Substituted phosphonamides, a process for preparing the same and a pharmaceutical composition which is useful in the treatment of hypertension.

摘要

There are disclosed substituted phosphonamides and related compounds of the general formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="23" wi="54" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>R, is alkyl or substituted alkyl of C<Sub>1</Sub>-C<Sub>6</Sub> wherein the substituent is halo, amino, acylamino; aralkyl wherein the alkyl is C<Sub>1</Sub>-C<Sub>4</Sub> optionally substituted by amino or acylamino and wherein the aryl function is phenyl or naphthyl optionally substituted by halo or hydroxyl; or, heteroaralkyl wherein the alkyl is C<Sub>1</Sub>-C<Sub>4</Sub> optionally substituted by amino or acylamino and wherein the heteroaryl group can be indolyl or thienyl;</ListItem><ListItem>R<Sub>2</Sub> is H, lower alkyl of C<Sub>1</Sub>-C<Sub>4</Sub>, aralkyl.</ListItem><ListItem>R<Sub>3</Sub> is lower alkyl of C<Sub>1</Sub>-C<Sub>6</Sub> optionally substituted by an amino group;</ListItem><ListItem>R<Sub>4</Sub> is H, lower alkyl of C<Sub>1</Sub>-C<Sub>6</Sub>, aralkyl.</ListItem><ListItem>X is (CH<Sub>2</Sub>)<Sub>n</Sub> wherein n is 1 or 2, CH-OCH<Sub>3</Sub>, CH-OH, or S; and,
the pharmaceutically acceptable salts thereof. THese compounds are useful as converting enzyme inhibitors and as antihypertensives.</ListItem></UnorderedLists>