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AR088611A1 - Derivados de quinolina carboxamida y quinolina carbonitrilo como moduladores alostericos negativos de mglur2, composiciones, y su uso - Google Patents

Derivados de quinolina carboxamida y quinolina carbonitrilo como moduladores alostericos negativos de mglur2, composiciones, y su uso

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Publication number
AR088611A1
AR088611A1 ARP120104094A ARP120104094A AR088611A1 AR 088611 A1 AR088611 A1 AR 088611A1 AR P120104094 A ARP120104094 A AR P120104094A AR P120104094 A ARP120104094 A AR P120104094A AR 088611 A1 AR088611 A1 AR 088611A1
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AR
Argentina
Prior art keywords
alkyl
group
phenyl
cycloalkyl
independently selected
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ARP120104094A
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English (en)
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Merck Sharp & Dohme
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Publication of AR088611A1 publication Critical patent/AR088611A1/es

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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen 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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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract

Reivindicación 1: Un compuesto de fórmula (1) o un estereoisómero del mismo, o una sal farmacéuticamente aceptable de dicho compuesto o dicho estereoisómero, en la que: el anillo A es un resto seleccionado entre el grupo que consiste en: fenilo, -cicloalquilo C₅₋₆, -cicloalquenilo C₅₋₆, -piridinilo, pirimidinilo, -pirazolilo, -tienilo, -tiazolilo, -tiadiazolilo, y -oxazolilo; RQ se selecciona entre el grupo que consiste en -CN y -C(O)NH₂; -L- es un enlace o resto divalente seleccionado entre el grupo que consiste en: -(C(R¹L)₂)ₚ-, un resto de fórmula (2), -C(O)-, -S(O)- y -S(O)₂-; p es 1, 2 ó 3; cada R¹L se selecciona independientemente entre el grupo que consiste en H, -CH₃, -CF₃, -OH, -C(O)-, halógeno, -ciclopropilo, -O-CH₃, y -O-CF₃; R¹ se selecciona entre el grupo que consiste en: {1} heterocicloalquilo y heterocicloalquenilo, en el que dicho heterocicloalquilo y dicho heterocicloalquenilo son sistemas anulares monocíclicos o multicíclicos que comprenden de 3 a 10 átomos en el anillo en los que 1, 2 ó 3 de los átomos de cada uno de dichos sistemas anulares es un heteroátomo en el anillo seleccionado independientemente entre el grupo que consiste en N, S, S(O), S(O)₂, y O, y en el que cada uno de dichos grupos heterocicloalquilo y cada uno de dichos grupos heterocicloalquenilo están sin sustituir o sustituidos con 1 a 5 grupos seleccionados independientemente entre el grupo que consiste en oxo, CN, -OH, halógeno, -alquilo C₁₋₆, -alquilo C₁₋₆ hidroxisustituido, -alquinilo C₁₋₆, -haloalquilo C₁₋₆, -haloalquilo C₁₋₆ hidroxisustituido, -O-alquilo C₁₋₆, -cicloalquilo C₃₋₈, -alquil-cicloalquilo, -CH(OH)cicloalquilo, fenilo, -alquil-fenilo, heteroarilo monocíclico, -alquil-heteroarilo monocíclico, -espirocicloalquilo C₃₋₈, -espiroheterocicloalquilo C₃₋₈, -C(O)H, -C(O)OH, -C(O)alquilo C₁₋₆, -C(O)O-alquilo C₁₋₆, -N(R¹A)C(O)alquilo C₁₋₆, -N(R¹A)₂, -C(O)N(R¹A)₂, -S(O)₂H, -S(O)-fenilo, -S(O)-alquil C₁₋₆-fenilo, -S(O)₂-fenilo, -S(O)₂-alquil C₁₋₆-fenilo, -S(O)₂OH, y -S(O)₂-alquilo C₁₋₆, en el que cada grupo R¹A se selecciona independientemente entre el grupo que consiste en H y -(alquilo C₁₋₆); {2} heteroarilo, en el que dicho heteroarilo es un sistema anular monocíclico o multicíclico que comprende de 5 a 10 átomos en el anillo en el que de 1 a 4 de los átomos de dicho sistema anular es un átomo de nitrógeno en el anillo, y en el que dicho heteroarilo está sin sustituir o sustituido con 1 a 5 grupos seleccionados independientemente entre el grupo que consiste en oxo, CN, -OH, halógeno, -alquilo C₁₋₆, -alquilo C₁₋₆ hidroxisustituido, -alquinilo C₁₋₆, -haloalquilo C₁₋₆, -haloalquilo C₁₋₆ hidroxisustituido, -O-alquilo C₁₋₆, -cicloalquilo C₃₋₈, -alquil-cicloalquilo, -CH(OH)cicloalquilo, fenilo, -alquil-fenilo, heteroarilo monocíclico, -alquil-heteroarilo monocíclico, -espirocicloalquilo C₃₋₈, -C(O)H, -C(O)OH, -C(O)alquilo C₁₋₆, -C(O)O-alquilo C₁₋₆, -N(R¹B)C(O)alquilo C₁₋₆, -N(R¹B)₂, -C(O)N(R¹B)₂, -S(O)₂H, -S(O)-fenilo, -S(O)-alquil C₁₋₆-fenilo, -S(O)₂-fenilo, -S(O)₂-alquil C₁₋₆-fenilo, -S(O)₂OH, y -S(O)₂-alquilo C₁₋₆, en el que cada grupo R¹B se selecciona independientemente entre el grupo que consiste en H y -(alquilo C₁₋₆), con la condición de que R¹ no sea triazolilo sin sustituir o sustituido, y con la condición adicional de que cuando R¹ es oxadiazolilo sustituido, tiazolilo sustituido, o tiadiazolilo sustituido, entonces -L- se selecciona entre el grupo que consiste en -(C(R¹L)₂)ₚ-, y el resto de fórmula (2); {3} fenilo, en el que dicho fenilo está sin sustituir o sustituido con 1 a 5 grupos seleccionados independientemente entre el grupo que consiste en oxo, CN, -OH, halógeno, -alquilo C₁₋₆, -alquinilo C₁₋₆, -haloalquilo C₁₋₆, -O-alquilo C₁₋₆, -cicloalquilo C₃₋₈, -alquil-cicloalquilo -CH(OH)cicloalquilo, heteroarilo monocíclico, -alquil-heteroarilo monocíclico, -espirocicloalquilo C₃₋₈, -C(O)H, -C(O)OH, -C(O)alquilo C₁₋₆, -C(O)O-alquilo C₁₋₆, N(R¹C)C(O)alquilo C₁₋₆, -N(R¹C)₂, -C(O)N(R¹C)₂, -S(O)₂H, -S(O)-fenilo, -S(O)-alquil C₁₋₆-fenilo, -S(O)₂-fenilo, -S(O)₂-alquil C₁₋₆-fenilo, -S(O)₂OH, y -S(O)₂-alquilo C₁₋₆, en el que cada grupo R¹C se selecciona independientemente entre el grupo que consiste en H y -(alquilo C₁₋₆); {4} H y -alquilo C₁₋₆; {5} -CH₂N(R¹D)R¹E, en el que: R¹D se selecciona entre el grupo que consiste en H, -alquilo C₁₋₆, y -C(O)OR¹H; y R¹E se selecciona entre el grupo que consiste en -O-alquilo C₁₋₆, heteroalquilo, -alquil-C(O)N(R¹H), y -C(O)OR¹H, en el que cada R¹H se selecciona independientemente entre el grupo que consiste en H y -alquilo C₁₋₆; y {6} -CH₂N(R¹F)OR¹G, en el que: R¹F se selecciona entre el grupo que consiste en H, -alquilo C₁₋₆, y -C(O)OR¹H, en el que cada R¹H se selecciona independientemente entre el grupo que consiste en H y -alquilo C₁₋₆; y R¹G se selecciona entre el grupo que consiste en H y -alquilo C₁₋₆; n es 0, 1, 2 ó 3; cada R² (cuando está presente) se selecciona independientemente entre el grupo que consiste en halógeno, -CN, -OH, -alquilo C₁₋₆, -O-alquilo C₁₋₆, -haloalquilo C₁₋₆, -O-haloalquilo C₁₋₆, ciclopropilo, ciclobutilo, ciclopentilo, ciclohexilo, -NH₂, -NH-alquilo C₁₋₆, -N(alquil C₁₋₆)₂, -C(O)O-alquilo C₁₋₆, y fenilo; y R³ se selecciona entre el grupo que consiste en hidrógeno y flúor.
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