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AR073403A1 - DERIVADOS DE IMIDAZO[4, 5 - B]PIRIDINA Y SU USO EN EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA INHIBICIoN DE UN MIEMBRO DE LA FAMILIA MAPEG. - Google Patents

DERIVADOS DE IMIDAZO[4, 5 - B]PIRIDINA Y SU USO EN EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA INHIBICIoN DE UN MIEMBRO DE LA FAMILIA MAPEG.

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Publication number
AR073403A1
AR073403A1 ARP090103706A ARP090103706A AR073403A1 AR 073403 A1 AR073403 A1 AR 073403A1 AR P090103706 A ARP090103706 A AR P090103706A AR P090103706 A ARP090103706 A AR P090103706A AR 073403 A1 AR073403 A1 AR 073403A1
Authority
AR
Argentina
Prior art keywords
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alkyl
groups
last
cycloalkyl
Prior art date
Application number
ARP090103706A
Other languages
English (en)
Inventor
Henri Doods
Klaus Klinder
Norbert Hauel
Kirsten Arndt
Raimund Kuelzer
Roland Pfau
Original Assignee
Boehringer Ingelheim Int
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40344110&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR073403(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR073403A1 publication Critical patent/AR073403A1/es

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  • Vascular Medicine (AREA)

Abstract

Estos compuestos son utiles en el tratamiento de enfermedades en las cuales se desea y/o se requiere inhibicion de la actividad de la familia MAPEG, y en particular en el tratamiento de inflamacion y/o cáncer. Reivindicacion 1: Compuestos caracterizados porque tienen la formula (1) en donde Q2, Q3, Q3a y Q4 representan respectivamente -C(R2)=, -C(R3)=, -C(R3a)= y -C(R4)=; o bien uno cualquiera o dos cualesquiera de Q2, Q3, Q3a y Q4 pueden representar de manera alternativa e independiente -N=; R1 representa halo, -CN, -N(Ry1)Ry2, -N(Ry3)-CO)-Ry4, -N(Ry5)-S(O)2-Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)mRy11, -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)mRy11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 y -C(O)Ry15]; o bien 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)mRy11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14, -C(ORy15; 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)mRy11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 y -C(O)Ry15]; o bien 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 de los anillos que contienen 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 bien 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)mRy11, -S(O)2N(Ry13)Ry14, -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, -SO)2-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 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)mRy11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14, -C(O)Ry15, alquilo C1-3, 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, 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)mRy11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14, y -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 fluoro, -CN, -N(Ry1)Ry2, -N(Ry3)-C(O)-Ry4, -N(Ry5)S(O)2Ry6, -C(O)ORy7, -C(O)N(Ry8)Ry9, -ORy10, -S(O)mRy11, -S(O)2O-Ry12, -S(O)2N(Ry13)Ry14 y -C(O)Ry15]; o bien 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 fluoro 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 bien 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 estar enlazados entre si para formar, junto con los átomos esenciales del grupo A a los que les 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 fluoro y -O-alquilo C1-3; o bien dos grupos cualesquiera, cuando se unen al mismo átomo de nitrogeno (es decir, Ry1 y Ry2, Ry8 y Ry9, y Ry13 y Ry14), pueden estar enlazados entre si para formar, junto con el átomo de nitrogeno al que están necesariamente unidos, 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.
ARP090103706A 2008-09-25 2009-09-25 DERIVADOS DE IMIDAZO[4, 5 - B]PIRIDINA Y SU USO EN EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA INHIBICIoN DE UN MIEMBRO DE LA FAMILIA MAPEG. AR073403A1 (es)

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