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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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AR
Argentina
Prior art keywords
unsubstituted
substituted
alkyl
alkynyl
alkenyl
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ARP160102304A
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English (en)
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Esteve Labor Dr
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Publication of AR105522A1 publication Critical patent/AR105522A1/es

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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/72—Nitrogen atoms
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    • C07D295/12—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 substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
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    • C07D295/13—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 substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07D295/135—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 substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
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    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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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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