AR064505A1 - Derivados ester o amida de imidazolilo, composiciones farmaceuticas que los comprenden,proceso de preparacion, y usos como medicamentos para el tratamiento de enfermedades inflamatorias, entre otras. - Google Patents

Derivados ester o amida de imidazolilo, composiciones farmaceuticas que los comprenden,proceso de preparacion, y usos como medicamentos para el tratamiento de enfermedades inflamatorias, entre otras.

Info

Publication number
AR064505A1
AR064505A1 ARP070105870A ARP070105870A AR064505A1 AR 064505 A1 AR064505 A1 AR 064505A1 AR P070105870 A ARP070105870 A AR P070105870A AR P070105870 A ARP070105870 A AR P070105870A AR 064505 A1 AR064505 A1 AR 064505A1
Authority
AR
Argentina
Prior art keywords
4alkyl
6alkyl
4alkylc
3alkyl
hydrogen
Prior art date
Application number
ARP070105870A
Other languages
English (en)
Inventor
Dahmen J
Thomas Hansson
Krister Henriksson
Hemmerling M
Balint Gabos
Markus Berger
Taflin C
Mckerrecher D
Matti Lepistoe
Af Rosenschoeld Magnus Munck
Ivanova C
Rehwinkel Hartmut
Bjoern Eriksson
Nilsson S
Original Assignee
Bayer Schering Pharma Ag
Astrazeneca Ab
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
Application filed by Bayer Schering Pharma Ag, Astrazeneca Ab filed Critical Bayer Schering Pharma Ag
Publication of AR064505A1 publication Critical patent/AR064505A1/es

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  • Ophthalmology & Optometry (AREA)

Abstract

Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1), en donde: A es alquilo C1-6, hidroxialquilo C1-6, cianoalquilo C1-6, ciano, nitroalquilo C1-6, nitro, S(O)nalquilo C1-6, alcoxi C1-6, cicloalquil C3-7-alquiIo C1-6, cicloalquilo C3-7, heterocicloalquilo C3-7, heterocicloalquilo C3-7-alquilo C1-6, haloalquilo C1-6, alquiI C1-6-tioalquilo C1-6, tioalquilo C1-6, C1-6alqulOC1-6alquilo, C1-6alquiIOC1-6alquilOC1-6alquilo, C1-6aIquiOC1-6alquilO, C1-6 alquilC(O)C1-6 alquilo, C1-6 aIquiIC(O), C1-6 alquiIC(O)OC1-6alquilo, C1-6alquilC(O)O, C1-6alquiIOC(O)C1-6alquilo, C1-6aIquilOC(O), HOC(O), NR5R6C1-6alquilo, NR5R6, NR5R6C(O)C1-6alquilo, NR5R6C(O), NR5R6OC(O)C1-6alquilo, NR5R6OC(O), R7NH, C5-10arilC1-3alquiIo, C5- 10arilo, C5-10heteroarilC1-3alquilo, C5-10heteroarilo, en donde el cicloalquilo, heterocicloalquilo, arilo o heteroarilo puede estar opcionalmente sustituido por uno o más sustituyentes seleccionados en forma independiente entre halo, ciano, hidroxi, C1-4alquilo, C1-4alcoxi, C1-4haloalquilo, Ci-4aIquilOC(O), C1-4alquilOC1-4alquilo, C1-4alquiIS(O)2 y C1-4haloalquilO, y Rx es hidrogeno, o A forma junto con Rx un anillo heterocíclico de 5 o 6 miembros que tiene uno o más heteroátomos seleccionados en forma independiente entre O, N y S; R1 y R1a se seleccionan en forma independiente entre hidrogeno, C1-4alquilo, C1-4hidroxialquilo, C1-4alquilOC1-4alquilo, C1-4alquilSC1-4alquilo y C1-4haloalquilo; R2 es hidrogeno o C1-4 alquilo; R3 es C5-10arilo, C5-10arilC1-4alquilo, C5-10arilO, C5-10ariIOC1-4alquilo o C5-10heteroarilo, que puede estar opcionalmente sustituido por uno o más sustituyentes seleccionados en forma independiente entre B; B es C1-3hidroxialquilo, hidroxi, C1- 4alquilo, C1-4alcoxi, C1-4alquilC1-4tioalquilo, C1-4tioalquilo, C3-6cicloalquilC1-4tioalquilo, C3-6cicloalquilS, C1-3alquilS(O)nC1-4alquilo, C1-3alquilS(O)n, C1-4haloalquilo, C1-4haloalquilO, halo, nitro, ciano, C1-4alquilOC1-4alquilOC1-4alquilo, C1- 4alquilC(O)C1-4alquilo, C1-4aIquilC(O), C1-4alquilC(O)OC1-4aIquilo, C1-4alquilC(O)O, C1-4alquiIOC(O)C1-4alquilo, C1-4alquilOC(O), NR8R9C1-4alquilo, NR8R9, NR8R9C(O)C1-4alquilo, NR8R9C(O), NR8R9OC(O)C1-4alquilo, NR8R9OC(O), NR8R9C(O)OC1-4alquilo, NR8R9C(O)O, R9C(O)R8NC1-4alquilo, R9C(O)R8NH, C1-4alquilNH, C1- 4aIquilOC(C)NH, C1-4alquilC(O)OC1-4alquilNH, C1-4alquilC(O)ONH, C1-4alquilC(O)C1-4aIquiINH, C1-4aIquilC(O)NH, NR8R9S(O)nC1-4alquiIo o NR8R9S(O)n; n es 1 o 2; R4 es hidrogeno, hidroxi, halo, C1-4alquilo o C1-4 haloalquilo; W es hidrogeno, o fenilo, C1-4alquilo, C3-7cicloalquilo, tienilo, isoxazolilo, pirazolilo, piridinilo, piridazinilo o pirimidinilo todos los cuales están opcionalmente sustituidos con uno o más sustituyentes seleccionados en forma independiente entre C1-3hidroxialquilo, hidroxi, C1-4alquilo, C1-4alcoxi, C1-4alquilC1-4tioalquilo, C1- 4tioalquilo, C3-6cicloalquilC1-4tioalquilo, C3-6cicloalquilS, C3-6cicloalquilo, C3-6cicloalquilC1-4alquilo, C3- 6heterocicloalquilo, C3-6heterocicloalquilC1-4alquilo, C1-4alquilS(O)nC1-4alquilo, C1-4alquilS(O)n, C1-4haloalquilo, C1-4haloalquilO, halo, nitro, ciano, C1-4alquilOC1-4alquilo, C1-4alquilOC1-4alquilOC1-4alquilo, C1-4alquiIC(O)C1-4alquilo, C1- 4alquilC(O), C1-4alquilC(O)OC1-4alquilo, C1-4alquilC(O)O, C1-4alquilOC(O)C1-4alquilo, C1-4aIquilOC(O), NR10R11C1-4alquilo, NR10R11, NR10R11C(O)C1-4alquilo, NR10R11C(O), NR10R11C(O)OC1-4alquilo, NR10R11C(O)O, NR10R11OC(O)C1-4alquilo, NR10R11OC(O), R11C(O)R10NC1-4alquilo, R11C(O)R10NH, C1-4alquilOC(O)C1-4alquilNH, C1-4alquilOC(O)NH, C1-4aIquilC(O)OC1-4alquilNH, C1-4alquiIC(O)ONH, C1-4alquilC(O)C1-4alquilNH, C1- 4alquiIC(O)NH, NR10R11S(O)nC1-4alquilo o NR10R11S(O)n; X es CH2, O, S, S(O)n, NH o NC1-4 alquilo; Y es hidrogeno, halo, C1-4alquilo, C1-4alcoxi, C1-4tioalquilo, C1-4haloalquilo, C-4 haloalquilO, nitro, ciano, hidroxi, R12C(O), R12OC(O), R12C(O)O, S(O)nC1-4alquilo, R12R13NS(O)n, benciloxi, imidazolilo, C1-4alquilNHC(O), NR12R13C(O), C1-4alquilC(O)NH o NR12R13; Z es O o S; R5, R6, R8, R9, R10 R11, R12 y R13 se seleccionan en forma independiente entre hidrogeno, C1-6alquilC(O) y C1-6alquilo; y R7 es C1-6alquilo, C1-6alquilC(O)OC1-3alquilo, C1-6alquilC(O)O, C1- 6alquilOC(O)C1-3alquilo, C1-6alquilOC(O), C1-6alquilC(O), C5-10heteroarilC1-3alquilo, C5-10heteroarilo, C5-10arilC1-3alquilo, C5-10arilo, C3-6cicloalquilC1-3alquilo o C3-6cicloalquilo; o una sal aceptable para uso farmacéutico del mismo; A es C1- 6alquilo, C1-6hidroxialquilo, C1-6cianoalquilo, ciano, C1-6nitroalquilo, nitro, S(O)nC1-6alquilo, C1-6alcoxi, C3-7cicloalquilC1-6alquilo, C3-7cicloalquilo, C3-7heterocicloalquilo, C3-7heterocicloalquiC1-6alquilo, C1-6haloalquilo, C1-6alquilC1- 6tioalquilo, C1-6tioalquilo, C1-6alquilOC1-6alquilo, C1-6aIquilOC1-6alquilOC1-6alquilo, C1-6aIquilOC1-6aIquilO, C1-6alquilC(O)C1-6alquilo, C1-6alquilC(O), C 6aIquiIC(O)OC1-6alquilo, C1-6alquiIC(O)O, C1-6alquiIOC(O)C1-6alquilo, C1-6alquilOC(O), HOC(O), NR5R6C1-6alquilo, NR5R6, NR5R6C(O)C1-6alquilo, NR5R6C(O), NR5R6OC(O)C1-6alquilo, NR5R6OC(O), R7NH, C5-10arilC1-3alquilo, C5-10arilo, C5-10heteroarilC1-3alquilo, C5-10heteroarilo, en donde el cicloalquilo, heterocicloalquilo, arilo o heteroarilo puede estar opcionalmente sustituido por uno o más sustituyentes seleccionados en forma independiente entre halo, ciano, hidroxi, C1-4alquilo, C1-4alcoxi, C1-4haloalquilo, C1-4alquiIOC(O), C1- 4aIquiIOC1-4alquilo, C1-4alquiIS(O)2 y C1- 4haloalquilO, y Rx es hidrogeno, o A forma junto con Rx un anillo heterocíclico de 5 o 6 miembros que tiene uno o más heteroátomos seleccionados en forma independiente entre O, N y S; R1 y R1a se seleccionan en forma independiente entre un enlace, hidrogeno, oxi, C1-4aIquilo, C1-4hidroxialquilo, C1-4aIquiIOC1-4alquilo, C1-4alquiISC1-4alquilo y C1-4haloalquilo; R2 es hidrogeno o C1-4 alquilo; R3 es C5-10arilo, C5-10arilC1-4alquilo, C5-10arilO, C5-10arilOC1-4alquilo o C5-10heteroarilo, que puede estar opcionalmente sustituido por uno o más sustituyentes seleccionados en forma independiente entre B; B es C1-3hidroxialquilo, hidroxi, C1-4alquilo, C1-4alcoxi, C1-4alquilC1-4tioalquilo, C1-4tioalquilo, C3-6cicloalquilC1-4tioalquilo, C3- 6cicloalquilS, C1-3alquilS(O)nC1-4alquilo, C1-3alquilS(O)n, C1-4haloalquilo, C1-4haloalquilO, halo, nitro, ciano, C1-4alquiIOC1-4alquilOC1-4alquilo, C1-4alquilC(O)C1-4alquilo, C1-4 alquiIC(O), C1-4alquilC(O)OC1-4alquilo, C1-4alquiIC(O)O, C1- 4alquilOC(O)C1-4alquilo, C1-4aIquilOC(O), NR8R9C1-4alquilo, NR8R9, NR8R9C(O)C1-4alquilo, NR8R9C(O), NR8R9OC(O)C1-4alquilo, NR8R9OC(O), NR8R9C(O)OC1-4alquilo, NR8R9C(O)O, R9C(O)R8NC1-4alquilo, R9C(O)R8NH, C1-4alquilNH, C1-4alquilOC(O)NH, C1- 4alquilC(O)OC1-4alquilNH, C1-4aIquilC(O)ONH, C1-4alquilC(O)C1-4alquilNH, C1-4alquiIC(O)NH, NR8R9S(O)nC1-4alquilo o NR8R9S(O)n; n es 1 o 2; R4 es hidrogeno, hidroxi, halo, C1-4alquiIo o C1-4 haloalquilo; W es hidrogeno, o fenilo, C1-4alquilo, C3- 7cicloalquilo, tienilo, isoxazolilo, pirazolilo, piridinilo, piridazinilo o pirimidinilo todos los cuales están opcionalmente sustituidos con uno o más sustituyentes seleccionados en forma independiente entre C1-3 hidroxialquilo, hidroxi, C1- 4alquiIo, C1-4alcoxi, C1-4alquilC1-4tioalquilo, C1-4tioalquilo, C3-6cicloalquilC1-4tioalquilo, C3-6cicloalquilS, C3-6cicloalquilo, C3-6cicloalquilC1-4alquilo, C3-6heterocicloalquilo, C3-6heterocicloalquilC1-4alquilo, C1-4alquilS(O)nC1-4alquilo, C1- 4alquilS(O)n, C1-4haloalquilo, C1-4haloalquilO, halo, nitro, ciano, C1-4alquilOC1-4alquilo, C1-4alquiíOC1-4alquilOC1-4alquilo, C1-4alquilC(O)C1-4alquiIo, C1-4aIquilC(O), C1-4alquilC(O)OC1-4alquilo, C1-4alquilC(O)O, C1-4alquiIOC(O)C1-4alquilo, C1- 4alquilOC(C), NR10R11C1-4alquilo, NR10R11, NR10R11C(O)C1-4alquilo, NR10R11C(O), NR10R11C(O)OC1-4aIquilo, NR10R11C(O)O, NR10R11OC(O)C1-4alquilo, NR10R11OC(O), R11C(O)R10NC1-4alquilo, R11C(O)R10NH, C1-4alquilOC(O)C1-4alquilNH, C1-4alquilOC(O)NH, C1- 4aIquilC(O)OC1-4alquilNH, C1-4alquilC(O)ONH, C1-4alquilC(O)C1-4alquilNH, C1-4alquilC(O)NH, NR10R11S(O)nC1-4alquilo o NR10R11S(O)n; X es CH2, O, S, S(O)n, NH o NC1-4 alquilo; Y es hidrogeno, halo, C1-4alquilo, C1-4alcoxi, C1-4tioalquilo, C1- 4haloalquilo, C1-4 haloalquilO, nitro, ciano, hidroxi, R12C(O), R12OC(O), R12C(O)O, S(O)nC1-4alquilo, R12R13NS(O)n, benciloxi, imidazolilo, C1-4alquilNHC(O), NR12R13C(O), C1-4aIquilC(O)NH o NR12R13; Z es O o S; R5, R6, R8, R9, R10 R11, R12 y R13se seleccionan en forma independiente entre hidrogeno, C1-6aIquiIC(O), NHR7C(O) y C1-5alquilo; y R7 es hidrogeno, C1-6alquilo, C1-6aIquilC(O)OC1-3alquilo, C1-6alquilC(O)O, C1-6alquiIOC(O)C1-3alquilo, C1-6alquiIOC(O), C1-6alquilC(O), C5-10heteroarilC1- 3alquilo, C5-10heteroarilo, C5-10arilC1-3alquilo, C5-10arilo, C3-6cicloalquilC1-3alquilo o C3-6cicloalquilo; o una sal aceptable para uso farmacéutico del mismo.
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