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112. 发明专利

DE60317353T2 未知
公开(公告)号：DE60317353T2
公开(公告)日：2008-08-28
申请号：DE60317353
申请日：2003-09-19
申请人： SCHERING CORP
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
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.

113. 发明专利

PE09742008A1 NUEVAS PIROZOLOPIRIMIDINAS COMO INHIBIDORES DE QUINASA DEPENDIENTES DE CICLINA 未知
公开(公告)号：PE09742008A1
公开(公告)日：2008-07-19
申请号：PE0013312007
申请日：2007-10-02
申请人： SCHERING CORP
发明人： GUZI TIMOTHY J , DWYER MICHAEL P , LABROLI MARC , KEERTIKAR KARTIK M , PARUCH KAMIL
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： SE REFIERE A UN COMPUESTO DERIVADO DE PIRAZOLO[1,5-a]PIRIMIDINA SELECCIONADA DE 3-(TIAZOL-4-IL)-5-(PIPERAZIN-3-IL)-6-BROMO-7-AMINO-PIRAZOLO[1,5-a]PIRIMIDINA; 3-(1-METIL-PIRAZOL-4-IL)-5-(PIPERAZIN-3-IL)-6-IODO-7-AMINO-PIRAZOLO[1,5-a]PIRIMIDINA; 3-(1-METILPIRAZOL-4-IL)-5-(1-AMINOCICLOPENTIL-3-IL)-6-BROMO-7-AMINO-PIRAZOLO[1,5-a]PIRIMIDINA; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASA DEPENDIENTE DE CICLINA CDK1, CDK2, CDK9, UTILES EN EL TRATAMIENTO DE UNA ENFERMEDAD PROLIFERATIVA SELECCIONADA DE CANCER DE VEJIGA, MAMA, COLON, RINON, HIGADO, PULMON, OVARIO, ENTRE OTROS

114. 发明专利

ES2297203T3 PIRAZOLOPIRIDINAS COMO INHIBIDORES DE QUINASAS DEPENDIENTES DE CICLINA. 未知
公开(公告)号：ES2297203T3
公开(公告)日：2008-05-01
申请号：ES03752559
申请日：2003-09-17
申请人： SCHERING CORP
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
摘要： Un compuesto representado por la fórmula estructural: (Ver fórmula) o una de sus sales o solvatos farmacéuticamente aceptables en donde: R se selecciona del grupo que consiste en alquilo, arilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, arilalquilo, cicloalquilo, -NR 6 R 7 , -C(O)R 7 , -C(O)OR 6 , -C(O)NR 6 R 7 y -S(O2)R 7 , en donde cada uno de dichos alquilo, arilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, cicloalquilo y arilalquilo pueden estar no sustituidos u opcionalmente sustituidos independientemente con uno o más restos que pueden ser iguales o diferentes, seleccionándose cada resto independientemente del grupo que consiste en halógeno, alquilo, CF3, CN, -OCF3, -OR 6 , -C(O)R 7 , -NR 6 R 7 , -C(O)OR 6 , -C(O)NR 6 R 7 , -SR 6 , -S(O2)R 7 , -S(O2)NR 6 R 7 , -N(R 5 )S(O2)R 7 , -N(R 6 )C(O)R 8 y -N(R 5 )C (O)NR 6 R 7 y NO2; R 2 se selecciona del grupo que consiste en hidrógeno, R 9 , alquilo, alquenilo, alquinilo, alquenilalquilo, alquinilalquilo, arilo, arilalquilo, heteroarilo, heteroarilquilo, heterociclilo, heterociclilalquilo, cicloalquilo, cicloalquilalquilo, -CF3, -C(O)R 7 , -NR 6 R 7 , -C(O)OR 6 , -C(O)NR 5 R 6 , alquilo sustituido con 1-6 grupos R 9 , pudiendo dichos grupos ser iguales o diferentes con cada R 9 que se selecciona independientemente, (Ver fórmula) en donde cada uno de dichos arilo, heteroarilo, arilalquilo y heterociclilo pueden estar no sustituido u opcionalmente sustituido de forma independiente con uno o más restos que pueden ser iguales o diferentes, seleccionándose cada resto independientemente del grupo que consiste en halógeno, alquilo, cicloalquilo, CF3, CN, -OCF3, -OR 6 , -C(O) R 7 , -NR 6 R 7 , -C(O)OR 6 , -C(O)NR 5 R 6 , -SR 6 , -S(O2)R 7 , -S(O2)NR 5 R 6 , -N(R 5 )S(O2)R 7 , -N(R 5 )C(O)R 7 y -N(R 5 )C(O) NR 5 R 6 ; R 3 se selecciona de...

115. 发明专利

ES2293068T3 IMIDAZOPIRIDINAS COMO INHIBIDORES DE QUINASAS DEPENDIENTES DE CICLINA. 未知
公开(公告)号：ES2293068T3
公开(公告)日：2008-03-16
申请号：ES03786514
申请日：2003-09-17
申请人： SCHERING CORP
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
摘要： Un compuesto de la fórmula: (Ver fórmula) o una deUn compuesto de la fórmula: (Ver fórmula) sus sales o solvatos farmacéuticamente aceptables.

116. 发明专利

DE60318321D1 PYRAZOLOPYRIMDINE ALS HEMMSTOFFE CYCLIN ABHÄNGIGER KINASEN 未知
公开(公告)号：DE60318321D1
公开(公告)日：2008-02-07
申请号：DE60318321
申请日：2003-09-17
申请人： SCHERING CORP
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
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.

117. 发明专利

AU2005217617B2 Pyrazolotriazines as kinase inhibitors 未知
公开(公告)号：AU2005217617B2
公开(公告)日：2007-12-06
申请号：AU2005217617
申请日：2005-02-23
申请人： SCHERING CORP
发明人： GUZI TIMOTHY J , PARUCH KAMIL
IPC分类号： A61K31/53 , 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.

118. 发明专利

AU2003215389B2 Farnesyl protein transferase inhibitors as antitumor agents 未知
公开(公告)号：AU2003215389B2
公开(公告)日：2007-10-18
申请号：AU2003215389
申请日：2003-02-25
申请人： PHARMACOPEIA INC , SCHERING CORP
发明人： DOLL RONALD J , BALDWIN JOHN J , ZHU HUGH Y , COOPER ALAN B , BISHOP W ROBERT , DESAI JAGDISH A , LI GE , VIBULBHAN BANCHA , PINTO PATRICK A , MINOR KEITH P , WANG JAMES J-S , NJOROGE F GEORGE , KEERTIKAR KARTIK M , SANTHANAM BAMA , HUANG CHIA-YU , RANE DINANATH F , ALVAREZ CARMEN S , GIRIJAVALLABHAN VIYYOOR MOOPIL , GUZI TIMOTHY J , JAMES RAY A
IPC分类号： C07D221/16 , A61K31/496 , A61K45/00 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/06 , C07D401/14 , C07D521/00
摘要： Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

119. 发明专利

PE07232007A1 IMIDAZOPIRAZINAS COMO INHIBIDORES DE QUINASAS DEPENDIENTES DE CICLINA 未知
公开(公告)号：PE07232007A1
公开(公告)日：2007-08-10
申请号：PE0013972006
申请日：2006-11-08
申请人： SCHERING CORP
发明人： GUZI TIMOTHY J , DWYER MICHAEL P , ZHAO LIANYUN , CURRAN PATRICK J , BELANGER DAVID B , HAMANN BLAKE , REDDY PANDURANGA A , SIDDIQUI M ARSHAD , PARUCH KAMIL
IPC分类号： A61K31/498 , A61K31/506 , C07D487/00 , C07D487/02
CPC分类号： C07D487/04
摘要： REFERIDA A UN COMPUESTO DERIVADO DE IMIDAZOPIRAZINA DE FORMULAS (a), (b), (c), (d), ENTRE OTRAS O UNA SAL, SOLVATO O ESTER DE LOS MISMOS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE PROTEINA QUINASA TALES COMO QUINASAS DEPENDIENTES DE CICLINA, PROTEINA QUINASA ACTIVADA POR MITOGENO, GLUCOGENO SINTASA QUINASA 3 Y SIMILARES, Y SON UTILES EN EL TRATAMIENTO DEL CANCER, INFLAMACION, ARTRITIS, ENFERMEDADES VIRALES, ENFERMEDADES NEURODEGENERATIVAS, CARIOVASCULARES Y FUNGICAS

120. 发明专利

CA2624822A1 PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS FOR THE TREATMENT OF CANCER 未知
公开(公告)号：CA2624822A1
公开(公告)日：2007-04-19
申请号：CA2624822
申请日：2006-10-04
申请人： SCHERING CORP
发明人： GUZI TIMOTHY J , DWYER MICHAEL P , PARUCH KAMIL
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
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, fura.pi.yl 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.

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