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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
Other languages
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.)
Filing date
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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  • Orthopedic Medicine & Surgery (AREA)

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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