AR041508A1 - Compuestos con actividad en los receptores de glutamato metabotropicos - Google Patents

Compuestos con actividad en los receptores de glutamato metabotropicos

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Publication number
AR041508A1
AR041508A1 ARP030102892A ARP030102892A AR041508A1 AR 041508 A1 AR041508 A1 AR 041508A1 AR P030102892 A ARP030102892 A AR P030102892A AR P030102892 A ARP030102892 A AR P030102892A AR 041508 A1 AR041508 A1 AR 041508A1
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AR
Argentina
Prior art keywords
6alkyl
nr6r7
4alkyl
3alkyl
6alkylnr6
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ARP030102892A
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English (en)
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Astra Ab
Nps Pharma Inc
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Application filed by Astra Ab, Nps Pharma Inc filed Critical Astra Ab
Publication of AR041508A1 publication Critical patent/AR041508A1/es

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Abstract

Los compuestos exhiben actividad en los receptores de glutamato metabotrópicos en especial a nivel del receptor m GluR5 por lo tanto son útiles para trastornos neurológicos, psiquiátricos agudos y dolor. También se reivindican formulaciones farmacéuticas, procesos para preparar los compuestos, usos y métodos. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1) donde: P se selecciona entre el grupo formado por C3-7 alquilo y un anillo de entre 3 y 8 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O o S, donde dicho anillo puede fusionarse con un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O o S; R1 se selecciona entre el grupo formado por H, hidroxi, halo, nitro, C1-6alquilhalo, OC1-6alquilhalo, C1-6alquilo, OC1-6alquilo, C2-6alquenilo, OC2-6alquenilo, C2-6alquinilo, OC2-6alquinilo, C0-6alquilC3-6cicloalquilo, OC0-6alquilC3-6cicloalquilo, C0-6alquilarilo, OC0-6alquilarilo, (CO)R6, O(CO)R6, O(CO)OR6, C1-6alquilOR6, OC2-6alquilOR6, C1-6alquil(CO)R6, OC1-6alquil(CO)R6, C0-6alquilCO2R6, OC1-6alquilCO2R6, C0-6alquilciano, OC2-6alquilciano, C0-6alquilNR6R7, OC2-6alquilNR6R7, C1-6alquil(CO)NR6R7, OC1-6alquil(CO)NR6R7, C0-6alquilNR6(CO)R7, OC2-6alquilNR6(CO)R7, C0-6alquilNR6(CO)NR6R7, C0-6alquilSR6, OC2-6alquilSR6, C0-6alquil(SO)R6, OC2-6alquil(SO)R6, C0-6alquilSO2R6, OC2-6alquilSO2R6, C0-6alquil(SO2)NR6R7, OC2-6alquil(SO2)NR6R7, C0-6alquilNR6(SO2)R7, OC2-6alquilNR6(SO2)R7, C0-6alquilNR6(SO2)NR6R7, OC2-6alquilNR6(SO2)NR6R7, (CO)NR6R7, O(CO)NR6R7, NR6OR7, C0-6alquilNR6(CO)OR7, OC2-6alquilNR6(CO)OR7, SO3R6 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O o S, donde dicho anillo puede estar sustituido por uno o más A; M1 se selecciona entre el grupo formado por un enlace, C1-3alquilo, C2-3alquenilo, C2-3alquinilo, C0-4alquil(CO)C0-4alquilo, C0-3alquilOC0-3alquilo, C0-3alquil(CO)NR7R6, C0-3alquil(CO)NR7R6C1-3alquilo, C0-4alquilNR7R6, C0-3alquilSC0-3alquilo, C0-3alquil(SO)C0-3alquilo y C0-3alquil(SO2)C0-3alquilo; X1, X2 y X3 se seleccionan en forma independiente entre el grupo formado por CR, CO, N, NR, O y S; R se selecciona entre el grupo formado por H, C0-3alquuilo, halo, C0-3alquilOR5, C0-3alquilNR5R6, C0-3alquil(CO)OR5, C0-3alquilNR5R6 y C0-3alquilarilo; R2 se selecciona entre el grupo formado por H, hidroxi, oxo, =NR6, =NOR6, C1-4alquilhalo, halo, C1-4alquilo, OC1-4alquilo, O(CO)C1-4alquilo, C1-4alquil(SO)C0-4alquilo, C1-4alquil(SO2)C0-4alquilo, (SO)C0-4alquilo, (SO2)C0-4alquilo, OC1-4alquilo, C0-4alquilciano, C1-4alquilOR6 y C0-4alquilNR6R7; M2 se selecciona entre el grupo formado por un enlace, C1-3alquilo, C2-3 alquenilo, C2-3alquinilo, C0-4alquil(CO)C0-4alquilo, C0-3alquilOC0-3alquilo, C0-3alquilNR6C1-3alquilo, C0-3alquil(CO)NR6, C0-4alquilNR6R7, C0-3alquilSC0-3alquilo, C0-3alquil(SO)C0-3alquilo y C0-3alquil(SO2)C0-3alquilo; R3 se selecciona entre el grupo formado por H, hidroxi, oxo, =NR6, =NOR6, C1-4alquilhalo, halo, C1-4alquilo, OC1-4alquilo, O(CO)C1-4alquilo, C1-4alquil(SO)C0-4alquilo, C1-4alquil(SO2)C0-4alquilo, (SO)C0-4alquilo, (SO2)C0-4alquilo, C0-4alquilciano, C1-4alquilOR6 y C0-4alquilNR6R7; X4 se selecciona entre C, CR o N; X5 se selecciona entre C, CR, o N; Q es un anillo de 4 a 8 miembros o biciclo que contiene uno o más átomos seleccionados en forma independiente entre C, N, O o S, donde dicho anillo o biciclo puede fusionarse con un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O o S y donde el anillo fusionado puede sustituirse con uno o más A; R4 se selecciona entre el grupo formado por H, hidroxi, halo, nitro, oxo, C1-6alquilhalo, C1-6alquilo, OC1-6alquilo, C0-6alquilC3-6cicloalquilo, C0-6alquilarilo, OC0-6alquilarilo, (CO)R6, O(CO)R6, C1-6alquilOR6, OC2-6alquilOR6, C1-6alquil(CO)R6, OC1-6alquil(CO)R6, C0-6alquilCO2R6, OC1-6alquilCO2R6, C0-6alquilciano, OC1-6alquilciano, C0-6alquilNR6R7, OC2-6alquilNR6R7, C0-6alquil(CO)NR6R7, OC0-6alquil(CO)NR6R7, C0-6alquilNR6(CO)R7, OC2-6alquilNR6(CO)R7, C0-6alquilNR6(CO)NR6R7, C0-6alquilSR6, OC2-6alquilSR6, C0-6alquil(SO)R6, OC2-6alquil(SO)R6, C0-6alquilSO2R6, OC0-6alquilSO2R6, C0-6alquil(SO2)NR6R7, OC0-6alquil(SO2)NR6R7, C0-6alquilNR6(SO2)R7, OC2-6alquilNR6(SO2)R7, NR6OR7, NR6(CO)OR7, SO3R6 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O o S, donde dicho anillo puede estar sustituido por uno o más A; R5 se selecciona entre el grupo formado por H, hidroxi, halo, oxo, C1-6alquilhalo, OC1-6alquilhalo, C1-6alquilo, OC1-6alquilo, C0-6alquilC3-6cicloalquilo, C0-6alquilarilo, OC0-6alquilarilo, (CO)R6, O(CO)R6, O(CO)OR6, (CO)OR6, C1-6alquilOR6, OC2-6alquilOR6, C1-6alquil(CO)R6, OC1-6alquil(CO)R6, C0-6alquilCO2R6, OC1-6alquilCO2R6, C0-6alquilciano, OC0-6alquilciano, C0-6alquilNR6R7, OC2-6alquilNR6R7, C1-6alquil(CO)NR6R7, C0-6alquil(CO)heteroarilo, C0-6alquil(CO)arilo, OC1-6alquil(CO)NR6R7, C1-6alquil(CO)NR6R7, C0-6alquilNR6(CO)R7, OC2-6alquilNR6(CO)R7, C0-6alquilNR6(CO)NR6R7, C1-6alquilNR6(CO)OR7, C0-6alquilSR6, OC2-6alquilSR6, C0-6alquil(SO)R6, OC1-6alquil(SO)R6, C0-6alquilSO2R6, OC0-6alquilSO2R6, C0-6alquil(SO2)NR6R7, OC0-6alquil(SO2)NR6R7, C0-6alquilNR6(SO2)R7, OC2-6alquilNR6(SO2)R7, C0-6alquilNR6(SO2)NR6R7, OC2-6alquilNR6(SO2)NR6R7, (CO)NR6R7, O(CO)NR6R7, NR6OR7, NR6(CO)OR7, SO3R6 y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N, O o S, donde dicho anillo puede estar sustituido por uno o más A; R6 y R7 se seleccionan en forma independiente entre H, C1-6alquilo, C0-6alquilC3-6cicloalquilo, C0-6alquilarilo, C1-6alquilheteroarilo y un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N O, o S, y donde R6 Y R7 pueden formar juntos un anillo de 5 o 6 miembros que contiene uno o más átomos seleccionados en forma independiente entre C, N O o S; donde cualquier C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C0-6alquilC3-6cicloalquilo, C0-6alquilarilo y C0-6alquilheteroarilo definido bajo R1, R2, R3, R4, R5, R6 y R7 puede sustituirse con uno o más A; A se selecciona entre el grupo formado por H, hidroxi, oxo, halo, nitro, C1-6alquilhalo, OC1-6alquilhalo, C1-6alquilo, C0-4alquilC3-6cicloalquilo, C2-6alquenilo, OC1-6alquilo, C0-3alquilarilo, C1-6alquilOR6, OC2-6alquilOR6, C1-6alquilSR6, OC2-6alquilSR6, (CO)R6, O(CO)R6, OC2-6alquilciano, C0-6alquilciano, C0-6alquilCO2R6, OC1-6alquilCO2R6, O(CO)OR6, OC1-6alquil(CO)R6, C1-6alquil(CO)R6, NR6OR7, C0-6alquiNR6R7, OC2-6alquilNR6R7, C0-6alquil(CO)NR6R7, OC1-6alquil(CO)NR6R7, OC2-6alquilNR6(CO)R7, C0-6alquilNR6(CO)R7, C0-6alquilNR6(CO)NR6R7, O(CO)NR6R7, NR6(CO)OR7, C0-6alquil(SO2)NR6R7, OC2-6alquil(SO2)NR6R7, C0-6alquilNR6(SO2)R7, OC2-6alquilNR6(SO2)R7, SO3R6, C1-6alquilNR6(SO2)NR6R7, OC2-6alquil(SO2)R6, C0-6alquil(SO2)R6, C0-6alquil(SO)R6 y OC2-6alquil(SO)R6; m y p se seleccionan en forma independiente entre el grupo formado por 0, 1, 2, 3 y 4; n o y q se seleccionan cada uno en forma independiente entre 0, 1, 2, o 3; o su sal.
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US20040132726A1 (en) 2004-07-08
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