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 farmacéuticasInfo
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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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- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
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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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EP3455226B1 (en) | 2016-05-12 | 2020-12-30 | Lundbeck La Jolla Research Center, Inc. | Spirocycle compounds and methods of making and using same |
US10899737B2 (en) | 2016-09-19 | 2021-01-26 | Lundbeck La Jolla Research Center, Inc. | Piperazine carbamates and methods of making and using same |
JOP20190105A1 (ar) * | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
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UA124884C2 (uk) | 2016-11-16 | 2021-12-08 | Лундбек Ла Джолла Ресеарч Центер, Інк. | Фармацевтичні склади |
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BR112020003946A2 (pt) | 2017-08-29 | 2020-09-08 | Lundbeck La Jolla Research Center, Inc. | compostos de espirociclo e métodos para produzir e usar os mesmos |
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CN107660199A (zh) | 2018-02-02 |
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CA2979537C (en) | 2023-08-29 |
TW201702221A (zh) | 2017-01-16 |
US9994537B2 (en) | 2018-06-12 |
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EP3271352A2 (en) | 2018-01-24 |
CA2979537A1 (en) | 2016-09-22 |
JP2018513119A (ja) | 2018-05-24 |
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