AR102177A1 - Compuestos de heteroarilo como inhibidores de btk y usos de los mismos - Google Patents

Compuestos de heteroarilo como inhibidores de btk y usos de los mismos

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AR102177A1
AR102177A1 ARP150103209A ARP150103209A AR102177A1 AR 102177 A1 AR102177 A1 AR 102177A1 AR P150103209 A ARP150103209 A AR P150103209A AR P150103209 A ARP150103209 A AR P150103209A AR 102177 A1 AR102177 A1 AR 102177A1
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Argentina
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ring
sulfur
nitrogen
oxygen
independently selected
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Merck Patent Gmbh
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Publication of AR102177A1 publication Critical patent/AR102177A1/es

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Abstract

Compuestos de imidazo piridina, y composiciones farmacéuticamente aceptables de los mismos, útiles como inhibidores de BTK. Reivindicación 1: Un compuesto de fórmula (1), o un tautómero, o una sal farmacéuticamente aceptable del mismo, donde: el Anillo A es un arilo o heteroarilo de 5 a 6 miembros; R¹ es H, halo, (C(R⁵)(R⁵))ₘNR², N(R⁴)C(O)R, N(R⁴)C(O)NR₂, N(R⁴)CO₂R, N(R⁴)S(O)₂R, N(R⁴)S(O)R, N(R⁴)(R⁴), anillo heterocíclico opcionalmente sustituido de 3 a 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre, o anillo heteroarilo monocíclico opcionalmente sustituido de 5 a 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre; o R¹ está ausente; R² es H, (C(R⁵)(R⁵))ₘOR⁴, (C(R⁵)(R⁵))ₘN(R⁴)COR, (C(R⁵)(R⁵))ₘN(R⁴)C(O)C(O)NR₂, (C(R⁵)(R⁵))ₘN(R⁴)(R⁴), anillo heterocíclico opcionalmente sustituido de 3 a 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre, o anillo heteroarilo monocíclico opcionalmente sustituido de 5 a 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre; o R² está ausente; o R¹ y R² junto con los átomos a los que están conectados, forman un anillo condensado de 3 a 7 miembros que está opcionalmente sustituido; donde R¹ y R² no son ninguno H; y donde R¹ y R² no está ninguno ausente; cada R³ es independientemente halógeno, alifático C₁₋₆, arilo C₅₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre, o un anillo heteroarilo monocíclico de 5 a 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre; cada uno de los cuales está opcionalmente sustituido; cada R⁴ es independientemente -R, -SO₂R, -SOR, -C(O)R, -CO₂R o -C(O)N(R)₂; cada R⁵ es independientemente -R, halógeno, -OR, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, -NRC(O)N(R)₂, -NRSO₂R o -N(R)₂; cada R es independientemente hidrógeno, alifático C₁₋₆, arilo C₅₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre, o un anillo heteroarilo monocíclico de 5 a 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre; cada uno de los cuales está opcionalmente sustituido; o dos grupos R en el mismo átomo se toman junto con el átomo al que están unidos para formar un arilo C₅₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre, un anillo heteroarilo monocíclico de 5 a 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre; un anillo arilo condensado de 10 a 15 miembros; un anillo carbocíclico condensado saturado o parcialmente insaturado de 6 a 15 miembros; un anillo heteroarilo condensado de 10 a 15 miembros; o un anillo heterocíclico condensado saturado o parcialmente insaturado de 6 a 15 miembros; cada uno de los cuales está opcionalmente sustituido; el Anillo Z es arilo C₅₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre, o un anillo heteroarilo monocíclico de 5 a 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno o azufre; cada uno de los cuales está opcionalmente sustituido; o el Anillo Z está ausente; cada Rᵃ es independientemente -R, halógeno, -OR, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, -NRC(O)N(R)₂, -NRSO₂R o -N(R)₂; m es 1, 2 ó 3; n es 0, 1 ó 2; y p es 0, 1, 2 ó 3.
ARP150103209A 2014-10-06 2015-10-06 Compuestos de heteroarilo como inhibidores de btk y usos de los mismos AR102177A1 (es)

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