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AR045747A1 - Derivados de 2,4 di (hetero)-arilamino-pirimidina como zap-70 inhibidores - Google Patents

Derivados de 2,4 di (hetero)-arilamino-pirimidina como zap-70 inhibidores

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Publication number
AR045747A1
AR045747A1 ARP040103281A ARP040103281A AR045747A1 AR 045747 A1 AR045747 A1 AR 045747A1 AR P040103281 A ARP040103281 A AR P040103281A AR P040103281 A ARP040103281 A AR P040103281A AR 045747 A1 AR045747 A1 AR 045747A1
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AR
Argentina
Prior art keywords
alkoxy
alkyl
atoms
cycloalkyl
ring
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ARP040103281A
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English (en)
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Novartis Ag
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Publication date
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Publication of AR045747A1 publication Critical patent/AR045747A1/es

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Abstract

Reivindicación 1: Un compuesto de la fórmula (1) en donde: Z es =CR2- o =N-; cada uno de R0, R1,R2, R3 y R4 independientemente es H, hidroxi, alquilo C1-8, alquenilo C2-8, cicloalquilo C3-8, cicloalquilo C3-8-alquilo C1-8, hidroxialquilo C1-8, alcoxi C1-8-alquilo C1-8, hidroxialcoxi C1-8-alquilo C1-8, arilo-alquilo C1-8, que opcionalmente pueden estar sustituidos sobre el anillo a través de hidroxi, alcoxi C1-8, carboxi o alcoxicarbonilo C1-8; o R3 y R4 forman junto con los átomos de N y de C a los cuales están unidos, un anillo heterocíclico de 5 a 10 miembros y que comprenden además 1, 2, o 3 átomos heterogéneos seleccionados de N, O y S; o cada uno de R1, R2 y R3, independientemente es halógeno, haloalquilo C1-8, alcoxi C1-8, alqueniloxi C2-8, alquiniloxi C2-8, haloalcoxi C1-8, cianoalcoxi C1-8, hidroxialcoxi C1-8, alcoxi C1-8-alcoxi C1-8, alcoxi C1-8-alcoxi C1-8-alcoxi C1-8, arilo, arilalcoxi C1-8, heteroarilo, heteroarilalquilo C1-4; un anillo heterocíclico de 5 a 10 miembros, nitro, carboxi, alcoxicarbonilo C2-8, alquilcarbonilo C2-8, -N(alquilo C1-8)C(O)-alquilo C1-8, -N(R10)R11, -CON(R10)R11, -SO2N(R10)R11; o alqueno C1-4-SO2N(R10)R11; en donde cada uno de R10 y R11 independientemente es H, OH, alquilo C1-8, alquenilo C2-8, alqueniloxi C2-8, haloalqueniloxi C2-8, cicloalquilo C3-8, cicloalquilo C3-8-alquilo C1-8, alcoxi C1-8-alquilo C1-8, hidroxialcoxi C1-8-alquilo C1-8, hidroxialquilo C1-8; (alquilo C1-8)-carbonilo, arilalquilo C1-8, el cual está opcionalmente sustituido sobre el anillo a través de hidroxi, alcoxi C1-8, carboxi o alcoxicarbonilo C2-8, o un anillo heterocíclico de 5 a 10 miembros; o R1 y R2 forman junto con los átomos de C a los cuales están unidos, arilo o un residuo de heteroarilo de 5 a 10 miembros que comprende 1 o 2 átomos heterogéneos seleccionados de N, O y S; o R1 y R2 forman junto con los átomos de C a los cuales están unidos, un residuo carbocíclico o heterocíclico no aromático de 5 a 15 miembros, en donde el residuo heterocíclico comprende de 1 a 5 átomos heterogéneos seleccionados de N, O y S; o cada uno de R5 y R6 independientemente es H, halógeno, ciano, alquilo C1-8, haloalquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, cicloalquilo C3-8-alquilo C1-8, arilo C5-10-alquilo C1-8; y (I) por lo menos uno de R7, R8 y R9 es: (vi) halógeno; o (vii) tetrahidropiran-2-ilmetoxi, tetrahidrofuran-2-ilmetoxi, tiazol-2-ilmetoxi, 2-(2-oxo-pirrolidin-1-il)-etoxi, 3-piridilmetoxi o fenil; o (viii) 2-hidroxi-etilamino, piperazin-1-ilo, 4-isopropil-piperazin-1-ilo, 4-(2-metoxietil)-piperazin-1-ilo, 4-fenil-piperazin-1-ilo o 4-acetil-piperazin-1-ilo; o (ix) alquilsulfanilo C1-8; o (x) alcoxi C1-8-alcoxi C1-8-alcoxi C1-8; o (II) R7 y R8 o R8 y R9, respectivamente, forman junto con los átomos de C a los cuales están unidos: (a) un anillo heterocíclico de 5 miembros conteniendo 2 átomos de N, en donde el anillo heterocíclico está sustituido por halógeno, 2-dimetilaminoetilo o 2,2,2,-trifluoroetilo; o (b) un anillo heterocíclico de 5 o 6 miembros que comprende un átomo de N; o (c) un residuo heterocíclico de 5 a 20 miembros, en donde el residuo heterocíclico comprende de 1 a 7 átomos de O; y en donde (I) hasta dos, y en (II) hasta uno de R7, R8 y R9 es H, hidroxi, alquilo C1-8, alquenilo C2-8, haloalquilo C1-8, alcoxi C1-8, cicloalquilo C3-8, cicloalquilo C3-8-alquilo C1-8, arilalquilo C1-8, -Y-R12, en donde Y es un enlace directo, O, alquileno C1-8, o -O-(CH2)1.8- , y R12un anillo heterocíclico de 5, 6 o 7 miembros sustituidos o no sustituidos, que comprende 1, 2 o 3 átomos heterogéneos seleccionados de N, O y S; carboxi; (alcoxi C1-8)-carbonilo; -N(alquilo C1-8)-CO-NR10R11, -CONR10R11; -N(R10)(R11), - SO2N(R10)(R11); o R7 y R8 o R8 y R9, respectivamente, forman junto con los átomos de C a los cuales están unidos, un heteroarilo de 5 a 6 miembros comprendiendo 1, 2 o 3 átomos heterogéneos seleccionados de N, O y S, o un anillo carbocíclico de 5 o 6 miembros; o (III) cada uno de R7, R8 y R9 es independientemente H, hidroxi, halógeno, alquilo C1-8, alquenilo C2-8, haloalquilo C1-8, alquilsulfanilo C1-8. alcoxi C1-8, alcoxi C1-8-alcoxi C1-8; alcoxi C1-8-alcoxi C1-8-alcoxi C1-8, cicloalquilo C3- 8, cicloalquilo C3-8-alquilo C1-8, arilalquilo C1-8, -Y-R12, en donde Y es un enlace directo, O, alquileno C1-8, o -O-(CH2)1.8-, y R12 es un anillo heterocíclico de 5, 6, o 7 miembros sustituido o no sustituido, que comprende 1, 2 o 3 átomos heterogéneos seleccionados de N, O y S; carboxi, (alcoxi C1-8)-carbonilo,-N(alquilo C1-8)-CO-NR10R11-, -CONR10R11; -N(R10)(R11), -SO2N(R10)(R11); o R7 y R8 o R8 y R9, respectivamente, forman junto con los átomos de C a los cuales están unidos, un residuo heteroarilo o heterocíclico de 5 o 6 miembros comprendiendo 1, 2 o 3 átomos heterogéneos seleccionados de N, O y S, o un anillo carbocíclico de 5 o 6 miembros, o un residuo heterocíclico de 7 a 20 miembros que comprenden de 1 a 7 átomos de O; y (A) Z es =CR2- y (e) R1 y R2 forman junto con los átomos de C a los cuales están unidos, un residuo carbocíclico o heterocíclico no aromático de 5 a 15 miembros, en donde el residuo heterocíclico comprende de 1 a 5 átomos heterogéneos seleccionados de N, O y S; o (f) R1 y R2 juntos forman un residuo de la fórmula -C(CH3)=CH-O-, -CH=CH-NH- o -N=C(CH3)-C(CH3)=N-; o (g) R1 y R2 juntos forman un residuo de la fórmula -CH=N-NH- y R3 es -SO2N(R10)R11; o (h) R2 es (i) fluoroalcoxi C1-5 comprendiendo de 2 a 5 átomos de F; o (ii) alcoxi C1-8-alcoxi C1-8-alcoxi C1-8; o (iii) alqueniloxi C2-8, o (iv) haloalqueniloxi C2-8, o (v) benciloxi; o (vi) -N(CH3)(R13), en donde R13 es metilo o bencilo; o (vii) alcoxi C1-4; o (B) Z es =N; o una sal del mismo.
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