Carboxyalkanoyl and hydroxycarbamoylalkanoyl derivatives of substituted prolines.

摘要

Compounds, compositions and method of alleviating hypertension using a compound of the formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="14" wi="63" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry><UnorderedLists id="ula01" listStyle="none"><ListItem>wherein R is hydrogen or lower alkyl;</ListItem><ListItem>R<Sub>1</Sub> is hydrogen, lower alkyl or phenyl-lower alkyl;</ListItem><ListItem>R<Sub>2</Sub> is hydrogen, lower alkyl, phenyl lower alkyl or halo substituted lower alkyl;</ListItem><ListItem>R<Sub>3</Sub> is hydroxy, -NHOH or lower alkoxy;</ListItem><ListItem>Pr-COOR is a substituted proline of the structures
<Chemistry id="chema02" num="0002"><Image id="ia02" he="26" wi="65" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>or
<Chemistry id="chema03" num="0003"><Image id="ia03" he="20" wi="48" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry></ListItem><ListItem>R<Sub>4</Sub> is halogen, keto, azido, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, substituted phenyl-lower alkyl,
<Chemistry id="chema04" num="0004"><Image id="ia04" he="15" wi="59" file="IMGA0004.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry></ListItem><ListItem>R<Sub>5</Sub> is hydrogen or lower alkyl;</ListItem><ListItem>Y is oxygen or sulfur;</ListItem><ListItem>R<Sub>6</Sub> is lower alkyl, phenyl, substituted phenyl, phenyl-lower alkyl, substituted phenyl-lower alkyl, 1- or 2-naphthyl, substituted 1- or 2- naphthyl, biphenyl, or substituted biphenyl;</ListItem><ListItem>R<Sub>7</Sub> is halogen or -Y-R<Sub>8</Sub>;</ListItem><ListItem>R<Sub>8</Sub> is lower alkyl, phenyl, phenyl-lower alkyl substituted phenyl-lower alkyl, biphenyl, napthyl, or the R<Sub>8</Sub> groups join to complete an unsubstituted 5- or 6- membered ring or such ring wherein one or more carbon atoms are substituted by a lower alkyl or di(lower alkyl) group;</ListItem><ListItem>R<Sub>9</Sub> is keto, phenyl, 2- or 4-hydroxyphenyl;</ListItem><ListItem>n is 0 or 1; and salts thereof.</ListItem></UnorderedLists>