AR119047A1 - Esteroides neuroactivos como moduladores de gabaa y su uso en el tratamiento de trastornos del snc - Google Patents

Esteroides neuroactivos como moduladores de gabaa y su uso en el tratamiento de trastornos del snc

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AR119047A1
AR119047A1 ARP200101529A ARP200101529A AR119047A1 AR 119047 A1 AR119047 A1 AR 119047A1 AR P200101529 A ARP200101529 A AR P200101529A AR P200101529 A ARP200101529 A AR P200101529A AR 119047 A1 AR119047 A1 AR 119047A1
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Argentina
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substituted
unsubstituted
rga
group
alkyl
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ARP200101529A
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Francesco G Salituro
Maria Jesus Blanco-Pillado
Marshall Lee Morningstar
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Sage Therapeutics Inc
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Abstract

Compuestos esteroides con actividad moduladora de GABAA, composiciones farmacéuticas que los comprenden y su uso para el tratamiento de trastornos del SNC, en particular un trastorno de humor tal como depresión y específicamente un trastorno de depresión severo y depresión posparto. Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable de este; caracterizado porque: ⁻ ⁻ ⁻ ⁻ ⁻ ⁻ representa un enlace simple o doble, siempre que haya un enlace doble presente, entonces uno de R⁶ᵃ o R⁶ᵇ está ausente y R⁵ está ausente; RX se selecciona del grupo que consiste en halo, -CN, -OH, -ORQ¹ y alquilo sustituido o no sustituido, donde RQ¹ es alquilo sustituido o no sustituido; RY es halo o alquilo sustituido o no sustituido o RY y RX pueden unirse con los átomos que intervienen para formar un carbociclilo sustituido o no sustituido o un heterociclilo sustituido o no sustituido; R³ se selecciona del grupo que consiste en alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, carbociclilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido y heteroarilo sustituido o no sustituido; R⁵ es hidrógeno o metilo; cada instancia de R²² se selecciona de forma independiente del grupo que consiste en halógeno, -NO₂, -CN, -ORGA, -N(RGA)₂, -C(=O)RGA, -C(=O)ORGA, -OC(=O)RGA, -OC(=O)ORGA, -C(=O)N(RGA)₂, -N(RGA)C(=O)RGA, -OC(=O)N(RGA)₂, -N(RGA)C(=O)ORGA, -N(RGA)C(=O)N(RGA)₂, -SRGA, -S(=O)RGA, -S(=O)₂RGA, -S(=O)₂ORGA, -OS(=O)₂RGA, -S(=O)₂N(RGA)₂, -N(RGA)S(=O)₂RGA, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, carbociclilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido y heteroarilo sustituido o no sustituido, donde cada instancia de RGA se selecciona de forma independiente del grupo que consiste en hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆ sustituido o no sustituido, carbociclilo C₃₋₆ sustituido o no sustituido, heterociclilo de 3 a 6 miembros sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, un grupo protector de oxígeno cuando se une a oxígeno y un grupo protector de nitrógeno cuando se une a nitrógeno, o se toman dos grupos RGA con los átomos que intervienen para formar un anillo heterocíclico o heteroarilo sustituido o no sustituido; R¹ᵃ, R¹ᵇ, R²ᵃ, R²ᵇ, R⁴ᵃ, R⁴ᵇ, R⁷ᵃ, R⁷ᵇ, R¹¹ᵃ, R¹¹ᵇ, R¹²ᵃ y R¹²ᵇ se seleccionan cada uno de forma independiente del grupo que consiste en hidrógeno, halógeno, ciano, -NO₂, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, carbociclilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, -ORA¹, -N(RA¹)₂, -SRA¹, -C(=O)RA¹, -C(=O)ORA¹, -C(=O)SRA¹, -C(=O)N(RA¹)₂, -OC(=O)RA¹, -OC(=O)ORA¹, -OC(=O)N(RA¹)₂, -OC(=O)SRA¹, -OS(=O)₂RA¹, -OS(=O)₂ORA¹, -OS(=O)₂N(RA¹)₂, -N(RA¹)C(=O)RA¹, -N(RA¹)C(=NRA¹)RA¹, -N(RA¹)C(=O)ORA¹, -N(RA¹)C(=O)N(RA¹)₂, -N(RA¹)C(=NRA¹) N(RA¹)₂, -N(RA¹)S(=O)₂RA¹, -N(RA¹)S(=O)₂ORA¹, -N(RA¹)S(=O)₂N(RA¹)₂, -SC(=O)RA¹, -SC(=O)ORA¹, -SC(=O)SRA¹, -SC(=O)N(RA¹)₂, -S(=O)₂RA¹, -S(=O)₂ORA¹ o -S(=O)₂N(RA¹)₂, donde cada instancia de RA¹ se selecciona de forma independiente del grupo que consiste en hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆sustituido o no sustituido, carbociclilo C₃₋₆ sustituido o no sustituido, o heterociclilo de 3 a 6 miembros sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, un grupo protector de oxígeno cuando se une a oxígeno, un grupo protector de nitrógeno cuando se une a nitrógeno y un grupo protector de azufre cuando se une a azufre, o se toman dos grupos RA¹ con los átomos que intervienen para formar un anillo heterocíclico sustituido o no sustituido; R⁶ᵃ y R⁶ᵇ se seleccionan cada uno de forma independiente del grupo que consiste en hidrógeno, halógeno, ciano, -NO₂, -OH, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido y alquinilo sustituido o no sustituido; o R⁶ᵃ y R⁶ᵇ se unen para formar un grupo oxo (=O); R¹⁵ᵃ, R¹⁵ᵇ, R¹⁶ᵃ y R¹⁶ᵇ se seleccionan cada uno de forma independiente del grupo que consiste en hidrógeno, halógeno, -CN, -NO₂, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, carbociclilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, -ORC³, -N(RC³)₂, -SRC³, -C(=O)RC³, -C(=O)ORC³, -C(=O)SRC³, -C(=O)N(RC³)₂, -OC(=O)RC³, -OC(=O)ORC³, -OC(=O)N(RC³)₂, -OC(=O)SRC³, -OS(=O)₂RC³, -OS(=O)₂ORC³, -OS(=O)₂N(RC³)₂, -N(RC³)C(=O)RC³, -N(RC³)C(=NRC³)RC³, -N(RC³)C(=O)ORC³, -N(RC³)C(=O)N(RC³)₂, -N(RC³)C(=NRC³)N(RC³)₂, -N(RC³)S(=O)₂RC³, -N(RC³)S(=O)₂ORC³, -N(RC³)S(=O)₂N(RC³)₂, -SC(=O)RC³, -SC(=O)ORC³, -SC(=O)SRC³, -SC(=O)N(RC³)₂, -S(=O)₂RC³, -S(=O)₂ORC³ o -S(=O)₂N(RC³)₂, donde cada instancia de RC³ se selecciona de forma independiente del grupo que consiste en hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆ sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, carbociclilo sustituido o no sustituido o heterociclilo sustituido o no sustituido, un grupo protector de oxígeno cuando se une a oxígeno, un grupo protector de nitrógeno cuando se une a nitrógeno y un grupo protector de azufre cuando se une a azufre, o se toman dos grupos RC³ con los átomos que intervienen para formar un anillo heterocíclico sustituido o no sustituido; R¹⁹ es hidrógeno o alquilo sustituido o no sustituido y n se selecciona del grupo que consiste en 0, 1, 2 y 3.
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