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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

UA98946C2 未知
公开(公告)号：UA98946C2
公开(公告)日：2012-07-10
申请号：UAA200907051
申请日：2007-12-05
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： BAYLISS TRACY , CHUCKOWREE IRINA , FOLKES ADRIAN , OXENFORD SALLY , WAN NAN CHI , CASTANELO GEIRGETTE , GOLDSMITH RICHARD , GUNZNER JANER , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , STABEN STEVEN , SUTHERLIN DANIEL P , XHU BING-YAN
IPC分类号： C07D491/04 , A61K31/519 , A61K31/5377 , A61P35/00 , C07D495/04
摘要： Соединенияформулы Ia-d, вкоторых X представляетсобой S илиО, mor представляетсобойморфолиновуюгруппуи Rпредставляетсобоймоноцикличнуюгетероарильнуюгруппу, включаяихстереоизомеры, геометрическиеизомеры, таутомеры, сольваты, метаболитыи фармацевтическиприемлемыесоли, применимыедлямодулированияактивностилипидныхкиназ, включая PI3K, идлялечениянарушений, такихкакрак, опосредствованныхлипиднымикиназами.Раскрытыспособыприменениясоединенийформулы Ia-d длядиагностики in vitro, in situ i in vivo, профилактикиилилечениятакихнарушенийв клеткахмлекопитающихилиассоциированныхпатологическихсостояний.Ic,Id.

3. 发明专利

MA31146B1 COMPOSES INHIBANT LA PHOSPHOINOSITIDE 3 KINASE ET PROCEDES D'UTILISATION 未知
公开(公告)号：MA31146B1
公开(公告)日：2010-02-01
申请号：MA32069
申请日：2009-07-02
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： C07D491/04 , A61K31/5377 , A61P35/00
摘要： L'invention concerne des composés représentés par les formules Ia-d, dans lesquelles X représente S ou O, mor représente un groupe morpholine et R3 représente un groupe hétéroaryle monocyclique, y compris les stéréo-isomères, les isomères géométriques, les tautomères, les solvates, les métabolites et les sels pharmaceutiquement acceptables de ces composés, ces composés étant utiles pour moduler l'activité de kinases lipidiques comprenant PI3K, et dans le traitement de troubles tels que le cancer induits par des kinases lipidiques. L'invention concerne des procédés d'utilisation des composés représentés par les formules Ia-d pour le diagnostic in vitro, in situ et in vivo, le traitement prophylactique ou thérapeutique de tels troubles ou d'états pathologiques associés dans des cellules de mammifère. [Insérer formules Ic et Id]

4. 发明专利

PE20081353A1 COMPUESTOS DEL INHIBIDOR DE FOSFOINOSITIDA 3-CINASA 未知
公开(公告)号：PE20081353A1
公开(公告)日：2008-11-12
申请号：PE2007001727
申请日：2007-12-05
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： CASTANEDO GEORGETTE , DOTSON JENNAFER , GOLDSMITH RICHARD , GUNZNER JANET , HEFFRON TIM , MATHIEU SIMON , OLIVERO ALAN , SUTHERLIN DANIEL P , WANG SHUMEI , ZHU BING-YAN , STABEN STEVEN , TSUI VICKIE , BAYLISS TRACY , CHUCKOWREE IRINA , FOLKES ADRIAN , WAN NAN CHI
IPC分类号： A61K31/519 , A61P35/00 , C07D491/00 , C07D491/048 , C07D495/00 , C07D495/04
摘要： REFERIDA A UN DERIVADO DE PIRIMIDINA DE FORMULA (Ic) O (Id), DONDE X ES O O S; R1 ES H, F, -C(ALQUILO C1-C6)2NR10R11, ENTRE OTROS; R2 ES H, ARILO DE 6 A 20 MIEMBROS, ALQUILO C1-C6, ENTRE OTROS; R3 ES PIRIDILO, ISOXAZOLILO, IMIDAZOLILO, ENTRE OTROS; R10 Y R11 SON H, ALQUILO C1-C12, ALQUENILO C2-C8, ENTRE OTROS; mor ES UN GRUPO MORFOLINO OPCIONALMENTE SUSTITUIDO CON F, Br, -C(ALQUILO C1-C6)2NR10R11, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-(2-(2-AMINOPIRIMIDI-5-NIL)-4-MORFOLINOTIENO[3,2-d]PIRIMIDI-6-NIL)N-METILSULFONILPIPERIDI-4-NOL, N-((2-(2-AMINOPIRIMIDI-5-NIL)-4-MORFOLINOTIENO[2,3-dPIRIMIDI-6-NIL)METIL)-N-METILBENZAMIDA, N-((2-(2-AMINOPIRIMIDI--5-NIL)-4-MORFOLINOTIENO[2,3-d]PIRIMIDI-6--NIL)METIL)-N-METILNICOTINAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE CINASAS LIPIDICAS, PARTICULARMENTE FOSFOINOSITIDA 3-CINASA (PI3) Y SON UTILES EN EL TRATAMIENTO DEL CANCER

5. 发明专利

CA2671845A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OFUSE 未知
公开(公告)号：CA2671845A1
公开(公告)日：2008-06-19
申请号：CA2671845
申请日：2007-12-05
申请人： GENENTECH INC , HOFFMANN LA ROCHE
发明人： WAN NAN CHI , TSUI VICKIE , SUTHERLIN DANIEL P , WANG SHUMEI , ZHU BING-YAN , CASTANEDO GEORGETTE , BAYLISS TRACY , HEFFRON TIM , GOLDSMITH RICHARD , GUNZNER JANET , OLIVERO ALAN , STABEN STEVEN , FOLKES ADRIAN , MATHIEU SIMON , DOTSON JENNAFER , CHUCKOWREE IRINA
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, geomet ric isomers, tautomers, solvates, metabolites and pharmaceutically acceptabl e salts thereof, are useful for modulating the activity of lipid kinases inc luding PI3K, and for treating disorders such as cancer mediated by lipid kin ases. 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 ce lls, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).

6. 发明专利

CA2671782A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OFUSE 未知
公开(公告)号：CA2671782A1
公开(公告)日：2008-06-12
申请号：CA2671782
申请日：2007-12-05
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： MATHIEU SIMON , HEFFRON TIM , CASTANEDO GEORGETTE , GOLDSMITH RICHARD , FOLKES ADRIAN , GUNZNER JANET , WAN NAN CHI , CHUCKOWREE IRINA , BAYLISS TRACY , SUTHERLIN DANIEL P , ZHU BING-YAN , OXENFORD SALLY , OLIVERO ALAN , STABEN STEVEN
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, geomet ric isomers, tautomers, solvates, metabolites and pharmaceutically acceptabl e salts thereof, are useful for modulating the activity of lipid kinases inc luding PI3K, and for treating disorders such as cancer mediated by lipid kin ases. Methods of using compounds of Formulas Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian ce lls, or associated pathological conditions, are disclosed. [Insert Formula I c and Id]

7. 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

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).

9. 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]

10. 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.

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