AR045445A1 - Compuestos ihinibidores de canales ionicos regulados por voltaje - Google Patents

Compuestos ihinibidores de canales ionicos regulados por voltaje

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Publication number
AR045445A1
AR045445A1 ARP040102793A ARP040102793A AR045445A1 AR 045445 A1 AR045445 A1 AR 045445A1 AR P040102793 A ARP040102793 A AR P040102793A AR P040102793 A ARP040102793 A AR P040102793A AR 045445 A1 AR045445 A1 AR 045445A1
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Argentina
Prior art keywords
ring
chr4
hydrogen
unsubstituted phenyl
optionally substituted
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ARP040102793A
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English (en)
Inventor
Dean Mitchell Wilson
Andreas Peter Termin
Thimothy Neubert
Jian Wang
Yulian Zhang
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Vertex Pharma
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Publication of AR045445A1 publication Critical patent/AR045445A1/es

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Abstract

La presente se refiere para el tratamiento de dolor agudo, crónico, neuropático o inflamatorio, artritis, migraña, cefaleas acuminadas, neuralgia del trigémino, neuralgia herpética, neuralgia generales, epilepsia, trastornos neurodegenerativos, ansiedad, depresión, miotonia, ataxia, esclerosis múltiple. Reivindicación 1: Un compuesto de la fórmula (1), o una de sus sales farmacéuticamente aceptables, en donde: p es 0, 1 ó 2; X1, X2, X3 y X4 se seleccionan, cada uno de modo independiente, de NR3, C=O, CHR4, S, O, S=O o SO2; R1 y R2 son cada uno, de modo independiente, hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C16, un anillo arilo de 5-6 miembros que tiene 0-5 heteroátomos seleccionados de modo independiente de nitrógeno, oxígeno o azufre o un anillo saturado o parcialmente insaturado de 3-7 miembros que tiene 0-3 heteroátomos seleccionados de modo independiente de nitrógeno, oxígeno o azufre; o R1 y R2 forman, junto con el átomo de nitrógeno al que están unidos, un anillo heterociclilo o heteroarilo opcionalmente sustituido de 3-8 miembros que tiene 1-3 heteroátomos seleccionados de modo independiente de nitrógeno, oxígeno o azufre, en donde R1, R2 o cualquier anillo formado por R1 y R2 tomados juntos están opcionalmente sustituidos cada uno, de modo independiente, en uno o varios átomos de carbono con 0-4 apariciones de -R5 y en uno o varios átomos de nitrógeno sustituibles con -R6; Anillo A es un anillo arilo monocíclico de 5-6 miembros o bicíclicos de 8-10 miembros que tiene 0-5 heteroátomos seleccionados de modo independiente de nitrógeno, oxígeno o azufre o un anillo saturado o parcialmente insaturado de 3-7 miembros que tiene 0-3 heteroátomos seleccionados de modo independiente de nitrógeno, oxígeno o azufre, opcionalmente sustituidos en uno o varios átomos de carbono con 0-5 apariciones de -R7 y en uno o varios átomos de nitrógeno sustituibles con -R8; cada aparición de R4, R5 y R7 es, de modo independiente, Q-Rx; en donde Q es un enlace o es una cadena de alquilideno C1-6, en donde hasta dos unidades de metileno no adyacentes de Q están opcional e independientemente reemplazados por CO, CO2, COCO, CNR, OCONR, NRNR, NRNRCO, NRCO, NRCO2, NRCONR, SO, SO2, NRSO2, SO2NR, NRSO2NR, O, S o NR; cada aparición de Rx se selecciona de modo independiente de R', halógeno, NO2 o CN; cada aparición de R se selecciona del modo independiente de hidrógeno o un grupo alifático C1-6 opcionalmente sustituido; cada aparición de R' se selecciona de modo independiente de hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C1-8, arilo C6-10, un anillo heteroarilo que tiene 5-10 átomos de anillo o un anillo heterociclilo que tiene 3-10 átomos de anillo o en donde R y R' tomados junto con los átomos a los que están unidos o dos apariciones de R' tomadas junto con los átomos a los que están unidas, forman un anillo cicloalquilo, heterociclilo, arilo o heteroarilo de 5-8 miembros que tiene 0-3 heteroátomos seleccionados de modo independiente de nitrógeno, oxígeno o azufre; y cada aparición de R3, R6 o R8 es, de modo independiente, R', -COR', -CO2(alifático C1-6), -CON(R')2 o -SO2R'; con la condición de que: a) R1 no sea hidrógeno cuando R2 es indazol-3-ilo opcionalmente sustituido; b) R1 no sea hidrógeno cuando R2 es pirazol-3-ilo opcionalmente sustituido; c) R1 no sea hidrógeno cuando R2 es 1,2,4-triazol-3-ilo; d) cuando p es 1, entonces: i) cuando R1 y R2, tomados con el átomo de nitrógeno, es N-morfolino y Anillo A es fenilo insustituido, entonces X1, X2, X3, y X4 no sean, respectivamente: a) CH2, CH(CH2)Ph, NR3 y CHCH3; b) CH2, CH2, CH2 y S; c) CH2, S, CH2 y S; d) CH2, CH2, S y CH2; e) CH2, CHMe, S y CH2; o f) CHMe, CH2, N(CH2)Ph y CH2; ii) R1 no sea hidrógeno y R2 no sea CH2Ph, (CH2)2O(CH2)2OH o -CH2(1,3-benzodioxol-5-il) cuando el Anillo A es imidazol-1-ilo; iii) cuando R1 y R2, tomados junto con el átomo de nitrógeno, es N-piperidinilo, entonces: a) cuando X1, X2 y X3 son CH2 Y CH4 es S, entonces el Anillo A no sea fenilo insustituido; y b) cuando X1, X2 y X4 son CH2; y X3 es S, entonces el Anillo A no sea fenilo insustituido; iv) cuando R1 y R2, tomados junto con el átomo de nitrógeno, es N-piperizinilo, X1, X2 y X3 son CH2, y X4 es S, entonces el Anillo A no sea 3-NO2Ph, 4-piridinilo o fenilo insustituido; v) cuando uno de X1, X2, X3 o X4 es NR3 y los otros de X1, X2, X3 o X4 son cada uno CH2 y R1 y R2 son cada uno Me, H, CH2Ph o (CH2)2NMe2, entonces el Anillo A no sea pirid-2-ilo sustituido en la posición (6); vi) cuando X1, X2 y X3 son cada uno CH2, X4 es S, R1 es H y R2 es -CH-C:::CH, entonces el Anillo A no sea fenilo insustituido; vii) cuando X1 es NMe; X2, X3 y X4 son cada uno CH2, R1 es H y R2 es fenilo insustituido, entonces el Anillo A no sea fenilo insustituido; y viii) cuando X1, X2 y X4 son cada uno CH2, X3 es S, R1 y R2 son cada uno Me, entonces el Anillo A no sea fenilo insustituido; y e) cuando o es 0, entonces: i) cuando X1 es CH2, X2 es NR3, X3 es C=O; o X1 es C=O, X2 es ChR4 y X3 es NR3; o X2 es NR3, X2 es C=O, y X3 es CHR4; o X1 es CH2, X2 es O y X3 es C=O, entonces cuando R1 es hidrógeno y R2 es fenilo insustituido o -CH2CH2Cl o cuando R1 y R2, tomados juntos forman piperazinilo, morfolino, piperidinilo o pirrolidinilo opcionalmente sustituido, entonces el Anillo A no es piperidinilo, piperazinilo, morfolino o pirrolidinilo opcionalmente sustituido; ii) cuando X1 es CHR4, X2 es SO2 y X3 es CHR4 y R1 y R2, tomados juntos son piperazinilo, entonces el Anillo A no sea fenilo insustituido; iii) cuando X1 y X2 son CHR2, X3 es O, R1 es hidrógeno y R2 es - C(=O)CH3, entonces el Anillo A no sea furilo sustituido; iv) cuando X1 es S, X2 es CHR4, X3 es CHR4; o X1 es CHR4, X2 es S y X3 es CHR4; o X1 y X2 son CHR4 y X3 es S, entonces el Anillo A no sea morfolino, pirrolidinilo, piperazinilo, piperidinilo ligado con N opcionalmente sustituido o no sea fenilo insustituido o ciclopropilo; v) cuando X1 es CHR4, X2 es NR3, X3 es CHR4 y R1 y R2 son ambos metilo, entonces el Anillo A no sea 6-metil-2-piridilo; vi) cuando X1 es NR3, X2 es C=O, X2 es NR3 y R1 y R2 son ambos metilo, entonces el Anillo A no sea fenilo insustituido; y vii) cuando X1 y X2 son CHR4, X3 es NR3, R1 es hidrógeno y R2 es fenilo insustituido, entonces el Anillo A no sea fenilo insustituido; y además, con la condición de que: a) cuando cada uno de X1, X2, X3 y X4 es CHR4 y p es 0 ó 1, entonces al menos un r4 sea distinto de hidrógeno; b) cuando cada uno de X1, X2, X3 y X4 es CHR4 y el Anillo A es un grupo piperizinilo sustituido o insustituido, entonces al menos un R4 sea distinto de hidrógeno; c) cuando cada uno de X1, X2, X3 y X4 es CHR4, R1 es hidrógeno y R2 es 1H-indazol-3-ilo, 7-fluoro-1H-indazol-3-ilo, 5-fluoro-1H-indazol-3-ilo, 5,7-difluoro-1H-indazol-3-ilo o 5-metil-1H-pirazolilo y el Anillo A es un grupo fenilo insustituido o es un grupo fenilo sustituido en la posición orto con Cl o CF3, entonces al menos un R4 sea distinto de hidrógeno; y d) 5(6H)-quinazolinona, 4-anilino-7,8-dihidro-2,7-difenil- y 5(6H)-quinazolinona, 4-anilino-7,8-dihidro-7,7- dimetil-2-fenil- quedan excluidos.
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