AR100712A1 - Compuestos de pirazol como bloqueadores de los canales de calcio tipo t - Google Patents

Compuestos de pirazol como bloqueadores de los canales de calcio tipo t

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AR100712A1
AR100712A1 ARP150101743A ARP150101743A AR100712A1 AR 100712 A1 AR100712 A1 AR 100712A1 AR P150101743 A ARP150101743 A AR P150101743A AR P150101743 A ARP150101743 A AR P150101743A AR 100712 A1 AR100712 A1 AR 100712A1
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Argentina
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alkyl
cycloalkyl
fluoroalkyl
cyano
alkoxy
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Actelion Pharmaceuticals Ltd
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Abstract

Estos compuestos son útiles como bloqueadores de los canales de calcio tipo T. Reivindicación 1: Un compuesto de fórmula (1) en donde X representa un átomo de carbono anular o de nitrógeno anular; R¹ representa alquilo C₂₋₆; alquilo C₂₋₄ monosustituido con ciano o alcoxi C₁₋₃; fluoroalquilo C₁₋₄; fluoroalcoxi C₁₋₃; pentafluoro-sulfanilo; cicloalquilo C₃₋₆-L¹- en donde dicho cicloalquilo C₃₋₆ opcionalmente contiene un átomo de oxígeno anular; en donde dicho cicloalquilo C₃₋₆ no está sustituido o está monosustituido con flúor, alquilo C₁₋₃, alcoxi C₁₋₃, hidroxi, ciano o fluoroalquilo C₁₋₃ o disustituido con flúor o trisustituido con dos sustituyentes flúor y un sustituyente seleccionado entre alquilo C₁₋₃ y ciano; y el conector L¹ representa un enlace directo, alquileno C₁₋₂, oxígeno o alquilen C₁₋₂-oxi; heteroarilo de 5 ó 6 miembros, de manera independiente opcionalmente monosustituido con alquilo C₁₋₃; -NR¹¹R¹², en donde R¹¹ y R¹² independientemente representan hidrógeno, alquilo C₁₋₃, fluoroalquilo C₂₋₃, cicloalquilo C₃₋₆, cicloalquilo C₃₋₆ monosustituido o disustituido con flúor, cicloalquil C₃₋₆-alquilo C₁₋₃, alcoxi C₁₋₃-alquilo C₂₋₃; o R¹¹ y R¹², junto con el átomo de nitrógeno al cual están unidos, forman un anillo de 4 a 6 miembros opcionalmente monosustituido o disustituido con flúor; un grupo 2-oxo-pirrolidinilo o un grupo morfolinilo; y (R⁴)ₙ representa uno o dos sustituyentes opcionales independientemente seleccionados entre alquilo C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄, fluoroalquilo C₁₋₃, fluoroalcoxi C₁₋₃, halógeno y ciano; o R¹ junto con (R⁴)ₙ forman un anillo no aromático de 5 ó 6 miembros que está fusionado al anillo fenilo / piridina; en donde dicho anillo de 5 ó 6 miembros opcionalmente contiene uno o dos heteroátomos seleccionados independientemente entre oxígeno y nitrógeno; en donde dicho anillo no aromático de 5 ó 6 miembros fusionado está, de manera independiente, a su vez opcionalmente monosustituido con oxo o alquilo C₁₋₃; disustituido con alquilo C₁₋₃; o di-, tri- o tetra-sustituido en donde un sustituyente es oxo y los demás son alquilo C₁₋₃; o R¹ junto con (R⁴)ₙ forman un anillo aromático de 5 ó 6 miembros que está fusionado al anillo fenilo / piridina; en donde dicho anillo de 5 ó 6 miembros opcionalmente contiene uno o dos heteroátomos seleccionados de nitrógeno, en donde dicho anillo aromático de 5 ó 6 miembros fusionado está, de manera independiente, a su vez opcionalmente monosustituido o disustituido en donde los sustituyentes se seleccionan de manera independiente entre alquilo C₁₋₃, cicloalquilo C₃₋₆, fluoroalquilo C₁ o ciano; o R¹ representa metilo o halógeno; y (R⁴)ₙ representa un sustituyente seleccionado de fluoroalcoxi C₁₋₃ que está unido al anillo fenilo / piridinilo en la posición orto o meta por el punto de unión del grupo -CH₂-CO-NH-; Y representa un átomo de carbono anular o de nitrógeno anular; y R² representa alquilo C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄, cicloalquil C₃₋₆-oxi, fluoroalquilo C₁₋₃, fluoroalcoxi C₁₋₃, alcoxi C₁₋₃-alcoxi C₂₋₃, halógeno, ciano, o -NR²¹R²², en donde R²¹ y R²² independientemente representan hidrógeno o alquilo C₁₋₃, o R²¹ y R²², junto con el átomo de nitrógeno al cual están unidos, forman un anillo de 4 a 6 miembros opcionalmente monosustituido o disustituido con flúor o un grupo morfolinilo; y (R⁵)ₘ representa uno o dos sustituyentes opcionales independientemente seleccionados entre alquilo C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄, halógeno, ciano, fluoroalquilo C₁₋₃ y fluoroalcoxi C₁₋₃; o una sal de dicho compuesto.
ARP150101743A 2014-06-03 2015-06-02 Compuestos de pirazol como bloqueadores de los canales de calcio tipo t AR100712A1 (es)

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JP (1) JP6195684B2 (es)
KR (1) KR101906031B1 (es)
CN (1) CN106414429B (es)
AR (1) AR100712A1 (es)
AU (1) AU2015270118C1 (es)
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