| 摘要 |
<p>A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal an effective amount of a compound of formula (1):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="26" wi="80" 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>1-6</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> alklylsulphinylamino or 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</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>2-5</Sub> polymethylene;</ListItem><ListItem>either R<Sub>5</Sub> is hydrogen, hydroxy, C<Sub>1-6</Sub> alkoxy or C<Sub>1-7</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>I</Sub>-<Sub>8</Sub> alkyl optionally substituted by hydroxy, C<Sub>1-6</Sub> alkoxy, C<Sub>1-6</Sub> alkoxycarbonyl or carboxy, C<Sub>1-6</Sub> alkyl substituted by halogen, or C<Sub>2-6</Sub> alkenyl; aryl or heteroaryl either being optionally substituted by one or more groups or atoms selected from the class of 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;</ListItem><ListItem>R<Sub>8</Sub> is hydrogen or C<Sub>1-6</Sub> alkyl; or</ListItem><ListItem>R<Sub>7</Sub> and R<Sub>e</Sub> are joined together to form C<Sub>3-4</Sub> polymethylene or -CH<Sub>2</Sub>-(CH<Sub>2</Sub>)<Sub>n-</Sub>Z-(CH<Sub>2</Sub>)m- where m and n are integers 0 to 2 such that m+n is 1 or 2 and Z is oxygen, sulphur or NR<Sub>9</Sub> wherein R<Sub>9</Sub> is hydrogen, 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 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; and the R<Sub>8</Sub>NCXR<Sub>7</Sub> moiety is trans to the R<Sub>5</Sub> group when R<Sub>6</Sub> is hydroxy, C<Sub>1-6</Sub> alkoxy or C<Sub>1-7</Sub> acyloxy; or a pharmaceutically acceptable salt or solvate thereof.</ListItem></UnorderedLists></p> |
