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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ARP150101743A
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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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EP (1) EP3152199B1 (es)
JP (1) JP6195684B2 (es)
KR (1) KR101906031B1 (es)
CN (1) CN106414429B (es)
AR (1) AR100712A1 (es)
AU (1) AU2015270118C1 (es)
CA (1) CA2947002C (es)
CL (1) CL2016003092A1 (es)
CY (1) CY1120864T1 (es)
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EA (1) EA031104B1 (es)
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HR (1) HRP20181670T1 (es)
HU (1) HUE040489T2 (es)
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