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AR100702A1 - Compuestos inhibidores de quinasa de unión tank - Google Patents

Compuestos inhibidores de quinasa de unión tank

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Publication number
AR100702A1
AR100702A1 ARP150101733A ARP150101733A AR100702A1 AR 100702 A1 AR100702 A1 AR 100702A1 AR P150101733 A ARP150101733 A AR P150101733A AR P150101733 A ARP150101733 A AR P150101733A AR 100702 A1 AR100702 A1 AR 100702A1
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Argentina
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nrarb
nrac
cycloalkyl
ora
alkyl
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ARP150101733A
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Gilead Sciences Inc
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Abstract

Se divulgan compuestos, métodos para su uso y preparación, que pueden inhibir o modular la actividad de la quinasa de unión TANK (TBK1), la quinasa I-Kappa-B (IKKe, IKBKE) útiles en el tratamiento, por ejemplo, del cáncer. Reivindicación 1: Un compuesto de la fórmula (1), donde: A es un anillo arilo o heteroarilo de 6 miembros; X¹ es CR² o N; X² y X³ son, de manera independiente, CR³ o N, siempre que, como máximo, solo uno de X² y X³ sea N; R¹ se selecciona del grupo que consiste en H, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -ORᵃ, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃRᵇ, -CN, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, donde cada C₁₋₆ alquilo, C₂₋₆ alquenilo y C₂₋₆ alquinilo está opcionalmente sustituido con de uno a cinco grupos R²⁰; o R¹ tiene la estructura de fórmula (2) donde B se selecciona del grupo que consiste en C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros y heterociclilo de 3 - 12 miembros; R² se selecciona del grupo que consiste en H, C₁₋₆ alquilo, C₃₋₁₀ cicloalquilo, heterociclilo de 3 - 12 miembros, C₁₋₆ heteroalquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -NRᵃRᵇ, halógeno, -CN, -NO₂, -ORᵃ, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ y -NRᵃS(O)₂Rᵇ; cada R³ se selecciona de manera independiente del grupo que consiste en H, C₁₋₆ alquilo, C₃₋₁₀ cicloalquilo, heterociclilo de 3 - 12 miembros, C₁₋₆ heteroalquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -NRᵃRᵇ, halógeno, -CN, -NO₂, -ORᵃ, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ y -NRᵃS(O)₂Rᵇ; cada R⁴ se selecciona de manera independiente del grupo que consiste en H, C₁₋₆ alquilo, C₁₋₆ heteroalquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -NRᵃRᵇ, halógeno, C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, -N₃, -CN, -NO₂ y -ORᵃ; R⁵ se selecciona del grupo que consiste en H, C₁₋₆ alquilo, C₁₋₆ heteroalquilo, -NRᵃRᵇ, halógeno, C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros, heterociclilo de 3 - 12 miembros y -O-R⁹, donde cada C₁₋₆ alquilo, C₁₋₆ heteroalquilo, C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros y heterociclilo de 3 - 12 miembros está opcionalmente sustituido con de uno a cinco grupos R²⁰; o R⁵ y un R⁴ se toman juntos para formar un arilo fusionado C₆, heteroarilo de 5 - 10 miembros, heterociclilo de 5 - 10 miembros o C₃₋₆ cicloalquilo cada uno, opcionalmente sustituido con uno a cinco grupos R²⁰; R⁶ es -CN ubicado en la posición meta (3) con respecto al punto de unión del anillo A; R⁷ se selecciona del grupo que consiste en H, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ heteroalquilo, -NRᵃRᵇ, halógeno, C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, -N₃, -CN, -NO₂, -ORᵃ, C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros y heterociclilo de 3 - 12 miembros, donde cada C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ heteroalquilo, C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros y heterociclilo de 3 - 12 miembros está opcionalmente sustituido con 1 - 5 grupos R²⁰; cada R⁸ se selecciona de manera independiente del grupo que consiste en H, C₁₋₆ alquilo, C₁₋₆ heteroalquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros y heterociclilo de 3 - 12 miembros, -NRᵃRᵇ, halógeno, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᶜ, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, -N₃, -CN, -NO₂ y -ORᵃ, donde cada C₁₋₆ alquilo, C₁₋₆ heteroalquilo, C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros y heterociclilo de 3 - 12 miembros está opcionalmente sustituido con de uno a cinco grupos R²⁰; o R⁷ y R⁸ se toman juntos para formar un C₃₋₁₀ cicloalquilo fusionado, espiro o puenteado o heterociclilo de 3 - 12 miembros, que están opcionalmente sustituidos con 1 - 5 grupos R²⁰; R⁹ es C₁₋₆ alquilo, heterociclilo de 3 - 12 miembros, C₆₋₁₀ arilo, C₃₋₁₀ cicloalquilo, heteroarilo de 5 - 10 miembros o heterociclilo de 3 - 12 miembros, cada uno de los cuales esté opcionalmente sustituido con de uno a cinco grupos R²⁰; n es 0 - 2; m es 0 - 3; cada R²⁰ es, de manera independiente, C₁₋₆ alquilo, C₃₋₁₀ cicloalquilo, C₁₋₆ heteroalquilo, heterociclilo de 3 - 12 miembros, C₆₋₁₀ arilo, heteroarilo de 5 - 10 miembros, halógeno, oxo, -ORᵃ, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, -N₃, -CN, o -NO₂, o dos grupos R²⁰ pueden unirse entre sí para formar un C₃₋₁₀ cicloalquilo fusionado, espiro o puenteado o anillo heterociclilo de 3 - 12 miembros, donde cada C₁₋₆ alquilo, C₃₋₁₀ cicloalquilo, C₁₋₆ heteroalquilo, heterociclilo de 3 - 12 miembros, C₆₋₁₀ arilo, heteroarilo de 5 - 10 miembros está opcionalmente sustituido con de uno a cinco halógeno, oxo, -ORᵃ, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃRᵇ, -NRᵃC(O)Rᵇ, -NRᵃC(O)ORᵇ, -S(O)₀₋₂Rᵃ, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, -N₃, -CN, o -NO₂; cada R²¹ es, de manera independiente, C₁₋₆ alquilo, C₃₋₁₀ cicloalquilo, C₁₋₆ heteroalquilo, heterociclilo de 3 - 12 miembros, C₆₋₁₀ arilo, heteroarilo de 5 - 10 miembros, hidroxilo, amino, C₁₋₆ alquilamino, -CN o halógeno; y cada Rᵃ y Rᵇ es, de manera independiente, H; o C₁₋₆ alquilo, C₃₋₁₀ cicloalquilo, C₁₋₆ heteroalquilo, heterociclilo de 3 - 12 miembros, C₆₋₁₀ arilo, heteroarilo de 5 - 10 miembros, cada uno de los cuales está opcionalmente sustituido con de uno a cinco grupos R²¹; o Rᵃ y Rᵇ junto con los átomos a los cuales están unidos forman un heterociclilo de 3 - 12 miembros opcionalmente sustituido con uno a cinco grupos R²¹; con la condición de que si R¹ es H, entonces todos los grupos R² y R³ son H; o una de sus sales farmacéuticamente aceptables.
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IL248888A0 (en) 2017-01-31
MA40058A (fr) 2015-12-10
KR20180131640A (ko) 2018-12-10
US10259811B2 (en) 2019-04-16
AU2015271837B2 (en) 2018-06-14
EA201692203A1 (ru) 2017-06-30
KR101926245B1 (ko) 2018-12-06
KR20170005876A (ko) 2017-01-16
AU2018208766A1 (en) 2018-08-16
JP2018150358A (ja) 2018-09-27
EP3152210C0 (en) 2023-07-05
ES2961577T3 (es) 2024-03-12
EP3152210A1 (en) 2017-04-12

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