Pharmaceutically active aminobenzopyrans.

摘要

Compounds of formula (I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="29" wi="68" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>either one of R, and R<Sub>2</Sub> is hydrogen and the other is selected from the class of C<Sub>1-6</Sub> alkylcarbonyl, C<Sub>1-6</Sub> alkoxycarbonyl, C<Sub>1-6</Sub> alkylcarbonyloxy, C<Sub>1-6</Sub> alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C<Sub>1-6</Sub> alkylsulphinyl, C<Sub>1-6</Sub> alkylsulphonyl, C<Sub>1-6</Sub> alkoxysulphinyl, C<Sub>1-6</Sub> alkoxysulphonyl, C<Sub>1-6</Sub> alkylcarbonylamino, C<Sub>1-6</Sub> alkoxycarbonylamino, C<Sub>1-6</Sub> alkyl- thiocarbonyl, C<Sub>1-6</Sub> alkoxy-thiocarbonyl, C<Sub>1-6</Sub> alkyl- thiocarbonyloxy, C<Sub>1-6</Sub> alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C<Sub>1-6</Sub> alkyl groups, or C<Sub>1-6</Sub> alkylsulphinylamino, C<Sub>1-6</Sub> alkylsulphonylamino C<Sub>1-6</Sub> alkoxysulphinylamino or C<Sub>1-6</Sub> alkoxysulphonylamino or ethylenyl terminally substituted by C<Sub>1-6</Sub> alkylcarbonyl, nitro or cyano, or -C(C<Sub>1-6 </Sub>alkyl)NOH or -C(C<Sub>1-6</Sub> alkyl)NNH<Sub>2</Sub>, or one of R, and R<Sub>2 </Sub>is nitro, cyano or C<Sub>1-3</Sub> alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C<Sub>1-6</Sub> alkyl or by C<Sub>2-7</Sub> alkanoyl;</ListItem><ListItem>one of R<Sub>3</Sub> and R<Sub>4</Sub> is hydrogen or C<Sub>1-4</Sub> alkyl and the other is C<Sub>1-4</Sub> alkyl or R<Sub>3</Sub> and R<Sub>4</Sub> together with the carbon atom to which they are attached are C<Sub>2-5</Sub> polymethylene;</ListItem><ListItem>either R<Sub>s</Sub> is hydroxy, C<Sub>1-6</Sub> alkoxy or C<Sub>2-7</Sub> acyloxy and R<Sub>6</Sub> is hydrogen or R<Sub>5</Sub> and R<Sub>6</Sub> together are a bond;</ListItem><ListItem>R<Sub>7</Sub> is hydrogen, C<Sub>1-6</Sub> alkyl optionally substituted by hydroxy, C<Sub>1-6</Sub> alkoxy, C<Sub>1-6</Sub> alkoxycarbonyl or carboxy, or C<Sub>1-2</Sub> alkyl substituted by halogen, or C<Sub>2</Sub>.<Sub>6</Sub> alkenyl;</ListItem><ListItem>R<Sub>8</Sub> is hydrogen or C<Sub>1-6</Sub> alkyl; and</ListItem><ListItem>X is oxygen or sulphur; the R<Sub>e</Sub>-N-CX-R<Sub>7</Sub> group being trans to the R<Sub>5</Sub> group when R<Sub>5</Sub> and R<Sub>6</Sub> together are not a bond; or, when one or the other of R, and R<Sub>2</Sub> is an amino or an amino-containing group, a pharmaceutically acceptable salt thereof, having anti-hypertensive activity.</ListItem></UnorderedLists>