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101. 发明专利

NO20013462L 未知
公开(公告)号：NO20013462L
公开(公告)日：2001-09-12
申请号：NO20013462
申请日：2001-07-12
申请人： GENENTECH INC
发明人： ALIAGAS-MARTIN IGNACIO , ARTIS DEAN R , DINA MICHAEL S , FLYGARE JOHN A , GOLDSMITH RICHARD A , MUNROE REGINA A , OLIVERO ALAN G , PASTOR RICHARD , RAWSON THOMAS E , ROBARGE KIRK D , SUTHERLIN DANIEL P , WEESE KENNETH J , ZHOU AIHE , ZHU YAN
IPC分类号： A61K31/18 , C07C257/18 , A61K31/196 , C07D333/34 , A61K31/216 , A61K31/381 , A61P7/02 , A61P9/10 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51 , C07C317/00
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

103. 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)

104. 发明专利

EA026393B1 N-ЗАМЕЩЕННЫЕ БЕНЗАМИДЫ И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ БОЛИ 未知
公开(公告)号：EA026393B1
公开(公告)日：2017-04-28
申请号：EA201492166
申请日：2013-05-21
申请人： GENENTECH INC , XENON PHARMACEUTICALS INC
发明人： ANDREZ JEAN-CHRISTOPHE , CHOWDHURY SULTAN , DECKER SHANNON , DEHNHARDT CHRISTOPH MARTIN , FOCKEN THILO , GRIMWOOD MICHAEL EDWARD , HEMEON IVAN WILLIAM , JIA QI , LI JUN , ORTWINE DANIEL F , SAFINA BRIAN , SHENG TAO , SUN SHAOYI , SUTHERLIN DANIEL P , WILSON MICHAEL SCOTT , ZENOVA ALLA YUREVNA
IPC分类号： C07C311/51 , A61K31/18 , A61K31/44 , A61K31/445 , A61P25/04 , C07D207/08 , C07D213/82 , C07D307/12
摘要： Изобретениеобеспечиваетновыесоединенияобщейформулы (I)иихфармацевтическиприемлемыесоли, гдепеременные R, подстрочныйиндекс n, кольцоА, X, L, подстрочныйиндекс m, X, B, R, R, R, R, Rи Rимеютзначения, описанныев описанииизобретения; композиции, содержащиетакиесоединения, испособыприменениятакихсоединенийи композиций.

105. 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.

106. 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.

109. 发明专利

MX2015000164A BENZAMIDAS N-SUSTITUIDAS Y METODOS PARA USARLAS. 未知
公开(公告)号：MX2015000164A
公开(公告)日：2015-08-12
申请号：MX2015000164
申请日：2013-07-05
申请人： GENENTECH INC
发明人： CHOWDHURY SULTAN , SAFINA BRIAN , SUTHERLIN DANIEL P , DEHNHARDT CHRISTOPH MARTIN , FOCKEN THILO , GRIMWOOD MICHAEL EDWARD , HEMEON IVAN WILLIAM
IPC分类号： C07C307/04
摘要： La invención provee compuestos novedosos que tienen la fórmula general: (ver Fórmula) y sales farmacéuticamente aceptables de estos, donde las variables RA, n en subíndice, anillo A, X2, L, m subíndice, X1, anillo D, R1 y RN tienen el significado se describió en la presente, y las composiciones que contienen tales composiciones y métodos para utilizar tales compuestos y composiciones.

110. 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).

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