Patent ID: 6323228
Filing Date: 2001-11-27
Classification: A61P,C07D

Abstract:
A compound of formula (I), ##STR4##or a therapeutically acceptable salt thereof, whereina is 0, 1, 2, 3, or 4;each R.sup.1 is independently selected from the group consisting of alkoxy, amino, halo, hydroxy and nitro;R.sup.2 is selected from the group consisting of alkenyl, alkyl, alkynyl, aryl, and heterocycle;R.sup.3 is selected from the group consisting of hydrogen, alkyl, and a nitrogen protecting group; andR.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, (cycloalkyl)alkyl, heterocycle, and (heterocycle)alkyl wherein the aryl, cycloalkyl and heterocycle may be optionally substituted;with the proviso that one of R.sup.4 and R.sup.5 is hydrogen; andwith the proviso that when a is 1, R.sup.1 is C.sub.1 -alkyl, C.sub.1 -alkoxy, halo, or nitro, R.sup.2 is C.sub.1 -alkyl, and R.sup.3 and R.sup.4 are hydrogen, R.sup.5 is not hydrogen, C.sub.3 -alkyl, C.sub.5 -alkyl, N-(phenyl-C.sub.1 -alkyl)indolyl, unsubstituted phenyl, or phenyl substituted with one member selected from the group consisting of C.sub.3 -alkyl, C.sub.1- C.sub.4 -alkoxy, halo, hydroxy, and nitro; andwith the proviso that when a is 1, R.sup.1 is C.sub.1 -alkoxy or halo, R.sup.2 is unsubstituted phenyl, and R.sup.3 and R.sup.4 are hydrogen, R.sup.5 is not hydrogen, unsubstituted indolyl, phenyl substituted with one member selected from the group consisting of C.sub.1 -alkoxy, C.sub.4 -alkoxy, halo, hydroxy, and nitro, or phenyl substituted with one hydroxy and one nitro substituent; andwith the proviso that when a is 0, R.sup.2 is unsubstituted phenyl, and R.sup.3 and R.sup.4 are hydrogen, R.sup.5 is not hydrogen or unsubstituted phenyl.