AR073686A1 - Derivados de imidazo[4,5-c]piridin-6-carboxamida inhibidores de enzimas de la familia mapeg, utiles como agentes farmaceuticos en el tratamiento de enfermedades inflamatorias incluyendo enfermedades respiratorias. - Google Patents
Derivados de imidazo[4,5-c]piridin-6-carboxamida inhibidores de enzimas de la familia mapeg, utiles como agentes farmaceuticos en el tratamiento de enfermedades inflamatorias incluyendo enfermedades respiratorias.Info
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- AR073686A1 AR073686A1 ARP090103705A ARP090103705A AR073686A1 AR 073686 A1 AR073686 A1 AR 073686A1 AR P090103705 A ARP090103705 A AR P090103705A AR P090103705 A ARP090103705 A AR P090103705A AR 073686 A1 AR073686 A1 AR 073686A1
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Abstract
Reivindicacion 1: Compuestos caracterizados porque tienen la formula 1, en el que Q2, Q3, Q3a y Q4 representan respectivamente -C(R2)=, -C(R3)=, -C(R3a)= y -C(R4)=; o uno o dos cualesquiera de Q2, Q3, Q3a y Q4 puede representar, alternativa e independientemente, -N=; R1 representa halo, -CN, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)m-Ry11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 o -C(O)Ry15; alquilo C1-7, alquenilo C2-7, alquinilo C2-7, cicloalquilo [donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre fluoro, -CN, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, ORy10, -S(O)m-Ry11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 y -C(O)Ry15]; o heterocicloalquilo o heteroarilo (donde los dos ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R9); R2, R3, R3a y R4 representan, independientemente, hidrogeno, halo, , -CN, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)m-Ry11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 o -C(O)Ry15; alquilo C1-7, alquenilo C2-7, alquinilo C2-7, cicloalquilo [donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre fluor, , -CN, -N(Ry1)Ry2, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)m-Ry11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 o -C(O)Ry15]; con la condicion que si R3 o R3a es un grupo alquilo C1-6 sustituido, entonces el sustituyente no puede ser -N(Ry5)-S(O)2-Ry6; o cualquier par adyacente de R1, R2, R3, R3a y R4 (es decir, R1 y R3a, R2 y R3, R3 y R4 y R4 y R3a) pueden unirse para formar, junto con los átomos de carbono esenciales del anillo que contiene Q2 a Q4 a los que están necesariamente unidos, un anillo adicional de 5 a 7 miembros, que contiene opcionalmente de uno a tres heteroátomos, donde dicho anillo puede contener una o dos insaturaciones más y que está opcionalmente sustituido con uno o más sustituyentes alquilo C1-3 y/o =O; R6 representa hidrogeno; heterocicloalquilo, arilo o heteroarilo (donde los tres ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R9); o alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo, donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre fluor, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)m-Ry11, -S(O)2N(Ry13)Ry14 o -C(O)Ry15; heterocicloalquilo, cicloalquilo, arilo y heteroarilo (donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R9); cada R8 representa, independientemente, hidrogeno, halo, -N(Ry1)Ry2, -ORy10, -S(O)m-Ry11; alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo, -O-alquilo C1-6, -O-alquenilo C2-6, -O-alquinilo C2-6, -O-cicloalquilo, -O-heterocicloalquilo [donde los nueve ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre fluor, , -CN, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)m-Ry11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 o -C(O)Ry15; cicloalquilo, heterocicloalquilo, arilo y heteroarilo (donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R9)]; heterocicloalquilo o heteroarilo (donde los dos ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R9); A representa arilo, heteroarilo, heterocicloalquilo, cicloalquilo, alquilo C1-12, alquenilo C2-12 o alquinilo C2-12, estando todos ellos opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R9; R9 representa, en cada caso en el que se usa en la presente memoria: halo, , -CN, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)m-Ry11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 o -C(O)Ry15; alquilo C1-7, alquenilo C2-7, alquinilo C2-7, cicloalquilo, heterocicloalquilo [donde los cinco ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre fluor, -, -CN, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)m-Ry11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 o -C(O)Ry15]; o arilo o heteroarilo [donde los dos ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre halo, -CN, alquilo C1-7, alquenilo C2-7, alquinilo C2-7, cicloalquilo (donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre fluor y -ORx2), -O-alquilo C1-7, -O-alquenilo C2-7, -O-alquinilo C2-7 y -O-cicloalquilo (donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más átomos de fluor)] o dos sustituyentes R9 cualesquiera: cuando se unen a átomos adyacentes del grupo A; y, en caso de que los sustituyentes R9 estén unidos a un grupo A no aromático, cuando se unen a los mismos átomos, pueden unirse para formar, junto con los átomos esenciales del grupo A a los que los sustituyentes R9 pertinentes están necesariamente unidos, un anillo adicional de 3 a 8 miembros, que contiene opcionalmente uno o dos heteroátomos adicionales, y donde el anillo adicional contiene opcionalmente una o dos insaturaciones y está opcionalmente sustituido con uno o más sustituyentes alquilo C1-3 y/o =O; m representa 0, 1 o 2; cada Ry4, Ry6, Ry11 y Ry15: representa independientemente alquilo C1-7 alquenilo C2-7, alquinilo C2-7, cicloalquilo, donde los cuatro ultimos grupos están opcionalmente sustituidos con uno o más átomos de fluor; cada RX2, Ry1, Ry2, Ry3, Ry5, Ry7, Ry8, Ry9, Ry10, Ry12, Ry13 y Ry14 representa, independientemente, hidrogeno o alquilo C1-7, alquenilo C2-7, alquinilo C2-7, cicloalquilo, heterocicloalquilo, donde los cinco ultimos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre fluor y -O-alquilo C1-3: o dos grupos cualesquiera, cuando se unen al mismo átomo de nitrogeno (es decir, Ry1 y Ry2, Ry8 y Ry9, y Ry13 y Ry14), pueden unirse, junto con el átomo de nitrogeno al que están necesariamente unidos, para formar un anillo de 3 a 8 miembros, que contiene opcionalmente uno o dos heteroátomos adicionales y donde el anillo contiene opcionalmente una o dos insaturaciones y está opcionalmente sustituido con uno o más sustituyentes alquilo C1-3 y/o =O, o una sal farmacéuticamente aceptable del mismo.
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