Acylaminoquinazoline derivatives, a process for their preparation and a pharmaceutical composition containing them.

摘要

Acylaminoquinazoline derivatives of formula (I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="50" wi="80" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>(in which:
<UnorderedLists id="ula01" listStyle="none"><ListItem>R<Sup>1</Sup> represents a lower alkoxy group, a substituted or unsubstituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a vinyl group having an optionally substituted phenyl or furyl substituent, an optionally substituted phenyl group, a furyl group, an oxazolyl group, a methylthiooxadiazolyl group or a tetrahydrofuryl group;</ListItem><ListItem>R<Sup>2</Sup> represents a hydrogen atom or a lower alkyl group;</ListItem><ListItem>R<Sup>3</Sup> represents a lower alkyl group or an optionally substituted phenyl group;</ListItem><ListItem>R<Sup>4</Sup> represents a hydrogen atom or an acyloxy- substituted phenyl group;</ListItem><ListItem>X represents a methylene group or a sulphur atom; and n is 2 or 3)</ListItem></UnorderedLists>
and pharmaceutically acceptable acid addition salts thereof are valuable antihypertensive agents and inhibit the activity of the angiotension I-converting enzyme. They may be prepared by reacting a 4-aminoquinazoline derivative with a carboxylic acid or reactive derivative thereof corresponding to the amide group which it is desired to introduce at the 4- position of said compound of formula (I). The compounds of the invention may be formulated with conventional pharmaceutically acceptable carriers or diluents to provide a pharmaceutical composition.