AR105522A1 - Derivados de amida sustituida que tienen actividad multimodal contra el dolor - Google Patents

Derivados de amida sustituida que tienen actividad multimodal contra el dolor

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Publication number
AR105522A1
AR105522A1 ARP160102304A ARP160102304A AR105522A1 AR 105522 A1 AR105522 A1 AR 105522A1 AR P160102304 A ARP160102304 A AR P160102304A AR P160102304 A ARP160102304 A AR P160102304A AR 105522 A1 AR105522 A1 AR 105522A1
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Argentina
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unsubstituted
substituted
alkyl
alkynyl
alkenyl
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ARP160102304A
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Esteve Labor Dr
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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Abstract

La presente se refiere a derivados de amida sustituida que tienen actividad farmacológica dual hacia el receptor sigma (s) y el receptor opioide m, a procesos de preparación de dichos compuestos, a composiciones farmacéuticas que los comprenden y a su uso en terapia, en particular para el tratamiento del dolor. Reivindicación 1: Un compuesto de fórmula general (1), donde m es 1 ó 2; n es 0 1 ó 2; p es 0 1 ó 2; W es nitrógeno o carbono; X es un enlace, -C(RˣRˣ)-, C=O, -C(O)O- u -O-; en donde Rˣ se selecciona entre halógeno, -OR¹⁵, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; Rˣ se selecciona entre hidrógeno, halógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; R¹⁵ se selecciona entre hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; R¹ se selecciona entre alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆ sustituido o no sustituido, cicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido y heterociclilo sustituido o no sustituido; en donde dicho cicloalquilo, arilo o heterociclilo en R¹, si está sustituido, está sustituido con uno o más sustituyentes que se seleccionan de halógeno, -R¹¹, -OR¹¹, -NO₂, -NR¹¹R¹¹, NR¹¹C(O)R¹¹, -NR¹¹S(O)₂R¹¹, -S(O)₂NR¹¹R¹¹, -NR¹¹C(O)NR¹¹R¹¹, -SR¹¹, S(O)R¹¹, S(O)₂R¹¹, -CN, haloalquilo, haloalcoxi, -C(O)OR¹¹, -C(O)NR¹¹R¹¹, -NR¹¹S(O)₂NR¹¹R¹¹ y C(CH₃)₂OR¹¹; adicionalmente, cicloalquilo o heterociclilo no aromático en R¹, si está sustituido, también puede estar sustituido por un resto de fórmula (2) o =O; en donde el alquilo, alquenilo o alquinilo en R¹, si está sustituido, está sustituido con uno o más sustituyentes que se seleccionan de -OR¹¹, halógeno, -CN, haloalquilo, haloalcoxi, -SR¹¹,-S(O)R¹¹ y -S(O)₂R¹¹; donde R¹¹, R¹¹ y R¹¹ se seleccionan independientemente entre hidrógeno, alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido y alquinilo C₂₋₆ no sustituido; y donde R¹¹ se selecciona entre hidrógeno, alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido, alquinilo C₂₋₆ no sustituido y -Boc; R² se selecciona entre hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆ sustituido o no sustituido, cicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido y heterociclilo sustituido o no sustituido; en donde dicho cicloalquilo, arilo o heterociclilo en R², si está sustituido, está sustituidos por uno o más sustituyentes que se seleccionan de halógeno, -R¹², -OR¹², -NO₂, -NR¹²R¹²-, NR¹²C(O)R¹², -NR¹²S(O)₂R¹², -S(O)₂NR¹²R¹², -NR¹²C(O)NR¹²R¹², -SR¹², -S(O)R¹², S(O)₂R¹², -CN, haloalquilo, haloalcoxi, -C(O)OR¹², -C(O)NR¹²R¹², -NR¹²S(O)₂NR¹²R¹² y C(CH₃)₂OR¹²; adicionalmente, el cicloalquilo o heterociclilo no aromático en R², si está sustituido, también puede estar sustituido por el resto de fórmula (2) o =O; donde el alquilo, alquenilo o alquinilo en R², si está sustituido, está sustituido con uno o más sustituyentes seleccionados entre -OR¹², halógeno, -CN, haloalquilo, haloalcoxi, -SR¹², -S(O)R¹² y -S(O)₂R¹²; en donde R¹², R¹² y R¹² se seleccionan independientemente de hidrógeno, alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido y alquinilo C₂₋₆ no sustituido; y donde R¹² se selecciona entre hidrógeno, alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido, alquinilo C₂₋₆ no sustituido y -Boc; R³ se selecciona entre alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆ sustituido o no sustituido, cicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, -NR⁹R⁹ y -CH₂OR⁹; en donde R⁹ y R⁹ se seleccionan independientemente de hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆ sustituido o no sustituido, cicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido y heterociclilo sustituido o no sustituido; R⁴ y R⁴ se seleccionan independientemente de alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido, de forma alternativa, R⁴ y R⁴ pueden formar junto con el átomo de carbono al que están unidos un ciclo de fórmula (3) (en donde · marca el átomo de carbono al que R⁴ y R⁴ están unidos), donde q es 0 ó 1, r es 0, 1 ó 2; Y es -CH₂-, -N(Rʸ)-, -S- u -O-; R⁸ y R⁸ se seleccionan independientemente de hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; de forma alternativa, R⁸ y R⁸, tomados junto con el átomo de carbono al que están unidos, pueden formar un cicloalquilo C₃₋₆; Rʸ se selecciona entre hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; R⁵ y R⁵ se seleccionan independientemente de hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido, alquinilo C₂₋₆ sustituido o no sustituido, -CH₂OR¹⁰ y -C(O)OR¹⁰; en donde R¹⁰ se selecciona entre hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; R⁶ y R⁶ se seleccionan independientemente de hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; R⁷ y R⁷ se seleccionan independientemente de hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, alquenilo C₂₋₆ sustituido o no sustituido y alquinilo C₂₋₆ sustituido o no sustituido; y donde el resto de fórmula (4) se selecciona de los compuestos del grupo de fórmulas (5), en donde Rⁿ se selecciona entre alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido y alquinilo C₂₋₆ no sustituido; el alquilo, alquenilo o alquinilo, diferente del definido en R¹ o R², si está sustituido, está sustituido con uno o más sustituyentes que se seleccionan de -OR¹³, halógeno, -CN, haloalquilo, haloalcoxi, -SR¹³, -S(O)R¹³ y -S(O)₂R¹³; donde R¹³ se selecciona entre hidrógeno, alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido y alquinilo C₂₋₆ no sustituido; el arilo, heterociclilo o cicloalquilo diferente del definido en R¹ o R², si está sustituido, está sustituido con uno o más sustituyentes que se seleccionan de halógeno, -R¹⁴, -OR¹⁴, -NO₂, -NR¹⁴R¹⁴, NR¹⁴C(O)R¹⁴, -NR¹⁴S(O)₂R¹⁴, -S(O)₂NR¹⁴R¹⁴, -NR¹⁴C(O)NR¹⁴R¹⁴, -SR¹⁴, -S(O)R¹⁴, S(O)₂R¹⁴, -CN, haloalquilo, haloalcoxi, -C(O)OR¹⁴, -C(O)NR¹⁴R¹⁴, -NR¹⁴S(O)₂NR¹⁴R¹⁴ y C(CH₃)₂OR¹⁴; adicionalmente, el cicloalquilo o heterociclilo no aromático, diferente del definido en R¹ o R², si está sustituido, también puede estar sustituido por el resto de fórmula (2) o =O; donde R¹⁴, R¹⁴, y R¹⁴ se seleccionan independientemente entre hidrógeno, alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido, alquinilo C₂₋₆ no sustituido, arilo no sustituido, cicloalquilo no sustituido y heterociclilo no sustituido; y donde R¹⁴ se selecciona entre hidrógeno, alquilo C₁₋₆ no sustituido, alquenilo C₂₋₆ no sustituido, alquinilo C₂₋₆ no sustituido y -Boc; opcionalmente en forma de uno de los estereoisómeros, preferentemente enantiómeros o diastereómeros, un racemato o en forma de una mezcla de al menos dos de los estereoisómeros, preferentemente enantiómeros y/o diastereómeros, en cualquier proporción de mezcla, o una de sus sales correspondientes, o uno de sus solvatos correspondientes; con las condiciones de que: -[CR⁵R⁵]ₘ-X-(CR⁶R⁶)ₙ-R² no sea metilo no sustituido; o R¹ no sea un compuesto no sustituido ni sustituido por N-alquilo de la fórmula (6).
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