Patent ID: 6127357
Filing Date: 2000-10-03
Classification: A61P,C07D

Abstract:
A compound of the formula ##STR13## or a pharmaceutically acceptable acid addition salt thereof, wherein A is an alkylene chain of 2 to 4 carbon atoms optionally substituted by one or more lower alkyl groups;Z is oxygen or sulphur;R is hydrogen or lower alkyl;R.sup.1 is aryl, tetrahydronaphthyl, heteroaryl, wherein aryl is phenyl or naphthyl each of which may be optionally substituted by one or more substituents independently selected from lower alkyl, lower alkoxy, halogen, haloloweralkyl, nitro, nitrile, aminocarbonyl, loweralkoxycarbonyl, amino, loweralkylamino, or di-loweralkylamino, and heteroaryl is a monocyclic aromatic heterocyclic ring having 5 ring members and having as heteroatoms one or two N atoms or one N atom and one O or S atom, or a monocyclic aromatic heterocyclic ring having 6 ring members and having as heteroatoms one or two N atoms, or a bicyclic aromatic heterocyclic ring system having one such 5 or 6 membered monocyclic aromatic heterocyclic ring fused to a benzene ring, wherein such heteroaryl or tetrahydronaphthyl ring may be optionally substituted as for aryl,or R.sup.1 is a bicyclic oxygen-containing aryl radical of the formula ##STR14## wherein the heterocyclic oxygen-containing ring has 5 to 7 ring members, said heterocyclic ring being non-aromatic and optionally having one further hetero ring member selected from --O--, --S--, --SO.sub.2 or NR.sup.7, wherein R.sup.7 is hydrogen or lower alkyl and wherein R.sup.8 and R.sup.9 represent hydrogen or one or more substituents independently selected from lower alkyl, halogen, hydroxy, loweralkoxy, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkanoyloxy(loweralkyl), loweralkylcarbonyl, loweralkylcarbonyl(loweralkyl), amino, loweralkylamino or di-loweralkylamino,or R.sup.1 is an bicyclic oxygen-containing aryl radical of the formula ##STR15## wherein R.sup.8 and R.sup.9 are as defined above; R.sup.2 is a monocyclic aromatic heterocyclic ring having 6 members and having as heteroatoms one or two N atoms or a bicyclic aromatic heterocyclic ring system having one such 6 membered monocyclic aromatic heterocyclic ring fused to a benzene ring, which may be optionally substituted as for aryl, provided that, said bicyclic heterocyclic radical is connected to the amino nitrogen of formula I via such heterocyclic ring; andR.sup.3 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkyl(loweralkyl), aryl, aryl(loweralkyl), a group of formula --NR.sup.4 R.sup.5, or a group of formula OR.sup.6, in which R.sup.4 is hydrogen, lower alkyl, aryl or aryl(loweralkyl) and R.sup.5 is hydrogen, lower alkyl, --CO(loweralkyl), aryl, --COaryl, aryl(loweralkyl), cycloalkyl or cycloalkyl(loweralkyl), or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are both attached represent azetidino, pyrrolidino, piperidino, hexahydroazepino, morpholino or piperazino which may be optionally substituted by lower alkyl, aryl or aryl(loweralkyl), and R.sup.6 is lower alkyl, cycloalkyl, cycloalkyl(loweralkyl), aryl, or aryl(loweralkyl),wherein aryl is as defined for R.sup.1 and cycloalkyl or cycloalkenyl is a mono-, bi-, tri-, or tetracyclic hydrocarbon group of 3 to 12 carbon atoms.