Patent ID: 6251894
Filing Date: 2001-06-26
Classification: A61P,C07D

Abstract:
A compound of formula ##STR27##a N-oxide form, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, whereinn is 0, 1 or 2;m is 1 or 2, provided that if m is 2, then n is 1;.dbd.Q is .dbd.O or .dbd.NR.sup.3 ;X is a covalent bond or a bivalent radical of formula --O--, --S--, --NR.sup.3 --;R.sup.1 is Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl or di(Ar.sup.1)C.sub.1-6 alkyl, wherein each C.sub.1-6 alkyl group is optionally substituted with hydroxy, C.sub.1-4 alkyloxy, oxo or a ketalized oxo substituent of formula --O--CH.sub.2 --CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --CH.sub.2 --O--;R.sup.2 is Ar.sup.2, Ar.sup.2 C.sub.1-6 alkyl, Het or HetC.sub.1-6 alkyl;R.sup.3 is hydrogen or C.sub.1-6 alkyl;L is a radical of formula ##STR28##wherein the dotted line is an optional bond;each --A--B-- independently is a bivalent radical of formula--Y--CR.sup.7.dbd.CH-- (b-1);or--CH.dbd.CR.sup.7 --Y-- (b-2);wherein each Y independently is a bivalent radical of formula --S--;each R.sup.7 independently is C.sub.1-6 alkyl; halo; ethenyl substituted with carboxyl or C.sub.1-6 alkyloxycarbonyl, hydroxyC.sub.1-6 alkyl; formyl; carboxyl or hydroxycarbonylC.sub.1-6 alkyl; orR.sup.7 is hydrogen in case --A--B-- is a radical of formula (b-1) or (b-2);each Z independently is Z.sup.1 or Z.sup.2 ;wherein Z.sup.1 is a bivalent radical of formula --CH.sub.2 --CH.sub.2 -- or --CH--CH--;Z.sup.2 is a bivalent radical of formula --CH.sub.2 --CHOH--, --CH.sub.2 --C(.dbd.O)-- or --CH.sub.2 --C(.dbd.NOH)--, provided that the --CH.sub.2 -- moiety of said bivalent radicals is connected to the nitrogen of the imidazole ring;each R.sup.4 independently is hydrogen; C.sub.1-6 alkyl; halo; ethenyl substituted with carboxyl or C.sub.1-6 alkyloxycarbonyl; C.sub.1-6 alkyl substituted with carboxyl or C.sub.1-6 alkyloxycarbonyl; hydroxyC.sub.1-6 alkyl: formyl or carboxyl;each R.sup.5 independently is hydrogen, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, Ar.sup.1 or halo; orR.sup.4 and R.sup.5 taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 ;each R.sup.6 is hydrogen, C.sub.1-6 alkyl or Ar.sup.1 C.sub.1-6 alkyl;Ar.sup.1 is phenyl; phenyl substituted with 1, 2 or 3 substituents each independently selected from halo, C.sub.1-4 alkyl, haloC.sub.1-4 alkyl, cyano, aminocarbonyl, C.sub.1-4 alkyloxy or haloC.sub.1-4 alkyloxy;Ar.sup.2 is naphthalenyl; phenyl; phenyl substituted with 1, 2 or 3 substituents each independently selected from hydroxy, halo, cyano, nitro, amino, mono- or di(C.sub.1-4 alkyl)amino, C.sub.1-4 alkyl, haloC.sub.1-4 alkyl, C.sub.1-4 alkyloxy, haloC.sub.1-4 alkyloxy, carboxyl, C.sub.1-4 alkyloxycarbonyl, aminocarbonyl and mono- or di(C.sub.1-4 alkyl) aminocarbonyl; andHet is a monocyclic heterocycle selected from pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyrazinyl and pyridazinyl, or a bicyclic heterocycle selected from quinolinyl, quinoxalinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzofuranyl and benzothienyl; each monocyclic and bicyclic heterocycle may optionally be substituted on a carbon atom by 1 or 2 substituents selected from halo, C.sub.1-4 alkyl or mono-, di- or tri(halo)methyl.