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AR044496A1 - N-arilheterociclos sustituidos, procedimientos para su preparacion, y su empleo como medicamentos - Google Patents

N-arilheterociclos sustituidos, procedimientos para su preparacion, y su empleo como medicamentos

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Publication number
AR044496A1
AR044496A1 ARP040100469A ARP040100469A AR044496A1 AR 044496 A1 AR044496 A1 AR 044496A1 AR P040100469 A ARP040100469 A AR P040100469A AR P040100469 A ARP040100469 A AR P040100469A AR 044496 A1 AR044496 A1 AR 044496A1
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alkyl
independently
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Aventis Pharma Gmbh
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Abstract

N-arilheterociclos substituidos, sus sales fisiológicamente tolerables y derivados fisiológicamente funcionales. Los compuestos son útiles como aneroxígenos. Reivindicación 1: Un compuesto de fórmula (1) en la cual R1, R2 significan de manera independiente H, alquilo C1-8, -(CR78R79)o-R12, alcoxi C1-4-alquilo C1-4, ariloxi-alquilo C1-4, alquenilo C3-8, alquinilo C3-8, CO-alquilo C1-8, -CO-(CH2)o-R12, CO-ariloxi-alquilo C1-4, CO-alquenilo C2-8, CO-alquinilo C2-8, COCH-CH(R13), COCC(R14), CO-alquil C1-4-S(O)p-alquilo C1-4, CO(C(R15)(R16))qN(R17)(R18), CO(C(R19)(R20))rCON(R21)(R22) o CO(C(R23)(R24))sO(R25); o bien R1 y R2, forman junto con el átomo de nitrógeno al cual están unidos, un anillo mono-, bi- o espirocíclico de 4 a 10 eslabones que además del átomo de nitrógeno, puede contener o a 4 heteroátomos adicionales seleccionados del grupo de oxígeno, nitrógeno y azufre, pudiendo el sistema anular heterocíclico estar substituido adicionalmente con F, Cl, Br, CF3, NO2, CN, alquilo C1-6, O-alquilo C1-8, alcoxi C1-4-alquilo C1-4, hidroxi-alquilo C1-4, alquilen C0-8-arilo, oxo, CO(R26), CON(R27)(R28), hidroxi, COO(R29), N(R30)COalquilo C1-6, N(R31)(R32) o SO2CH3; o vale 0, 1, 2, 3, 4, 5 ó 6; p vale 0, 1 ó 2; q, r, s valen de manera independiente 0, 1, 2, 3 ó 4; R13, R14 significan de manera independiente entre sí, un sistema anular aromático de 5 a 10 eslabones, que puede contener 0-2 heteroátomos adicionales del grupo de nitrógeno, oxígeno y azufre, y que puede estar substituido con F, Cl, Br, CF3, NO2, CN, alquilo C1-6 o O-alquilo C1-8; R15, R16, R17, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32 significan de manera independiente entre sí H o alquilo C1-6; R18 significa H, alquilo C1-6, COalquilo C1-6 o CO(R33); o bien R17 y R18, R21 y R22, R27 y R28, y R31 y R32, significan de manera independiente entre sí, y opcionalmente junto con el átomo de nitrógeno al cual al cual están unidos, un anillo de 5-6 eslabones que, además del átomo de nitrógeno, puede contener aún 0-1 heteroátomos adicionales del grupo de N-alquilo C1-6, oxígeno y azufre; R33 significa un sistema anular aromático de 5-10 eslabones, que puede contener 0-2 heteroátomos adicionales del grupo de nitrógeno, oxígeno y azufre, y que puede estar substituido con F, Cl, Br, CF3, NO2, CN, alquilo C1-6 o O-alquilo C1-8; R12 significa OH, O-alquilo C1-6, Oalquilen C0-8-arilo, CN, S-alquilo C1-6, COO(R80), CON(R81)(R93), N(R82)(R83) o anillo mono-, bi- o espirocíclico de 3-12 eslabones, que puede contener uno o varios heteroátomos del grupo de N, O y S, y el anillo de 3-12 eslabones puede contener substituyentes adicionales tales como F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, oxo, O-alquilo C1-6, 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, O-cicloalquenilo C3-8, alquinilo C2-6, O-alquilen C0-8-arilo, N(R34)(R35), COCH-CH(R36), (C(R37)(R38))t(R39), CO(C(R37)(R38))t(R39), COalquilo C1-6, COCOOalquilo C1-6, COO(R40), S(O)u(R41) o COOH; t vale 0, 1, 2, 3, 4, 5 ó 6; u vale 0, 1 ó 2; o bien R34, R35, R37, R38 significan de manera independiente entre sí H o alquilo C1-8; R34 y R35, significan opcionalmente junto con el átomo de nitrógeno al cual al cual están unidos, un anillo de 5-6 eslabones que, además del átomo de nitrógeno, puede contener aún 0-1 heteroátomos adicionales del grupo de N-alquilo C1-6, oxígeno y azufre, y opcionalmente puede estar substituido con 1 o 2 grupos oxo; R36, R39 significan de manera independiente entre sí cicloalquilo C3-8, un sistema anular aromático de 5-10 eslabones, que puede contener 0-2 heteroátomos adicionales del grupo de nitrógeno, oxígeno y azufre, y que puede estar substituido con F, Cl, Br, CF3, NO2, CN, alquilo C1-6 o O-alquilo C1-8; R40 significa H, alquilo C1-8, alquenilo C2-6 o alquilen C0-8-arilo; R41 significa alquilo C1-8, un sistema anular aromático de 5-10 eslabones, que puede contener 0-2 heteroátomos adicionales del grupo de nitrógeno, oxígeno y azufre, y que puede estar substituido con F, Cl, Br, CF3, NO2, CN, alquilo C1-6 o O-alquilo C1-8; R78, R79 significan de manera independiente entre sí H, alquilo C1-8, hidroxi-alquilo C1-4, OH o alcoxi C1-4-alquilo C1-4; R80, R81, R93 significan de manera independiente entre sí alquilo C1-8, alquenilo C2-6, alquilen C0-8-arilo; R82, R83 significan de manera independiente entre sí H o alquilo C1-6; o bien R82 y R83, significan, opcionalmente junto con el átomo de nitrógeno al cual al cual están unidos, un anillo de 5-6 eslabones que, además del átomo de nitrógeno, puede contener aún 0-1 heteroátomos adicionales del grupo de N-alquilo C1-6, oxígeno y azufre, y opcionalmente puede estar substituido con 1 o 2 grupos oxo; R3 significa H, alquilo C1-6; R4, R5 significan, de manera independiente entre sí H, alquilo C1-6, OH, O-alquilo C1-6, O-COalquilo C1-6 o S-alquilo C1-6; o bien R6, R7, R8, R9 significan de manera independiente entre sí H o alquilo C1-8; o bien R6 y R7, y R8 y R9, significan de manera independiente entre sí y opcionalmente, oxo; n, m valen de manera independiente entre sí 0, 1 o 2; A, B, D, G significan de manera independiente entre sí N o C(R42); o bien los grupos A y B, o los grupos D y G son en cada caso C(R42) y forman juntos un radical carbocíclico o heterocíclico de 5 o 6 eslabones, de manera tal que se origina en conjunto un sistema bicíclico; R42 significa H, F, Cl, 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, O-cicloalquenilo C3-8, alquinilo C2-6, alquilenC0-8-arilo, O-alquilen C0-8-arilo, S-arilo, N(R43)(R44), SO2-CH3, COOH, COO-alquilo C1-6, CON(R45)(R46), N(R47)CO(R48), N(R49)SO2(R50), CO(R51), -(CR84R85)x-O(R86); R43, R44, R45, R46, R47, R49 significan de manera independiente entre sí H o alquilo C1-8; o bien R43 y R44, y R45 y R46, significan de manera independiente entre sí y opcionalmente junto con el átomo de nitrógeno al cual al cual están unidos, un anillo de 5-6 eslabones que, además del átomo de nitrógeno, puede contener aún 0-1 heteroátomos adicionales del grupo de N-alquilo C1-6, oxígeno y azufre; R48, R50, R51 significan de manera independiente entre sí H, alquilo C1-8 o arilo; R84, R85 significan de manera independiente entre sí H o alquilo C1-8; R86 significa H, alquilo C1-6 o arilo; x vale 1, 2, 3, 4, 5 ó 6; R10 significa H, alquilo C1-8, alquenilo C3-6 o alquinilo C3-6; X significa N(R52), O, un enlace, C=C, C(R53)(R54), C(R55)(R56)O, CO, C:::C, o un grupo de fórmula -(CR87R88)y-, en la cual uno o más grupos -(CR87R88)- pueden haber sido reemplazados por Y, originándose un radical químicamente con sentido; Y significa O, S o N(R89); R52, R53, R54, R55, R56 significan, de manera independiente entre sí H o alquilo C1-8; R87, R88 significan de manera independiente entre sí H o alquilo C1-4, pudiendo tener R87 y R88 en los grupos "y", en cada caso, los mismos significados o significados diferentes; y vale 2, 3, 4, 5 ó 6; E significa una estructura anular carbo- o heterocíclica, bivalente de 3 a 14 eslabones, y con 0 a 4 heteroátomos del grupo de N, O y S, que opcionalmente puede portar substituyentes del grupo de H, F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, oxo, 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, O-cicloalquenilo C3-8, alquinilo C2-6, alquilen C0-8-arilo, O-alquilen C0-8-arilo, S-arilo, N(R57)(R58), SO2-CH3, COOH, COO-alquilo C1-6, CON(R59)(R60), N(R61)CO(R62), N(R63)SO2(R64), CO(R65) y que puede ser mono- o bicíclica; R57, R58, R59, R60, R61, R63 significan de manera independiente entre sí H o alquilo C1-8; o bien R57 y R58, y R59 y R60, significan de manera independiente entre sí y opcionalmente junto con el átomo de nitrógeno al cual al cual están unidos, un anillo de 5-6 eslabones que, además del átomo de nitrógeno, puede contener aún 0-1 heteroátomos adicionales del grupo de N-alquilo C1-6, oxígeno y azufre; R62, R64, R65 significan de manera independiente entre sí H, alquilo C1-8, arilo; K significa un enlace, O, OCH2, CH2O, S, SO, SO2, N(R66), N(R67)CO, CON(R68), (C(R69)(R70))v, CO, C:::C, C=C un grupo de fórmula -(CR90R91)z-, en donde uno o varios grupos -(CR90R91)- pueden haber sido reemplazados por Z, originándose un radical químicamente con sentido; v vale 1, 2, 3 ó 4; R66, R67, R68, R69, R70 significan de manera independiente entre sí H o alquilo C1-8; Z significa O, S, N(R92), CO, SO o SO2; R90, R91 significan de manera independiente entre sí H, alquilo C1-8, hidroxi-alquilo C1-4, hidroxi, alcoxi C1-4-alquilo C1-4, y pudiendo tener R90 y R91 en los grupos "z" en cada caso los mismos significados o significados diferentes; z vale 2, 3, 4, 5 ó 6; R92 significa H o alquilo C1-8; R11 significa H, alquilo C1-8, alcoxi C1-4-alquilo C1-4, alquenilo C3-8, alquinilo C3-8, un anillo mono-, bi-, tri- o espirocíclico, de 3 a 10 eslabones que puede contener 1, 2, 3 o 4 heteroátomos seleccionados del grupo de oxígeno, nitrógeno y azufre, pudiendo estar el sistema anular substituido adicionalmente con F, Cl, Br, CF3, NO2, CN, alquilo, O-alquilo C1-8, alcoxi C1-4-alquilo C1-4, alquilen C0-8-arilo, oxo, CO(R71), CON(R72)(R73), hidroxi, hidroxi-alquilo C1-4, COO(R74), N(R75)COalquilo C1-6, N(R76)(R77), SO2CH3 o SCF3; R71, R72, R73, R74, R75, R76, R77 significan de manera independiente entre sí y opcionalmente junto con el átomo de nitrógeno al cual al cual están unidos, un anillo de 5-6 eslabones que, además del átomo de nitrógeno, puede contener aún 0-1 heteroátomos adicionales del grupo de N-alquilo C1-6, oxígeno y azufre; o bien E, K y R11 forman juntos un triciclo, pudiendo ser los anillos, de manera independiente entre sí, saturados, parcialmente saturados o insaturados, y pudiendo contener en cada caso 3-8 átomos en el anillo; sus N-óxidos y sus sales fisiológicamente tolerables.
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