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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
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
heteroaryl
atoms
heterocyclic
Prior art date
Application number
ARP150101493A
Other languages
English (en)
Inventor
Jones Peter
Wadsworth Coe Jotham
Martin Dehnhardt Christoph
Anil Sabnis Yogesh
Walter Strohbach Joseph
Michel Wakenhut Florian
Alistair Whitlock Gavin
Original Assignee
Pfizer
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
Family has litigation
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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