AR073247A1 - Derivados de aminoindano, tetrahidronaftaleno y sus analogos, composiciones farmaceuticas que los contienen y usos de los mismos para tratar enfermedades respiratorias y renales, entre otras. - Google Patents

Derivados de aminoindano, tetrahidronaftaleno y sus analogos, composiciones farmaceuticas que los contienen y usos de los mismos para tratar enfermedades respiratorias y renales, entre otras.

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AR073247A1
AR073247A1 ARP090103342A ARP090103342A AR073247A1 AR 073247 A1 AR073247 A1 AR 073247A1 AR P090103342 A ARP090103342 A AR P090103342A AR P090103342 A ARP090103342 A AR P090103342A AR 073247 A1 AR073247 A1 AR 073247A1
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Argentina
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alkyl
radicals
radical
cycloheteroalkyl
cycloalkyl
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Sanofi Aventis
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Abstract

Reivindicacion 1: Un compuesto de la formula (1) en la que A es un radical arilo C6-10 o un radical heteroarilo de 5 a 10 miembros, donde el radical arilo y el radical heteroarilo pueden ser monocíclicos o bicíclicos y el radical heteroarilo puede comprender uno o más heteroátomos seleccionados del grupo de nitrogeno, oxigeno y azufre; donde uno o más átomos de hidrogeno en dichos radicales arilo o heteroarilo monocíclicos o bicíclicos, pueden estar reemplazados por sustituyentes R1 que se seleccionan independientemente uno de otro, del grupo de F, CI, Br, I, alquil C1-10-, alquenil C2-10-, alquinil C2-10-, cicloalquil C3-14-, cicloalquilalquil C4-20-, cicloalquilalquiloxi C4-20-, alcoxi C1-10-, alquiltio C1-10, aril C6-14-, heteroaril C2-13-, -CN, -NR13R14, -C(O)R12, -SF5, -S(O)nR12, -C(O)OR12, -C(O)NR13R14 y -S(O)nNR13R14; donde dos radicales adyacentes R1 pueden formar también un radical cicloalquilo C5-10 saturado o parcialmente insaturado o un radical cicloheteroalquilo C2-9 saturado o parcialmente insaturado, donde el radical cicloheteroalquilo puede comprender 1, 2 o 3 átomos de nitrogeno, 1 o 2 átomos de oxígeno, 1 o 2 átomos de azufre, 1 o 2 átomos de nitrogeno y 1 átomo de oxígeno o 1 átomo de azufre; donde dichos radicales alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquilalquiloxi, cicloheteroalquilo, alcoxi, y alquiltio, pueden estar sustituidos independientemente uno de otro, una más veces con F, OH o alcoxi C1-10; B es un radical monocíclico o bicíclico condensado, seleccionado del grupo de radicales arilo de 6 a 10 miembros, de radicales heteroarilo de 5 a 10 miembros, de radicales cicloalquilo de 3 a 10 miembros, de radicales cicloalquilarilo de 9 a 14 miembros, de radicales cicloalquilheteroarilo de 8 a14 miembros, radicales cicloheteroalquilo de 3 a 10 miembros, de radicales cicloheteroalquilarilo de 9 a 14 miembros y de radicales cicloheteroalquilheteroarilo de 8 a 14 miembros, donde las unidades de cicloalquilo o cicloheteroalquilo pueden ser saturadas o parcialmente insaturadas, y donde los grupos heterocíclicos pueden comprender uno o más heteroátomos seleccionados del grupo de nitrogeno, oxígeno y azufre; donde uno o más átomos de hidrogeno en los radicales B, pueden estar reemplazados por sustituyentes R5 que se seleccionan independientemente uno de otro, del grupo de radicales alquilo C1-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10, alquiltio C1-10, cicloalquilo C3-14, cicloalquilalquilo C4-20, cicloalquilalquiloxi C4-20, cicloheteroalquilo C2-19, cicloheteroalquilalquilo C3-19, cicloalquiloxi C3-11, cicloheteroalquiloxi C2-11, arilo C6-10, heteroarilo C1-9, cicloalquilarilo C9-14, cicloalquilheteroarilo C5-13, cicloheteroalquilarilo C7-13, cicloheteroalquilheteroarilo C4-12, donde las unidades de cicloalquilo y cicloheteroalquilo pueden ser saturadas o parcialmente insaturadas, y donde uno o más átomos de hidrogeno en dichos radicales R5 pueden estar reemplazados por otros radicales que se seleccionan independientemente uno de otro, del grupo de radicales R11, es posible además que R5 sea uno o más radicales que se seleccionan independientemente uno de otro, del grupo de OH, (=O), NH2, F, CI, Br, I, CN, NO2, -NR17R18, -NR16COR17, -NR16COOR17, -NR16CONR17R18, -NR16-S(O)2-R17, -NR16-S(O)2-NR17R18, -COOR16, -COR16; -CO(NR17R18), S(O)nR16 y -S(O)2NR17R18, donde R16, R17 y R18 independientemente uno de otro, para un radical, se seleccionan del grupo de H, radicales cicloheteroalquilo C2-19, cicloalquilo C3-14), arilo C6-10, alquilo C1-10, todos los cuales pueden estar sustituidos independientemente uno de otro, con OH, (=O), F, CI, Br, I, CN, NO2, -NR13R14, -NR13COR12, -NR13COOR12, -NR12CONR13R14, -NR13-S(O)2-R12, -NR12-S(O)2-NR13R14, -COOR12, -COR12; -CO(NR13R14), S(O)nR12, -S(O)2NR13R14, cicloalquilo C3-14, cicloalquilalquilo C4-20, cicloheteroalquilo C2-19, cicloheteroalquilalquilo C3-19, arilo C6-10 y heteroarilo C1-9, y donde R17 y R18 pueden formar junto con el nitrogeno al que están unidos, un heterociclo de 4-7 miembros, saturado, insaturado o parcialmente insaturado, que tiene 1 a 13 átomos de carbono que puede comprender adicionalmente uno o más heteroátomos de la lista de -O-, -S(O)n-, =N- y -NR15-, donde el heterociclo formado puede estar sustituido independientemente uno de otro, una o más veces con F, OH, (=O), NH2, NH-alquilo C1-4, N(alquil C1-4)2, CN o alcoxi C1-10, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-14, cicloalquilalquilo C4-20, cicloheteroalquilo C2-20, cicloheteroalquilalquilo C3-19, cada uno de los cuales puede llevar a su vez, independientemente uno de otro, uno o más radicales F, OH, (=O), NH2, NH-alquilo C1-4, N(alquil C1-4)2, CN o alcoxi C1-10; L es un enlace covalente; X es un grupo -O-; R2 está ausente o es uno o más sustituyentes que se pueden seleccionar independientemente uno de otro, del grupo de F, alquilo C1-10 y alcoxi C1-10, donde los radicales alquilo y alcoxi pueden estar sustituidos independientemente uno de otro, una o más veces con F; R3 y R4 son independientemente uno de otro, un radical hidrogeno o un radical que se selecciona del grupo de los radicales alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-14, cicloalquilalquilo C4-20, cicloheteroalquilo C2-19, cicloheteroalquilalquilo C3-19, arilo C6-10, arilalquilo C7-20, heteroarilo C1-9, heteroarilalquilo C2-19, donde los radicales R3 y R4 pueden estar sustituidos independientemente uno de otro, una o más veces con un radical del grupo de OH, NH2, (=O), F, CI, Br, I, CN, NO2, -NR13R14, -NR13COR12, -NR13COOR12, -NR12CONR13R14, -NR13-S(O)2-R12, -NR13-S(O)2-NR13R14, -COOR12, -COR12; -CO(NR13R14) y S(O)nR12, -S(O)2R13R14, o R3 y R4 forman junto con el nitrogeno al que están unidos, un heterociclo de 4-10 miembros, saturado, insaturado o parcialmente insaturado, que puede comprender adicionalmente uno o más heteroátomos de la lista de -O-, -S(O)n-, =N- y -NR8-, donde los radicales heterocíclicos pueden estar sustituidos independientemente uno de otro, una o más veces con radicales seleccionados del grupo de R7 y R9, y donde los radicales heterocíclicos formados por R3 y R4 pueden estar unidos con un puente constituido por un enlace, por una cadena saturada o insaturada de alquilo C1-10 o heteroalquilo C1-9 o por -NR15-, -O- o -S-, y donde las cadenas de alquilo y heteroalquilo pueden formar también un sistema de anillos espirocíclicos con el sistema de anillos formado por R3 y R4, donde los puentes de alquilo y heteroalquilo pueden estar sustituidos independientemente uno de otro, una o más veces con radicales seleccionados del grupo de R7 y R9, y donde R8 en el grupo -NR8 puede formar con el anillo que pueden constituir R3 y R4, un heterociclo adicional, saturado, insaturado o parcialmente insaturado, que puede estar sustituido independientemente uno de otro, una o más veces con radicales seleccionados del grupo de R7 y R9, y puede comprender adicionalmente uno o más heteroátomos de la lista de -O-, -S(O)n-, -N= y -NR19-; R7 es un radical alquilo C1-10 o un radical cicloalquilo C3-14, donde el radical alquilo puede estar sustituido independientemente uno de otro, una o más veces con R9; R8 es un H, un radical alquilo C1-10 o un radical cicloalquilo C1-14, COR12, -CO(NR13R14), S(O)nR12, -S(O)2NR13R14, donde el radical alquilo puede estar sustituido independientemente uno de otro, una o más veces con R10; R9 es un radical seleccionado del grupo de OH, (=O), F, CI, Br, I, CN, NO2, -NR13R14, -NR13COR12, -NR13COOR12, -NR12CONR13R14, -NR13-S(O)2-R12, -NR13-S(O)2-NR13R14, -COOR12, -COR12, -CO(NR13R14), S(O)nR12, -S(O)2NR13R14, cicloalquilo C3-14, cicloalquilalquilo C4-20, alcoxi C1-10, cicloheteroalquilo C2-19, cicloheteroalquilalquilo C3-19, radicales arilo C6-10 y radicales heteroarilo C1-9; R10 es un radical seleccionado del grupo de F, OH, CN, alcoxi C1-10, alquiltio C1-10, NO2, -NR13R14, -NR13COR12, -NR13COOR12, -NR13CONR13R14, -NR13-S(O)2-R12, -NR12-S(O)2-NR13R14, -COOR12, -COR12, -CO(NR13R14), S(O)nR12 y -S(O)2NR13R14; R11 es un radical seleccionado del grupo de alquilo C1-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10, alquiltio C1-20, cicloalquilo C3-14, cicloalquilalquilo C4-10, cicloheteroalquilo C2-13, cicloheteroalquilalquilo C4-19, cicloalquiloxi C3-14 y cicloheteroalquiloxi C2-13, todos los cuales pueden estar sustituidos independientemente uno de otro, una o más veces con R10; (=O), Cl, Br, I y R10; R12, R13 y R14 pueden ser independientemente uno de otro, H, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-14, cicloalquilalquilo C4-10, cicloheteroalquilo C2-13, cicloheteroalquilalquilo C3-19, arilo C6-10, cada uno de los cuales puede estar sustituido independientemente uno de otro, una o más veces con F, OH, (=O), NH2, NH-alquilo C1-4, N(alquil C1-4)2, CN o alcoxi C1-10; o R13 y R14 pueden formar junto con el nitrogeno al que están unidos, un heterociclo de 4-7 miembros, saturado, insaturado o parcialmente insaturado, que tiene 1 a 13 átomos de carbono, que puede comprender adicionalmente uno o más heteroátomos de la lista de -O-, -S(O)n,-, =N- y -NR15-, donde el heterociclo formado puede estar sustituido independientemente uno de otro, una o más veces con F, OH, (=O), NH2, NH-alquilo C1-4, N(alquil C1-4)2, CN o alcoxi C1-10, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-14, cicloalquilalquilo C4-20, cicloheteroalquilo C2-20, cicloheteroalquilalquilo C3-19, cada uno de los cuales puede llevar a su vez independientemente uno de otro, uno o más radicales F, OH, (=O), NH2, NH-alquilo C1-4, N(alquil C1-4)2, CN o alcoxi C1-10; R15 es un radical seleccionado del grupo de H, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-14, cicloalquilalquilo C4-20, cicloheteroalquilo C2-13, cicloheteroalquilalquilo C3-19, cada uno de los cuales puede estar sustituido independientemente uno de otro, una o más veces con F, OH, CN o alcoxi C1-10; R19 es un H, un radical alquilo C1-10
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