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AR098136A1 - 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

Info

Publication number
AR098136A1
AR098136A1 ARP140103948A ARP140103948A AR098136A1 AR 098136 A1 AR098136 A1 AR 098136A1 AR P140103948 A ARP140103948 A AR P140103948A AR P140103948 A ARP140103948 A AR P140103948A AR 098136 A1 AR098136 A1 AR 098136A1
Authority
AR
Argentina
Prior art keywords
nitrogen
membered
sulfur
oxygen
independently selected
Prior art date
Application number
ARP140103948A
Other languages
English (en)
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR098136A1 publication Critical patent/AR098136A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

La presente se refiere a compuestos de piridina, pirimidina, pirazina, y piridazina, y a composiciones farmacéuticamente aceptables de los mismos, útiles como inhibidores de BTK. Son útiles para tratar dolencias como alergia y asma. Reivindicación 1: Compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: el Anillo A es un anillo heteroarilo de 6 miembros que tiene 1 ó 2 nitrógenos, seleccionado entre piridina, pirazina, piridazina, y pirimidina; R² se selecciona entre -R, halógeno, -haloalquilo, -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; R³ se selecciona entre -R, halógeno, haloalquilo, -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; en la que al menos uno de R² o R³ es -C(O)N(R)₂, o CN; cada R es independientemente hidrógeno, alifático C₁₋₆, arilo C₃₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 - 8 miembros, un anillo heterocíclico de 3 - 7 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre, o un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente 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 C₃₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 - 8 miembros, un anillo heterocíclico de 3 - 7 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre, o un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre; cada uno de los cuales está opcionalmente sustituido; L es un grupo divalente seleccionado entre alifático C₁₋₆, arilo C₃₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 - 8 miembros, un anillo heterocíclico de 3 - 7 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre, y un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre; cada uno de los cuales está opcionalmente sustituido; o L es un grupo divalente seleccionado entre alifático C₁₋₆-arilo C₃₋₁₀, alifático C₁₋₆-anillo carbocíclico saturado o parcialmente insaturado de 3 - 8 miembros, alifático C₁₋₆-anillo heterocíclico de 3 - 7 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre, y un alifático C₁₋₆-anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre; cada uno de los cuales está opcionalmente sustituido; Y es O, S, SO₂, SO, C(O), CO₂, C(O)N(R), -NRC(O), -NRC(O)N(R), -NRSO₂ o N(R); o Y está ausente; R¹ es alifático C₁₋₆, arilo C₃₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 - 8 miembros, un anillo heterocíclico de 3 - 7 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre, o un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1-4heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre; cada uno de los cuales está opcionalmente sustituido; X es O, S, SO₂, SO, C(O), CO₂, C(O)N(R), -NRC(O), -NRC(O)N(R), -NRSO₂, o N(R); o X está ausente; y R⁴ es hidrógeno, alifático C₁₋₆, arilo C₃₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 - 8 miembros, un anillo heterocíclico de 3 - 7 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre, o un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre; cada uno de los cuales está opcionalmente sustituido; o X-R⁴ está ausente.
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