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71. 发明公开

EP2217595A1 DIAMIDO THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： DIAMIDOTHIAZOLDERIVATE ALS PROTEINKINASEINHIBITOREN
公开(公告)号：EP2217595A1
公开(公告)日：2010-08-18
申请号：EP08843554.0
申请日：2008-10-27
申请人： Schering Corporation
发明人： LABROLI, Marc, A. , POKER, Cory, Seth , WONG, Tzu, T. , REDDY, Panduranga, Adulla, P. , GUZI, Timothy, J. , SIDDIQUI, M. Arshad
IPC分类号： C07D417/12 , C07D417/14 , A61K31/427 , A61P35/00
CPC分类号： C07D417/14 , C07D417/12
摘要： The present invention relates to novel Diamido Thiazole Derivatives of structure I, compositions comprising the Diamido Thiazole Derivatives, and methods for using the Diamido Thiazole Derivatives for treating or preventing a proliferative disorder, an anti -proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase. Formula (I) wherein: M is -C(O)-, -C(S)-. -S(O)-. -S(O)2-. -NHS(O)2-. -OC(O)- or -NHC(O)-; Q is:formula (II).

72. 发明授权

EP1572299B1 17 BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 3 INHIBITORS FOR THE TREATMENT OF ANDROGEN DEPENDENT DISEASES 有权
标题翻译：第17β-羟基TYPE 3用于治疗雄激素病抑制剂
公开(公告)号：EP1572299B1
公开(公告)日：2008-09-24
申请号：EP03790505.6
申请日：2003-12-15
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , LIU, Yi-Tsung , DOLL, Ronald, J. , SAKSENA, Anil , GIRIJAVALLABHAN, Viyyoor, M. , PACHTER, Jonathan, A.
IPC分类号： A61P5/28 , A61P35/00 , A61K31/496 , A61K31/4545 , C07D401/14
CPC分类号： C07D401/14 , A61K31/435 , A61K31/495 , A61K31/56 , A61K45/06 , C07D211/16 , C07D241/04 , C07D241/08 , C07D401/04 , C07D401/06 , A61K2300/00
摘要： The present invention provides a novel class of compounds of formula (I): as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17β-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.

73. 发明公开

EP1934224A1 PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS FOR THE TREATMENT OF CANCER 有权转让
标题翻译：吡唑并嘧啶作为细胞周期激酶用于治疗癌症的抑制剂
公开(公告)号：EP1934224A1
公开(公告)日：2008-06-25
申请号：EP06816244.5
申请日：2006-10-04
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P.
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to Pyrazolo [1,5-a]pyrimidine compounds of formula III usefu as protein kinase inhibitors, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases such as, for example, cancer, inflammation, arthritis, viral diseases, neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, and fungal diseases (Formula III), wherein : R is an aryl substituted with one or more heteroaryl; R2 is selected from the group consisting of R9, alkyl, alkynyl, alkynylalkyl, cycloalkyl, -CF3, -C(O2)R6, aryl, arylalkyl, heteroarylalkyl, heterocyclyl, alkyl substituted with 1-6 R9 groups which groups can be the same or different with each R9 being independently selected, aryl substituted with 1-3 aryl or heteroaryl groups which can be the same or different and are independently selected from phenyl, pyridyl, thiophenyl, furanyl and thiazolo groups, (a), (b), (c) and (d), and heteroaryl substituted with 0-3 aryl or heteroaryl groups which can be the same or different and are independently selected from alkyl, phenyl, pyridyl, thiophenyl, furaπyl and thiazolo groups; R3 is selected from the group consisting of H, halogen, -NR5R6, -C(O)NR5R6, alkyl, alkynyl, cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl, etc; R4 is H halo or alkyl.

74. 发明公开

EP1931677A2 NOVEL PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS 有权转让
标题翻译：新型吡AS细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：EP1931677A2
公开(公告)日：2008-06-18
申请号：EP06836186.4
申请日：2006-10-04
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , LABROLI, Marc , KEERTIKAR, Kartik, M.
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , Y02P20/582
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1 ,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

75. 发明授权

EP1539750B1 PYRAZOLOPYRIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS 有权转让
标题翻译： PYRAZOLOPYRIMDINE作为抑制剂细胞周期蛋白依赖性激酶
公开(公告)号：EP1539750B1
公开(公告)日：2007-12-26
申请号：EP03752559.9
申请日：2003-09-17
申请人： Schering Corporation
发明人： DWYER, Michael, P. , GUZI, Timothy, J. , PARUCH, Kamil , DOLL, Ronald, J. , KEERTIKAR, Kartik, M. , GIRIJAVALLABHAN, Viyyoor, M.
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyridine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

76. 发明公开

EP1543008A1 IMIDAZOPYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS 有权转让
标题翻译：咪唑并吡嗪作为CDK抑制剂的
公开(公告)号：EP1543008A1
公开(公告)日：2005-06-22
申请号：EP03754658.7
申请日：2003-09-19
申请人： SCHERING CORPORATION
发明人： PARUCH, Kamil , GUZI, Timothy, J. , DWYER, Michael, P. , DOLL, Ronald, J. , GIRIJAVALLABHAN, Viyyoor, M. , MALLAMS, Alan, K.
IPC分类号： C07D487/04 , A61K31/495 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds of formula (III) as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

77. 发明公开

EP1539750A1 PYRAZOLOPYRIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS 有权转让
标题翻译： PYRAZOLOPYRIMDINE作为抑制剂细胞周期蛋白依赖性激酶
公开(公告)号：EP1539750A1
公开(公告)日：2005-06-15
申请号：EP03752559.9
申请日：2003-09-17
申请人： SCHERING CORPORATION
发明人： DWYER, Michael, P. , GUZI, Timothy, J. , PARUCH, Kamil , DOLL, Ronald, J. , KEERTIKAR, Kartik, M. , GIRIJAVALLABHAN, Viyyoor, M.
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyridine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

78. 发明公开

EP2212318A1 THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权转让
标题翻译：噻唑衍生物作为蛋白激酶抑制剂
公开(公告)号：EP2212318A1
公开(公告)日：2010-08-04
申请号：EP08845572.0
申请日：2008-10-27
申请人： Schering Corporation
发明人： REDDY, Panduranga, Adulla, P. , WONG, Tzu, T. , ZHAO, Lianyun , TANG, Shuyi , LABROLI, Marc, A. , GUZI, Timothy, J. , SIDDIQUI, M. Arshad
IPC分类号： C07D417/12 , C07D417/14 , C07D491/056 , C07D495/04 , A61K31/427 , A61P35/00
CPC分类号： C07D417/12 , C07D417/14 , C07D471/10 , C07D491/056 , C07D495/04
摘要： The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.

79. 发明授权

EP1934224B1 PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS FOR THE TREATMENT OF CANCER 有权转让
标题翻译：吡唑并嘧啶作为细胞周期激酶用于治疗癌症的抑制剂
公开(公告)号：EP1934224B1
公开(公告)日：2010-06-09
申请号：EP06816244.5
申请日：2006-10-04
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P.
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to Pyrazolo [1,5-a]pyrimidine compounds of formula III usefu as protein kinase inhibitors, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases such as, for example, cancer, inflammation, arthritis, viral diseases, neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, and fungal diseases (Formula III), wherein : R is an aryl substituted with one or more heteroaryl; R2 is selected from the group consisting of R9, alkyl, alkynyl, alkynylalkyl, cycloalkyl, -CF3, -C(O2)R6, aryl, arylalkyl, heteroarylalkyl, heterocyclyl, alkyl substituted with 1-6 R9 groups which groups can be the same or different with each R9 being independently selected, aryl substituted with 1-3 aryl or heteroaryl groups which can be the same or different and are independently selected from phenyl, pyridyl, thiophenyl, furanyl and thiazolo groups, (a), (b), (c) and (d), and heteroaryl substituted with 0-3 aryl or heteroaryl groups which can be the same or different and are independently selected from alkyl, phenyl, pyridyl, thiophenyl, furaπyl and thiazolo groups; R3 is selected from the group consisting of H, halogen, -NR5R6, -C(O)NR5R6, alkyl, alkynyl, cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl, etc; R4 is H halo or alkyl.

80. 发明公开

EP2027127A1 PYRAZOLO [1, 5-A]PYRIMIDINES AS CDK INHIBITORS 审中-公开
标题翻译：吡咯并[1,5-A]吡咯烷酮ALS CDK-HEMMER
公开(公告)号：EP2027127A1
公开(公告)日：2009-02-25
申请号：EP07795066.5
申请日：2007-05-21
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , DOLL, Ronald, J. , NOMEIR, Amin, A.
IPC分类号： C07D487/04 , A61K31/52 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) which can have utility as inhibitors of cyclin dependent kinases ('CDKs') as well as methods of preparing such compounds. The compounds can have potential utility for the treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs.

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