AR086319A1 - Compuestos heterociclicos fusionados como moduladores de canal ionico - Google Patents

Compuestos heterociclicos fusionados como moduladores de canal ionico

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Publication number
AR086319A1
AR086319A1 ARP120101626A AR086319A1 AR 086319 A1 AR086319 A1 AR 086319A1 AR P120101626 A ARP120101626 A AR P120101626A AR 086319 A1 AR086319 A1 AR 086319A1
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AR
Argentina
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aryl
cycloalkyl
heteroaryl
heterocyclyl
alkyl
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English (en)
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Gilead Sciences Inc
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Publication of AR086319A1 publication Critical patent/AR086319A1/es

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Abstract

La presente descripción se refiere a compuestos que son inhibidores del canal de sodio y a su uso en el tratamiento de diversos estados de enfermedad, incluyendo enfermedades cardiovasculares y diabetes. Se refiere también a métodos para la preparación y uso de los compuestos y a composiciones farmacéuticas que contienen los mismos.Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque: la línea punteada representa un doble enlace opcional; Y es -C(R5)2- o -C(O)-; X1 es N y X2 es N, X1 es N y X2 es CR3, o X1 es CR3 y X2 es N, y la línea punteada es un doble enlace; o X1 es C(R3)2 y X2 es NR4, -O-, -S-, -S(O)- o -S(O)2-, o X1 y X2 son ambos C(R3)2, y la línea punteada es un enlace simple; siempre que: cuando la línea punteada es un enlace simple e Y es -C(R5)2-; entonces ambos X1 y X2 son C(R3)2; cuando la línea punteada es un enlace simple e Y es -C(O)-; entonces X1 es C(R3)2; y cuando la línea punteada es un enlace doble; Y es -C(O)-; Q es un enlace covalente o alquinileno C2-4; R1 es cicloalquilo C3-6, cicloalquenilo C3-6, arilo, heterociclilo o heteroarilo; en donde dichos cicloalquilo C3-6, cicloalquenilo C3-6, arilo, heterociclilo o heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, CN, -SF5, -Si(CH3)3, -O-R20, -S-R20, -C(O)-R20, -C(O)-OR20, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-S(O)2-R22, -S(O)2-R20, -S(O)2-N(R20)(R22), alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, arilo, heteroarilo y heterociclilo; y en donde dichos alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, arilo, heteroarilo o heterociclilo están opcionalmente sustituidos con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, arilo, heterociclilo, heteroarilo, alquilo C1-4, cicloalquilo C3-6, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN y -O-R20; R2 es -R6, alquileno C1-6-R6, -L-R6, -L-alquileno C1-6-R6, alquileno C1-6-L-R6 o alquileno C1-6-L-alquileno C1-6-R6; L es -O-, -S-, -C(O)-, -S(O)2-, -NR20S(O)2-, -S(O)2NR20-, -C(O)NR20- o -NR20C(O)-; siempre que cuando Y es -C(R5)2-, entonces L es -C(O)- o -S(O)2-, y R2 es -L-R6, -L-alquileno C1-6-R6, alquileno C1-6 o -alquileno C1-6-L-alquileno C1-6-R6; cada R3 es independientemente hidrógeno, alquilo C1-6, cicloalquilo C3-6, arilo, heteroarilo o heterociclilo; en donde dicho alquilo C1-6 está opcionalmente sustituido con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, cicloalquilo C3-6, arilo, heterociclilo, heteroarilo, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN y -O-R20; en donde dichos cicloalquilo, arilo, heterociclilo y heteroarilo están opcionalmente sustituidos adicionalmente con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, alquilo C1-6, aralquilo, cicloalquilo, arilo, heterociclilo, heteroarilo, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN y -O-R20; y en donde dichos alquilo C1-6, aralquilo, cicloalquilo C3-6, arilo, heterociclilo y heteroarilo están opcionalmente sustituidos adicionalmente con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN y -O-R20; o cuando X1 es C(R3)2, dos R3 pueden unirse entre sí con el átomo de carbón al cual están unidos para formar un cicloalquilo C3-6 o heterociclilo; R4 es hidrógeno, alquilo C1-6, alcoxilo C1-4, -C(O)-OR20, -C(O)-N(R20)(R22), -N(R20)-S(O)2-R20, cicloalquilo C3-6, arilo, heteroarilo o heterociclilo; en donde dicho alquilo C1-6 está opcionalmente sustituido con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, cicloalquilo C3-6, arilo, heterociclilo, heteroarilo, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN y -O-R20; en donde dichos cicloalquilo C3-6, arilo, heterociclilo o heteroarilo están opcionalmente sustituidos adicionalmente con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, alquilo C1-6, aralquilo, cicloalquilo, arilo, heterociclilo, heteroarilo, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN, y -O-R20; y en donde dichos alquilo C1-6, aralquilo, cicloalquilo, arilo, heterociclilo, heteroarilo, están opcionalmente sustituidos adicionalmente con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de hidroxilo, halo, -NO2, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN y -O-R20; cada R5 es independientemente hidrógeno o alquilo C1-6; R6 es cicloalquilo C3-6, arilo, heteroarilo o heterociclilo; en donde dichos cicloalquilo C3-6, arilo, heteroarilo o heterociclilo están opcionalmente sustituidos con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de alquilo C1-6, alquinilo C2-4, halo, -NO2, cicloalquilo C3-6, arilo, heterociclilo, heteroarilo, -N(R20)(R22), -N(R20)-S(O)2-R20, -N(R20)-C(O)-R22, -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -S(O)2-R20, -CN y -O-R20; en donde dichos alquilo C1-6, cicloalquilo C3-6, arilo, heterociclilo o heteroarilo están opcionalmente sustituidos adicionalmente con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de halo, -NO2, alquilo C, cicloalquilo C3-6, arilo, heterociclilo, heteroarilo, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN y -O-R20; y en donde dichos alquilo C1-6, cicloalquilo C3-6, arilo, heterociclilo o heteroarilo están opcionalmente sustituidos adicionalmente con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de alquilo C1-6, halo, arilo, -NO2, -CF3, -N(R20)(R22), -C(O)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN, -S(O)2-R20 y -O-R20; R20 y R22 son en cada caso independientemente hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo; y en donde los alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de hidroxilo, halo, alquilo C1-4, aralquilo, -N(R26)(R28), aminoacilo, -NO2, -S(O)2-R26, -CN, alcoxilo C1-3, -CF3, -OCF3, -OCH2CF3, -C(O)-NH2, -C(O)-R26, -C(O)-OR26, arilo, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo; en donde dicho aralquilo, heterociclilo o heteroarilo está opcionalmente sustituido adicionalmente con alquilo C1-4, -CF3, arilo o cicloalquilo C3-6; o cuando R20 y R22 están unidos a un átomo de nitrógeno común R20 y R22 pueden unirse para formar un anillo heterocíclico o heteroarilo el cual es luego opcionalmente sustituido con uno, dos o tres sustituyentes independientemente seleccionados a partir del grupo que consiste de hidroxilo, halo, alquilo, aralquilo, arilo, ariloxilo, aralquiloxilo, heteroariloxilo, amino sustituido, aminoacilo, -NO2, -S(O)2-R26, -CN, alcoxilo C1-3, hidroximetilo, -CF3, -OCF3, arilo, heteroarilo y cicloalquilo C3-6; y R26 y R28 están cada uno independientemente seleccionados a partir del grupo que consiste de hidrógeno, alquilo C1-6, alquenilo C1-6, cicloalquilo C3-6, arilo y heteroarilo; y en donde el alquilo C1-6, cicloalquilo C3-6, arilo o heteroarilo puede estar adicionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados a partir del grupo que consiste de hidroxilo, halo, alcoxilo C1-4, -CF3, -OCF3 y cicloalquilo C3-6; o una sal, estereoisómero y/o tautómero farmacéuticamente aceptable del mismo.
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US9115096B2 (en) 2015-08-25
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