Patent ID: 6057451
Filing Date: 2000-05-02
Classification: A61P,C07D

Abstract:
A compound of the formula: ##STR302## wherein: R is selected from the group consisting of hydrogen, lower alkyl, amino, lower alkylamino, di(lower alkyl)amino, lower alkanoylamino, (lower alkoxycarbonyl)amino, di(lower alkoxycarbonyl)amino and {(lower alkylamino)carbonyl}amino; andZ is selected from the group consisting of:(i) NR.sup.2 --C(O)--Q--CH(R.sup.3)--NR.sup.4 R.sup.5 wherein:R.sup.2 is hydrogen or lower alkyl;Q is absent (i.e. a valance bond) or methylene;R.sup.3 is hydrogen, lower alkyl, phenyl(lower alkyl) or phenyl(lower alkyl) monosubstituted on the aromatic portion thereof with a halo, hydroxy, lower alkoxy or lower alkyl;R.sup.4 is hydrogen, (1-8C)alkyl, {di(lower alkyl)amino}-(lower alkyl), phenyl(lower)alkyl, phenyl(lower)alkyl monosubstituted or disubstituted on the aromatic portion thereof with a halo, hydroxy, lower alkoxy or lower alkyl; 1-indanyl, 2-indanyl, (lower cycloalkyl)-(lower alkyl); andR.sup.5 is (1-8C)alkyl, phenyl(lower alkyl), phenyl-(lower alkyl) monosubstituted on the aromatic portion thereof with a halo, hydroxy, lower alkoxy or lower alkyl; 1-indanyl, 2-indanyl, (lower cycloalkyl)-(lower alkyl), phenyl-sulfonyl, 1- or 2-naphthylsulphonyl, 5-(dimethylamino)-1-naphthylsulfonyl, (lower alkylamino)sulfonyl, {di(lower alkyl)amino}sulfonyl, lower alkanoyl, (lower cycloalkyl)-(lower alkanoyl), {1-(lower alkyl)-(lower cycloalkyl)}-carbonyl, (lower alkoxy)carbonyl, phenyl-Y--(CH.sub.2).sub.n C(O) wherein Y is oxy (--O--) or thio (--S--) and n is 0, 1 or 2 when Y is oxy or n is 1 or 2 when Y is thio, monosubstituted or disubstituted phenyl-Y--(CH.sub.2).sub.2 C(O) wherein Y and n are as defined in this claim and the monosubstitution or disubstitution occurs on the phenyl portion thereof with a substituent selected from the group consisting of halo, hydroxy, lower alkoxy and lower alkyl; phenyl(lower alkanoyl), phenyl(lower alkanoyl) monosubstituted or disubstituted on the phenyl portion thereof with a substituent selected independently from the group consisting of azido, halo, hydroxy, lower alkoxy and lower alkyl; 2-{(lower alkoxycarbonyl)amino}-1-oxoethyl, (lower alkylamino)carbonyl, {di(lower alkyl)amino}carbonyl or (lower alkylamino)thiocarbonyl;(ii) NR.sup.2A C(O)--A--NR.sup.3A R.sup.4A wherein:R.sup.2A is hydrogen or lower alkyl;A is absent or carbonyl;R.sup.3A is hydrogen, (1-8C)alkyl, 2-hydroxyethyl, 3-hydroxypropyl, (1-3C)alkyl monosubstituted with cyano, phenyl(lower alkyl), phenyl(lower alkyl) monosubstituted or disubstituted on the aromatic portion thereof with a halo, hydroxy, di(lower alkyl)amino, lower alkoxy or lower alkyl; (lower cycloalkyl)-(lower alkyl); andR.sup.4A is (1-8C)alkyl, phenyl(lower alkyl), phenyl-(lower alkyl) monosubstituted or disubstituted on the aromatic portion thereof with a halo, hydroxy, di(lower alkyl)amino, lower alkoxy or lower alkyl; 1-indanyl, 2-indanyl, phenyl(lower alkyl) monosubstituted on the aliphatic portion thereof with a hydroxy; (lower cycloalkyl)-(lower alkyl);or R.sup.3A and R.sup.4A independently are: ##STR303## wherein L is carbon, oxygen or nitrogen, with the proviso that when L is oxygen, one of R.sup.6A or R.sup.7A is absent; R.sup.5A and R.sup.6A are independently selected from the group defined for R.sup.3A in this claim; and R.sup.7A is independently selected from the group defined for R.sup.4A in this claim;or a therapeutically acceptable acid addition salt thereof.