Dihydropyridines.

摘要

1,4-Dihydropyridine derivatives of the formula:-
<Chemistry id="chema01" num="0001"><Image id="ia01" he="25" wi="83" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>and their pharmaceutically acceptable acid addition salts; where
<UnorderedLists id="ula01" listStyle="none"><ListItem>R is aryl or heteroaryl;</ListItem><ListItem>R<Sup>1</Sup> and R<Sup>2</Sup> are each independently C<Sub>1</Sub>-C<Sub>4</Sub> alkyl or 2-methoxyethyl;</ListItem><ListItem>Y is -(CH<Sub>2</Sub>)<Sub>2</Sub>-, -(CH<Sub>2</Sub>)<Sub>3</Sub>-, -CH<Sub>2</Sub>CH(CH<Sub>3</Sub>)- or -CH<Sub>2</Sub>C(CH<Sub>3</Sub>)<Sub>2</Sub>-;</ListItem><ListItem>R<Sup>3</Sup> is hydrogen or a group selected from:-</ListItem></UnorderedLists><UnorderedLists id="ula02" listStyle="none"><ListItem><Chemistry id="chema02" num="0002"><Image id="ia02" he="13" wi="26" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where R<Sup>4</Sup> is H, C<Sub>1</Sub>-C<Sub>4</Sub> alkyl, C<Sub>3</Sub>-C<Sub>6</Sub> cycloalkyl, -COO(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl), -CH<Sub>2</Sub>COO(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl), aryl, -S0<Sub>2</Sub>.aryl, or heteroaryl, and X is 0 or S;
<Chemistry id="chema03" num="0003"><Image id="ia03" he="12" wi="44" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry><Chemistry id="chema04" num="0004"><Image id="ia04" he="14" wi="25" file="IMGA0004.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where R<Sup>5</Sup> is 1-pyrrolidinyl, -NH<Sub>2</Sub>, -NH(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl), -N/C<Sub>1</Sub>-C<Sub>4</Sub> alkyl)<Sub>2</Sub>, or -NH(CH<Sub>2</Sub>)<Sub>2</Sub>N(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl)<Sub>2</Sub>;
<Chemistry id="chema05" num="0005"><Image id="ia05" he="12" wi="44" file="IMGA0005.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where R<Sup>6</Sup> is C<Sub>1</Sub>-C<Sub>4</Sub> alkyl or aryl;<!-- EPO <DP n="2"> --><Chemistry id="chema06" num="0006"><Image id="ia06" he="17" wi="37" file="IMGA0006.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where R<Sup>7</Sup> is -CONH(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl) or -COO(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl);
<Chemistry id="chema07" num="0007"><Image id="ia07" he="15" wi="48" file="IMGA0007.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry><Chemistry id="chema08" num="0008"><Image id="ia08" he="13" wi="33" file="IMGA0008.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where R<Sup>8</Sup> is -CN, -SO<Sub>2</Sub>(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl) or -SO<Sub>2</Sub> aryl;</ListItem><ListItem>(h) -CH<Sub>2</Sub>CO.R<Sup>9</Sup> where R<Sup>9</Sup> is -NH<Sub>2</Sub>, -NH(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl), -NH.aryl or C<Sub>1</Sub>-C<Sub>4</Sub> alkoxy;</ListItem><ListItem>(i) -SO<Sub>2</Sub>.R<Sup>10</Sup> where R<Sup>10</Sup> is -NH<Sub>2</Sub>, -N(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl)<Sub>2</Sub> or C<Sub>1</Sub>-C<Sub>4</Sub> alkyl; and</ListItem><ListItem>(j) -CO.R" where R" is H, halomethyl, -COO(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl), -CH<Sub>2</Sub>O(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl), -CH<Sub>2</Sub>CO(C<Sub>1</Sub>-C<Sub>4</Sub> alkyl), C<Sub>1</Sub>-C<Sub>4</Sub> alkyl, C<Sub>1</Sub>-C<Sub>4</Sub> alkoxy, aryl, heteroaryl, morpholino or 5-oxo-pyrrolidin-2-yl.</ListItem></UnorderedLists>

The compounds have utility as anti-ischaemic and antihypertensive agents.