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1. 发明专利

CA2671782C PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA2671782C
公开(公告)日：2017-01-10
申请号：CA2671782
申请日：2007-12-05
申请人： F HOFFMAN - LA ROCHE AG , GENENTECH INC
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： C07D491/04 , A61K31/519 , A61K31/5377 , 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. [Insert Formula Ic and Id]

2. 发明申请

WO2008073785A3 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：磷酸肌醇3-激酶抑制剂化合物及使用方法
公开(公告)号：WO2008073785A3
公开(公告)日：2008-08-28
申请号：PCT/US2007086533
申请日：2007-12-05
申请人： GENENTECH INC , PIRAMED LTD , 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
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
CPC分类号： C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R 3 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).
摘要翻译：其中X是S或O的式Ia-d化合物，mor是吗啉基，并且R 3是单环杂芳基，并且包括其立体异构体，几何异构体，互变异构体，溶剂化物，代谢物和药学上可接受的其盐可用于调节包括PI3K在内的脂质激酶的活性，并用于治疗诸如由脂质激酶介导的癌症等疾病。公开了使用式Ia-d化合物体外，原位和体内诊断，预防或治疗哺乳动物细胞中的此类病症或相关病理学病症的方法。式（Ic）和（Id）。

3. 发明申请

WO2007127175A3 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007127175A3
公开(公告)日：2007-12-27
申请号：PCT/US2007009866
申请日：2007-04-24
申请人： PIRAMED LTD , GENENTECH INC , GOLDSMITH RICHARD , 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
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
IPC分类号： C07D491/04 , A61K31/5025 , A61P35/00 , C07D495/04 , C07D519/00
CPC分类号： C07D495/04 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048
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.
摘要翻译：式Ia和Ib的化合物及其立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

4. 发明专利

MY180595A PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：MY180595A
公开(公告)日：2020-12-03
申请号：MYPI20092322
申请日：2007-12-05
申请人： GENENTECH INC , PIRAMED LTD
发明人： BAYLISS TRACY , FOLKES ADRIAN , WAN NAN CHI , CHUCKOWREE IRINA , OXENFORD SALLY , STABEN STEVEN , CASTANEDO GEORGETTE , GOLDSMITH RICHARD , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , SUTHERLIN DANIEL P , ZHU BING-YAN
摘要： Compounds of Formulas Ia-d where Xis Sor 0, 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 PBK, 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. (No suitable figure)

5. 发明专利

CA2704711C THIAZOLOPYRIMIDINE P13K INHIBITOR COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA2704711C
公开(公告)日：2016-07-05
申请号：CA2704711
申请日：2008-09-23
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： CASTANEDO GEORGETTE M , GUNZNER JANET L , MALESKY KIMBERLY , MATHIEU SIMON , OLIVERO ALAN G , SUTHERLIN DANIEL P , WANG SHUMEI , ZHU BING-YAN , CHUCKOWREE IRINA , FOLKES ADRIAN , OXENFORD SALLY , WAN NAN CHI
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
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. (see formula Ia) (see formula Ib) 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.

6. 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.

8. 发明专利

ES2533788T3 Compuestos inhibidores de PI3K de tipo purina y métodos de uso 未知
公开(公告)号：ES2533788T3
公开(公告)日：2015-04-14
申请号：ES09755767
申请日：2009-05-29
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： CASTANEDO GEORGETTE , CHUCKOWREE IRINA , FOLKES ADRIAN , SUTHERLIN DANIEL , WAN NAN CHI
IPC分类号： C07D473/32 , A61K31/52 , A61P35/00
摘要： Un compuesto que tiene la estructura:**Fórmula** y estereoisómeros, isómeros geométricos, tautómeros o sales farmacéuticamente aceptables de los mismos, en la que: R1 se selecciona entre H, alquilo C1-C12 y -(alquileno C1-C12)-(heterociclilo C2-C20), en donde alquilo, alquileno y heterociclilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente entre F, Cl, Br, I, -CH3, -CH2OH, -CN, -CF3, -CO2H, -COCH3, -CO2CH3, -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. R2 se selecciona entre alquilo C1-C12, alquenilo C2-C8, alquinilo C2-C8, -(alquileno C1-C12)-(carbociclilo C3-C12)-, -(alquileno C1-C12)-(heterociclilo C2-C20)-, -(alquileno C1-C12)-C(>=O)-(C2-C20 heterociclilo), -(alquileno C1-C12)-(arilo C6-C20)- y -(alquileno C1-C12)-(heteroarilo C1-C20), en donde alquilo, alquenilo, alquinilo, alquileno, carbociclilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente entre F, Cl, Br, I, -CH3, -CH2OH, -CN, -CF3, -CO2H, -COCH3, -CO2CH3, -CONH2, -CONHCH3, -CON(CH3)2, -NO2, -NHz, -NHCH3,-NHCOCH3, -NHS(O)2CH3, -OH, -OCH3, -S(O)2N(CH3)2, -SCH3, -CH2OCH3 y -S(O)2CH3; y R3 es un heteroarilo monocíclico seleccionado entre:**Fórmula** en las que la línea ondulada indica el sitio de la unión.

9. 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).

10. 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.

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