| 摘要 |
<p>Compounds of formula (I) and pharmaceutically acceptable salts thereof: R
<Chemistry id="chema01" num="0001"><Image id="ia01" he="39" wi="82" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>one of R, and R<Sub>2</Sub> is hydrogen or C<Sub>1-4</Sub> alkyl and the other is C<Sub>1-4</Sub> alkyl or R, and R<Sub>2</Sub> together are C<Sub>2-5</Sub>-polymethylene; either R<Sub>3</Sub> is hydrogen, hydroxy, C<Sub>1-6</Sub> alkoxy or C<Sub>1-7</Sub> acyloxy and R<Sub>4</Sub> is hydrogen or R<Sub>3</Sub> and R<Sub>4</Sub> together are a bond; R<Sub>5</Sub>is hydrogen, C<Sub>1-6</Sub> alkyl optionally substituted by halogen, hydroxy, C<Sub>1-6</Sub> alkoxy, C<Sub>1-6</Sub> alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C<Sub>1-6</Sub> alkyl groups, or C<Sub>2-6</Sub> alkenyl, amino optionally substituted by a C<Sub>1-6</Sub> alkyl or C<Sub>1-6</Sub> alkenyl group or by a C<Sub>1-6</Sub> alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C<Sub>1-6</Sub> alkyl, C<Sub>1-6</Sub> alkoxy or halogen, or aryl or heteroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C<Sub>1-6</Sub> alkyl, C<Sub>1-6</Sub> alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, C<Sub>1-12</Sub> carboxylic acyl, or amino or aminocarbonyl optionally substituted by one or two C<Sub>1-6</Sub> alkyl groups and R<Sub>6</Sub> is hydrogen or C<Sub>1-6</Sub> alkyl, or R<Sub>5</Sub> and R<Sub>6</Sub> together are-CH<Sub>2</Sub>-(CH<Sub>2</Sub>)<Sub>n</Sub>-Z-(CH)<Sub>m</Sub>- wherein m and n are 0 to 2 such that m + n is 1 or 2 and Z is CH<Sub>2</Sub>, 0, S or NR wherein R is hyydrogen, C<Sub>1-9</Sub> alkyl, C<Sub>2-7</Sub> alkanoyl, phenyl C<Sub>1-4</Sub>-alkyl, naphthylcarbonyl, phenylcarbonyl or benzylcarbonyl optionally substituted in the phenyl or naphthyl ring by one or two of C<Sub>1-6</Sub> alkyl, C<Sub>1-6</Sub> alkoxy or halogen; mono- or bi-cyclic- heteroarylcarbonyl;</ListItem><ListItem>X is oxygen or sulphur;</ListItem><ListItem>Y and Q are electron withdrawing groups; and the nitrogen-containing group in the 4-position being trans to the R<Sub>3</Sub> group when R<Sub>3</Sub> is hydroxy, C<Sub>1-6</Sub> alkoxy or C<Sub>1-7</Sub> acyloxy; having blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.</ListItem></UnorderedLists></p> |
