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AR084507A1 - Derivados de indazoliltriazol - Google Patents

Derivados de indazoliltriazol

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Publication number
AR084507A1
AR084507A1 ARP110104813A ARP110104813A AR084507A1 AR 084507 A1 AR084507 A1 AR 084507A1 AR P110104813 A ARP110104813 A AR P110104813A AR P110104813 A ARP110104813 A AR P110104813A AR 084507 A1 AR084507 A1 AR 084507A1
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AR
Argentina
Prior art keywords
alkyl
hal
denotes
cycloalkyl
het1
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ARP110104813A
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English (en)
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Merck Serono Sa
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Publication of AR084507A1 publication Critical patent/AR084507A1/es

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Abstract

Compuestos de la fórmula (1) se usan para el tratamiento de inflamación y trastornos autoinmunes. Composición farmacéutica, proceso de preparación y uso como moduladores de interleuquina-IRAK.Reivindicación 1: Un compuesto de la formula (1) en donde Q denota Ar o Het; E denota -(CH2)mCO-, -(CH2)mSO2, -(CH2)mNHCO- o un enlace simple; R1 denota H, OH, NH-alquilo C1-6, O-alquilo C1-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Cyc, Hal, Het1, O-Het1, CO-Het1, NH-Het1, CO-Ar1, O-Ar1, Ar1, NH-Ar1, -(CH2)qHet1, -CONH-(CH2)qHet1, -CONH-Het1, -(CH2)qO-Het1, -(CH2)qO-Ar1, -(CH2)qAr1, -CONH-(CH2)qAr1, -CONH-Ar1, -CONH-cicloalquilo C3-6, -(CH2)qHal, -(CH2)qCyC, CF3, -(CH2)sNH-(CH2)q-Het1, -(CH2)sNH-(CH2)q-Ar1, en donde NH-alquilo C1-6, O-alquilo C1-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 puede estar sustituido con 1 a 3 grupos seleccionados, de modo independiente, de O-alquilo C1-3, OH, CONH2, NH2; R2 denota H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Hal, CF3, con preferencia H; R3 denota Het1, Ar1, NRaRb, COOH, -(CH2)qHet1, -(CH2)qAr1, -(CH2)qNRaRb, -(CH2)qCOOH o alquilo C1-6, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados, de modo independiente, por OH o CF3; R4 denota H, alquilo C1-6, alquenilo C2-6, Hal; Ra denota H, alquilo C1-6 lineal, ramificado o cíclico; Rb denota H, Hetb, Arb, -CO-Hetb, -CO-Arb, un cicloalquilo C3-8 o un alquilo C1-6 lineal o ramificado, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados por Hetb, Arb, NH2, N(alquilo C1-6)2, NH(alquilo C1-6), N(alquilo C1-6)(cicloalquilo C3-8), NH(cicloalquilo C3-8), O(alquilo C1-6), CN, OH, CF3, Hal; n es 0, 1, 2, 3 ó 4; m es 0, 1, 2, 3 ó 4; q es 1, 2 ó 3; s es 0, 1, 2 ó 3; Hal denota Cl, Br, I, F, con preferencia Cl o F; Ar denota un grupo arileno monocíclico divalente o bicíclico fusionado que tiene 6 a 14 átomos de carbono, que también puede estar sustituido con 1 a 4 sustituyentes seleccionados de Hal, alquilo C1-6, -(CH2)mO-alquilo C1-6, CN, OH, NO2, CF3, -(CH2)mCOOH, -(CH2)mCOO-alquilo C1-6; Het denota un grupo heterocíclico insaturado, saturado o aromático monocíclico divalente o bicíclico fusionado que tiene 1 a 5 heteroátomos seleccionados de modo independiente de N, O, S y/o un grupo -C=O que también puede estar sustituido con 1 a 4 sustituyentes seleccionados de Hal, alquilo C1-6, -(CH2)mO-alquilo C1-6, CN, OH, NO2, CF3, -(CH2)mCOOH, -(CH2)mCOO-alquilo C1-6; Ar1 denota un anillo carbocíclico aromático monocíclico o bicíclico que tiene 6 a 14 átomos de carbono, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, alquilo C1-6 lineal o ramificado, cicloalquilo, -OH, -O-alquilo C1-6, -COalquilo C1-6, -NH2, -COH, -COOH, -CONH2, un grupo Rb tales como -CH2O(alquilo C1-6), -SO2NRaRb o SO2(alquilo C1-6); Het1 denota un anillo heterocíclico saturado, insaturado o aromático monocíclico o bicíclico (fusionado, en puente o espiro) que tiene 1 a 4 heteroátomos seleccionados de modo independiente de N, O, S y/o un grupo CO, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, alquilo C1-6 lineal o ramificado, cicloalquilo C3-8, -OH, -O-alquilo C1-6, -NH2, -N(alquilo C1-6)2, -COH, -COOH, -CONH2, -COalquilo C1-6, -NHCO(cicloalquilo C3-6), un grupo Rb tales como -SO2NRaRb o SO2(alquilo C1-6); Hetb denota un anillo heterocíclico saturado, insaturado o aromático monocíclico o bicíclico (fusionado o espiro) que tiene 1 a 4 heteroátomos seleccionados de modo independiente de N, O, S y/o un grupo CO, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, CN, perfluoroalquilo, -OH, -O-alquilo C1-6, -NH2, -COH, -COOH, - CONH2 o con un alquilo C1-6 lineal o ramificado, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados por NH2, N(alquilo C1-6)2, NH(alquilo C1-6), N(alquilo C1-6)(cicloalquilo C3-8), NH(cicloalquilo C3-8), O(alquilo C1-6), CN, OH, CF3, Hal, cicloalquilo C3-8, o con un anillo heterocíclico de 4 a 8 miembros que contiene un heteroátomo seleccionado de O, S y N; Arb denota un anillo carbocíclico aromático monocíclico o bicíclico que tiene 6 a 14 átomos de carbono, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, -OH, -O-alquilo C1-6, -NH2, -COH, -COOH, -CONH2 o con un alquilo C1-6 lineal o ramificado, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados por NH2, N(alquilo C1-6)2, NH(alquilo C1-6), N(alquilo C1-6)(cicloalquilo C3-8), NH(cicloalquilo C3-8), O(alquilo C1-6), CN, OH, CF3, Hal, cicloalquilo C3-8 o con un anillo heterocíclico de 4 a 8 miembros que contiene un heteroátomo seleccionado de O, S y N; Cyc denota un anillo carbocíclico saturado o insaturado que tiene 3 a 8 átomos de carbono, con preferencia 5 ó 6 átomos de carbono, en donde 1 a 5 átomos de H están reemplazados por Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, alquilo C1-6 lineal o ramificado, cicloalquilo, -OH, -O-alquilo C1-6, -COalquilo C1-6, -NH2, -COH, -COOH, -CONH2, un grupo Rb tales como -CH2O(alquilo C1-6), -SO2NRaRb o SO2(alquilo C1-6); y sus derivados, solvatos, tautómeros, sales, hidratos y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
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