| 摘要 |
The invention concerns the applicable in medicine compounds of formula a prodrug, a N-oxide, an addition salt, and quaternary amine or a stereochemically isomeric form thereof therein R1 is hydrogen, C1-C6 alkyl, halo, formyl, carboxyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, N(R3R4)C(=O)-, N(R3R4)C(=O)N(R5)-, ethenyl substituted with carboxyl or C1-6 alkyloxycarbonyl, or C1-6 alkyl substituted with hydroxy, carboxyl, C1-6 alkyloxy, C1-6alkyloxycarnonyl, N(R3R4)C(=O)-, C1-6 alkylC(=O)N(R5)-, C1-6 alkylS(=O)2N(R5)-, or N(R3R4)C(=O))N(R5)-, wherein each R3 and each R4 independently are hydrogen or C1-4 alkyl and R5 is hydrogen or hydroxy; R2 is hydrogen, C1-6 alkyl, hydroxyC1-6 alkyl, C1-6 alkyloxyC1-6alkyl, N(R3R4)C(=O)-, aryl or halo; n is1 or 2; -A-B- represents a bivalent radical of formula -Y-CH=CH-, -CH=CH-Y-, or -CH=CH-CH=CH-, wherein each hydrogen atom may independently be replaced by R6 wherein R6 is C1-4 alkyl, halo, hydroxy, C1-6 alkoxy, ethenyl substituted wi5th carboxyl or C1-6 alkyloxycarbonyl or C1-6 alkyloxycarbonyl, hydroxy C1-6 alkyl, formyl, carboxyl or hydroxycarbonyl C1-6 alkyl, and each Y independently is a bivalent radical of formula -O-, -S-, or NR7-, wherein R7 is hydrogen, C1-6 alkyl or C1-6 alkylcarbonyl; Z is a bivalent radical of formula -(CH2)p-, -CH=CH-, -CH2-CHOH-, -CH2-O-, -CH2-O-, -CH2-C(=O), or -CH2-C(=NOH)-, provided that the bivalent radicals are connected to the nitrogen of the imidazole ring via their -CH2- moiety; and wherein p is 1, 2, 3 or 4; L is hydrogen; C-16 alkyl; C2-6 aslkenyl;C1-6 alkylcarbonyl; C1-6 alkyloxycarbonyl; C1-6 alkyl substituted with hydroxy, carboxyl, C1-6 alkyloxy, C1-6 alkyloxycabonyl, aryl, aryloxy, cyano or R8NH- wherein R8 is hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, C1-6 alkylcarbonyl; or L represents a radical of formula -Alk-Y-Het1, -Alk-NH-CO-Het2 or -Alk-Het3 wherein Alk represents C1-4 alkanediyl; Y represents O, S or NH; Het1 and Het2each represent an optionally substituted heterocycle; for use as a medicine. 15 claims, 1 figure |
