摘要 |
Compounds of the general formula: <CHEM> wherein R<1> represents hydrogen, a C1-6 alkyl group or an acetyl group; R<2> represents halogen; R<3> represents a group of the formula: <CHEM> wherein R<5> represents hydrogen or a phenyl or non-aromatic cyclic ether group and n is 2 or 3; R<4> represents a C3-6 cycloalkyl, cyclohexenyl, C1-6 alkoxy, trifluoromethyl, tetrahydrofuryl, 1,3-dioxolanyl or phenoxy group; m is 0, 1, 2, 3 or 4 with the proviso that when m is 0, R<4> is only a C3-6 cycloalkyl or tetrahydrofuryl group; and pharmacologically acceptable acid addition salts, quaternary ammonium salts and N-oxides thereof have pharmacological properties rendering them useful as antiematic agents with reduced undesirable side-effects. Various methods are described for their preparation involving formation of the amide link, etherification of the 2-hydroxy derivative, introducing the R<5>CH2 group on the N-unsubstituted azabicyclooctane or nonane or, for 4-amino compounds, by hydrolysing a 4-acylamino derivative. |