AR048939A1 - Derivados de fenol y tiofenol 3 - o 4 - monosustituidos utiles como ligandos de h3; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurologicos e inflamatorios. - Google Patents

Derivados de fenol y tiofenol 3 - o 4 - monosustituidos utiles como ligandos de h3; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurologicos e inflamatorios.

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Publication number
AR048939A1
AR048939A1 ARP050101824A ARP050101824A AR048939A1 AR 048939 A1 AR048939 A1 AR 048939A1 AR P050101824 A ARP050101824 A AR P050101824A AR P050101824 A ARP050101824 A AR P050101824A AR 048939 A1 AR048939 A1 AR 048939A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
amino
cycloalkyl
Prior art date
Application number
ARP050101824A
Other languages
English (en)
Original Assignee
Warner Lambert Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from EP04291187A external-priority patent/EP1593679A1/en
Priority claimed from GB0504564A external-priority patent/GB0504564D0/en
Application filed by Warner Lambert Co filed Critical Warner Lambert Co
Publication of AR048939A1 publication Critical patent/AR048939A1/es

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Abstract

Tales derivados de fenol y tiofenol 3- o 4-monosustituidos son ligandos H3 y son utiles en numerosas enfermedades, trastornos y afecciones, en particular enfermedades, trastornos y afecciones inflamatorias, alérgicas y respiratorias. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable y/o un solvato (incluyendo hidrato) del mismo donde: el sustituyente de formula -Z-R está en la posicion meta o para del grupo fenilo; X se selecciona entre -CN, -CH2OH, -CH2-O- alquilo C1-4, -C(O)OH,-C(O)Oalquilo C1-4, -CH2-NR1R2, -C(O)NR3R4, -CH2-O-het2, -CH2-het1 y het1, estando el grupo het1 tanto en -CH2-het1 como en het1 opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halo, ciano, alquilo C1-4, -S-alquilo C1-4 y alcoxi C1-4; R1 es H o alquilo C1-4 opcionalmente sustituido con cicloalquilo C3-6; R2 se selecciona entre el grupo compuesto por H, alquilo C1-6 opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre cicloalquilo C3-6, hidroxi, -S-alquilo C1-4, -O-alquilo C1-4, -SO2-alquilo C1-4, -SO-alquilo C1-4, halo, het1, amino, alquil(C1-4)amino, [alquil C1-4]2amino y fenilo, estando dicho fenilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halo, hidroxi, ciano, alquilo C1-4 y alcoxi C1-4, cicloalquilo C3-6, het2, opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halo, ciano, alquilo C1-4, NH2 y alcoxi C1-4; -SO2-R5 donde R5 se selecciona entre el grupo compuesto por alquilo C1-4, amino, alquilo(C1-4)amino, [alquil C1-4]2amino, fenilo y -alquil (C1-4)-fenilo, estando dicho fenilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halo, ciano, alquilo C1-4 y alcoxi C1-4, y -C(O)-R6 donde R6 se selecciona entre el grupo compuesto por alquilo C1-4, amino, alquil(C1-4)amino, [alquil C1-4]2amino, fenilo y -alquil(C1- 4)-fenilo, estando dicho fenilo opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halo, ciano, alquilo C1-4 y alcoxi C1-4; o R1 y R2 forman conjuntamente con el átomo de N al que están unidos un heterociclo saturado de 3, 4, 5, 6 o 7 miembros donde un átomo de C puede reemplazarse por N, O, S, SO o SO2 y donde dicho heterociclo saturado está opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre hidroxi, halo, =O, alquilo C1-4, -alquil(C1-4)cicloalquilo C3-6, alcoxi C1-4, hidroxialquilo C1-4, alcoxi(C1-4)alquilo C1-4, -SO2alquilo C1-4, -C(O)alquilo C1-4, [alquil C1-4]2amino, amino, alquil(C1-4)amino, -C(O)NH2, C(O)Oalquilo C1-4 y pirrolidinona; cada uno de R3 y R4 se selecciona independientemente entre H, cicloalquilo C3-6, y alquilo C1-4, estando dicho cicloalquilo C3-6 y alquilo C1-4 opcionalmente sustituidos con amino, alquil(C1-4)amino, [alquil C1-4]2amino o cicloalquilo C3-6, o R3 y R4 forman junto con el átomo de N al que están unidos un heterociclo saturado de 4, 5, 6 o 7 miembros donde un átomo de C puede reemplazarse por N u O y donde dicho heterociclo saturado está opcionalmente sustituido con alquilo C1-4, [alquil C1-4]2amino, amino, alquil(C1- 4)amino, o -C(O)alquilo C1-4, estando dicho -C(O)alquilo C1-4 opcionalmente sustituido con metoxi o etoxi, Y se selecciona entre CH2, CH(OH), O, C=O y N, estando dicho N sustituido con H, alquilo C1-4, C(O)alquilo C1-4 o alcoxi C1-4-alquilo C1-4; Z se selecciona entre O, S, SO y SO2; m y p son ambos numeros enteros que son independientemente 1, 2 o 3, con la condicion de que m+p sea igual a o menor que 4 de forma que el anillo formado por la estructura (2) sea un anillo de 4, 5 o 6 miembros; y R es un grupo de formula (3), en la que * representa el punto de union a Z, L es un alquileno C2-6 de cadena lineal o ramificada y cada uno de R7 y R8 se selecciona independientemente entre H, alquilo C1-6, cicloalquilo C3-6, hidroxialquilo C1-6 o R7 y R8 forman junto con el átomo de N al que están unidos un heterociclo saturado de 4, 5, 6 o 7 miembros donde un átomo de C está opcionalmente reemplazado por N, O, S, SO o SO2 y donde dicho heterociclo saturado está opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre alquilo C1-4, alcoxi C1-4, alcoxi C1-4-alquilo C1-4, hidroxialquilo C1-4, hidroxi, C(O)Oalquilo C1-4, -C(O)-alquil C1-4-NH2, -C(O)NH2, halo, amino, alquil(C1-4)amino y [alquil C1-4]2amino; o R es un grupo de formula (4) en la que * representa el punto de union a Z, el anillo que contiene N es un heterociclo saturado de 4 a 7 miembros, n es un numero entero igual a 0, 1 o 2, y R9 representa un sustituyente seleccionado entre H, alquilo C1- 4, hidroxi(alquilo C1-6) y cicloalquilo C3-6; het1 se selecciona entre grupos heteroaromáticos monocíclicos o bicíclicos que tienen de 5 a 10 miembros en el anillo, que contienen 1, 2, 3 o 4 heteroátomo(s) seleccionado(s) entre N, O y S y het2 se selecciona entre grupos heteroaromáticos monocíclicos o bicíclicos que tienen de 5 a 10 miembros en el anillo, que contienen 1, 2, 3 o 4 heteroátomo(s) seleccionado(s) entre N, O y S.
ARP050101824A 2004-05-07 2005-05-05 Derivados de fenol y tiofenol 3 - o 4 - monosustituidos utiles como ligandos de h3; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurologicos e inflamatorios. AR048939A1 (es)

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