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1. 发明专利

AU2007243457A1 Pharmaceutical compounds 未知
公开(公告)号：AU2007243457A1
公开(公告)日：2007-11-08
申请号：AU2007243457
申请日：2007-04-24
申请人： HOFFMANN LA ROCHE , GENENTECH INC , RICHARD GOLDSMITH
发明人： CASTANEDO GEORGETTE , ZHU BING-YAN , FOLKES ADRIAN , SUTHERLIN DANIEL P , WAN NAN CHI , OLIVERO ALAN , HEFFRON TIM , OXENFORD SALLY , SHUTTLEWORTH STEPHEN , GUNZNER JANET , CHUCKOWREE IRINA , MATHIEU SIMON
IPC分类号： C07D491/04 , A61K31/5025 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Compounds of Formulae la and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula la and Ib for in vitro , in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

2. 发明专利

BRPI0710943A2 未知
公开(公告)号：BRPI0710943A2
公开(公告)日：2012-06-26
申请号：BRPI0710943
申请日：2007-04-24
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： GOLDSMITH RICHARD , FOLKES ADRIAN , SHUTTLEWORTH STEPHEN , CHUCKOWREE IRINA S , OXENFORD SALLY , WAN NAN CHI , CASTANEDO GEORGETTE , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , ZHU BING-YAN , SUTHERLIN DANIEL P
IPC分类号： C07D491/04 , A61K31/5025 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Compounds of Formulae la and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula la and Ib for in vitro , in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

3. 发明专利

AU2007243466B2 Phosphoinositide 3-kinase inhibitor compounds and pharmaceutical compositions containing them 未知
公开(公告)号：AU2007243466B2
公开(公告)日：2012-01-19
申请号：AU2007243466
申请日：2007-04-24
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： GUNZNER JANET , WANG SHUMEI , SUTHERLIN DANIEL P , HANCOX TIM , HEFFRON TIM , OXENFORD SALLY , MATHIEU SIMON , ZHU BING-YAN , DOTSON JENNAFER , GOLDSMITH RICHARD , CASTANEDO GEORGETTE , SHUTTLEWORTH STEPHEN , TSUI VICKIE , FOLKES ADRIAN , BAYLISS TRACY , WEISMANN CHRISTIAN , MALESKY KIMBERLY , OLIVERO ALAN
IPC分类号： C07D491/04 , A61K31/519 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Compounds of Formulas (Ia) and (Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula (Ia) and (Ib) for ianddiagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

4. 发明专利

ZA200809546B Pharmaceutical compounds 未知
公开(公告)号：ZA200809546B
公开(公告)日：2010-04-28
申请号：ZA200809546
申请日：2008-11-07
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： FOLKES ADRIAN , SHUTTLEWORTH STEPHEN , CHUCKOWREE IRINA , OXENFORD SALLY , WAN NAN CHI , CASTANEDO GEORGETTE , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , SUTHERLIN DANIEL P , ZHU BING-YAN , GOLDSMITH RICHARD
IPC分类号： A61K20100101 , A61P20100101 , C07D20100101
摘要： Compounds of Formulae la and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula la and Ib for in vitro , in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

5. 发明专利

HK1127356A1 PHARMACEUTICAL COMPOUNDS 未知
公开(公告)号：HK1127356A1
公开(公告)日：2009-09-25
申请号：HK09107370
申请日：2009-08-11
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： FOLKES ADRIAN , SHUTTLEWORTH STEPHEN , CHUCKOWREE IRINA , OXENFORD SALLY , WAN NAN CHI , CASTANEDO GEORGETTE , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , SUTHERLIN DANIEL P , ZHU BING-YAN , GOLDSMITH RICHARD
IPC分类号： C07D20060101
摘要： Compounds of Formulae la and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula la and Ib for in vitro , in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

6. 发明专利

AU2007243466A1 Phosphoinositide 3-kinase inhibitor compounds and pharmaceutical compositions containing them 未知
公开(公告)号：AU2007243466A1
公开(公告)日：2007-11-08
申请号：AU2007243466
申请日：2007-04-24
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： GUNZNER JANET , WANG SHUMEI , SUTHERLIN DANIEL P , HANCOX TIM , HEFFRON TIM , OXENFORD SALLY , MATHIEU SIMON , ZHU BING-YAN , DOTSON JENNAFER , GOLDSMITH RICHARD , CASTANEDO GEORGETTE , SHUTTLEWORTH STEPHEN , TSUI VICKIE , FOLKES ADRIAN , BAYLISS TRACY , WEISMANN CHRISTIAN , MALESKY KIMBERLY , OLIVERO ALAN
IPC分类号： C07D491/04 , A61K31/519 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

7. 发明专利

CA2650295A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OFUSE 未知
公开(公告)号：CA2650295A1
公开(公告)日：2007-11-08
申请号：CA2650295
申请日：2007-04-24
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： WANG SHUMEI , TSUI VICKIE , WEISMANN CHRISTIAN , GUNZNER JANET , OLIVERO ALAN , HANCOX TIM , SUTHERLIN DANIEL P , BAYLISS TRACY , OXENFORD SALLY , SHUTTLEWORTH STEPHEN , HEFFRON TIM , MALESKY KIMBERLY , ZHU BING-YAN , MATHIEU SIMON , CASTANEDO GEORGETTE , GOLDSMITH RICHARD , FOLKES ADRIAN , DOTSON JENNAFER
IPC分类号： C07D491/04 , A61K31/519 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

8. 发明专利

CA2650295C PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：CA2650295C
公开(公告)日：2015-12-29
申请号：CA2650295
申请日：2007-04-24
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： CASTANEDO GEORGETTE , GOLDSMITH RICHARD , GUNZNER JANET , HEFFRON TIM , MALESKY KIMBERLY , MATHIEU SIMON , OLIVERO ALAN , SUTHERLIN DANIEL P , TSUI VICKIE , WANG SHUMEI , WEISMANN CHRISTIAN , ZHU BING-YAN , DOTSON JENNAFER , FOLKES ADRIAN , SHUTTLEWORTH STEPHEN , OXENFORD SALLY , HANCOX TIM , BAYLISS TRACY
IPC分类号： C07D491/04 , A61K31/519 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Compounds of Formulas (Ia) and (Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula (Ia) and (Ib) for in vitro, in situ, and in vivodiagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

9. 发明专利

CA2650290C PHARMACEUTICAL COMPOUNDS 未知
公开(公告)号：CA2650290C
公开(公告)日：2015-11-17
申请号：CA2650290
申请日：2007-04-24
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： FOLKES ADRIAN , SHUTTLEWORTH STEPHEN , CHUCKOWREE IRINA , OXENFORD SALLY , WAN NAN CHI , CASTANEDO GEORGETTE , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , SUTHERLIN DANIEL P , ZHU BING-YAN , GOLDSMITH RICHARD
IPC分类号： C07D491/04 , A61K31/5025 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

10. 发明专利

ES2377358T3 Compuestos farmacéuticos 未知
公开(公告)号：ES2377358T3
公开(公告)日：2012-03-26
申请号：ES07755937
申请日：2007-04-24
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： FOLKES ADRIAN , SHUTTLEWORTH STEPHEN , CHUCKOWREE IRINA , OXENFORD SALLY , WAN NAN CHI , CASTANEDO GEORGETTE , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , SUTHERLIN DANIEL , ZHU BING-YAN , GOLDSMITH RICHARD
IPC分类号： C07D491/04
摘要： Un compuesto que es una pirimidina fusionada de la fórmula (la) o (Ib) : en donde X es O o S; R1 es un grupo de la fórmula: R2 es H, halo o alquilo C1-C6, R4 y R5 forman, junto con el átomo de N al que están unidos, un grupo seleccionado de piperazina, piperidina, pirrolidina, oxazolidinona, diazepan y 2, 5-diaza-biciclo[2, 2, 1]heptano que no está sustituido o que está sustituido con -[ (alk) q-NR]r-S (O) 2- (alk) q-Z o -C (O) - (alk) q-S (O) 2Z, en donde Z es R10 o &8211;NR11R12 o por alquilo C1-C6 no sustituido, hidroxil-alquilo C1-C6, oxo (=O), - (alk) q-OR, -C (O) -C (R') 2-N (R) 2, -C (R) 2C (O) -N (R) 2, C (O) - (NR) q- (alk) q-OR, -C (O) -ciclilo, -C (O) R, -C (O) OR, -C (O) -Tet o &8211;NR13R14; o uno de R4 y R5 es alquilo C1-C6, - (alk) q-heterociclilo o - (alk) q-OR y el otro es un grupo piperazina, piperidina, pirrolidina, sulfonilpirano o - (alk) q-heterociclilo, en donde dicha piperazina, piperidina, pirrolidina, sulfonilpirano o heterociclilo no está sustituido o está sustituido con alquilo C1-C6, - (alk) q-OR o S (O) 2R10; R es H o alquilo C1-C6 que no está sustituido; cada R' es, de modo independiente, H o alquilo C1-C6 que no está sustituido o los dos grupos R' forman, 20 junto con el átomo de C al que están unidos, un grupo ciclilo; R10 es H, alquilo C1-C6 que no está sustituido o CF3; R11 y R12 están seleccionados cada uno, de modo independiente, de H, alquilo C1-C6 que no está sustituido y - (alk) q-OR o R11 y R12 forman, junto con el átomo de N al que están unidos, un grupo heterocíclico con contenido de N saturado de 5 ó 6 miembros con 0 ó 1 heteroátomos adicionales seleccionados de O, N y S; R13 y R14 están seleccionados cada uno, de modo independiente, alquilo C1-C6, -S (O) 2R10 y - (alk) q-OR; Tet es un grupo tetrahidrofuranilo o tetrahidropiranilo, que no está sustituido o que está sustituido; heterociclilo es un grupo heterocíclico con contenido de N saturado de 5 ó 6 miembros que contiene 0 ó 1 heteroátomos adicionales seleccionados de O, N y S; ciclilo es un grupo cicloalquilo C3-C6; cada q es, de modo independiente, 0 ó 1; r es 0 ó 1; alk es alquileno C1-C6; y R3 está seleccionado de: (a) un grupo de la siguiente fórmula: en donde B es un anillo fenilo que no está sustituido o que está sustituido y Z está seleccionado de H, -OR, -SR, CH2OR, -CO2R, CF2OH, CH (CF3) OH, C (CF3) 2OH, - (CH2) qOR, (CH2) qNR2, -C (O) N (R) 2, -NR2, -NRC (O) R, -S (O) mN (R) 2, -OC (O) R, OC (O) N (R) 2, -NRS (O) mR, -NRC (O) N (R) 2, CN, halógeno y -NO2, en donde cada R está seleccionado, de modo independiente, de H, alquilo C1-C6, cicloalquilo C3-C10 y un grupo arilo o heteroarilo de 5 a 12 miembros, estando el grupo no sustituido o sustituido, m es 1 ó 2 y q es 0, 1 ó 2; (b) un grupo heteroarilo que contiene 1, 2, 3 ó 4 átomos de nitrógeno del anillo y 0, 1 ó 2 heteroátomos adicionales seleccionados de O y S, que es monocíclico o bicíclico y que no está sustituido o que está 10 sustituido; y (c) un grupo que comprende un anillo benceno que no está sustituido o que está sustituido y que está fusionado con un grupo heteroarilo tal como se definió con anterioridad; o una de sus sales farmacéuticamente aceptables; siempre que: (i) cuando X en la fórmula (Ia) es S, entonces R3 es distinto de un grupo indol o 3-hidroxifenilo; (ii) cuando X en la fórmula (Ib) es S, entonces R3 es distinto de un grupo indol; (iii) en la fórmula (Ia) sólo, cuando X es S y R2 es H y R3 es indazol-4-ilo, R4 y R5 no forman: (i) piperazina que no está sustituida o que está sustituida con un grupo seleccionado de metilo, -S (O) 2Me, -S (O) 2NMe2, alk-OH, -alk-OMe, -S (O) 2-alkNMe2 y -S (O) ralk-morfolino; o (ii) piperidina que está sustituida con un grupo seleccionado de -S (O) 2Me, -C (O) -NR- (alk) q-OR, -NMe-S (O) 2-Me, metilo, piperidina y &8211;NR13R14, en donde uno de R13 y R14 es - (alk) q-OR.

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