AR104963A1 - Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak - Google Patents

Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak

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AR104963A1
AR104963A1 ARP160101733A ARP160101733A AR104963A1 AR 104963 A1 AR104963 A1 AR 104963A1 AR P160101733 A ARP160101733 A AR P160101733A AR P160101733 A ARP160101733 A AR P160101733A AR 104963 A1 AR104963 A1 AR 104963A1
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group
branched
linear
amino
ylpyrimidin
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Vidal Juan Bernat
Gonzalez Rodriguez Jacob
Taltavull Moll Joan
Esteve Trias Cristina
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Almirall Sa
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

Se describen derivados de 2-(pirazolopiridin-3-il)pirimidina, así como un procedimiento para su preparación, composiciones farmacéuticas que los comprenden y su uso en terapia como inhibidores de cinasas Janus (JAK). Reivindicación 1: Derivado de 2-(pirazolopiridin-3-il)pirimidina, para su uso en el tratamiento del cuerpo humano o animal, derivado de 2-(pirazolopiridin-3-il)pirimidina que es un compuesto de fórmula (1), o una sal, o solvato, o N-óxido, o estereoisómero o derivado deuterado farmacéuticamente aceptable del mismo, en la que X representa un grupo -O- o -NR³-; R¹ y R² se seleccionan independientemente del grupo que consiste en un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo C₁₋₄ lineal o ramificado, un grupo alcoxilo C₁₋₄ lineal o ramificado y un grupo -CN; R³ se selecciona del grupo que consiste en un átomo de hidrógeno, un grupo alquilo C₁₋₄ lineal o ramificado, un grupo -(CH₂)₁₋₃NRR y un grupo -(CH₂)₁₋₃-pirrolidina; G¹ se selecciona del grupo que consiste en un grupo -CN, un grupo -CO-Rᵃ, un grupo -O-R⁶, un grupo -(CHR⁷)ₘ-NRR, un grupo fenilo, un grupo cicloalquilo C₅₋₇ monocíclico, un grupo heteroarilo de 5 a 6 miembros monocíclico que contiene al menos un heteroátomo seleccionado de O, S y N y un grupo heterociclilo de 5 a 6 monocíclico que contiene al menos un heteroátomo seleccionado de O, S y N, en el que los grupos fenilo, cicloalquilo, heteroarilo y heterociclilo no están sustituidos o están sustituidos con uno o más sustituyentes seleccionados de un átomo de halógeno, un grupo hidroxilo, un grupo alquilo C₁₋₄ lineal o ramificado, un grupo hidroxialquilo C₁₋₆ lineal o ramificado, un grupo alcoxilo C₁₋₄ lineal o ramificado, un grupo -(CH₂)₀₋₂NRR, un grupo -(CH₂)₀₋₂CN y un grupo -CO-Rᵃ, en el que Rᵃ representa un átomo de hidrógeno, un grupo hidroxilo, un grupo alquilo C₁₋₃ lineal o ramificado, un grupo alcoxilo C₁₋₃ lineal o ramificado, o un grupo amino; Q se selecciona del grupo que consiste en los compuestos del grupo de fórmulas (2) en las que R⁴ se selecciona del grupo que consiste en un grupo alquilo C₁₋₄ lineal o ramificado, un grupo -CO-R, un grupo -CO(CH₂)₁₋₂-OH; un grupo -CO(CH₂)₁₋₂-CN, un grupo -CO(CH₂)₁₋₂-CF₃, un grupo cianotiazol, un grupo heterociclilo de 4 a 6 miembros monocíclico que contiene al menos un heteroátomo seleccionado de O, S y N y un grupo heteroarilo de 5 a 6 miembros monocíclico que contiene al menos un heteroátomo seleccionado de O, S y N, en el que el grupo heterociclilo y heteroarilo no están sustituidos o están sustituidos con uno o más sustituyentes seleccionados de un grupo -(CH₂)ₘ-CN y un grupo hidroxialquilo C₁₋₂; R⁵ representa un grupo -(CH₂)ₘ-CN o un grupo -(CH₂)ₘ-OH; G² representa un grupo fenilo, un grupo pirimidino o un grupo piridino en el que los grupos fenilo, pirimidino y piridino están sin sustituidos con uno o más sustituyentes seleccionados de un átomo de halógeno, un grupo alquilo C₁₋₄ lineal o ramificado, un grupo hidroxilo, un grupo -CN; R⁶ se selecciona del grupo que consiste en un átomo de hidrógeno, un grupo -(CH₂)₁₋₂-CO-O-R, un grupo (alcoxi C₁₋₆)-(alquilo C₁₋₆) lineal o ramificado y un grupo alquilo C₁₋₆ lineal o ramificado en el que dicho grupo alquilo C₁₋₆ lineal o ramificado no está sustituido o está sustituido con uno o más sustituyentes seleccionados de un átomo de halógeno, un grupo hidroxilo y un grupo -NRR; R⁷ representa un átomo de hidrógeno, un grupo hidroxilo o alquilo C₁₋₂; R y R representan independientemente un átomo de hidrógeno, un grupo alquilo C₁₋₃ lineal o ramificado, un grupo hidroxialquilo C₁₋₃ lineal o ramificado, un grupo alcoxilo C₁₋₃ lineal o ramificado; R representa un grupo alquilo C₁₋₂ o un grupo bencilo; y m tiene independientemente un valor de 0 a 3; en el que el derivado de 2-(pirazolopiridin-3-il)pirimidina no es: 3-{(3R)-3-[[2-(dimetilamino)etil](5-fluoro-6-morfolin-4-il-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il)amino]piperidin-1-il}-3-oxopropanonitrilo, 3-{(3R)-3-[(5-fluoro-6-morfolin-4-il-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il)amino]piperidin-1-il}-3-oxopropanonitrilo, (3-{(3R)-3-[(5-fluoro-6-morfolin-4-il-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il)amino]piperidin-1-il}oxetan-3-il)acetonitrilo, (3R)-3-[(5-fluoro-6-morfolin-4-il-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il)amino]piperidin-1-carboxilato de etilo, 2-{(3R)-3-[(5-fluoro-6-morfolin-4-il-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il)amino]piperidin-1-il}-2-oxoetanol, 3-[(3R)-3-({5-fluoro-6-[4-(hidroximetil)piperidin-1-il]-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il}amino)piperidin-1-il]-3-oxopropanonitrilo, 3-[(3R)-3-({5-fluoro-6-[4-(hidroximetil)fenil]-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il}amino)piperidin-1-il]-3-oxopropanonitrilo, 3-((3R)-3-{[5-fluoro-6-(4-formilfenil)-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il]amino}piperidin-1-il)-3-oxopropanonitrilo, 3-{(3R)-3-[(5-fluoro-6-{3-hidroxi-4-[(metilamino)metil]fenil}-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il)amino]piperidin-1-il}-3-oxopropanonitrilo.
ARP160101733A 2015-06-11 2016-06-10 Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak AR104963A1 (es)

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