Aminophenol derivatives.

摘要

The invention provides compounds of the general formula (I)
<Chemistry id="chema01" num="0001"><Image id="ia01" he="22" wi="87" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C<Sub>1-6</Sub> alkyl, C<Sub>1-6</Sub> alkoxy, nitro, -(CH<Sub>2</Sub>)<Sub>q</Sub>R, [where R is hydroxy, -NR<Sup>3</Sup>R<Sup>4</Sup> (where R<Sup>3</Sup> and R<Sup>4</Sup> each represents a hydrogen atom, or a C<Sub>1-4</Sub> alkyl group, or-NR<Sup>3</Sup>R<Sup>4</Sup> forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from -0- or -S- or a group -NH- or -N(CH<Sub>3</Sub>)-). -NR<Sup>5</Sup>COR<Sup>6</Sup> (where R<Sup>5</Sup> represents a hydrogen atom or a C<Sub>1-5</Sub> alkyl group, and R<Sup>6</Sup> represents a hydrogen atom or a C<Sub>1-4</Sub> alkyl, C<Sub>1-4</Sub> alkoxy, phenyl or-NR<Sup>3</Sup>R<Sup>4</Sup> group), -NR<Sup>6</Sup>SO<Sub>2</Sub>R<Sup>7</Sup> (where R<Sup>7</Sup> represents a C<Sub>1-4</Sub> alkyl, phenyl or -NR<Sup>3</Sup>R<Sup>4</Sup> group), -COR<Sup>8</Sup> (where R<Sup>8</Sup> represents hydroxy, C<Sub>1-4</Sub> alkoxy or-NR<Sup>3</Sup>R<Sup>4</Sup>), -SR<Sup>8</Sup> (where R<Sup>9</Sup> is a hydrogen atom, or a C<Sub>1-4</Sub> alkyl or phenyl group),-SOR<Sup>9</Sup>,-SO<Sub>2</Sub>R<Sup>9</Sup>, or -CN, and q represents an integer from 0 to 31, -(CH<Sub>2</Sub>)<Sub>r</Sub>R<Sup>10</Sup>, [where R<Sup>10</Sup> is a C<Sub>1-4</Sub> alkoxy group and r represents an integer from 1 to 3] or -O(CH<Sub>2</Sub>)<Sub>t</Sub>T<Sup>11</Sup> [where R" represents a hydroxy or C<Sub>1-4</Sub> alkoxy group and t is 2 or 3] or Ar is a phenyl group substituted by an alkylenedioxy group of formula -O(CH<Sub>2</Sub>)<Sub>p</Sub>O-, where p represents 1 or 2; R' and R<Sup>2</Sup> each represent a hydrogen atom or a C<Sub>1-3</Sub> alkyl group with the proviso that the sum total of carbon atoms in</ListItem><ListItem>R<Sup>1</Sup> and R<Sup>2</Sup> is not more than 4;</ListItem><ListItem>X represents a C<Sub>1-7</Sub> alkylene, C<Sub>2</Sub> alkenylene or C<Sub>2-7</Sub> alkynylene chain;</ListItem><ListItem>Y represents a bond, or a C<Sub>1-6</Sub> alkylene, C<Sub>2-6</Sub> alkenylene or C<Sub>2-6</Sub> alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is 2 to 10;</ListItem><ListItem>Q represents a group R<Sup>12</Sup>CO-, R<Sup>12</Sup>NHCO-, R<Sup>12</Sup>R<Sup>13</Sup>NSO<Sub>2</Sub>- or R<Sup>14</Sup>SO<Sub>2</Sub>, where R<Sup>12</Sup> and R<Sup>13</Sup> each represents a hydrogen atom or a C<Sub>1-3</Sub> alkyl group, and R<Sup>14</Sup> represents a C<Sub>1-4</Sub> alkyl group, with the proviso that when X represents C<Sub>1-7</Sub> alkylene, and Y represents a bond or C<Sub>1-6</Sub> alkylene, then the group Ar does not represent an unsubstituted phenyl group or a phenyl group substituted by one or more substituents selected solely from halogen atoms or C<Sub>1-6</Sub> alkyl or C<Sub>1-6</Sub> alkoxy groups or an alkylenedioxy group -O(CH<Sub>2</Sub>)<Sub>p</Sub>O-;</ListItem><!-- EPO <DP n="2"> --><ListItem>and physiologically acceptable salts and solvates thereof.</ListItem></UnorderedLists>

The compounds have a selective stimulant action at β<Sub>2</Sub>-adrenoreceptors and may be used, inter alia, in the treatment of disease associated with reversible airways obstruction such as asthma and chronic bronchitis.