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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

ES2571028T3 Compuestos inhibidores de fosfoinositida 3-cinasa y métodos de uso 未知
公开(公告)号：ES2571028T3
公开(公告)日：2016-05-23
申请号：ES07865255
申请日：2007-12-05
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： CASTANEDO GEORGETTE , DOTSON JENNAFER , GOLDSMITH RICHARD , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , STABEN STEVEN , SUTHERLIN DANIEL P , TSUI VICKIE , WANG SHUMEI , ZHU BING-YAN , BAYLISS TRACY , CHUCKOWREE IRINA , FOLKES ADRIAN , WAN NAN CHI
IPC分类号： C07D491/048 , A61K31/519 , A61P35/00 , C07D495/04
摘要： Un compuesto seleccionado de la Fórmula Ia y la Fórmula Ib:**Fórmula** y sus estereoisómeros, tautómeros y sales farmacéuticamente aceptables, en donde: X es O o S; R1 se selecciona entre F, Cl, Br, I, -C(alquil C1-C6)2NR10R11,-(CR14R15)tNR10R11, -C(R14R15)nNR12C(>=Y)R10, - (CR14R15)nNR12S(O)2R10, -CH(OR10)R10, - (CR14R15)nOR10, -(CR14R15)nS(O)2R10, -(CR14R15)nS(O)2NR10R11, - C(>=Y)R10, -C(>=Y)OR10, -C(>=Y)NR10R11, -C(>=Y)NR12OR10, -C(>=O)NR12S(O)2R10, -C(>=O)NR12(CR14R15)mNR10R11, NO2, -NHR12, -NR12C(>=Y)R11, -NR12C(>=Y)OR11, -NR12C(>=Y)NR10R11, -NR12(O)2R10, -NR12SO2NR10R11, -S(O)2R10, - S(O)2NR10R11, -SC(>=Y)R10, -SC(>=Y)OR10, alquilo C1-C12, alquenilo C2-C8, alquinilo C2-C8, carbociclilo C3-C12, heterociclilo C2-C20, arilo C6-C20 o heteroarilo C1-C20; R2 se selecciona entre H, F, Cl, Br, I, arilo C6-C20, heteroarilo C1-C20 y alquilo C1-C6; R3 es un grupo heteroarilo monocíclico seleccionado entre**Fórmula** R10, R11 y R12 son independientemente H, alquilo C1-C12, alquenilo C2-C8, alquinilo C2-C8, carbociclilo C3-C12, heterociclilo C2-C20, arilo C6-C20 o heteroarilo C1-C20, o R10 y R11 junto con el nitrógeno al que están unidos opcionalmente forman un anillo heterocíclico C3-C20 que opcionalmente contiene uno o más átomos de anillos adicionales seleccionados entre N, O o S, en donde dicho anillo heterocíclico está opcionalmente sustituido con uno o más grupos independientemente seleccionados entre oxo, (CH2)mOR10, CH2)mNR10R11, CF3, F, Cl, Br, I, SO2R10, C(>=O)R10, NR12C(>=Y)R11, C(>=Y)NR10R11, alquilo C1-C12, alquenilo C2-C8, alquinilo C2-C8, carbociclilo C3-5 C12, heterociclilo C2-C20, arilo C6-C20 y heteroarilo C1-C20; R14 y R15 se seleccionan independientemente entre H, alquilo C1-C12 o -(CH2)n-arilo, o R14 y R15 junto con los átomos a los que están unidos forman un anillo carbocíclico saturado o parcialmente insaturado C3-C12, en donde dicho alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno o más grupos independientemente seleccionados entre F, Cl, Br, I, -CN, CF3, -NO2, oxo, - C(>=Y)R10, -C(>=Y)OR10, -C(>=Y)NR10R11, -(CR14R15)nNR10R11, (CR14R15)nC(>=Y)NR10R11, -(CR14R15)nC(>=Y)OR10, - (CR14R15)nNR12SO2R10,-(CR14R15)nOR10, -(CR14R15)nR10, -(CR14R15)nSO2R10, -NR10Rn, -NR12C(>=Y)R10, - NR12C(>=y)OR11, -NR12C(>=Y)NR10R11, -NR12SO2R10, >=NR12, OR10, -OC(>=Y)R10, OC(>=Y)OR10, -OC(>=Y)NR10R11, - OS(O)2(OR10, -OP(>=Y)(OR10)(OR11), -OP(OR10)(OR11), SR10, -S(O)R10, -S(O)2R10, -S(O)2NR10R11, -S(OXOR10), - S(O)2(OR10), -SC(>=Y)R10,-SC(>=Y)OR10, -SC(>=Y)NR10R11, alquilo C1-C12 opcionalmente sustituido, alquenilo C2-C8 opcionalmente sustituido, arilo C2-C8 opcionalmente sustituido, carbociclilo C3-C12 opcionalmente sustituido, heterociclilo C2-C20 opcionalmente sustituido, arilo C6-C20 opcionalmente sustituido y heteroarilo C1-C20 opcionalmente sustituido; Y es O, S o NR12; m es 0, 1, 2, 3, 4, 5 o 6; n es 1, 2, 3, 4, 5 o 6; y t es 2, 3, 3, 4 o 6. con la excepción de: 6-(4-metanosulfonil-piperazin-1-ilmetil)-2-(2-(metoxi-pirimidin-5-il)-4-morfolin-4-il-tieno[2,3-d]pirimidina.

3. 发明专利

CA2671845C PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA2671845C
公开(公告)日：2015-03-24
申请号：CA2671845
申请日：2007-12-05
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： CASTANEDO GEORGETTE , DOTSON JENNAFER , GOLDSMITH RICHARD , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , STABEN STEVEN , SUTHERLIN DANIEL P , TSUI VICKIE , WANG SHUMEI , ZHU BING-YAN , BAYLISS TRACY , CHUCKOWREE IRINA , FOLKES ADRIAN , WAN NAN CHI
IPC分类号： C07D491/048 , A61K31/519 , A61P35/00 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).

4. 发明专利

SG171765A1 PYRAZOLOPYRIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：SG171765A1
公开(公告)日：2011-07-28
申请号：SG2011036381
申请日：2009-11-19
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： DOTSON JENNAFER , HEFFRON TIM , OLIVERO ALAN G , SUTHERLIN DANIEL P , STABEN STEVEN , WANG SHUMEI , ZHU BING-YAN , CHUCKOWREE IRINA S , FOLKES ADRIAN J , WAN NAN CHI
摘要： Compounds of Formula (I), 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 or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) 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

CA2711759A1 PYRAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA2711759A1
公开(公告)日：2009-08-06
申请号：CA2711759
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： Compounds of Formula I, 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 Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Fomula I]

6. 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.

7. 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.

8. 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.

9. 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.

10. 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.

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