Patent ID: 6110939
Filing Date: 2000-08-29
Classification: A61P,C07D

Abstract:
A compound of formula ##STR61## 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;X is a covalent bond or a bivalent radical of formula --O--, --S--OR, --NR.sup.3 --;.dbd.Q is .dbd.O or .dbd.NR.sup.3 ;R.sup.1 is Ar.sup.1 l, Ar.sup.1 C.sub.1-6 alkyl or di(Ar.sup.1)C.sub.1-6 alkyl wherein the 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;L is a radical of formula ##STR62## wherein p is 0, 1 or 2;..... Y-- is a bivalent radical of formula --CH.sub.2 --, --CH(OH)--, --C(.dbd.O)--, --O--, --S--, --S(.dbd.O)--, --S(.dbd.O).sub.2 --, --NR.sup.3 --, --CH.sub.2 --NR.sup.3 -- or --C(.dbd.O)--NR.sup.3 --; or a trivalent radical of formula .dbd.CH--;--A.dbd.B-- is a bivalent radical of formula --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--;R.sup.3 independently is hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl or a radical of formula--Alk--R.sup.7 (c- 1)or--Alk--Z--R.sup.8 (c- 2);wherein Alk is C.sub.1-6 alkanediyl;Z is a bivalent radical of formula --O--, --S-- or --NR.sup.3 --;R.sup.7 is phenyl; phenyl substituted with 1 or 2 substituents selected from halo, C.sub.1-6 alkyl and C.sub.1-6 alkyloxy; furanyl; furanyl substituted with 1 or 2 substituents selected from C.sub.1-6 alkyl and hydroxyC.sub.1-6 alkyl; thienyl; thienyl substituted with 1 or 2 substituents selected from halo and C.sub.1-6 alkyl;oxazolyl; oxazolyl substituted with 1 or 2 C.sub.1-6 alkyl substituents;thiazolyl; thiazolyl substitued with 1 or 2 C.sub.1-6 alkyl substituents;R.sup.8 is C.sub.1-6 alkyl or C.sub.1-6 alkyl substituted with hydroxy, carboxyl or C.sub.1-6 alkyloxycarbonyl;R.sup.5 is hydrogen, halo, hydroxy or C.sub.1-6 alkyloxy;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 and haloC.sub.1-4 alkyloxy;Ar.sup.2 is naphtalenyl; 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 and isothiazolyl; or a bicyclic heterocycle selected from 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 and mono-, di- or tri(halo)methyl.