Imidazolilo amide or ester derivatives, Pharmaceutical compositions containing Same, Preparation Process and use as Medicines for the treatment of inflammatory diseases, among others.

摘要

Item 1: a compound whose characteristic is the response formula (1),wherein: A is C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl, cyano, C 1-6 nitroalkyl, nitro, S (O) C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl -6, C3-7 cycloalkyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl-C1-6 alkyl, C1-6 haloalkyl, C1-6 alkyl-C1-6 thioalkyl, C1-6 thioalkyl, C1-6alkylOC1-6alkyl, C1 -6alkIOC1-6alkylOC1-6alkyl, C1-6aIquiOC1-6alkylO, C1-6alkyl C (O) C1-6alkyl, C1-6alkylIC (O)C1-6 alquiIC (O) OC1-6alquilo C1-6alquilC (O) O C1-6alquiIOC (O) C1-6alquilo C1-6aIquilOC (O)Temporary, specialNr5r6c1-6 tar, nr5r6, nr5r6c (o) C1-6 tar, nr5r6c (o),Nr5r6oc (o) C1-6 tar, nr5r6oc (o),R7NH, C5-10arylC1-3alkyl, C5-10aryl, C5-10heteroarylC1-3alkyl, C5-10heteroaryl, wherein the cycloalkyl, heterocycloalkyl, aryl or heteroaryl may be optionally substituted by one or more substituents independently selected from halo, cyano, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4haloalkyl, Ci-4a alkylOC (O),C1-4alkylOC1-4alkyl, C1-4alkyl (O) 2 and C1-4haloalkyl, and Rx is hydrogen, or A together with Rx forms a 5 or 6 membered heterocyclic ring having one or more heteroatoms independently selected from O, N and S; R1 and R1a are independently selected from hydrogen, C1-4alkyl, C1-4hydroxyalkyl, C1-4alkylC1-4alkyl, C1-4alkylSC1-4alkyl and C1-4haloalkyl; R2 is hydrogen or C1-4 alkyl; R3 is C5-10aryl, C5-10arylC1-4alkyl, C5-10arylO, C5-10ariIOC1-4alkyl or C5-10heteroaryl, which may be optionally substituted by one or more substituents independently selected from B; B is C1-3 hydroxyalkyl, hydroxy, C1-4alkyl, C1-4alkoxy,14c14c1-hc (or c14c4c4c4c4c14C1-4alquilC (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) OC1-4alkyl, NR8R9C (O) O, R9C (O) R8NC1-4alkyl, R9C (O) R8NH, C1-4alkylNH, C1-4alkyl (C) NH, C1-4alkylC (O) OC1-4alkylNH, C1-4alkylC (O) ONH, C1-4alkylC (O) C1-4aIQUINH, C1-4aCylC (O) NH, NR8R9S (O) nC1-4alkyl or NR8R9S (O) n; n is 1 or 2; R4 is hydrogen, hydroxy, halo, C1-4alkyl or C1-4 haloalkyl; W is hydrogen, or phenyl, C1-4alkyl, C3-7cycloalkyl, thienyl, isoxazolyl, pyrazolyl, pyridinyl, pyridazinyl or pyrimidinyl all of which are optionally substituted with one or more substituents independently selected from C1-3hydroxyalkyl, hydroxy, C1- 4alkyl, C1-4alkoxy, C1-4alkylC1-4thioalkyl, C1-4thioalkyl, C3-6cycloalkylC1-4thioalkyl,C11-1-1, 1-1-1 (o) c1-4oquilo, c1-4oquilc (o),C1-4alquilC (O) OC1-4alquilo C1-4alquilC (O) O C1-4alquilOC (O) C1-4alquilo C1-4aIquilOC (O)Nr10r11c1-4 rental, nr10r11, nr10r11c (o) C1-4 rental, nr10r11c (o),N10r11c (o) oc1-4, n10r11c (o) O, n10r11oc (o) C1-4, n10r11oc (o),Or nnnnnnn1 s, s (o) n, NH or nc1-4 tar; hydrogen, halogen, c1-4oquilo, c1-4oxi, c1-4tioalquilo, c1-4oquilo, C-4 halogenated tar, nitro, cyanogen, hydrogen, r12c (o),R12OC (O)R12C (O) O S (O) nC1-4alquilo R12R13NS (O) n benciloxi imidazolilo C1-4alquilNHC (O)No. 12r13c (o)- hc-hc-hc-hcC1-6 tar (o),C5-10 heteroarylC1-3alkyl, C5-10heteroaryl, C5-10arylC1-3alkyl, C5-10aryl, C3-6cycloalkylC1-3alkyl or C3-6cycloalkyl; or a salt acceptable for pharmaceutical use thereof; A is C1-6alkyl, C1-6hydroxyalkyl, C1-6cyanoalkyl, cyano, C1- nitroalkyl, nitro, S (O) nC1-6alkyl, C1-6alkoxy, C3-7cycloalkylC1-6alkyl, C3-7cycloalkyl, C3-7heterocycloalkyl, cycloalkyl- 7-heterocycloalkylC1-6alkyl, C1-6haloalkyl, C1-6alkylC1- 6thioalkyl, C1-6thioalkyl, C1-6alkylOC1-6alkyl, C1-6aIQUOC1-6alkyl1C1-6alkyl, C1-6a 6 alkyl C (O),C 6aIquiIC (O) OC1-6alquilo C1-6alquiIC (O) O C1-6alquiIOC (O) C1-6alquilo C1-6alquilOC (O)Temporary, specialNr5r6c1-6 tar, nr5r6, nr5r6c (o) C1-6 tar, nr5r6c (o),Nr5r6oc (o) C1-6 tar, nr5r6oc (o),R7NH, C5-10arylC1-3alkyl, C5-10aryl, C5-10heteroarylC1-3alkyl, C5-10heteroaryl, wherein the cycloalkyl, heterocycloalkyl, aryl or heteroaryl may be optionally substituted by one or more substituents independently selected from halo, cyano, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4haloalkyl, C1-4alkylIOC (O),C1-4aiCIOC1-4alkyl, C1-4alkyl (O) 2 and C1-4haloalkyl, and Rx is hydrogen, or A together with Rx forms a 5- or 6-membered heterocyclic ring having one or more heteroatoms independently selected from O, N and S; R1 and R1a are independently selected from a bond, hydrogen, oxy, C1-4a alkyl, C1-4hydroxyalkyl, C1-4aIQUIOC1-4alkyl, C1-4alkyISC1-4alkyl and C1-4haloalkyl; R2 is hydrogen or C1-4 alkyl; R3 is C5-10aryl, C5-10arylC1-4alkyl, C5-10arylO, C5-10arylOC1-4alkyl or C5-10heteroaryl, which may be optionally substituted by one or more substituents independently selected from B; B is C1-3hydroxyalkyl, hydroxy,14c14c14c14c14c14c14c14c14c14c14-4, C1-4, 1, 1C1-4alquilC (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) OC1-4alkyl, NR8R9C (O) O, R9C (O) R8NC1-4alkyl, R9C (O) R8NH, C1-4alkylNH, C1-4alkylOC (O) NH, C1-4alkylC (O) OC1-4alkylNH, C1-4aC1C (O) ONH, C1-4alkylC (O) C1-4alkylNH, C1-4alkylIC (O) NH, NR8R9S (O) nC1-4alkyl or NR8R9S (O) n; n is 1 or 2; R4 is hydrogen, hydroxy, halo, C1-4alkyl or C1-4 haloalkyl; W is hydrogen, or phenyl, C1-4alkyl, C3-7cycloalkyl, thienyl, isoxazolyl, pyrazolyl, pyridinyl, pyridazinyl or pyrimidinyl all of which are optionally substituted with one or more substituents independently selected from C1-3 hydroxyalkyl, hydroxy, C1 - 4alkyl, C1-4alkoxy, C1-4alkylC1-4thioalkyl, C1-4thioalkyl, C3-6cycloalkylC1-4thioalkyl,11-4c11, any c11-4c11-4c11-4c11 c1-4aquilc (o) c1-4aquilc (o),C1-4alquilC (O) OC1-4alquilo C1-4alquilC (O) O C1-4alquiIOC (O) C1-4alquilo C1- 4alquilOC (C)Nr10r11c1-4 rental, nr10r11, nr10r11c (o) C1-4 rental, nr10r11c (o),Nr10r11c (o) oc1-4aiquilo, nr10r11c (o) O, nr10r11oc (o) C1-4 tar, nr10r11oc (o),R11C (O) R10NC1-4alkyl, R11C (O) R10NH, C1-4alkylOC (O) C1-4alkylNH, C1-4alkylOC (O) NH, C1-4alkylC (O) OC1-4alkylNH, C1-4alkylC (O) ONH, C1-4alkylC (O) C1-4alkylNH, C1-4alkylC (O) NH, NR10R11S (O) nC1-4alkyl or NR10R11S (O) n; X is CH2, O, S, S (O) n, NH or NC1-4 alkyl; Y is hydrogen, halo, C1-4alkyl, C1-4alkoxy, C1-4thioalkyl, C1-4haloalkyl, C1-4 haloalkylO, nitro, cyano, hydroxy, R12C (O),R12OC (O)R12C (O) O S (O) nC1-4alquilo R12R13NS (O) n benciloxi imidazolilo C1-4alquilNHC (O)No. 12r13c (o)C1-4aiquilc (o) NH or nr12r13; Z is o or s; R5, R6, R8, R9, R10 R11, R12 and R13 are independently selected from hydrogen, c1-6aiquic (o),NHR7C (O) and C1-5alkyl; and R7 is hydrogen, C1-6alkyl, C1-6aC1C (O) OC1-3alkyl, C1-6alkylC (O) O, C1-6alkIOC (O) C1-3alkyl, C1-6alkIOC (O),C1-6 tar (o),C5-10 heterosexual 1-3, c5-10 heterosexual, c5-10arilc1-3aquilo, c5-10arilo, c3-6cycleoquilc1-3aquilo or c3-6cycleoquil; or acceptable salt for drug use.