AR059458A1 - Arildihidroisoquinolinonas sustituidas con azaciclilo, procedimiento para su preparacion y su uso como medicamentos - Google Patents

Arildihidroisoquinolinonas sustituidas con azaciclilo, procedimiento para su preparacion y su uso como medicamentos

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Publication number
AR059458A1
AR059458A1 ARP070100658A ARP070100658A AR059458A1 AR 059458 A1 AR059458 A1 AR 059458A1 AR P070100658 A ARP070100658 A AR P070100658A AR P070100658 A ARP070100658 A AR P070100658A AR 059458 A1 AR059458 A1 AR 059458A1
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Argentina
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alkyl
independently
nitrogen atom
group
aryl
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ARP070100658A
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Deutschland Gmb Sanofi-Aventis
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Deutschland Gmb Sanofi-Aventis
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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Abstract

Se refiere a arildihidroisoquinolinonas azaciclil-sustituidas, a sus derivados, a sales fisiologicamente toleradas y derivados fisiologicamente funcionales, a su preparacion, a medicamentos que comprenden al menos una arildihidroisoquinolinona azaciclil-sustituida de la invencion o su derivado, y al uso de las arildihidroisoquinolinonas azaciclil-sustituidas de la presente y sus derivados como antagonistas de MCH. Reivindicacion 1: Un compuesto de la formula (1), en la que los significados son, R1, R1', R1ö, R1'ö independientemente entre si H, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-alquilo C1-6, O-alcoxi C1-4-alquilo C1-4, S-alquilo C1-6, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, O-cicloalquilo C3-8, cicloalquenilo C3-8, alquinilo C2-6, alquileno C0-8-arilo, O-alquileno C0-8-arilo, S-arilo, N(R3)(R4), SO2-CH3, COOH, COO-alquilo C1-6, CON(R5)(R6), N(R7)CO(R8), N(R9)SO2(R10), CO(R11), (C(R12)(R13))x-O(R14); R3, R4, R5, R6, R7, R9 independientemente entre sí H, alquilo C1-8; o R3 y R4, R5 y R6 forman independientemente entre sí opcionalmente junto con el átomo de nitrogeno al que están unidos un anillo de 5-6 miembros que, aparte del átomo de nitrogeno, también puede comprender 0-1 heteroátomos adicionales del grupo de NH, N-alquilo C1-8, oxígeno y azufre; R8, R10, R11 independientemente entre sí H, alquilo C1-8, arilo; R12, R13 independientemente entre sí H, alquilo C1-8; R14 H, alquilo C1-6, arilo; x 0, 1, 2, 3, 4, 5 o 6; R2 H, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-alquilo C1-6, O-alcoxi C1-4alquilo C1-4, S-alquilo C1-6, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, O-cicloalquilo C3-8, cicloalquenilo C3-8, alquinilo C2-6, alquileno C0-8-arilo, O- alquileno C0-8-arilo, S-arilo, N(R15)(R16), SO2-CH3, COOH, COO-alquilo C1-8, CON(R17)(R18), N(R19)CO(R20), N(R21)SO2(R22), CO(R23), (C(R24)(R25))x'-O(R26); R15, R16, R17, R18, R19, R21 independientemente entre si H, alquilo C1-8; o R15 y R16, R17 y R18 forman independientemente entre si y opcionalmente junto con el átomo de nitrogeno al que están unidos un anillo de 5-6 miembros que, aparte del átomo de nitrogeno, también puede comprender 0-1 heteroátomos adicionales del grupo de NH, N-alquilo C1-6, oxigeno y azufre; R20, R22, R23 independientemente entre si H, alquilo C1-8, arilo; R24, R25 independientemente entre si H, alquilo C1-8; R26 H, alquilo C1-6, arilo; x' 0, 1, 2, 3, 4, 5 o 6; Y C(R27)(R27')C(R28)(R28'), C(R29)=C(R29'); R27, R27', R28, R28', R29, R29' independientemente entre si H, F, CI, Br, CN, alquilo C1-8, alquenilo C2-6, alquinilo C2-6; X S, O, C(R30)=C(R30'); R30, R30' independientemente entre sí H, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-alquilo C1-6, O-alcoxi C1- 4-alquilo C1-4, S-alquilo C1-6, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, O-cicloalquilo C3-8, cicloalquenilo C3-8, alquinilo C2-6, alquileno C0-8-arilo, O-alquileno C0-8-arilo, S-arilo, N(R15)(R16), SO2CH3, COOH, COO-alquilo C1-6, CON(R17)(R18), N(R19)CO(R20), N(R21)SO2(R22), CO(R23), (C(R24)(R25))x'-O(R26); A un enlace o un enlazador que tiene de 1 a 8 miembros, donde los miembros se seleccionan entre el grupo que consiste en O, S, SO2, N(R31), CO, C(R32)(R33), C(R34)=C(R34'), ciclopropileno, C?C, dando como resultado un radical químicamente razonable; R31, R34, R34' independientemente entre si H, alquilo C1-8; R32, R33 independientemente entre si H, alquilo C1-6, OH, O-alquilo C1-6; B H, N(R35)(R36), hidroxi-alquilo C1-4, alquilo C1-8, alcoxi C1-4-alquilo C1-4, alquenilo C2-8, alquinilo C2-8, un anillo mono-, bi-, tri- o espirocíclico de 3 a 10 miembros que puede comprender de 0 a 4 heteroátomos seleccionados entre el grupo de oxigeno, nitrogeno y azufre, donde el sistema de anillos puede estar sustituido adicionalmente con uno o más de los siguientes sustituyentes: F, CI, Br, CF3, NO2, CN, alquilo C1-6, O-alquilo C1-6, alcoxi C1-4-alquilo C1-4, hidroxi-alquilo C1-4, oxo, CO(R37), CON(R38)(R39), hidroxi, COO(R40), N(R41)COalquilo C1-6, N(R42)(R43), SO2CH3, SCF3 o S-alquilo C1-6; R35, R36, R37, R38, R39, R40, R41, R42, R43 independientemente entre si H, alquilo C1-8; o R38 y R39, R42 y R43 forman independientemente entre si opcionalmente junto con el átomo de nitrogeno al que están unidos un anillo de 5-6 miembros que, aparte del átomo de nitrogeno, también puede comprender 0-1 heteroátomos adicionales del grupo de NH, N-alquilo C1-6, oxigeno y azufre; Q estructura de anillos mono-, bi-, tri- o espirocíclicos saturados o parcialmente insaturados que tienen un átomo de nitrogeno y 0-3 heteroátomos adicionales seleccionados entre el grupo de N, O y S, donde los anillos de la estructura pueden estar espiro-unidos, condensados o enlazados, y donde el sistema de anillos puede estar unido con uno o más de los siguientes sustituyentes: F, OH, CF3, CN, OCF3, oxo, O-alquilo C1-8, alcoxi C1-4-alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, CO(R44), (C(R45)(R46))o-R47, CO(C(R45)(R46))p-R48, donde Q comprende en total al menos dos átomos de N; R44 H, alquilo C1-8; R45, R46 independientemente entre si H, alquilo C1-8, OH, cicloalquilo C3-8, alcoxi C1-4-alquilo C1-4; o, p independientemente entre si 0, 1, 2, 3, 4, 5 o 6; R47, R48 independientemente entre si OH, F, O-alquilo C1-8, CON(R49)(R50), N(R51)CO(R52), N(R53)(R54), CO2(R55), SO2Me, CN, un sistema de anillos de 3-10 miembros que tiene de 0 a 3 heteroátomos seleccionados entre el grupo de N, O y S, que puede estar sustituido con uno o más de los siguientes sustituyentes: F, CI, Br, CF3, alquilo C1-8, O-alquilo C1-8, alcoxi C1-4-alquilo C1-4, CO(R56), oxo, OH; R49, R50, R51, R52, R55, R56 independientemente entre si H, alquilo C1- 8; o R49 y R50 forman opcionalmente junto con el átomo de nitrogeno al que están unidos un anillo de 5-6 miembros que, aparte del átomo de nitrogeno, también puede comprender 0-1 heteroátomos adicionales del grupo de NH, N-alquilo C1-6, oxígeno y azufre; R53, R54 independientemente entre sí H, alquilo C1-8, alcoxi C1-4-alquilo C1-4, alquenilo C3-8, alquinilo C3-8, CO(R57), (C(R58)(R59))q-R60, CO(C(R61)(R62))r-R63. CO-O-alquilo C1-8; o R53 y R54 forman junto con el átomo de nitrogeno al que están unidos un anillo mono-, bi-, o espirocíclico de 4 a 10 miembros que, aparte del átomo de nitrogeno, comprende de 0 a 3 heteroátomos adicionales seleccionados entre el grupo de N, O y S y puede estar adicionalmente sustituido con uno o más de los siguientes sustituyentes: F, CI, Br, CF3, O-alquilo C1-8, alquilo C1-6, CO(R64), oxo, OH, alcoxi C1-4-alquilo C1-4, hidroxi-alquilo C1-4, CON(R65)(R66), N(R67)CO(R68), N(R69)(R70), CO2(R71), SO2-alquilo C1-6; R58, R59 independientemente entre sí H, alquilo C1-6, OH; R57, R61, R62, R64, R65, R66, R67, R68, R69, R70, R71 independientemente entre si H, alquilo C1-6; o R69 y R70 forman opcionalmente junto con el átomo de nitrogeno al que están unidos un anillo de 5-6 miembros que, aparte del átomo de nitrogeno, también puede comprender 0-1 heteroátomos adicionales del grupo de NH, N-alquilo C1-6, oxígeno y azufre; q, r independientemente entre si 0, 1, 2, 3, 4, 5 o 6; R60, R63 independientemente entre si OH, F, O-alquilo C1-6, CN, COO(R78), N(R74)COalquilo C1-6, N(R76)(R77), CON(R72)(R73), SO2-alquilo C1-6, un anillo mono-, bi- o espirocíclico de 3-12 miembros que puede comprender uno o más heteroátomos del grupo de N, O y S, y el anillo de 3-12 miembros puede comprender sustituyentes adicionales tales como F, CI, Br, OH, CF3, NO2, CN, OCF3, oxo, O-alquilo C1-6, alcoxi C1-4-alquilo C1-4, hidroxi-alquilo C1-4, S-alquilo C1-6, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, O-cicloalquilo C3-8, cicloalquenilo C3-8, O- cicloalquenilo C3-8, alquinilo C2-6, N(R76)(R77), COO(R78), SO2-alquilo C1-8y COOH; R72, R73, R74, R76, R77, R78 independientemente entre si H, alquilo C1-8; o R72 y R73, R76 y R77 forman independientemente entre si opcionalmente junto con el átomo de nitrogeno al que están unidos un anillo de 5-6 miembros que, aparte del átomo de nitrogeno, también puede comprender 0-1 heteroátomos adicionales del grupo de NH, N-alquilo C1-6, oxigeno y azufre.
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