| 摘要 |
This invention concerns the compounds of formula (I) a prodrug, a N-oxide, a n addition salt, a quaternary amine or a stereochemically isomeric form thereo f wherein R1 is hydrogen, C1-6alkyl, halo, formyl, carboxyl, C1- 6alkyloxycarbonyl, C1-6alkylcarbonyl, N(R3R4)C(=O)-, N(R3R4)C(=O)N(R5)-, ethenyl substituted with carboxyl or C1-6alkyloxycarbonyl, or C1-6alkyl substituted with hydroxy, carboxyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, N(R3R4)C(=O)-, C1-6alkylC(=O)N(R5)-, C1-6alkylS(=O)2N(R5)- or N(R3R4)C(=O)N(R5)- wherein each R3 and each R4 independently are hydrogen or C1-4alkyl, and R5 is hydrogen or hydroxy; R2 is hydrogen, C1-6alkyl, hydroxy C1- 6alkyl, C1-6alkyloxyC1-6alkyl, N(R3R4)C(=O)-, aryl or halo; n is 1 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 C1-6alkyl, halo, hydroxy, C1-6alkyloxy, ethenyl substituted with carboxyl or C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, formyl, carboxyl or hydroxycarbonylC 1- 6alkyl, and each Y independently is a bivalent radical of formula -O-, -S- o r - NR7-, wherein R7 is hydrogen, C1-6alkyl or C1-6alkylcarbonyl; Z is a bivalen t radical of formula -(CH2)p-, -CH=CH-, -CH2-CHOH-, -CH2-O-, -CH2-C(=O), or -C H2- 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; C1-6alkyl; C2-6alkenyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; C 1- 6alkyl substituted with hydroxy, carboxyl, C1-6alkyloxy, C1-6alkyloxycarbony l, aryl, aryloxy, cyano or R8HN- wherein R8 is hydrogen, C1-6alkyl, C1- 6alkyloxycarbonyl, C1-6alkylcarbonyl; or L represents a radical of formula - Alk-Y-Het1, -Alk-NH-CO-Het2 or -Alk-Het3 wherein Alk represents C1- 4alkanediyl; Y represents O, S or NH; Het1, Het2 and Het3 each represent an optionally substituted heterocycle; for use as a medicine.
|
