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61. 发明专利

MXPA04003611A PIPERIDINA- Y PIPERAZINACETAMINAS COMO INHIBIDORES DE LA 17 BETA-HIDROXIESTEROIDE DESHIDROGENASA TIPO 3 PARA EL TRATAMIENTO DE ENFERMEDADES ANDROGENO-DEPENDIENTES. 未知
公开(公告)号：MXPA04003611A
公开(公告)日：2004-07-30
申请号：MXPA04003611
申请日：2002-10-15
申请人： SCHERING CORP
发明人： PARUCH KAMIL
IPC分类号： C07D401/06 , A61K31/496 , A61K45/00 , A61P5/28 , A61P13/08 , A61P15/00 , A61P17/10 , A61P17/14 , A61P35/00 , A61P35/02 , A61P43/00 , C07D211/34 , C07D401/12 , C07D401/14 , A61K31/495
摘要： Se describen compuestos de la formula (I)Sus profarmacos, o las sales aceptables para uso farmaceutico de los compuestos o de dichos profamacos, que son utiles como inhibidores de la 17??-Hidroxiesteroide Deshidrogenasa Tipo 3; se describen, ademas, compasiones farmaceuticas que contienen dichos compuestos y su uso para el tratamiento o la prevencion de enfermedades androgeno-dependientes.

62. 发明专利

AU2003295332A1 NOVEL IMIDAZOPYRIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS 未知
公开(公告)号：AU2003295332A1
公开(公告)日：2004-04-08
申请号：AU2003295332
申请日：2003-09-17
申请人： SCHERING CORP
发明人： PARUCH KAMIL , DOLL RONALD J , KEERTIKAR KARTIK M , GIRIJAVALLABHAN VIYYOOR M , DWYER MICHAEL P , GUZI TIMOTHY J
IPC分类号： A61P35/00 , C07D471/04 , C07D471/00
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.

63. 发明专利

CA2499874A1 NOVEL IMIDAZOPYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS 未知
公开(公告)号：CA2499874A1
公开(公告)日：2004-04-01
申请号：CA2499874
申请日：2003-09-19
申请人： SCHERING CORP
发明人： DWYER MICHAEL P , PARUCH KAMIL , DOLL RONALD J , GUZI TIMOTHY J , GIRIJAVALLABHAN VIYYOOR M
IPC分类号： C07D487/04 , A61P35/00 , A61K31/4985
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.

64. 发明专利

AU2003265901A1 PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS 未知
公开(公告)号：AU2003265901A1
公开(公告)日：2004-03-29
申请号：AU2003265901
申请日：2003-09-03
申请人： SCHERING CORP
发明人： KNUTSON CHAD , MCKITTRICK BRIAN , DILLARD LAWRENCE W , TRAN VINH D , HE ZHEN MIN , JAMES RAY ANTHONY , PARK HAENGSOON , GUZI TIMOTHY J , PARUCH KAMIL , DWYER MICHAEL P , DOLL RONALD J , GIRIJAVALLABHAN VIYYOOR MOOPIL
IPC分类号： A61P35/00 , C07D487/04 , A61K31/50
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.

65. 发明专利

NZ567187A Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 未知
公开(公告)号：NZ567187A
公开(公告)日：2011-09-30
申请号：NZ56718706
申请日：2006-10-04
申请人： SCHERING CORP
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
摘要： The disclosure relates to a particular class of pyrazolo[1,5-a]pyrimidine compounds having the structure as shown herein, which are suitable as inhibitors of cyclin dependent kinases (CDK). The disclosure further relates to 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.

66. 发明专利

CA2463626C PIPERIDINE- AND PIPERAZINEACETAMINES AS 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 3 INHIBITORS FOR THE TREATMENT OF ANDROGEN DEPENDENT DISEASES 未知
公开(公告)号：CA2463626C
公开(公告)日：2011-05-24
申请号：CA2463626
申请日：2002-10-15
申请人： SCHERING CORP
发明人： GUZI TIMOTHY J , PARUCH KAMIL
IPC分类号： C07D401/06 , A61K31/495 , A61K31/496 , A61K45/00 , A61P5/28 , A61P13/08 , A61P15/00 , A61P17/10 , A61P17/14 , A61P35/00 , A61P35/02 , A61P43/00 , C07D211/34 , C07D401/12 , C07D401/14
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 17.beta.-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.

67. 发明专利

CA2497440C PYRAZOLOPYRIMIDINES AS CYCLIN-DEPENDENT KINASE INHIBITORS 未知
公开(公告)号：CA2497440C
公开(公告)日：2011-03-22
申请号：CA2497440
申请日：2003-09-03
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY
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 , A61K31/519 , C07D231/00 , C07D239/00
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.

68. 发明专利

ES2347643T3 PIPERIN- Y PIPERAZINACETAMIDAS COMO INHIBIDORES DE 17BETA HIDROXIESTEROIDE DESHIDROGENASA TIPO 3 PARA EL TRATAMIENTO DE ENFERMEDADES DEPENDIENTES DE ANDROGENOS. 未知
公开(公告)号：ES2347643T3
公开(公告)日：2010-11-03
申请号：ES02773770
申请日：2002-10-15
申请人： SCHERING CORP
发明人： GUZI TIMOTHY J , PARUCH KAMIL
IPC分类号： C07D401/06 , A61K31/495 , A61K31/496 , A61K45/00 , A61P5/28 , A61P13/08 , A61P15/00 , A61P17/10 , A61P17/14 , A61P35/00 , A61P35/02 , A61P43/00 , C07D211/34 , C07D401/12 , C07D401/14
摘要： Un compuesto de la fórmula (I): **(Fórmula)** 5 o una sal farmacéuticamente aceptable o solvato del compuesto, en la que, R1 se selecciona entre el grupo que consiste en arilo, heteroarilo, arilalquilo, heteroarilalquilo y difenilalquilo, cada uno opcionalmente sustituido con uno a seis grupos seleccionados entre el grupo que consiste en: a) halógeno; 10 b)-OCF3 o -OCHF2; c) -CF3; d) -CN; e) alquilo o R18-alquilo; f) heteroalquilo o R18-heteroalquilo; 15 g) arilo o R18-arilo; h) heteroarilo o R18-heteroarilo; i) arilalquilo o R18-arilalquilo; j) heteroarilalquilo o R18-heteroarilalquilo; k) hidroxi; 20 I) alcoxi; m) ariloxi; n) -SO2-alquilo; o)-NR11R12; p)-N(R11)C(O)R13, q) metilendioxi; 5 r) difluorometilendioxi; s) trifluoroalcoxi; t) -SCH3 o -SCF3; y u) -SO2CF3 o -NHSO2CF3; cada uno de R2 y R3 se selecciona independientemente entre el grupo que 10 consiste en H, -OH, alcoxi, alquilo, cicloalquilo, heterocicloalquilo, cicloalquilalquilo, trifluoroalquilo, heteroalquilo, arilalquilo, heteroarilalquilo, arilalcoxi, heteroarilalcoxi, -(CH2)n-NR11R12 y -(CH2)n-SR11, con la condición de que cuando X es N, entonces cada uno de R2 y R3 no sea -OH, alcoxi, arilalcoxi o heteroarilalcoxi; 15 cada uno de R4, R5, R7 y R8 se selecciona independientemente entre el grupo que consiste en H, -OR14, -NR11R12, -N(R11)C(O) R13, alquilo, arilo, cicloalquilo, arilalquilo, heteroalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo, con la condición de que cuando Z y/o X es N, entonces cada uno de R4, R5, R7 20 y R8 no sea -OR14, -NR11R12 o -N(R11)C(O)R13; R6 se selecciona entre el grupo que consiste en -C(O)R15 y -SO2R15; cada uno de R9 y R10 se selecciona independientemente entre el grupo que consiste en H, F, -CF3, -CHF2, alquilo, cicloalquilo, arilalquilo, heteroalquilo, heteroarilalquilo, heterocicloalquilo, hidroxi, alcoxi, ariloxi, -NR11R12 y - 25 N(R11)C(O)R13, con la condición de que cuando Z es N, entonces cada uno de R9 y R10 no sea F, hidroxi, alcoxi, ariloxi, -NR11R12 o -N(R11)C(O)R13; R11 se selecciona entre el grupo que consiste en H, alquilo, arilo y heteroarilo; R12 se selecciona entre el grupo que consiste en H, alquilo, arilo y heteroarilo; R13 se selecciona entre el grupo que consiste en alquilo, alcoxi y ariloxi; R14 se selecciona entre el grupo que consiste en H, alquilo, arilo y heteroarilo; R15 se selecciona entre el grupo que consiste en -NR16R17, -OR16, alquilo, cicloalquilo, heterocicloalquilo, arilo, arilalquilo y heteroarilalquilo, cada uno opcionalmente sustituido con R18; cada uno de R16 y R17 se selecciona independientemente entre el grupo que consiste en alquilo, arilo, arilalquilo, heteroalquilo y heteroarilo, cada uno opcionalmente sustituido con R18, y H, con la condición de que cuando R15 es - OR16, R16 no sea H; R18 es de uno a cuatro sustituyentes, cada uno seleccionado independientemente entre el grupo que consiste en alquilo inferior, halo, ciano, nitro, haloalquilo, hidroxi, alcoxi, carboxi, carboxialquilo, carboxamida, mercapto, amino, alquilamino, dialquilamino, sulfonilo, sulfonamido, arilo y heteroarilo; cada uno de X y Z se selecciona independientemente entre el grupo que consiste en C y N; y n es 1-4.

69. 发明专利

CA2497544C PYRAZOLO[1,5-A]PYRIMIDINES COMPOUNDS AS CYCLIN DEPENDENT KINASE INHIBITORS 未知
公开(公告)号：CA2497544C
公开(公告)日：2010-11-02
申请号：CA2497544
申请日：2003-09-03
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY
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 , C07D231/00 , C07D239/00
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.

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