| 摘要 |
<p>Compounds offormula(I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="28" wi="84" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>either one of R<Sub>1</Sub> and R<Sub>2</Sub> is hydrogen and the other is selected from the class of C<Sub>1</Sub>-<Sub>6</Sub> alkylcarbonyl, C<Sub>1</Sub>-<Sub>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</Sub>-<Sub>6</Sub> alkylthiomethyl, 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> alkoxy- sulfonylamino or ethylenyl terminally substituted by C<Sub>1-6</Sub> alkylcarbonyl, nitro or cyano, or one of R<Sub>1</Sub> 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</Sub>-<Sub>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 are C<Sub>2</Sub>-<Sub>5</Sub> polymethylene;</ListItem><ListItem>R<Sub>6</Sub> is hydrogen or C<Sub>1-6</Sub> alkyl and R<Sub>5</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, C<Sub>1-2</Sub> alkyl substituted by halogen, or C<Sub>2-6</Sub> alkenyl; or R<Sub>6</Sub> and R<Sub>5</Sub> together form C<Sub>3</Sub>-<Sub>4</Sub> polymethylene;</ListItem><ListItem>X is oxygen or sulphur; and the R<Sub>6</Sub>NCXR<Sub>5</Sub> and OCOH moieties are trans and, when one or the other of R<Sub>1</Sub> and R<Sub>2</Sub> is an amino group, pharmaceutically acceptable salts thereof, a process and intermediates for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.</ListItem></UnorderedLists></p> |
