AR072280A1 - Isoquinolinas e isoquinolinonas 6- sustituidas - Google Patents

Isoquinolinas e isoquinolinonas 6- sustituidas

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AR072280A1
AR072280A1 ARP090102284A ARP090102284A AR072280A1 AR 072280 A1 AR072280 A1 AR 072280A1 AR P090102284 A ARP090102284 A AR P090102284A AR P090102284 A ARP090102284 A AR P090102284A AR 072280 A1 AR072280 A1 AR 072280A1
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Argentina
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alkyl
alkylene
aryl
heterocycloalkyl
cycloalkyl
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ARP090102284A
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Sanofi Aventis
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Abstract

Estos compuestos son utiles para el tratamiento y/o la prevencion de enfermedades asociadas con la cinasa Rho y/o la fosforilacion mediada por la cinasa Rho de la fosfatasa de miosina de cadena ligera, y a composiciones que contienen dichos compuestos. Reivindicacion 1: Un compuesto de la formula (1) en donde R1 es H, OH o NH2; R3 es H, halogeno, CN, alquilo C1-6, OH, NH2 o NHR'; R4 es H, halogeno, hidroxi, CN, alquilo C1-6, R' o alquilen C1-6-R'; R5 es H, halogeno, CN, alquilo C1-6, o R'; R7 es H, halogeno, CN, alquilo C1-6, O-alquilo C1-6, R' o SO2-NH2; R8 es H, halogeno o alquilo C1-6; R9 es R', OH, halogeno, alquilo C1-6, O-alquilo C1-6, alquilen C1-6-R', alquenilo C2-6, alquinilo C2-6, alquilen C1-6-O-R', alquilen C1-6-CH[R']2, alquilen C1-6-C(O)-R', alquilen C1-6-C(O)NH2, alquilen C1-6-C(O)NH-R', alquilen C1-6-C(O)NH-alquilo C1-6, alquilen C1-6-C(O)N[alquilo C1-6]2, alquilen C1-6-C(O)N[R']2, alquilen C1-6-C(O)O-alquilo C1-6, COOH, C(O)O-alquilo C1-6, C(O)OR', C(O)-alquilo C1-6, C(O)R', CONH2, C(O)-NH-alquenilo C2-6, C(O)-NH-alquinilo C2-6, C(O)NH-alquilo C1-6, C(O)NHR', C(O)-NH-alquileno C1-6-R', C(O)N[alquilo C1-6]R', C(O)N[alquilo C1-6]2, C(O)-alquileno C1-6-R', o C(O)O-alquileno C1-6-R'; R6 está ausente, o es alquileno C1-4 unido al anillo cicloalquilo, en el que el alquileno C1-4 forma un segundo enlace a un átomo de carbono diferente del anillo de cicloalquilo para formar un sistema de anillo bicíclico, donde en el sistema de anillo bicíclico uno o dos átomos de carbono se reemplazan por un grupo independientemente seleccionado de O, N-R15, S, SO o SO2 o, si m y s son 2, m es 3 y s es 1, o m es 4 y s es 0, R6 es CH2-CH-(CH2)2, que está unido con un CH2 al anillo de cicloalquilo y los otros dos CH2 están unidos a diferentes átomos de carbono del anillo de cicloalquilo, y, si m es 3 y s es 3, R6 son dos grupos metileno unidos a átomos de carbono diferentes del anillo cicloalquilo, donde los grupos metileno o el grupo CH2-CH-(CH2)2 están unidos a átomos de carbono del anillo cicloalquilo de modo tal que forman un sistema de adamantano de la formula (2) donde L puede estar unido a cualquier átomo de carbono secundario o terciario, y donde el sistema de anillo bicíclico o el sistema de adamantano no está sustituido o está opcionalmente sustituido por R9; R10 es alquilo C1-6, heteroalquilo C1-8, cicloalquilo C3-8, heterocicloalquilo C3-8, alquilen C1-6-cicloalquilo C3-8, alquilen C1-6-arilo C6-10, alquilen C1-6-heteroarilo C5-10, alquilen C1-6-heterocicloalquilo C3-8, C(O)NH-alquilo C1-6, C(O)N[alquilo C1-6]2, C(O)NH-R', C(O)N-alquil C1-6-R', o C(O)NH-alquilen C1-6-R'; R11 es H, alquilo C1-6, alquilen C1-6-R', R', o R11 y R12, junto con el átomo de C al que están unidos, forman un anillo cicloalquilo C3-8 o un anillo heterocicloalquilo C3-8; R12 es alquilo C1-6, cicloalquilo C3-8, heteroarilo C5-10, heterocicloalquilo C3-8, o arilo C6-10; o R12 es H, siempre que r = 2 y el otro R12 no sea H; o R11 y R12, junto con el átomo de C al que están unidos, forman un anillo cicloalquilo C3-8 o un anillo heterocicloalquilo C3-8; R13 y R14 son independientemente uno del otro, H, R', alquilo C1-6, alquilen C1-6-R', alquilen C1-6-O-alquilo C1-6, alquilen C1-6-O-R', alquilen C1-6-CH[R']2, alquilen C1-6-C(O)-R', alquilen C1-6-C(O)NH2, alquilen C1-6-C(O)NH-R', alquilen C1-6-C(O)NH-alquilo C1-6, alquilen C1-6-C(O)N[alquilo C1-6]2, alquilen C1-6-C(O)N[R']2, alquilen C1-6-C(O)O-alquilo C1-6, C(O)O-alquilo C1-6, C(O)OR', C(O)-alquilo C1-6, C(O)R', C(O)NH-alquilo C1-6, C(O)NHR', C(O)N[alquil C1-6]R', C(O)N[alquilo C1-6]2, C(O)-alquilen C1-6-R', C(O)O-alquilen C1-6-R'; o R13 y R14, junto con el átomo de N al que están unidos, forman un heterocicloalquilo C3-8; R15 es H o alquilo C1-6; n es 0, 1, 2, 3 o 4; m es 1, 2, 3 o 4; s es 0, 1, 2 o 3; r es 1 o 2; L es O(CH2)p, S(CH2)p, S(O)(CH2)p, SO2(CH2)p, NH(CH2)p, N-alquil C1-6-(CH2)p, N-cicloalquil C3-6-(CH2)p; o N[alquilen C1-3-R']-(CH2)p; p es 0, 1, 2, 3 o 4; R' es cicloalquilo C3-8, heteroarilo C5-10, heterocicloalquilo C3-8, arilo C6-10; donde en los residuos R3 a R15, el alquilo o alquileno no está sustituido o está opcionalmente sustituido una o más veces con OH, OCH3, C(O)OH, C(O)OCH3, NH2, NHCH3, N(CH3)2, C(O)NH2, C(O)NHCH3 o C(O)N(CH3)2; donde en los residuos R3 a R15 cicloalquilo o heterocicloalquilo no está sustituido o está opcionalmente sustituido una o más veces con alquilo C1-6, halogeno, OH, OCH3, C(O)OH, C(O)OCH3, NH2, NHCH3, N(CH3)2, C(O)NH2, C(O)NHCH3 o C(O)N(CH3)2; donde en los residuos R3 a R15 alquilo o alquileno no está sustituido o está opcionalmente sustituido una o más veces por halogeno; donde en los residuos R3 a R15 arilo C6-10 y heteroarilo C5-10 no están sustituidos o están opcionalmente sustituidos, una o más veces, por un grupo independientemente seleccionado entre halogeno, OH, NO2, N3, CN, C(O)-alquilo C1-6, C(O)-arilo C6-10, C(O)OH, C(O)O-alquilo C1-6, C(O)NH2, C(O)NH-alquilo C1-6, C(O)N[alquilo C1-6]2, cicloalquilo C3-8, alquilo C1-6, alquilen C1-6-NH-alquilo C1-6, alquilen C1-6-N[alquilo C1-6]2, alquenilo C2-6, alquinilo C2-6, O-alquilo C1-6, O-C(O)-alquilo C1-6, PO3H2, SO3H, SO2-NH2, SO2NH-alquilo C1-6, SO2N[alquilo C1-6]2, S-alquilo C1-6; SO-alquilo C1-6, SO2-alquilo C1-6, SO2-N=CH-N[alquilo C1-6]2, SF5, C(NH)(NH2), NH2, NH-alquilo C1-6, N[alquilo C1-6]2, NH-C(O)-alquilo C1-6, NH-C(O)O-alquilo C1-6, NH-SO2-alquilo C1-6, NH-SO2-arilo C6-10, NH-SO2-heteroarilo C5-10, NH-SO2-heterocicloalquilo C3-8, N-alquil C1-6-C(O)-alquilo C1-6, N-alquil C1-6-C(O)O-alquilo C1-6, N-alquil C1-6-C(O)-NH-alquilo C1-6, arilo C6-10, alquilen C1-6-arilo C6-10, O-arilo C6-10, O-alquilen C1-6-arilo C6-10, heteroarilo C5-10, heterocicloalquilo C3-8, alquilen C1-6-heteroarilo C5-10, alquilen C1-6-heterocicloalquilo C3-8, O-alquilen C1-6-heteroarilo C5-10, O-alquilen C1-6-heterocicloalquilo C3-8, donde dicho arilo C6-10, o heteroarilo C5-10, o heterocicloalquilo C3-8 o cicloalquilo C3-8 puede estar sustituido, una a tres veces, por un grupo, independientemente seleccionado entre halogeno, OH, NO2, CN, O-alquilo C1-6, alquilo C1-6, NH2, NH-alquilo C1-6, N[alquilo C1-6]2, SO2CH3, C(O)OH, C(O)O-alquilo C1-6, C(O)NH2, alquilen C1-6-O-alquilo C1-6, alquilen C1-6-O-arilo C6-10 o O-alquilen C1-6-arilo C6-10; o en los que el grupo arilo C6-10 está sustituido vecinalmente con un grupo O-alquilen C1-4-O, por lo que se forma, junto con los átomos de carbono a los que están unidos los átomos de oxígeno, un anillo de 5-8 miembros; y en donde los sustituyentes arilo de grupos arilo C6-10, heteroarilo C5-10, cicloalquilo o heterocicloalquilo C3-8 pueden no estar más sustituidos por un grupo que contiene arilo, heteroarilo, cicloalquilo o heterocicloalquilo; sus formas estereoisoméricas y/o tautoméricas y/o sus sales farmacéuticamente aceptables.
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