公开(公告)号：EP1931676A1

公开(公告)日：2008-06-18

申请号：EP06816408.6

申请日：2006-10-04

申请人： Schering Corporation

发明人： PARUCH, Kamil ,  GUZI, Timothy, J. ,  DWYER, Michael, P. ,  ALVAREZ, Carmen, S.

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P25/00 ,  A61P19/00 ,  A61P9/00

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of amino- substituted pyrazolo[l , 5 -a] pyrimidine compounds represented by the structural formula (I) 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.

公开(公告)号：EP1539756B1

公开(公告)日：2007-11-14

申请号：EP03786514.4

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 imidazo[1,2-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.

公开(公告)号：EP1539756A2

公开(公告)日：2005-06-15

申请号：EP03786514.4

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 imidazo[1,2-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.

公开(公告)号：EP1534710A1

公开(公告)日：2005-06-01

申请号：EP03749347.5

申请日：2003-09-03

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

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 ,  A61K31/519 ,  A61K31/52 ,  A61K31/704 ,  A61K31/7072 ,  A61K45/06 ,  A61K2300/00

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.

公开(公告)号：EP1534709A1

公开(公告)日：2005-06-01

申请号：EP03749317.8

申请日：2003-09-03

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

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.

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抑制剂的新型吡唑并[1,5-a]嘧啶化合物，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包含一种或多种这样的化合物以及使用这些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。

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.

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.

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.

公开(公告)号：EP1945643A2

公开(公告)日：2008-07-23

申请号：EP06837219.2

申请日：2006-11-08

申请人： Schering Corporation

发明人： GUZI, Timothy, J. ,  PARUCH, Kamil ,  DWYER, Michael, P. ,  ZHAO, Lianyun ,  CURRAN, Patrick, J. ,  BELANGER, David, B. ,  HAMANN, Blake ,  REDDY, Panduranga, A. ,  SIDDIQUI, Arshad, M.

IPC分类号： C07D487/04 ,  A61K31/498 ,  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 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.

公开(公告)号：EP1543008B1

公开(公告)日：2007-11-07

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.