AR100438A1 - Pirazolopiridinas y pirazolopirimidinas - Google Patents

Pirazolopiridinas y pirazolopirimidinas

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Publication number
AR100438A1
AR100438A1 ARP150101493A ARP150101493A AR100438A1 AR 100438 A1 AR100438 A1 AR 100438A1 AR P150101493 A ARP150101493 A AR P150101493A AR P150101493 A ARP150101493 A AR P150101493A AR 100438 A1 AR100438 A1 AR 100438A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
heteroaryl
atoms
heterocyclic
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ARP150101493A
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English (en)
Inventor
Jones Peter
Wadsworth Coe Jotham
Martin Dehnhardt Christoph
Anil Sabnis Yogesh
Walter Strohbach Joseph
Michel Wakenhut Florian
Alistair Whitlock Gavin
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Pfizer
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53264695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR100438(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of AR100438A1 publication Critical patent/AR100438A1/es

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Abstract

Compuestos, composiciones y usos de tales compuestos en el tratamiento de diversas enfermedades, en particular asma y EPOC. Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1) o una de sus sales farmacéuticamente aceptables o un solvato farmacéuticamente aceptable de dicho compuesto o sal farmacéuticamente aceptable, en donde: A y A son, de modo independiente, C o N, donde C puede no estar sustituido o puede estar sustituido con halo o alquilo C₁₋₆; R y R⁰ se seleccionan, de modo independiente, del grupo que consiste en H, alquilo C₁₋₆, hidroxi(alquilo C₁₋₆), fenil(alquilo C₁₋₆) y -(CH₂)ₙ-W, donde W es cicloalquilo C₃₋₈, fenilo, naftilo, heteroarilo de 5 ó 6 miembros o heterocíclico que contiene 1 - 3 átomos de N, S y/u O, -SO₂-R, -NHSO₂-R, -NRSO₂-R y SR, donde R y R son, de modo independiente, alquilo C₁₋₆ o cicloalquilo C₃₋₈, amino, alquil C₁₋₆-amino, di(alquil C₁₋₆)amino, fenilo, heteroarilo o heterocíclico; en donde cada uno de dichos alquilo, cicloalquilo, heterocíclico, fenilo, naftilo o heteroarilo puede no estar sustituido o puede estar sustituido con fenilo, heteroarilo, heterocíclico, halo, ciano, hidroxi, alquilo C₁₋₆, alcoxi C₁₋₆, ariloxi, -SO₂-R, -CONRR, NRCOR, NRCONRR, -NRCO₂R, -(CH₂)ₙ-SO₂-R, -NHSO₂-R, -NRSO₂-R o SR, donde R y R son, de modo independiente, alquilo C₁₋₆, cicloalquilo C₃₋₈, fenilo, amino, hidroxialquilamino, heterocíclico o -(CH₂)ₙ-W, donde W es hidroxi, cicloalquilo C₃₋₈, fenilo, naftilo, heterocíclico o heteroarilo de 5 ó 6 miembros que contiene 1 - 3 átomos de N, S y/u O; o R y R⁰ y el átomo de N al que están unidos forman un anillo heterocíclico monocíclico o bicíclico que puede no estar sustituido o puede estar sustituido con (a) halo, hidroxi, heteroarilo, alquilo C₁₋₆, alcoxi C₁₋₆, (alcoxi C₁₋₆)alcoxi C₁₋₆, aril(alcoxi C₁₋₆), ariloxi, amino, aminoacilo, alquil C₁₋₆-aminoacilo, arilalquilaminoacilo, di(alquil C₁₋₆)aminoacilo, -SO₂-R, -SO₂-NR-(CH₂)ₙ-W, -NHSO₂-R, -NRSO₂-R o SR, donde R y R es, de modo independiente, amino, alquil C₁₋₆- amino, di(alquil C₁₋₆)amino, alquilo C₁₋₆ o cicloalquilo C₃₋₈ o (b) -(CH₂)ₙ-W, donde W es cicloalquilo C₃₋₈, fenilo, naftilo, heterocíclico, heteroarilo de 5 ó 6 miembros que contiene 1 - 3 átomos de N, -SO₂-R, -NHSO₂-R, -NRSO₂-R o SR, donde R y R es, de modo independiente, alquilo o cicloalquilo; en donde cada uno de dichos fenilo, arilo o heteroarilo puede no estar sustituido o puede estar sustituido con halo, alquilo C₁₋₆, alcoxi C₁₋₆, ciano o hidroxi; R¹ es H, halo o ciano; R² y R² son, de modo independiente, H, alquilo C₁₋₆, ciano, alcoxi C₁₋₆, alquil C₁₋₆-tio o cicloalquilo C₃₋₈, donde alquilo, alcoxi o cicloalquilo está opcionalmente sustituido con uno o varios átomos de flúor; X es un enlace, -CO-, -CONH-, -SO₂-, -SONH- o -(CH₂)ₘ-; R³ es H, alquilo C₁₋₄, fenilo, naftilo, heteroarilo de 6 miembros o heterocíclico que contiene 1 - 3 átomos de N, un heteroarilo de 5 miembros o heterocíclico que contiene (a) 1 - 4 átomos de N o (b) 1 átomo de O ó S y 0 - 3 átomos de N, un heteroarilo bicíclico de 10 miembros o heterocíclico que contiene 1 - 4 átomos de N, un heteroarilo bicíclico de 9 miembros o heterocíclico que contiene (a) 1 - 4 átomos de N o (b) 1 átomo de O ó S y 0 - 3 átomos de N o un heteroarilo bicíclico de 8 miembros o heterocíclico que contiene (a) 1 - 4 átomos de N o (b) 1 átomo de O ó S y 1 - 3 átomos de N o (c) 2 átomos de O ó S y 0 - 2 átomos de N; en donde cada uno de dichos fenilo, naftilo, heteroarilo o heterocíclico está opcionalmente sustituido con alquilo, 1 sustituyente -Y-R⁴ y/o 1 - 4 sustituyentes seleccionados cada uno, de modo independiente, de R⁵; siempre que, cuando X es -CO- o -SO₂-, R³ no sea H; Y es un enlace, -(CH₂)ₘ- u -O-; R⁴ es (a) H, alquilo C₁₋₆, cicloalquilo C₃₋₈, halo, oxo, -OR⁶, -NR⁷R⁸, -SR⁶, -SOR⁹, -SO₂R⁹, -COR⁶, -OCOR⁶, -COOR⁶, -NR⁶COR⁶, -CONR⁷R⁸, -NR⁶SO₂R⁹, -SO₂NR⁷R⁸, -NR⁶CONR⁷R⁸, -NR⁶COOR⁹ y -NR⁶SO₂NR⁷R⁸; (b) fenilo o naftilo, estando dicho fenilo y naftilo opcionalmente sustituidos con 1 - 5 sustituyentes seleccionados de alquilo C₁₋₆, cicloalquilo C₃₋₈, halo, ciano, -OR⁶, -NR⁷R⁸, -SR⁶, -SOR⁹, -SO₂R⁹, -COR⁶, -OCOR⁶, -COOR⁶, -NR⁶COR⁶, -CONR⁷R⁸, -NR⁶SO₂R⁹, -SO₂NR⁷R⁸, -NR⁶CONR⁷R⁸, -NR⁶COOR⁹ y -NR⁶SO₂NR⁷R⁸; o (c) un heteroarilo monocíclico saturado o parcialmente insaturado de 3 a 8 miembros, que contiene 1 ó 2 heteroátomos seleccionados de O y N, estando dicho heteroarilo opcionalmente sustituido con 1 - 5 sustituyentes seleccionados de alquilo C₁₋₆, cicloalquilo C₃₋₈, halo, ciano, oxo, -OR⁶, -NR⁷R⁸, -SR⁶, -SOR⁹, -SO₂R⁹, -COR⁶, -OCOR⁶, -COOR⁶, -NR⁶COR⁶, -CONR⁷R⁸, -NR⁶SO₂R⁹, -SO₂NR⁷R⁸, -NR⁶CONR⁷R⁸, -NR⁶COOR⁹ y -NR⁶SO₂NR⁷R⁸; R⁵ es alquilo C₁₋₆, cicloalquilo C₃₋₈, halo, ciano, -OR⁶, -NR⁷R⁸, -SR⁶, -SOR⁹, -SO₂R⁹,-COR⁶, -OCOR⁶, -COOR⁶, -NR⁶COR⁶, -CONR⁷R⁸, -NR⁶SO₂R⁹, -SO₂NR⁷R⁸, -NR⁶CONR⁷R⁸, -NR⁶COOR⁹ o -NR⁶SO₂NR⁷R⁸; R⁶ es H, alquilo C₁₋₆ o cicloalquilo C₃₋₈, dicho alquilo C₁₋₆ está opcionalmente sustituido con -NR⁷R⁸ o un heteroarilo monocíclico saturado o parcialmente insaturado de 3 a 8 miembros, que contiene 1 ó 2 heteroátomos seleccionados de O y N, estando dicho heteroarilo opcionalmente sustituido con 1 - 5 sustituyentes seleccionados de alquilo C₁₋₆, cicloalquilo C₃₋₈, halo, hidroxi y ciano; R⁷ y R⁸ son cada uno, de modo independiente, H, alquilo C₁₋₆ o cicloalquilo C₃₋₈ o se toman junto con el átomo de nitrógeno al que están unidos para formar un anillo heterocíclico saturado de 4, 5 ó 6 miembros que contiene 1 - 2 átomos de nitrógeno o 1 átomo de nitrógeno y 1 átomo de oxigeno, dicho alquilo C₁₋₆ está opcionalmente sustituido con cicloalquilo C₃₋₈, halo, hidroxi, amino, (alquil C₁₋₆)amino o di(alquil C₁₋₆)amino y estando dicho anillo heterocíclico opcionalmente sustituido con uno o varios grupos alquilo C₁₋₆ o cicloalquilo C₃₋₈; R⁹ es alquilo C₁₋₆ o cicloalquilo C₃₋₈; y, m y n son, de modo independiente, 0, 1, 2 ó 3.
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