AR064155A1 - Compuestos de inhibidores de fosfoinositido-3 quinasa y metodos de uso - Google Patents

Compuestos de inhibidores de fosfoinositido-3 quinasa y metodos de uso

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AR064155A1
AR064155A1 ARP070105449A ARP070105449A AR064155A1 AR 064155 A1 AR064155 A1 AR 064155A1 AR P070105449 A ARP070105449 A AR P070105449A AR P070105449 A ARP070105449 A AR P070105449A AR 064155 A1 AR064155 A1 AR 064155A1
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Genentech Inc
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Publication of AR064155A1 publication Critical patent/AR064155A1/es

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Abstract

Son utiles para modular la actividad de lipidoquinasas que incluyen PI3K, y para tratar trastornos tales como cáncer mediado por lipidoquinasas. Se describen métodos para usar compuestos de las formulas 1a-d para el diagnostico, la prevencion o el tratamiento in vitro, in situ e in vivo de dichos trastornos en células de mamíferos, o condiciones patologicas asociadas. Reivindicacion 1: Un compuesto seleccionado de las formulas 1c y 1d, y sus estereoisomeros, isomeros geométricos, tautomeros, solvatos, metabolitos y sales farmacéuticamente aceptables, en donde: X es O o S; R1 es un grupo de la formula: (R4)(R5)N-(CHR30)m-; R2 está seleccionado de H, F, CI, Br, I, arilo C6-20, heteroarilo C1-20, alquilo C1-6, alquenilo C2-8, y alquinilo C2-8; R3 es un grupo heteroarilo monocíclico seleccionado de piridilo, isoxazolilo, imidazolilo, pirazolilo, pirrolilo, tiazolilo, piridazinilo, pirimidinilo, pirazinilo, oxazolilo, furanilo, tienilo, triazolilo, tetrazolilo, donde el grupo heteroarilo monocíclico está opcionalmente sustituido con uno o varios grupos seleccionados de F, CI, Br, I, -CN, -NR10R11, -OR10, -C(O)R10, -NR10C(O)R11, -N(C(O)R11)2, -NR10C(O)NR10R11, -C(=O)OR10, -C(=O)NR10R11, alquilo C1-12 y alquil C1-12- OR10; R4 y R5 forman, junto con el átomo de N al que están unidos, un grupo seleccionado de piperazina, piperidina, pirrolidina, oxazolidinona, morfolina, tiomorfolina, diazepan y 2,5-diaza-biciclo[2,2,1]-heptano, cuyo grupo está opcionalmente sustituido con uno o varios grupos seleccionados, de modo independiente, de F, CI, Br, I, -CN, CF3, -NO2, oxo,-C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, -(CR14R15)nNR10R11, -(CR14R15)nNR12SO2R10, -(CR14R15)nOR10, -NR10R11, -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)2-alquil C1-6-S(O)2R10, -S(O)2R10, -S(O)2NR10R11, -S(O)(OR10), -S(O)2(OR10), -SC(=Y)R10, SC(=Y)OR10, -SC(=Y)NR10R11, alquilo C1-12 opcionalmente sustituido, alquenilo C2-8 opcionalmente sustituido, alquinilo C2-8 opcionalmente sustituido, carbociclilo C3-12 opcionalmente sustituido, heterociclilo C2-20 opcionalmente sustituido, arilo C6- 20 opcionalmente sustituido, y heteroarilo C1-20 opcionalmente sustituido; o uno de R4 y R5 es alquilo C1-6, -(alquil C1-6)q-heterociclilo C2-20, o -(alquil C1-6)q-OR10 y el otro es un grupo piperazina, piperidina, pirrolidina, sulfonilpirano, - (alk)q-heterociclilo C2-20 o un grupo -(alk)q-heteroarilo C1-20, en donde dicho grupo piperazina, piperidina, pirrolidina, sulfonilpirano, heterociclilo o heteroarilo no está sustituido o está sustituido con alquilo C1-6, -(alquil C1-6)q-OR10 o - S(O)2R10; R10, R11, R12 son, de modo independiente, H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20 o heteroarilo C1-20, o R10 y R11 junto con el nitrogeno al que están unidos, forman un anillo heterocíclico C3-20 que opcionalmente contiene uno o varios átomos de anillo adicionales seleccionados de N, O o S, en donde dicho anillo heterocíclico está opcionalmente sustituido con uno o varios grupos seleccionados, de modo independiente, de oxo, (CH2)nOR10, NR10R11, CF3, F, CI, Br, I, SO2R10, C(=O)R10, NR12C(=Y)R11, C(=Y)NR10R11, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20 y heteroarilo C1-20; R14 y R15 están seleccionados, de modo independiente, de H, alquilo C1-12, o -(CH2)n-arilo, o R14 y R15 junto con los átomos a los que están unidos, forman un anillo carbocíclico C3-12 saturado o parcialmente insaturado, R30 es H o alquilo C1-6; mor es un grupo morfolina opcionalmente sustituido con uno o varios grupos seleccionados de F, CI, Br, I, -C(alquil C1-6)2NR10R11, -(CR14R15)tNR10R11, -C(R14R15)nNR12C(=Y)R10, --(CR14R15)nNR12SO2R10, CH(OR10)R10, -(CR14R15)nOR10, -(CR14R15)nS(O)2R10, -(CR14R15)S(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, -NR12S(O)2R10, -NR12SO2NR10R11, -S(O)2R10, -S(O)2NR10R11, -SC(=Y)R10, -SC(=Y)OR10, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20 o heteroarilo C1-20; donde dicho alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno o varios grupos seleccionados, de modo independiente, de F, CI, Br, I, -CN, CF3, -NO2, oxo, -C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, -(CR14R15)nNR10R11, -(CR14R15)nNR12SO2R10, -(CR14R15)nOR10, -NR10R11, -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(O)(OR10), -S(O)2(OR10), -SC(=Y)R10, SC(=Y)OR10, -SC(=Y)NR10R11, alquilo C1-12 opcionalmente sustituido, alquenilo C2-8 opcionalmente sustituido, alquinilo C2-8 opcionalmente sustituido, carbociclilo C3-12 opcionalmente sustituido, heterociclilo C2-20 opcionalmente sustituido, arilo C6-20 opcionalmente sustituido, y heteroarilo C1-20 opcionalmente sustituido; Y es O, S o NR12; cada q es, de modo independiente, 0 o 1; m es 0 o 1; y r es 0 o 1; con la condicion de que: (i) cuando en la formula (1c) mor es morfolino no sustituido, X es S, R1 es un grupo (4-metilsulfonilpiperazin-1-iI)metilo y R2 es H, entonces R3 no sea un grupo seleccionado de imidazolilo que no está sustituido o que está sustituido con un grupo CH3, pirimidinilo que no está sustituido y piridinil que no está sustituido o que está sustituido con un grupo F; (ii) cuando en la formula (1c) mor es morfolino no sustituido, X es S, R1 es un grupo (4-metilpiperazin-1-il)metilo y R2 es H, entonces R3 no sea un grupo seleccionado de pirazolilo que no está sustituido y piridinilo que está sustituido con un grupo OH; y (iii) cuando en la formula (1d) mor es morfolino no sustituido, X es S, R1 es un grupo (4-metilsulfonilpiperazin-1-il)metilo y R2 es H, entonces R3 no sea un grupo seleccionado de piridinilo que no está sustituido y pirimidinilo que no está sustituido o que está sustituido con un grupo -OCH3 o -N(CH3)2.
ARP070105449A 2006-12-07 2007-12-05 Compuestos de inhibidores de fosfoinositido-3 quinasa y metodos de uso AR064155A1 (es)

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AU2007329352B2 (en) 2013-01-17
ES2544082T3 (es) 2015-08-27
MA31146B1 (fr) 2010-02-01
US20130129820A1 (en) 2013-05-23
US20080242665A1 (en) 2008-10-02
EP2518074A1 (en) 2012-10-31
US8383620B2 (en) 2013-02-26
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RU2468027C2 (ru) 2012-11-27
US7888352B2 (en) 2011-02-15
RU2009125897A (ru) 2011-01-20
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