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AR097431A1 - Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim - Google Patents

Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim

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AR097431A1
AR097431A1 ARP140103166A ARP140103166A AR097431A1 AR 097431 A1 AR097431 A1 AR 097431A1 AR P140103166 A ARP140103166 A AR P140103166A AR P140103166 A ARP140103166 A AR P140103166A AR 097431 A1 AR097431 A1 AR 097431A1
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Argentina
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alkyl
nrc6rd6
cycloalkyl
independently selected
nrc2rd2
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Li Yun
M Long - Burns David
Huang Taisheng
Mei Song
Pan Jun
Vechorkin Oleg
Ye Hai
Fen - Zhu Wenyu
Wang Anlai
xue Chu
Biao - Feng Hao
Rafalski Maria
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Incyte Corp
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Abstract

La presente divulgación describe compuestos de carboxamida de furo y tienopiridina, así como sus composiciones y métodos de uso. Los compuestos inhiben la actividad de las quinasas Pim y son útiles para el tratamiento de enfermedades relacionadas con la actividad de las quinasas Pim incluido, p. ej., el cáncer y otras enfermedades. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de este caracterizada por que: X es S u O; A⁵ es N o C-R⁵; CyA es un grupo heteroarilo monocíclico de 5 a 6 miembros, en donde los átomos del anillo del grupo heteroarilo que forman CyA consisten en átomos de carbono y en 1, 2 ó 3 heteroátomos seleccionados de N, O y S, y en donde el grupo heteroarilo monocíclico de 5 a 6 miembros que forma CyA es no sustituido o sustituido por 1, 2 ó 3 RA; cada RA se selecciona independientemente de RA¹, halógeno, haloalquilo C₁₋₆, CN, ORᵃ¹, SRᵃ¹, C(=O)Rᵇ¹, C(=O)NRᶜ¹Rᵈ¹, C(=O)ORᵃ¹, OC(=O)Rᵇ¹, OC(=O)NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C(=O)Rᵇ¹, NRᶜ¹C(=O)NRᶜ¹Rᵈ¹, NRᶜ¹C(=O)ORᵃ¹, C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹C(=NRᵉ¹)NRᶜ¹Rᵈ¹, S(=O)Rᵇ¹, S(=O)NRᶜ¹Rᵈ¹, S(=O)₂Rᵇ¹, NRᶜ¹S(=O)₂Rᵇ¹ y S(=O)₂NRᶜ¹Rᵈ¹; cada RA¹ se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆, en donde cada alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆ que forman RA¹ es no sustituido o sustituido por 1, 2, 3, 4 ó 5 sustituyentes seleccionados independientemente de halógeno, CN, ORᵃ¹, SRᵃ¹, C(=O)Rᵇ¹, C(=O)NRᶜ¹Rᵈ¹, C(=O)ORᵃ¹, OC(=O)Rᵇ¹, OC(=O)NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C(=O)Rᵇ¹, NRᶜ¹C(=O)NRᶜ¹Rᵈ¹, NRᶜ¹C(=O)ORᵃ¹, C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹C(=NRᵉ¹)NRᶜ¹Rᵈ¹, S(=O)Rᵇ¹, S(=O)NRᶜ¹Rᵈ¹, S(=O)₂Rᵇ¹, NRᶜ¹S(=O)₂Rᵇ¹ y S(=O)₂NRᶜ¹Rᵈ¹; CyB es arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros o heterocicloalquilo de 4 - 10 miembros en donde los átomos del anillo de heteroarilo o heterocicloalquilo que forman CyB consisten en átomos de carbono y 1, 2 ó 3 heteroátomos seleccionados de O, N y S, y en donde cada uno de dicho arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros o heterocicloalquilo de 4 - 10 miembros que forman CyB es no sustituido o sustituido por 1, 2, 3, 4 ó 5 RB; cada RB se selecciona independientemente de RB¹, RB², halógeno, haloalquilo C₁₋₆, CN, ORᵃ², SRᵃ², C(=O)Rᵇ², C(=O)NRᶜ²Rᵈ², C(=O)ORᵃ², OC(=O)Rᵇ², OC(=O)NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C(=O)Rᵈ², NRᶜ²C(=O)NRᶜ²Rᵈ², NRᶜ²C(=O)ORᵃ², C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²C(=NRᵉ²)NRᶜ²Rᵈ², S(=O)Rᵇ², S(=O)NRᶜ²Rᵈ², S(=O)₂Rᵇ², NRᶜ²S(=O)₂Rᵇ² y S(=O)₂NRᶜ²Rᵈ²; cada RB¹ se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆, en donde cada uno de dicho alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆ de RB¹ es no sustituido o sustituido por 1, 2, 3, 4 ó 5 RB³; cada RB² se selecciona independientemente de arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 4 - 10 miembros, en donde cada uno de dicho arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros y heterocicloalquilo de 4 - 10 miembros que forman RB² es no sustituido o sustituido por 1, 2, 3, 4 ó 5 RB⁴; cada RB³ se selecciona independientemente de RB², halógeno, haloalquilo C₁₋₆, CN, ORᵃ², SRᵃ², C(=O)Rᵇ², C(=O)NRᶜ²Rᵈ², C(=O)ORᵃ², OC(=O)Rᵇ², OC(=O)NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C(=O)Rᵇ², NRᶜ²C(=O)NRᶜ²Rᵈ², NRᶜ²C(=O)ORᵃ², C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²C(=NRᵉ²)NRᶜ²Rᵈ², S(=O)Rᵇ², S(=O)NRᶜ²Rᵈ², S(=O)₂Rᵇ², NRᶜ²S(=O)₂Rᵇ² y S(=O)₂NRᶜ²Rᵈ²; cada RB⁴ se selecciona independientemente de halógeno, haloalquilo C₁₋₆, CN, ORᵃ², SRᵃ², C(=O)Rᵇ², C(=O)NRᶜ²Rᵈ², C(=O)ORᵃ², OC(=O)Rᵇ², OC(=O)NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C(=O)Rᵇ², NRᶜ²C(=O)NRᶜ²Rᵈ², NRᶜ²C(=O)ORᵃ², C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²C(=NRᵉ²)NRᶜ²Rᵈ², S(=O)Rᵇ², S(=O)NRᶜ²Rᵈ², S(=O)₂Rᵇ², NRᶜ²S(=O)₂Rᵇ² y S(=O)₂NRᶜ²Rᵈ²; R² es H, halógeno o NH₂; R⁵ es H, halógeno, R⁵A, haloalquilo C₁₋₆, CN, ORᵃ³, SRᵃ³, C(=O)Rᵇ³, C(=O)NRᶜ³Rᵈ³, C(=O)ORᵃ³, OC(=O)Rᵇ³, OC(=O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(=O)Rᵇ³, NRᶜ³C(=O)NRᶜ³Rᵈ³, NRᶜ³C(=O)ORᵃ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, S(=O)Rᵇ³, S(=O)NRᶜ³Rᵈ³, S(=O)₂Rᵇ³, NRᶜ³S(=O)₂Rᵇ³ o S(=O)₂NRᶜ³Rᵈ³; R⁵A es alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, o fenilo, en donde cada uno de dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇ o fenilo que forman R⁵A es no sustituido o sustituido por 1, 2, 3, 4 ó 5 sustituyentes seleccionados independientemente de halógeno, CN, ORᵃ³, SRᵃ³, C(=O)Rᵇ³, C(=O)NRᶜ³Rᵈ³, C(=O)ORᵇ³, OC(=O)Rᵇ³, OC(=O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(=O)Rᵇ³, NRᶜ³C(=O)NRᵃ³Rᵈ³, NRᶜ³C(=O)ORᵃ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, S(=O)Rᵇ³, S(=O)NRᶜ³Rᵈ³, S(=O)₂Rᵇ³, NRᶜ³S(=O)₂Rᵇ³ y S(=O)₂NRᶜ³Rᵈ³; R⁶ es H, halógeno, R⁶A, haloalquilo C₁₋₆, CN, ORᵃ⁴, SRᵃ⁴, C(=O)Rᵇ⁴, C(=O)NRᶜ⁴Rᵈ⁴, C(=O)ORᵃ⁴, OC(=O)Rᵇ⁴, OC(=O)NRᶜ⁴Rᵈ⁴, NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=O)Rᵇ⁴, NRᶜ⁴C(=O)NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=O)ORᵃ⁴, C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, S(=O)Rᵇ⁴, S(=O)NRᶜ⁴Rᵈ⁴, S(=O)₂Rᵇ⁴, NRᶜ⁴S(=O)₂Rᵇ⁴ o S(=O)₂NRᶜ⁴Rᵈ⁴; R⁶A es alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₄-, arilo C₆₋₁₀-alquilo C₁₋₄-, heteroaril-alquilo C₁₋₄- de 5 - 10 miembros o heterocicloalquil-C₁₋₄ alquilo- de 4 - 10 miembros, en donde cada uno de dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₄-, arilo C₆₋₁₀-alquilo C₁₋₄-, heteroaril-alquilo C₁₋₄- de 5 - 10 miembros o heterocicloalquil-alquilo C₁₋₄- de 4 - 10 miembros que forman R⁶A es no sustituido o sustituido por 1, 2, 3, 4 ó 5 sustituyentes seleccionados independientemente de alquilo C₁₋₆, halógeno, haloalquilo C₁₋₆, CN, ORᵃ⁴, SRᵃ⁴, C(=O)Rᵇ⁴, C(=O)NRᶜ⁴Rᵈ⁴, C(=O)ORᵃ⁴, OC(=O)Rᵇ⁴, OC(=O)NRᶜ⁴Rᵈ⁴, NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=O)Rᵇ⁴, NRᶜ⁴C(=O)NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=O)ORᵃ⁴, C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, S(=O)Rᵇ⁴, S(=O)NRᶜ⁴Rᵈ⁴, S(=O)₂Rᵇ⁴, NRᶜ⁴S(=O)₂Rᵇ⁴ y S(=O)₂NRᶜ⁴Rᵈ⁴; R⁷ es H, halógeno, R⁷A, haloalquilo C₁₋₆, CN, ORᵃ⁵, SRᵃ⁵, C(=O)Rᵇ⁵, C(=O)NRᶜ⁵Rᵈ⁵, C(=O)ORᵃ⁵, OC(=O)Rᵇ⁵, OC(=O)NRᶜ⁵Rᵈ⁵, NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=O)Rᵇ⁵, NRᶜ⁵C(=O)NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=O)ORᵃ⁵, C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, S(=O)Rᵇ⁵, S(=O)NRᶜ⁵Rᵈ⁵, S(=O)₂Rᵇ⁵, NRᶜ⁵S(=O)₂Rᵇ⁵ o S(=O)₂NRᶜ⁵Rᵈ⁵; R⁷A es alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₄-, arilo C₆₋₁₀-alquilo C₁₋₄-, heteroaril-alquilo C₁₋₄- de 5 - 10 miembros o heterocicloalquil-alquilo C₁₋₄- de 4 - 10 miembros, en donde cada uno de dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₄-, arilo C₆₋₁₀-alquilo C₁₋₄-, heteroaril-alquilo C₁₋₄- de 5 - 10 miembros o heterocicloalquil-alquilo C₁₋₄- de 4 - 10 miembros que forman R⁷A es no sustituido o sustituido por 1, 2, 3, 4 ó 5 sustituyentes seleccionados independientemente de alquilo C₁₋₆, halógeno, haloalquilo C₁₋₆, CN, ORᵃ⁵, SRᵃ⁵, C(=O)Rᵇ⁵, C(=O)NRᶜ⁵Rᵈ⁵, C(=O)ORᵃ⁵, OC(=O)Rᵇ⁵, OC(=O)NRᶜ⁵Rᵈ⁵, NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=O)Rᵇ⁵, NRᶜ⁵C(=O)NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=O)ORᵃ⁵, C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, S(=O)Rᵇ⁵, S(=O)NRᶜ⁵Rᵈ⁵, S(=O)₂Rᵇ⁵, NRᶜ⁵S(=O)₂Rᵇ⁵ y S(=O)₂NRᶜ⁵Rᵈ⁵; Rᵃ¹, Rᵇ¹, Rᶜ¹ y Rᵈ¹ se seleccionan cada uno independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆; Rᵃ², Rᵇ², Rᶜ² y Rᵈ² se seleccionan cada uno independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆; Rᵃ³, Rᵇ³, Rᶜ³ y Rᵈ³ se seleccionan cada uno independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆; Rᵃ⁴, Rᵇ⁴, Rᶜ⁴ y Rᵈ⁴ se seleccionan cada uno independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₃, heteroaril-alquilo C₁₋₃ de 5 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₃ y heterocicloalquil-alquilo C₁₋₃ de 4 - 10 miembros, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₃, heteroaril-alquilo C₁₋₃ de 5 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₃ y heterocicloalquilo-alquilo C₁₋₃ de 4 - 10 miembros que forman Rᵃ⁴, Rᵇ⁴, Rᶜ⁴ y Rᵈ⁴ son cada uno no sustituido o sustituido por 1, 2, 3, 4 ó 5 sustituyentes seleccionados independientemente de alquilo C₁₋₆, halo, CN, ORᵃ⁶, SRᵃ⁶, C(=O)Rᵇ⁶, C(=O)NRᶜ⁶Rᵈ⁶, C(=O)ORᵃ⁶, OC(=O)Rᵇ⁶, OC(=O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)Rᵇ⁶, NRᶜ⁶C(=O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)ORᵃ⁶, C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, S(=O)Rᵇ⁶, S(=O)NRᶜ⁶Rᵈ⁶, S(=O)₂Rᵇ⁶, NRᶜ⁶S(=O)₂Rᵇ⁶ y S(=O)₂NRᶜ⁶Rᵈ⁶; o Rᶜ⁴ y Rᵈ⁴ unidos al mismo átomo de N, junto con el átomo de N al cual están unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o un grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido por 1, 2 ó 3 sustituyentes seleccionados independientemente de alquilo C₁₋₆, halo, CN, ORᵃ⁶, SRᵃ⁶, C(=O)Rᵇ⁶, C(=O)NRᶜ⁶Rᵈ⁶, C(=O)ORᵃ⁶, OC(=O)Rᵇ⁶, OC(=O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)Rᵇ⁶, NRᶜ⁶C(=O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)ORᵃ⁶, C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, S(=O)Rᵇ⁶, S(=O)NRᶜ⁶Rᵈ⁶, S(=O)₂Rᵇ⁶, NRᶜ⁶S(=O)₂RᵃRᵇ y S(=O)₂NRᶜ⁶Rᵈ⁶; Rᵃ⁵, Rᵇ⁵, Rᶜ⁵ y Rᵈ⁵ se seleccionan cada uno independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₃, heteroaril-alquilo C₁₋₃ de 5 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₃, y heterocicloalquil-alquilo C₁₋₃ de 4 - 10 miembros, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₇, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₃, heteroaril-alquilo C₁₋₃ de 5 - 10 miembros, cicloalquilo C₃₋₇-alquilo C₁₋₃ y heterocicloalquilo-alquilo C₁₋₃ de 4 - 10 miembros que forman Rᵃ⁵, Rᵇ⁵, Rᶜ⁵ y Rᵈ⁵ son cada uno no sustituido o sustituido por 1, 2, 3, 4 ó 5 sustituyentes seleccionados independientemente de alquilo C₁₋₆, halo, CN, ORᵃ⁶, SRᵃ⁶, C(=O)Rᵇ⁶, C(=O)NRᶜ⁶Rᵈ⁶, C(=O)ORᵃ⁶, OC(=O)Rᵇ⁶, OC(=O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)Rᵇ⁶, NRᶜ⁶C(=O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)ORᵃ⁶, C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, S(=O)Rᵇ⁶, S(=O)NRᶜ⁶Rᵈ⁶, S(=O)₂Rᵇ⁶, NRᶜ⁶S(=O)₂Rᵇ⁶ y S(=O)₂NRᶜ⁶Rᵈ⁶; o Rᶜ⁵ y Rᵈ⁵ unidos al mismo átomo de N, junto con el átomo de N al cual están unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o un grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido por 1, 2 ó 3 sustituyentes seleccionados independientemente de alquilo C₁₋₆, halo, CN, ORᵃ⁶, SRᵃ⁶, C(=O)Rᵇ⁶, C(=O)NRᶜ⁶Rᵈ⁶, C(=O)ORᵃ⁶, OC(=O)Rᵇ⁶, OC(=O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)Rᵇ⁶, NRᶜ⁶C(=O) NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=O)ORᵃ⁶, C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, S(=O)Rᵇ⁶, S(=O)NRᶜ⁶Rᵈ⁶, S(=O)₂Rᵇ⁶, NRᶜ⁶S(=O)₂Rᵇ⁶ y S(=O)₂NRᶜ⁶Rᵈ⁶; Rᵃ⁶, Rᵇ⁶, Rᶜ⁶ y Rᵈ⁶ se seleccionan cada uno independientemente de H, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, cicloalquilo C₃₋₇ y heterocicloalquilo de 4 - 10 miembros, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, cicloalquilo de C₃₋₇ y heterocicloalquilo de 4 - 10 miembros que forman Rᵃ⁶, Rᵇ⁶, Rᶜ⁶ y Rᵈ⁶ son cada uno opcionalmente sustituidos por 1, 2 ó 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(alquilo C₁₋₆), N(alquilo C₁₋₆)₂, halo, alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆ y haloalcoxi C₁₋₆; o Rᶜ⁶ y Rᵈ⁶ unidos al mismo átomo de N, junto con el átomo de N al cual están unidos, forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros o un grupo heteroarilo de 5 miembros, cada uno opcionalmente sustituido por 1, 2 ó 3 sustituyentes seleccionados independientemente de OH, CN, amino, NH(alquilo C₁₋₆), N(alquilo C₁₋₆)₂, halo, alquilo C₁₋₅, alcoxi C₁₋₆, haloalquilo C₁₋₆ y haloalcoxi C₁₋₆; y Rᵉ¹, Rᵉ², Rᵉ³, Rᵉ⁴, Rᵉ⁵ y Rᵉ⁶ son cada uno independientemente, H, alquilo C₁₋₄, CN o NO₂.
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