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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. 发明申请

WO2007022102A2 PENTACYCLIC KINASE INHIBITORS 审中-公开
标题翻译： PENTACYCLIC激酶抑制剂
公开(公告)号：WO2007022102A2
公开(公告)日：2007-02-22
申请号：PCT/US2006031682
申请日：2006-08-14
申请人： GENENTECH INC , HOFFMANN LA ROCHE , HOFFMANN LA ROCHE , ZHOU AIHE , RAWSON THOMAS E , SAFINA BRIAN , DOTSON JENNAFER , ALIAGAS-MARTIN IGNACIO , HALLADAY JASON , LIANG JUN , RUETH MATTHIAS , ZHU BING-YAN , BROOKFIELD FREDERICK , PRIME MICHAEL , ZHANG BIRONG , LI JUN M
发明人： RAWSON THOMAS E , SAFINA BRIAN , DOTSON JENNAFER , ALIAGAS-MARTIN IGNACIO , HALLADAY JASON , LIANG JUN , RUETH MATTHIAS , ZHU BING-YAN , BROOKFIELD FREDERICK , PRIME MICHAEL , ZHANG BIRONG , LI JUN M
IPC分类号： C07D487/04 , A61K31/4155 , A61P35/00 , C07D491/04
CPC分类号： C07D487/04 , C07D491/04
摘要： The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I (I) wherein A, X, Y, Z, Ra, Rb, Rc, R 1 , R 2 , R 3 and m are defined herein.
摘要翻译：本发明提供新的激酶抑制剂，其可用作例如治疗恶性肿瘤的治疗剂，其中化合物具有通式I（I），其中A，X，Y，Z，R a，R b，R c，R 1， R 2，R 3和M如本文所定义。

3. 发明专利

CA2719032C BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA2719032C
公开(公告)日：2016-11-08
申请号：CA2719032
申请日：2009-03-30
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： DO STEVEN , GOLDSMITH RICHARD , HEFFRON TIM , KOLESNIKOV ALEKSANDR , STABEN STEVEN , OLIVERO ALAN G , SIU MICHAEL , SUTHERLIN DANIEL P , ZHU BING-YAN , GOLDSMITH PAUL , BAYLISS TRACY , FOLKES ADRIAN , PEGG NEIL
IPC分类号： C07D495/04 , A61K31/38 , A61K31/429 , A61P35/00 , C07D513/04
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of P13K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

4. 发明专利

ES2494365T3 Compuestos de pirazolopirimidina que inhiben PI3K y métodos de uso 未知
公开(公告)号：ES2494365T3
公开(公告)日：2014-09-15
申请号：ES09706948
申请日：2009-01-29
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： DOTSON JENNAFER , HEFFRON TIM , OLIVERO ALAN , SUTHERLIN DANIEL P , WANG SHUMEI , ZHU BING-YAN , CHUCKOWREE IRINA , FOLKES ADRIAN , WAN NAN CHI
IPC分类号： C07D487/04 , A61K31/505 , A61P35/00 , C07D519/00
摘要： Un compuesto seleccionado entre la Fórmula I: y estereoisómeros, isómeros geométricos, tautómeros, o sales farmacéuticamente aceptables de los mismos, en donde: R1 se selecciona entre H, alquilo C1-C12, -C(>=O)NR10R11, -NR12C(>=O)R10, -NR12C(>=O)OR11, -NR12C(>=O)NR10R11, y heteroarilo C1-C20 donde heteroarilo C1-C20 está sustituido opcionalmente con uno o más grupos seleccionados independientemente entre alquilo C1-C12, alquil(C1-C12)-NR10R11, alquil(C1-C12)-OR10, arilo C6- C20, F, Cl, Br, I, -CN, -CF3, -CO2H,-C(>=O)NR10R11, -NO2, -NR10R11, -NHCOR10, -OR10, -S(O)2NR10R11, y -S(O)2R10; R2 es alquilo C1-C12; R3 se selecciona entre heterociclilo C2-C20 unido a carbono y heteroarilo C1-C20 unido a carbono, donde heterociclilo C2-C20 unido a carbono y heteroarilo C1-C20 unido a carbono están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre alquilo C1-C12, arilo C6-C20, F, Cl, Br, I, -CH3, -CN, -CF3, -CH2OH, -CO2H, -CONH2, -CON(CH3)2, -NO2,-NH2, -NHCH3, -NHCOCH3, -OH, -OCH3, -SH, -NHC(>=O)NHCH3, y -S(O)2CH3; R4 se selecciona entre -NR10R13, -NR12C(>=O)R10, -NR10(alquilo C1-C12)NR10R13, -NR10(alquilo C1-C12)OR10, -NR10(alquilo C1-C12)C(>=O)NR10R13, -NR10((alquileno C1-C12))-(carbociclilo C3-C12), -NR10((alquileno C1-C12))- (heterociclilo C2-C20), -NR10((alquileno C1-C12))-(arilo C6-C20), -NR10(alquileno C1-C12)-(heteroarilo C1-C20), -OR10, -O((alquileno C1-C12))-(carbociclilo C3-C12), -O((alquileno C1-C12))-(heterociclilo C2-C20), -O((alquileno C1-C12))-(arilo C6-C20), -O((alquileno C1-C12))-(heteroarilo C1-C20), -((alquileno C1-C12))NR10R13, -((alquileno C1-C12))-(carbociclilo C3-C12), -((alquileno C1-C12))-(heterociclilo C2-C20), -((alquileno C1-C12))-(arilo C6-C20), -((alquileno C1-C12))- (heteroarilo C1-C20), -(alquinileno C2-C8)NR10R13, -(alquinileno C2-C8)-(carbociclilo C3-C12), -(alquinileno C2-C8)- (heterociclilo C2-C20), -(alquinileno C2-C8)-(arilo C6-C20), -(alquinileno C2-C8)-(heteroarilo C1-C20), -(alquileno C1-C12)- (arileno C6-C20)-(heterociclilo C2-C20), -(arilo C6-C20)-((alquileno C1-C12))-(heterociclilo C2-C20), -C(>=O)NR10R11, alquilo C1-C12, alquinilo C2-C8, carbociclilo C3-C12, heterociclilo C2-C20, arilo C6-C20, y heteroarilo C1-C20, donde alquilo, alquileno, alquinilo, alquinileno, carbociclilo, heterociclilo, arilo, y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, Cl, Br, I, -CH3, -CH2OH, -CN, -CF3, -CO2H, -COCH3, -CONH2, -CONHCH3, -CON(CH3)2, -NO2, -NH2, -NHCH3, -NHCOCH3, -NHS(O)2CH3, -OH, -OCH3, -S(O)2N(CH3)2, -SCH3, -CH2OCH3, y -S(O)2CH3; R10, R11 y R12 se seleccionan independientemente entre H, alquilo C1-C12, alquenilo C2-C8, alquinilo C2-C8, carbociclilo C3-C12, heterociclilo C2-C20, arilo C6-C20, y heteroarilo C1-C20, donde alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo, y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, Cl, Br, I, -CH2OH, -CH2C6H5, -CN, -CF3, -CO2H, -CONH2, -CONHCH3, -NO2, -N(CH3)2, -NHCOCH3, -NHS(O)2CH3, -OH, -OCH3, -OCH2CH3, -S(O)2NH2, -SCH3, -S(O)CH3, -CH2OCH3, -CH3, y -S(O)2CH3; o R10 y R11 junto con el átomo de nitrógeno al cual están anclados forman un anillo de heterociclilo C2-C20; y R13 se selecciona entre alquilo C1-C12, alquenilo C2-C8, alquinilo C2-C8, carbociclilo C3-C12, heterociclilo C2-C20, arilo C6-C20, y heteroarilo C1-C20, donde alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo, y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, Cl, Br, I, -CH2OH, -CH2C6H5, -CN, -CF3, -CO2H, -CONH2, -CONHCH3, -NO2, -N(CH3)2, -NHCOCH3, -NHS(O)2CH3, -OH, -OCH3, -OCH2CH3, -S(O)2NH2, -SCH3, -S(O)CH3, -OCH2CH2-N(CH3)2, y -S(O)2CH3; o R10 y R13 junto con el átomo de nitrógeno al cual están anclados forman un anillo de heterociclilo C2-C20; y en donde el término "heteroarilo" indica un anillo de 5 a 7 miembros aromático monovalente que es monocíclico o forma parte de un sistema anular fusionado que comprende de 5 a 20 átomos anulares que contiene uno o más heteroátomos seleccionados independientemente entre O, N y S.

5. 发明专利

ZA201007218B BENZOPYRAN AND BENZOXEPIN P13K INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：ZA201007218B
公开(公告)日：2012-06-27
申请号：ZA201007218
申请日：2010-10-08
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： DO STEVEN , GOLDSMITH RICHARD , HEFFRON TIM , KOLESNIKOV ALEKSANDR , STABEN STEVEN , OLIVERO ALAN G , SIU MICHAEL , SUTHERLIN DANIEL P , ZHU BING-YAN , GOLDSMITH PAUL JOHN , BAYLISS TRACY , FOLKES ADRIAN , PEGG NEIL
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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

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.

7. 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.

8. 发明专利

NZ578162A PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：NZ578162A
公开(公告)日：2011-12-22
申请号：NZ57816207
申请日：2007-12-05
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： BAYLISS TRACY , CHUCKOWREE IRINA , FOLKES ADRIAN , OXENFORD SALLY , WAN NAN CHI , CASTANEDO GEORGETTE , GOLDSMITH RICHARD , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , STABEN STEVEN , SUTHERLIN DANIEL P , ZHU BING-YAN
IPC分类号： A61P35/00 , A61K31/519 , A61K31/5377 , C07D491/04 , C07D495/04
摘要： Provided is a compound of formula Ia or Ib, with specified substituents, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof. The compound is a phosphoinositide-3 (PI3) kinase inhibitor and can be used to treat various hyperproliferative diseases, including cancer, conditions involving cell death, infectious diseases and CNS disorders, among others.

9. 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.

10. 发明专利

CA2719032A1 BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA2719032A1
公开(公告)日：2009-10-08
申请号：CA2719032
申请日：2009-03-30
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： DO STEVEN , GOLDSMITH RICHARD , HEFFRON TIM , KOLESNIKOV ALEKSANDR , STABEN STEVEN , OLIVERO ALAN G , SIU MICHAEL , SUTHERLIN DANIEL P , ZHU BING-YAN , GOLDSMITH PAUL , BAYLISS TRACY , FOLKES ADRIAN , PEGG NEIL
IPC分类号： C07D495/04 , A61K31/38 , A61K31/429 , A61P35/00 , C07D513/04
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

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