AR104025A1 - Carbamatos de piperazina como moduladores de magl y/o abhd6, procesos para su preparación y composiciones farmacéuticas - Google Patents

Carbamatos de piperazina como moduladores de magl y/o abhd6, procesos para su preparación y composiciones farmacéuticas

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AR104025A1
AR104025A1 ARP160100743A ARP160100743A AR104025A1 AR 104025 A1 AR104025 A1 AR 104025A1 AR P160100743 A ARP160100743 A AR P160100743A AR P160100743 A ARP160100743 A AR P160100743A AR 104025 A1 AR104025 A1 AR 104025A1
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optionally substituted
nr8c
nr9r10
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Wang Dong
D Hui - Weber Olivia
K Jones Todd
A Grice Cheryl
S Cisar Justin
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Abide Therapeutics Inc
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Abstract

Se proporcionan en el presente documento carbamatos de piperazina y composiciones farmacéuticas que comprenden dichos compuestos. Los compuestos y composiciones objeto son útiles como moduladores de MAGL y/o ABHD6. Adicionalmente, los compuestos y composiciones objeto son útiles para el tratamiento del dolor. Reivindicación 1: Un compuesto de la fórmula (1), en donde: R¹ es halógeno, -OR³, -CN, arilo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), arilooxi (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), heteroarilo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), heteroarilooxi (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), heterociclo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), cicloalquilo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), C₁₋₆ alquilo sustituido opcionalmente, C₂₋₆ alquenilo sustituido opcionalmente, C₂₋₆ alquinilo sustituido opcionalmente, NR⁹R¹⁰, NR⁸C(O)R⁹, -NR⁸SO₂R⁹, -NR⁸C(O)OR⁹, -NR⁸C(O)NR⁹R¹⁰, -C(O)R⁹, -C(O)OR⁹, -C(O)NR⁹R¹⁰, -S(O)ʷR¹¹ o -SH; R² es -NR⁵R⁶, -alquilo(NR¹⁴R¹⁵) o -OR⁷; cada R³ se selecciona por separado de H, C₁₋₆ alquilo, haloalquilo y aminoalquilo; cada R⁴ se selecciona por separado de halógeno, -OR³, -CN, nitro, C₁₋₆ alquilo sustituido opcionalmente, C₁₋₆ alquenilo sustituido opcionalmente, C₁₋₆ alquinilo sustituido opcionalmente, cicloalquilo, -NR⁹R¹⁰, -NR⁸C(O)R⁹, -NR⁸SO₂R⁹, -NR⁸C(O)OR⁹, -NR⁸C(O)NR⁹R¹⁰,-C(O)R⁹, -C(O)OR⁹, -C(O)NR⁹R¹⁰, -S(O)ʷR¹¹ y -SH; R⁵ y R⁶, junto con el nitrógeno al cual están unidos, forman (i) un heterociclo monocíclico, un heterociclo bicíclico fusionado o un espirociclo; o (ii) un anillo heterocíclico enlazado de 7 - 8 miembros que contiene opcionalmente un O, N o S adicional; en donde el heterociclo monocíclico, el heterociclo bicíclico fusionado o el espirociclo es sustituido por uno o más sustituyentes seleccionados por separado de arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente, heterociclo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, haloalquilo, -OR⁷, -NR¹²R¹³, -C(O)OR⁹, -C(O)NR⁹R¹⁰, -NR⁸SO₂R⁹, -NR⁸C(O)OR⁹ y NR⁸C(O)NR⁹R¹⁰; y el heterociclo monocíclico, el heterociclo bicíclico fusionado o el espirociclo contiene opcionalmente un O, N o S adicional; y anillo heterocíclico enlazado de 7 - 8 miembros es sustituido opcionalmente por uno o más sustituyentes seleccionados por separado de halógeno, -CN, oxo, C₁₋₆ alquilo sustituido opcionalmente, arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente, heterociclo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, -S(O)ʷR¹¹, -OR³, -OR⁷, -C(O)R⁹, -C(O)OR⁹, -C(O)NR⁹R¹⁰, -NR⁹R¹⁰, -NR⁸C(O)R⁹, -NR⁸SO₂R⁹, -NR⁸C(O)OR⁹ y -NR⁸C(O)NR⁹R¹⁰; R⁷ es alquinilo o (alquinilo)alquilo; cada R⁸ se selecciona por separado de H, alquilo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente y heterocicloalquilo sustituido opcionalmente; cada R⁹ y R¹⁰ se selecciona por separado de H, alquilo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente y heterocicloalquilo sustituido opcionalmente; o R⁹ y R¹⁰ junto con el nitrógeno al cual están unidos forman un heterociclo sustituido opcionalmente que contiene opcionalmente un O, N o S adicional; cada R¹¹ se selecciona por separado de alquilo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente y heterocicloalquilo sustituido opcionalmente; R¹² y R¹³ junto con el nitrógeno al cual están unidos forman un heterociclo sustituido opcionalmente que contiene opcionalmente un O, N o S adicional; R¹⁴ y R¹⁵ junto con el nitrógeno al cual están unidos forman un heterociclo sustituido opcionalmente que contiene opcionalmente un O, N o S adicional; y w es 0, 1 ó 2; o un solvato, hidrato, tautómero, N-óxido, estereoisómero o sal del mismo aceptable farmacéuticamente. Reivindicación 22: Un compuesto de la fórmula (1a), en donde: R¹ es halógeno, -OR³, -CN, arilo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), arilooxi (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), heteroarilo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), heteroarilooxi (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), heterociclo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), cicloalquilo (sustituido opcionalmente por una, dos o tres fracciones seleccionadas cada una por separado de R⁴), C₁₋₆ alquilo sustituido opcionalmente, C₂₋₆ alquenilo sustituido opcionalmente, C₂₋₆ alquinilo sustituido opcionalmente, -NR⁹R¹⁰, -NR⁸C(O)R⁹, -NR⁸SO₂R⁹, -NR⁸C(O)OR⁹, -NR⁸C(O)NR⁹R¹⁰, -C(O)R⁹, -C(O)OR⁹, -C(O)NR⁹R¹⁰, -S(O)ʷR¹¹ o -SH; R² es -C(O)C(O)OR⁷; cada R³ se selecciona por separado de H, C₁₋₆ alquilo; cada R⁴ se selecciona por separado de halógeno, -OR³, haloalquilo y aminoalquilo; -CN, nitro, C₁₋₆ alquilo sustituido opcionalmente, C₁₋₆ alquenilo sustituido opcionalmente, C₁₋₆ alquinilo sustituido opcionalmente, cicloalquilo, -NR⁹R¹⁰, -NR⁸C(O)R⁹, -NR⁸SO₂R⁹, -NR⁸C(O)OR⁹, -NR⁸C(O)NR⁹R¹⁰, -C(O)R⁹, -C(O)OR⁹, -C(O)NR⁹R¹⁰, -S(O)ʷR¹¹ y -SH; R⁷ es H o C₁₋₆ alquilo; cada R⁸ se selecciona por separado de H, alquilo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente y heterocicloalquilo sustituido opcionalmente; cada R⁹ y R¹⁰ se selecciona por separado de H, alquilo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente y heterocicloalquilo sustituido opcionalmente; o R⁹ y R¹⁰ junto con el nitrógeno al cual están unidos forman un heterociclo sustituido opcionalmente que contiene opcionalmente un O, N o S adicional; cada R¹¹ se selecciona por separado de alquilo sustituido opcionalmente, cicloalquilo sustituido opcionalmente, arilo sustituido opcionalmente, heteroarilo sustituido opcionalmente y heterocicloalquilo sustituido opcionalmente; y w es 0, 1 ó 2; o un solvato, hidrato, tautómero, N-óxido o sal del mismo aceptable farmacéuticamente.
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