公开(公告)号：EP1945644A2

公开(公告)日：2008-07-23

申请号：EP06837322.4

申请日：2006-11-08

申请人： Schering Corporation

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

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 imidazopyrazine 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.

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.

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.

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.

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.

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.

公开(公告)号：EP2225247A1

公开(公告)日：2010-09-08

申请号：EP08854702.1

申请日：2008-11-25

申请人： Schering Corporation

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

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

CPC分类号： C07D487/04

摘要： Pyrazolo[1,5-a]pyrimidine-based inhibitors of various kinase, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions that contain such inhibitors are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 or CHK-1 inhibitor compounds, methods of inhibiting CDK-2 or CHK-1, and methods for treating disease or disease symptoms.

公开(公告)号：EP1436281B1

公开(公告)日：2010-06-16

申请号：EP02773770.9

申请日：2002-10-15

申请人： Schering Corporation

发明人： GUZI, Timothy, J. ,  PARUCH, Kamil

IPC分类号： C07D401/06 ,  A61K31/495

CPC分类号： C07D401/12 ,  C07D211/34

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 17β-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.

公开(公告)号：EP2069348A2

公开(公告)日：2009-06-17

申请号：EP07839217.2

申请日：2007-10-02

申请人： Schering Corporation

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

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.

公开(公告)号：EP1934225A1

公开(公告)日：2008-06-25

申请号：EP06825456.4

申请日：2006-10-04

申请人： Schering Corporation

发明人： PARUCH, Kamil ,  GUZI, Timothy, J. ,  DWYER, Michael, P. ,  SHIPPS, Gerald, W., Jr.

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. Formula (I).