Patent ID: 6177432
Filing Date: 2001-01-23
Classification: A61P,C07D

Abstract:
A compound of formula (I) ##STR23##a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, whereinthe dotted line represents an optional bond;X is oxygen or sulfur;R.sup.1 and R.sup.2 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxycarbonyl, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl, Ar.sup.1 oxy, Ar.sup.1 C.sub.1-6 alkyloxy;R.sup.3 and R.sup.4 each independently are hydrogen, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, Ar.sup.1 oxy, C.sub.1-6 alkylthio, di(C.sub.1-6 alkyl)amino, trihalomethyl or trihalomethoxy;R.sup.5 is hydrogen, halo, C.sub.1-6 alkyl, cyano, haloC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, cyanoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkylthioC.sub.1-6 alkyl, aminocarbonylC.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonylC.sub.1-6 alkyl, C.sub.1-6 alkylcarbonylC.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyloxyC.sub.1-6 alkyl; or a radical of formula ##STR24##whereinR.sup.10 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyl, Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonylC.sub.1-6 alkyl, or a radical of formula --Alk--OR.sup.13 or --Alk--NR.sup.14 R.sup.15 ;R.sup.11 is hydrogen, C.sub.1-6 alkyl, Ar.sup.1 or Ar.sup.1 C.sub.1-6 alkyl;R.sup.12 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylaminocarbonyl, Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyl-C.sub.1-6 alkyl, Ar.sup.1 carbonyl, Ar.sup.1 C.sub.1-6 alkylcarbonyl, aminocarbonylcarbonyl, C.sub.1-6 alkyloxyC.sub.1-6 alkylcarbonyl, hydroxy, C.sub.1-6 alkyloxy, aminocarbonyl, di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkylcarbonyl, amino, C.sub.1-6 alkylamino, C.sub.1-6 alkylcarbonylamino, or a radical or formula --Alk--OR.sup.13 or --Alk--NR.sup.14 R.sup.15 ; wherein Alk is C.sub.1-6 alkanediyl;R.sup.13 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyl, hydroxyC.sub.1-6 alkyl, Ar.sup.1 or Ar.sup.1 C.sub.1-6 alkyl;R.sup.14 is hydrogen, C.sub.1-6 alkyl, Ar.sup.1 or Ar.sup.1 C.sub.1-6 alkyl;R.sup.15 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyl, Ar.sup.1 or Ar.sup.1 C.sub.1-6 alkyl;R.sup.6 is a radical of formula ##STR25##whereinR.sup.16 is hydrogen, halo, Ar.sup.1, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylthioC.sub.1-6 alkyl, C.sub.1-6 alkylS(O)C.sub.1-6 alkyl or C.sub.1-6 alkylS(O).sub.2 C.sub.1-6 alkyl;R.sup.17 is hydrogen, C.sub.1-6 alkyl or di(C.sub.1-4 alkyl)aminosulfonyl;R.sup.7 is hydrogen or C.sub.1-6 alkyl provided that the dotted line does not represent a bond;R.sup.8 is hydrogen, C.sub.1-6 alkyl or Ar.sup.2 CH.sub.2 or Het.sup.1 CH.sub.2 ;R.sup.9 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or halo; orR.sup.8 and R.sup.9 taken together to form a bivalent radical of formula ##STR26##Ar.sup.1 is phenyl; or phenyl substituted with 1 or 2 substituents each independently selected from halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or trifluoromethyl;Ar.sup.2 is phenyl; or phenyl substituted with 1 or 2 substituents each independently selected from halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or trifluoromethyl; andHet.sup.1 is pyridinyl; pyridinyl substituted with 1 or 2 substituents each independently selected from halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or trifluoromethyl.