-18

申请人： SIGNAL PHARMACEUTICALS, INC. ,  YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM

发明人： MANNING, Anthony ,  MERCURIO, Frank ,  ALKALAY, Irit ,  BEN-NERIAH, Yinon ,  CIECHANOVER, Aaron ,  YARON, Avraham

IPC分类号： C12N15/12 ,  C07K14/47 ,  G01N33/50 ,  A61K38/10 ,  A61K38/17 ,  C07K7/00 ,  C07K14/435 ,  C12N5/10 ,  C12N1/21 ,  C12N1/19

CPC分类号： C07K14/4702 ,  A61K38/00

摘要： Compositions and methods for modulating the activation of nuclear factor λB (NF-λB) are provided. The compositions comprise one or more agents that modulate ubiquitination of phosphorylated IλBα and/or IλBβ. Such compositions may be used for treating diseases associated with NF-λB activation. Modulating agents include peptides that comprise a recognition domain for E3 ubiquitin ligase.

公开(公告)号：EP0850228A1

公开(公告)日：1998-07-01

申请号：EP96933070.0

申请日：1996-08-30

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： SUTO, Mark, J. ,  GOLDMAN, Mark, E. ,  GAYO, Leah, M. ,  RANSONE-FONG, Lynn, J. ,  PALANKI, Moorthy, S., S. ,  SULLIVAN, Robert, W.

IPC分类号： A61K31 ,  A61P29 ,  C07D239 ,  C07D241 ,  C07D403

CPC分类号： C07D239/28 ,  C07D239/30 ,  C07D239/34 ,  C07D239/42 ,  C07D241/24 ,  C07D403/12

摘要： Compounds having utility as anti-inflammatory agents in general and, more specifically, for the prevention and/or treatment of immuno-inflammatory and autoimmune diseases are disclosed. The compounds are pyrimidine- or pyrazine-containing compounds and, in one embodiment, are carboxyamides of the same. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof and effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

公开(公告)号：EP1450812A2

公开(公告)日：2004-09-01

申请号：EP02768950.4

申请日：2002-10-03

申请人： Signal Pharmaceuticals, Inc.

发明人： ZELDIS, Jerome, B.

IPC分类号： A61K31/535 ,  A61K31/445 ,  A61K31/415 ,  A61K31/40 ,  A61K31/35

CPC分类号： A61K31/5377 ,  A61K31/37 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4433

摘要： This invention relates to methods for using benzopyranones, or their pharaceutically acceptable salts, for treating or preventing a primary brain cancer or a brain metastasis. The benzopyranones have the formula (I), wherein R1, R2, R3, n and p are as defined herein.

公开(公告)号：EP1363891A2

公开(公告)日：2003-11-26

申请号：EP02720975.8

申请日：2002-02-13

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： SAKATA, Steven, T. ,  RAYMON, Heather, K.

IPC分类号： C07D275/04 ,  A61K31/425 ,  A61P43/00 ,  C07D417/12

CPC分类号： C07D275/04 ,  C07D417/12

摘要： Isothiazoloanthrones, isoxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula (VI), and pharmaceutically acceptable salts thereof, wherein R0 is -CH2-, -SO-, -O-, -SO2-, or -S-; compositions comprising the isothiazoloanthrones, isoxazoloanthrones, isoindolanthrones, and derivatives thereof; and methods for treating or preventing a disorder alleviated by inhibiting Jun N-terminal kinase (JNK) by administering the isothiazoloanthrones, isoxazoloanthrones, isoindolanthrones, and derivatives thereof are described herein.