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1.发明授权NOVEL 4-CYANO, 4-AMINO, AND 4-AMINOMETHYL DERIVATIVES OF PYRAZOLO[1,5-a]PYRIDINES, PYRAZOLO[1,5-c]PYRIMIDINES AND 2H-INDAZOLE COMPOUNDS AND 5-CYANO, 5-AMINO, AND 5-AMINOMETHYL DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINES, AND IMIDAZO[1,5-a]PYRAZINES COMPOUNDS AS CYCLIN DEPENDENT KINASE INHI 有权NEW 4-氰基，4-氨基，吡唑并和4- AMINOMETHYLDERIVATIVE [1,5-α]吡啶，吡唑并[1,5-C]嘧啶和用于-2H-吲唑和5-氰基，5-氨基和 咪唑并[1,2-A]吡啶的5- AMINOMETHYLDERIVATIVE，和咪唑并[1,5-a]吡嗪化合物作为CYCLINABHÄNGGEN激酶抑制剂
公开(公告)号：EP1931641B1
公开(公告)日：2010-08-25
申请号：EP06802808.3
申请日：2006-08-31
申请人： Schering Corporation
IPC分类号： C07D231/56 , C07D401/12 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/416 , A61P29/00 , A61P35/00
CPC分类号： C07D231/56 , C07D401/12 , C07D471/04 , C07D487/04
摘要： In its many embodiments, the present invention provides compounds (I) which are a novel class of 4- cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridine, pyrazolo[1,5-c]pyrimidine, and 2H-Indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridine and imidazo[1,5-a]pyrazine 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. Formula (I) wherein X is C or N.
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公开(公告)号：EP2155725A1
公开(公告)日：2010-02-24
申请号：EP08768096.3
申请日：2008-06-04
申请人： Schering Corporation
发明人： LABROLI, Marc, A. , POKER, Cory, Seth , GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , KEERTIKAR, Kartik, M. , ALVAREZ, Carmen, S.
IPC分类号： C07D403/04
CPC分类号： C07D231/38 , C07D401/04 , C07D417/04
摘要： The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1′H-4,4′-bispyrazole.
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公开(公告)号：EP2069349A2
公开(公告)日：2009-06-17
申请号：EP07839218.0
申请日：2007-10-02
申请人： Schering Corporation
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), 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.
摘要翻译： 在其许多实施方案中，本发明提供了一类作为细胞周期蛋白依赖性激酶（CDK）抑制剂的吡唑并[1,5-a]嘧啶化合物，制备这类化合物的方法，含有一种或多种此类化合物的药物组合物，制备 包含一种或多种此类化合物的药物制剂，以及使用此类化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。
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公开(公告)号：EP1931675A2
公开(公告)日：2008-06-18
申请号：EP06816216.3
申请日：2006-10-04
申请人： Schering Corporation
IPC分类号： C07D487/04 , A61K31/4162 , A61P35/00
CPC分类号： C07D487/04
摘要： in its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.
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公开(公告)号：EP1534709B1
公开(公告)日：2007-06-13
申请号：EP03749317.8
申请日：2003-09-03
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , DOLL, Ronald, J. , GIRIJAVALLABHAN, Viyyoor, Moopil , DILLARD, Lawrence, W. , TRAN, Vinh, D. , HE, Zhen Min , JAMES, Ray, Anthony , PARK, Haengsoon
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P35/00
CPC分类号： C07D487/04
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.
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6.发明授权17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 3 INHIBITORS FOR THE TREATMENT OF ANDROGEN DEPENDENT DISEASES 有权17β-羟基类固醇脱氢酶3抑制剂FOR疾病治疗的雄激素依赖性的
公开(公告)号：EP1423381B1
公开(公告)日：2007-01-03
申请号：EP02761567.3
申请日：2002-09-05
申请人： SCHERING CORPORATION
发明人： GUZI, Timothy J. , PARUCH, Kamil , MALLAMS, Alan K. , RIVERA, Jocelyn, D. , DOLL, Ronald, J. , GIRIJAVALLABHAN, Viyyoor, M. , PACHTER, Jonathan , LIU, Yi-Tsung , SAKSENA, Anil, K.
IPC分类号： C07D401/06 , A61K31/496 , C07D241/04 , C07D409/14 , A61P35/00
CPC分类号： C07D211/34 , C07D211/48 , C07D295/185 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/02 , C07D409/12 , C07D409/14 , C07D417/12
摘要： There are disclosed compounds of the formula (I), prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17beta-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.
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公开(公告)号：EP1720883A1
公开(公告)日：2006-11-15
申请号：EP05723498.1
申请日：2005-02-23
申请人： SCHERING CORPORATION
发明人： GUZI, Timothy, J. , PARUCH, Kamil
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, 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 kinases using such compounds or pharmaceutical compositions.
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8.发明公开PYRAZOLO[1,5-A]PYRIMIDINE COMPOUNDS AS CYCLIN DEPENDENT KINASE INHIBITORS 有权并[1,5-A]嘧啶类作为抑制剂细胞周期蛋白依赖性激酶
公开(公告)号：EP1534712A2
公开(公告)日：2005-06-01
申请号：EP03796321.2
申请日：2003-09-03
发明人： GUZI, Timothy, J. , PARUCH, Kamil , DWYER, Michael, P. , DOLL, Ronald, J. , GIRIJAVALLABHAN, Viyyoor, Moopil , ALVAREZ, Carmen, S. , CHAN, Tin-Yau , KNUTSON, Chad , MADISON, Vincent , FISCHMANN, Thierry, O. , DILLARD, Lawrence, W. , TRAN, Vinh, D. , HE, Zhen Min , JAMES, Ray, Anthony , PARK, Haengsoon
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P35/00
CPC分类号： C07D487/04
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.
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9.发明授权PYRAZOLOPYRIMIDINE-DERIVATIVES AS CYCLIN DEPENDENT KINASE INHIBITORS 有权PYRAZOLOPYRIMIDINDERIVATE作为抑制剂细胞周期蛋白依赖性激酶
公开(公告)号：EP1720882B1
公开(公告)日：2011-01-05
申请号：EP05722809.0
申请日：2005-02-08
发明人： GUZI, Timothy J. , PARUCH, Kamil , DWYER, Michael P. , DOLL, Ronald J. , GIRIJAVALLABHAN, Viyyoor Moopil , MALLAMS, Alan , ALVAREZ, Carmen S. , KEERTIKAR, Kartik M. , RIVERA, Jocelyn , CHAN, Tin-Yau , MADISON, Vincent , FISCHMANN, Thierry O. , DILLARD, Lawrence W. , TRAN, Vinh D. , HE, Zhen Min , JAMES, Ray Anthony , PARK, Haengsoon , PARADKAR, Vidyadhar M. , HOBBS, Douglas Walsh
IPC分类号： C07D487/04 , A61K31/495 , A61P35/00
CPC分类号： C07D487/04 , A61K31/495
摘要： In its many embodiments, the present invention provides 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.
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10.发明公开NOVEL MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS 有权细胞周期检查点和新的调节剂及其使用结合CHECKPOINT激酶抑制剂
公开(公告)号：EP2217611A1
公开(公告)日：2010-08-18
申请号：EP08847725.2
申请日：2008-11-05
申请人： Schering Corporation
发明人： GUZI, Timothy, J. , PARRY, David, A. , LABROLI, Marc, A. , DWYER, Michael, P. , PARUCH, Kamil , ROSNER, Kristen, E. , SHEN, Ruichao , POPOVICI-MULLER, Janeta
IPC分类号： C07H19/073 , C07H19/067 , A61K31/7068 , A61P35/00
CPC分类号： C07H19/067 , C07H19/073
摘要： In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.
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