Patent ID: 6218381
Filing Date: 2001-04-17
Classification: A61P,C07D

Abstract:
A compound of formula (I) ##STR39##a N-oxide form, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, whereinthe dotted line is an optional bond;n is 1 or 2;R.sup.1 is hydrogen; halo; formyl; C.sub.1-4 alkyl; C.sub.1-4 alkyl substituted with 1 or 2 substituents each independently selected from hydroxy, C.sub.1-4 alkyloxy, C.sub.1-4 alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula--X--CO--OR.sup.5 (a-1);--X--CO--NR.sup.6 R.sup.7 (a-2);or--X--CO--R.sup.10 (a-3);wherein --X-- is a direct bond, C.sub.1-4 alkanediyl or C.sub.2-6 alkenediyl;R.sup.5 is hydrogen; C.sub.1-12 alkyl; Ar; Het; C.sub.1-6 alkyl substituted with C.sub.1-4 alkoxyloxy, C.sub.1-4 alkyloxycarbonylC.sub.1-4 alkyloxy, Ar or Het;R.sup.6 and R.sup.7 each independently are hydrogen or C.sub.1-4 alkyl;R.sup.10 is imidazolyl, thiazolyl or oxazolyl;R.sup.2 is hydrogen, halo, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, C.sub.1-4 alkyloxycarbonyl, carboxyl, formyl or phenyl;R.sup.3 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy;R.sup.4 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy or haloC.sub.1-4 alkyl;Z is Z.sup.1 or Z.sup.2 ; whereinZ.sup.1 is a bivalent radical of formula --CH.sub.2 --, --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; provided that when the dotted line is a bond, then Z.sup.1 is other than --CH.sub.2 --;Z.sup.2 is a bivalent radical of formula --CHOH--CH.sub.2 --, --O--CH.sub.2 --, --C(.dbd.O)--CH.sub.2 -- or --C(.dbd.NOH)--CH.sub.2 --;--A--B-- is a bivalent radical of formula--Y--CR.sup.8.dbd.CH-- (b-1);--CH.dbd.CR.sup.8 --Y-- (b-2);--CH.dbd.CR.sup.8 --CH.dbd.CH-- (b-3);--CH.dbd.CH--CR.sup.8.dbd.CH-- (b-4);or--CH.dbd.CH--CH.dbd.CR.sup.8 -- (b-5);wherein each R.sup.8 independently is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxyC.sub.1-4 alkyl, hydroxycarbonylC.sub.1-4 alkyl, formyl, carboxyl, ethenyl substituted with carboxyl, or ethenyl substituted with C.sub.1-4 alkyloxycarbonyl;each Y independently is a bivalent radical of formula --O--, --S-- or --NR.sup.9 --;wherein R.sup.9 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkylcarbonyl;--A.sup.1 -- is a direct bond; C.sub.1-6 alkanediyl; C.sub.1-6 alkanediyl-oxy-C.sub.1-6 alkanediyl; C.sub.1-6 alkanediyloxy; carbonyl; C.sub.1-6 alkanediylcarbonyl; C.sub.1-6 alkanediyloxy substituted with hydroxy; or C.sub.1-6 alkanediyl substituted with hydroxy or .dbd.NOH;--A.sup.2 -- is a direct bond or C.sub.1-6 alkanediyl;Q is optionally substituted phenyl, naphthalenyl, pyridinyl or quinolinyl wherein the substituents are halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy;Ar is phenyl or phenyl substituted with 1, 2 or 3 substituents each independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy;Het is furanyl; furanyl substituted with C.sub.1-4 alkyl, C.sub.1-4 alkyloxy or hydroxyC.sub.1-4 alkyl; oxazolyl; oxazolyl substituted with C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; or quinolinyl, with the proviso that Q is other than unsubstituted phenyl when A.sup.1 is carbonyl.