Isoquinolinesulfonyl derivatives and process for the preparation thereof.

摘要

A 5-isoquinolinesulfonyl derivative of Formula (I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="18" wi="77" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>f is zero or one;</ListItem><ListItem>m and n each is an integer of one to nine;</ListItem><ListItem>m+n is an integer of at least one;</ListItem><ListItem>R<Sub>1</Sub> is a hydrogen atom, a C<Sub>1-10</Sub> alkyl group, a C<Sub>5-6</Sub>cycloalkyl group or an aryl group; or</ListItem><ListItem>R<Sub>2</Sub> and R<Sub>3</Sub> each is a hydrogen atom, a C<Sub>1-10</Sub> alkyl group, a C<Sub>5-6</Sub> cycloalkyl group, an aryl group or an aralkyl group;</ListItem><ListItem>R<Sub>2</Sub> and R<Sub>3</Sub> are C<Sub>1-6</Sub> alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the
<Chemistry id="chema02" num="0002"><Image id="ia02" he="19" wi="21" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>group is a
<Chemistry id="chema03" num="0003"><Image id="ia03" he="16" wi="22" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>group wherein R<Sub>4</Sub> and R<Sub>s</Sub> each is a hydrogen atom, a C<Sub>1-10</Sub> alkyl group, an aryl group or an aralkyl group and R<Sub>6</Sub> is a hydrogen atom, a C<Sub>1-10</Sub> alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a
<Chemistry id="chema04" num="0004"><Image id="ia04" he="15" wi="27" file="IMGA0004.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>group wherein R, is a C<Sub>1-8</Sub> alkyl group, and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.</ListItem></UnorderedLists>