摘要 |
<p>A cycloalkylurea compound of the formula (I): <CHEM> wherein R<1> is a group of the formula (a): <CHEM> (wherein R<6>, R<7> and R<8> are the same or different and each is hydrogen or alkyl having 1 to 8 carbon atoms, with the proviso that compounds wherein two or three of R<6>, R<7> and R<8> are hydrogens are excluded), haloalkyl, cycloalkyl, alkoxy having 1 to 5 carbon atoms, phenyl, aralkyl or heteroaryl, or phenyl, aralkyl or heteroaryl each substituted on the aromatic ring by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 8 carbon atoms, cycloalkyl, cycloalkyloxy, haloalkyl, haloalkoxy, halogen, nitro, amino and substituted amino; R<2> is hydrogen, phenyl or phenyl substituted by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, haloalkyl and halogen, whererin R<1> and R<2> may be substituted on the same carbon atom of cycloalkyl ring; R<1> and R<2> together may form a substituted or unsubstituted cyclic hydrocarbon having 3 to 7 carbon atoms or a substituted or unsubstituted spiran; R<3> is hydrogen, alkyl having 1 to 8 carbon atoms, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, aralkyl substituted by alkylenedioxy, aralkyl, aralkyloxyalkyl, aralkyl or aralkyloxyalkyl each substituted on the aromatic ring by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 5 carbon atoms, halogen, nitro, hydroxy, amino, substituted amino, haloalkyl, alkylthio, benzyloxy and benzylthio, heteroarylalkyl, phenoxyalkyl, or heteroarylalkyl or phenoxyalkyl each substituted on the aromatic ring by 1 to 3 substituents selected from halogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, nitro, amino and haloalkyl, or a group of the formula (c) or (d): <CHEM> wherein m is 1 or 2, R<1><1> is hydrogen or alkyl having 1 to 4 carbon atoms, R<1><2> is hydrogen, alkyl having 1 to 4 carbon atoms or aralkyl; R<4> is phenyl substituted by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, haloalkyl, halogen, amino and substituted amino; n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and anti-atherosclerotic medicine.</p> |