Patent ID: 6323235
Filing Date: 2001-11-27
Classification: C07D

Abstract:
A benzene-condensed heterocyclic derivative of the formula (I): ##STR262##wherein R.sup.1 is --X--(CH.sub.2).sub.n COOR.sup.3 wherein X is --O--, --S--, or --CH.sub.2 --, R.sup.3 is hydrogen, C.sub.1 -C.sub.5 lower alkyl, or an atom or group which gives a pharmaceutically acceptable salt, and n is an integer of 1 to 3;R.sup.2 is --NR.sup.4 --CR.sup.5 R.sup.6 --CHR.sup.7 --whereinR.sup.4 is --(CH.sub.2).sub.m --Y--R.sup.8 wherein m is an integer of 1 to 4,Y is1) --O--,2) --CH.sub.2 --,3) --S(O).sub.p -- and p is an integer of 0 to 2,4) --CO--,5) --CH(OH)--,6) --NR.sup.9 SO.sub.2 --,7) --NR.sup.9 CO--,8) --CONR.sup.9,9) --NR.sup.9 --,10) --O--N.dbd.CR.sup.9 --, wherein R.sup.9 isa) hydrogen,b) C.sub.1 -C.sub.5 alkyl,c) phenyl or substituted phenyl,d) C.sub.1 -C.sub.5 alkyl substituted with a phenyl or with a substituted phenyl group, or11) the group represented by the formula (IIa) and (IIb) ##STR263##R.sup.8 is1) phenyl, thienyl, furyl, naphthyl or C.sub.3 -C.sub.8 cycloalkyl,2) substituted phenyl, substituted thienyl, substituted furyl or substituted naphthyl,3) C.sub.1 -C.sub.5 alkyl which is substituted with one or two substituents selected from the group consisting of phenyl, substituted phenyl, thienyl, substituted thienyl, furyl, substituted furyl, naphthyl, substituted naphthyl, C.sub.3 -C.sub.8 cycloalkyl and phenoxy;4) C.sub.2 -C.sub.5 alkenyl which is substituted with one or two substituents selected from the group consisting of phenyl, substituted phenyl, thienyl, substituted thienyl, furyl, substituted furyl, naphthyl, substituted naphthyl, C.sub.3 -C.sub.8 cycloalkyl and phenoxy;5) C.sub.3 -C.sub.5 alkynyl which is substituted with one or two substituents selected from the group consisting of phenyl, substituted phenyl, thienyl, substituted thienyl, furyl, substituted furyl, naphthyl, substituted naphthyl, C.sub.3 -C.sub.8 cycloalkyl and phenoxy;6) C.sub.2 -C.sub.8 alkoxyalkyl which is substituted with one or two substituents selected from the group consisting of phenyl, substituted phenyl, thienyl, substituted thienyl, furyl, substituted furyl, naphthyl, substituted naphthyl, C.sub.3 -C.sub.8 cycloalkyl and phenoxy;7) C.sub.1 -C.sub.5 hydroxyalkyl which is substituted with one or two substituents selected from the group consisting of phenyl, substituted phenyl, thienyl, substituted thienyl, furyl, substituted furyl, naphthyl, substituted naphthyl, C.sub.3 -C.sub.8 cycloalkyl and phenoxy;8) C.sub.2 -C.sub.8 alkylthioalkyl which is substituted with one or two substituents selected from the group consisting of phenyl, substituted phenyl, thienyl, substituted thienyl, furyl, substituted, naphthyl, substituted naphthyl, C.sub.3 -C.sub.8 cycloalkyl and phenoxy;9) C.sub.1 -C.sub.5 aminoalkyl which is substituted with one or two substituents selected from the group consisting of phenyl, substituted phenyl, thienyl, substituted thienyl, furyl, substituted furyl, naphthyl, substituted naphthyl, C.sub.3 -C.sub.8 cycloalkyl and phenoxy;10) --CH.sub.2 --C(O)--R.sup.10 wherein R.sup.10 is phenyl or substituted phenyl or C.sub.1 -C.sub.5 alkyl substituted with one or two phenyl groups or substituted phenyl;R.sup.5 is1) hydrogen,2) C.sub.1 -C.sub.5 alkyl,3) C.sub.1 -C.sub.5 hydroxyalkyl or acetoxyalkyl,4) C.sub.1 -C.sub.5 alkyl substituted with one or two phenyl groups or substituted phenyl; or5) C.sub.2 -C.sub.8 alkoxyalkyl substituted with one or two phenyl groups or substituted phenyl groups; andR.sup.6 and R.sup.7 represent hydrogen or R.sup.6 and R.sup.7 are covalently bonded to represent a double bond, with the proviso that when X is CH.sub.2, Y is not CH.sub.2.