| 摘要 |
<p>A compound of formula (I) or a pharmaceutically acceptable salt thereof:<!-- EPO <DP n="2"> --><Chemistry id="chema01" num="0001"><Image id="ia01" he="52" wi="99" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>one of R, and F<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</Sub>- <Sub>5</Sub>polymethylene;</ListItem><ListItem>either R<Sub>3</Sub> is hydrogen, hydroxy, C<Sub>1-6</Sub> alkoxy or C<Sub>1-7</Sub> acyloxy and R4 is hydrogen or R<Sub>3</Sub> and R<Sub>4</Sub> together are a bond;</ListItem><ListItem>R<Sub>s</Sub> is hydrogen; C <Sub>1-6</Sub> alkyl optionally substituted by up to three halo atoms, by hydroxy, C<Sub>1-6</Sub> alkoxy, C<Sub>1-</Sub><Sub>6</Sub>alkoxycarbonyl, carboxy, or amino optionally substituted by one or two independent C<Sub>1-6</Sub> alkyl groups or disubstituted by C<Sub>4</Sub>.<Sub>5</Sub> polymethylene; C <Sub>2</Sub>- <Sub>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; or (when X is 0), R<Sub>s</Sub> is selected from the class of carboxy, C<Sub>1-</Sub><Sub>6</Sub>alkoxycarbonyl, or aminocarbonyl optionally substituted by one or two C<Sub>1-6</Sub> alkyl groups; and</ListItem><ListItem>R<Sub>6</Sub> is hydrogen or C<Sub>1-6</Sub> alkyl; or</ListItem><ListItem>R<Sub>s</Sub> and R<Sub>6</Sub>together are -CH<Sub>2</Sub>-(CH<Sub>2</Sub>) -Z-(CH2)m-wherein m and n are 0 to 2 such that m + n is 1 or 2 and Z is CH<Sub>2</Sub>, O, S or NR wherein R is hydrogen, C <Sub>1-9</Sub> alkyl, <Sub>2-7</Sub>alkanoyl, phenyl C<Sub>1-4</Sub>-alkyl, naphthylcarbonyl, phenylcarbonyl or benzyl-carbonyl 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; or R is heteroarylcarbonyl;</ListItem><ListItem>or halogen, or aryl or heteroaryl, either being optionally substituted by one or more groups or atoms X is oxygen or sulphur; or</ListItem><ListItem>R<Sub>s</Sub>, R<Sub>6</Sub>, X and N together are tetrahydroisoquinolinone or tetrahydroisoquinolin- thione optionally substituted in the phenyl ring as defined for R above;</ListItem><ListItem>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 pharmacological activity, including blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.</ListItem></UnorderedLists></p> |
