AR066148A1 - Derivados puenteados de ciclohexeno bloqueadores del canal de calcio - Google Patents

Derivados puenteados de ciclohexeno bloqueadores del canal de calcio

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Publication number
AR066148A1
AR066148A1 ARP080101765A ARP080101765A AR066148A1 AR 066148 A1 AR066148 A1 AR 066148A1 AR P080101765 A ARP080101765 A AR P080101765A AR P080101765 A ARP080101765 A AR P080101765A AR 066148 A1 AR066148 A1 AR 066148A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
group
substituted
unsubstituted
Prior art date
Application number
ARP080101765A
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English (en)
Original Assignee
Actelion Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of AR066148A1 publication Critical patent/AR066148A1/es

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    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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Abstract

Reivindicacion 1: Un compuesto de formula (1) en el cual X representa un átomo de carbono, y R1a y R2a en conjunto forman un enlace; o X representa un átomo de carbono, R1a y R2a en conjunto forman un enlace, y R1 y R2 en conjunto forman el fragmento de formula (2) en donde el asterisco indica el punto de union de R2; o X representa un átomo de carbono, R1a representa hidrogeno o alcoxilo C1-4, y R2a representa hidrogeno; o X representa un átomo de carbono, R1 y R1a en conjunto forman un grupo 3H-benzofuran-2,2-diilo, y R2 y R2a ambos representan hidrogeno; o X representa un átomo de nitrogeno, R1a está ausente, y R2 y R2a ambos representan hidrogeno o y R2 y R2a en conjunto forman un grupo carbonilo; y R1 y R2, si no se indica de otra manera, representan de manera independiente hidrogeno; alquilo C1-5; arilo, que está no substituido, o de manera independientes, mono-, di-, o tri-substituido en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste en alquilo C1-4, alcoxilo C1-4, halogeno, trifluorometilo, trifluorometoxilo, ciano, y cicloalquilo C3-6; o heteroarilo, que está no substituido, o de manera independientes, mono-, di-, o tri-substituido en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste en alquilo C1-4, alcoxilo C1-4, halogeno, ciano, trifluorometilo, y trifluorometoxilo; con la condicion de que en el caso en que R2 represente arilo o heteroarilo, R1 no puede representar arilo o heteroarilo, en donde el arilo y el heteroarilo de manera independiente están no substituidos o substituidos tal como se define anteriormente; R3 representa hidrogeno, o -CO-R31; R31 representa alquilo C1-5, fluoroalquilo C1-5, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-3, alcoxilo C1-5, alcoxi C1-2-alquilo C1-3, o R32R33N-; R32 representa alquilo C1-5; R33 representa hidrogeno, o alquilo C1-5; n representa el entero 1, 2, 3 o 4; B representa un grupo -(CH2)m-, en donde m representa el entero 1, 2, 3, 4 o 5; o B en conjunto con R4 y el átomo de nitrogeno al cual B y R4 están unidos forman un anillo saturado de 4 a 6 miembros; A representa una cadena lineal alcan-diilo C1-3, en donde dicha cadena lineal alcan-diilo C1-3 está opcionalmente substituida con uno o más metilo; R4 representa hidrogeno; alquilo C1-5; alcoxi C1-2-alquilo C1-3; fluoroalquilo C1-3; cicloalquilo C3-6; cicloalquil C3-6-alquilo C1-3; o R4 en conjunto con B y el átomo de nitrogeno al cual R4 y B están unidos forman un anillo saturado de 4 a 6 miembros; W representa arilo, que está no substituido, mono-, di-, o tri-substituido (especialmente no substituido o di-substituido), en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste, en alquilo C1-4, alcoxilo C1-4, halogeno, trifluorometilo, trifluorometoxilo, ciano, y cicloalquilo C3-6 (especialmente de alcoxilo C1-4); o W representa heteroarilo, que está no substituido, mono-, di-, o tri-substituido, en donde los substituyentes se seleccionan de manera independiente desde el conjunto que consiste en alquilo C1-4, alcoxilo C1-4, halogeno, ciano, trifluorometilo, y trifluorometoxilo; o W representa un grupo seleccionado de entre radicales del grupo de formulas (3) en donde R5 representa hidrogeno, o alquilo C1-5; R6 y R7 representan de manera independiente hidrogeno; alquilo C1-5; o fenilo, que está independientemente no substituido, mono-, o di-substituido, en donde cada substituyente es independientemente seleccionado desde el conjunto que consiste en alquilo, alcoxilo, halogeno y trifluorometilo; R8, R9 y R10 representan de manera independiente hidrogeno, halogeno, alquilo C1-5, hidroxilo, alcoxilo C1-5, -O-CO-alquilo C1-5, fluoroalquilo C1-3, fluoroalcoxilo C1-3, -COOH, -CO-alcoxilo C1-5, alcoxi C1-2-alcoxilo C1-4, o -NH-CO-alquilo C1-5; R11 representa hidrogeno, o alquilo C1-5; R12 representa alquilo C1-5, que está no substituido, mono-, o di-substituido, en donde cada substituyente es independientemente seleccionado desde el conjunto que consiste en hidroxilo y alcoxilo C1-2; o R12 representa un anillo saturado de cuatro a ocho miembros carbono que opcionalmente contiene dos átomos oxígeno en el anillo, en donde los dos átomos de oxígeno en el anillo no están adyacentes entre sí; o una sal de tal compuesto. Reivindicacion 16: Un compuesto de formula (1) de acuerdo con cualquiera de las reivindicaciones 1 a 12, o una sal farmacéuticamente aceptable del mismo, para el tratamiento o la prevencion de angina cronica estable, hipertension, isquemia (renal y cardiaca), arritmias cardiacas incluyendo fibrilacion del atrio, hipertrofia cardiaca, o falla congestiva del corazon.
ARP080101765A 2007-04-27 2008-04-25 Derivados puenteados de ciclohexeno bloqueadores del canal de calcio AR066148A1 (es)

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