Pyrazolopyridines, their preparation and pharmaceutical compositions containing them.

摘要

Compounds of the formula (I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="36" wi="104" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>
wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>X is NR wherein R is hydrogen, C<Sub>1-6</Sub> alkyl or as defined hereinafter with R<Sub>3</Sub>; oxygen; sulphur; SO; or SO<Sub>2</Sub>;</ListItem><ListItem>R, is hydrogen or C<Sub>1-6</Sub>alkyl; and R<Sub>2</Sub> is CN, CR<Sub>5</Sub>R<Sub>6</Sub>Y where R<Sub>s</Sub> and R<Sub>6</Sub> are independently selected from hydrogen and C<Sub>1-4</Sub> alkyl and Y is selected from hydrogen, OR, or SR, where R<Sub>7</Sub> is hydrogen, C<Sub>1-4</Sub> alkyl or C<Sub>2</Sub>-<Sub>4</Sub> alkanoyl, and NR<Sub>8</Sub>R<Sub>9</Sub> where R<Sub>8</Sub> and R<Sub>9</Sub> are independently hydrogen, C<Sub>1-4</Sub> alkyl, C <Sub>2</Sub>.<Sub>4</Sub> alkenyl or C2-<Sub>4</Sub> alkanoyl or together are C <Sub>4-6</Sub> polymethylene, or COR<Sub>10</Sub> where R,<Sub>o</Sub> is C<Sub>1-4</Sub> alkyl, provided that Y is other than hydrogen when R, is hydrogen;
or</ListItem><ListItem>R<Sub>2</Sub> is hydrogen, C<Sub>1-6</Sub> alkyl or phenyl optionally substituted by halogen, CF<Sub>3</Sub>, C<Sub>1-4</Sub> alkoxy or C<Sub>1-4</Sub> alkyl; and R, is CN, CR<Sub>5</Sub>R<Sub>6</Sub>Y or COR<Sub>10</Sub> as defined for R<Sub>2</Sub> above;
or</ListItem><ListItem>R<Sub>1</Sub> and R<Sub>2</Sub> together form C<Sub>3</Sub>-C<Sub>6</Sub> polymethylene optionally substituted by C<Sub>1</Sub>-C<Sub>4</Sub> alkyl;</ListItem><ListItem>R<Sub>3</Sub> is C<Sub>1-10</Sub> alkyl or C<Sub>3-10</Sub> cycloalkyl, eitheroptionally substituted by hydroxy, C<Sub>1-4</Sub> alkoxy, thiol, C<Sub>1-4</Sub>alkylthio or NR<Sub>11</Sub>R<Sub>12</Sub> wherein R,, and R<Sub>12</Sub> are independently hydrogen, C<Sub>1-6</Sub> alkyl or C <Sub>2</Sub>-<Sub>7</Sub> alkanoyl or together are C<Sub>3</Sub>.<Sub>6</Sub> polymethylene; C<Sub>2-10</Sub> alkenyl; or phenyl optionally substituted by one or two of halogen, CF,, C<Sub>1-4</Sub> alkoxy, C<Sub>1-4</Sub> alkyl, hydroxy, nitro, cyano, <!-- EPO <DP n="2"> -->C<Sub>2-10</Sub> acyloxy, NR<Sub>13</Sub>R<Sub>14</Sub> wherein R<Sub>13</Sub> and R<Sub>14</Sub> are independently selected from hydrogen, C<Sub>1-6</Sub> alkyl, C<Sub>2-7</Sub>alkanoyl or C<Sub>1-6</Sub> alkylsulphonyl or COR<Sub>15</Sub> wherein R<Sub>15</Sub> is hydroxy, C<Sub>1-6</Sub> alkoxy or NR<Sub>16</Sub>R<Sub>17</Sub> wherein R<Sub>16</Sub> and R,<Sub>7</Sub> are independently selected from hydrogen or C<Sub>1-6</Sub> alkyl; or together with R is C <Sub>4</Sub>-<Sub>6</Sub> polymethylene; and</ListItem><ListItem>R<Sub>4</Sub> is hydrogen; or C<Sub>1-4</Sub> alkyl or benzyl optionally substituted in the phenyl ring by one or two of halogen, CF<Sub>3</Sub>, C<Sub>1-4</Sub> alkoxy or C<Sub>1-4</Sub> alkyl and is attached at nitrogen atom 1 or 2, are disclosed as having utility in the treatment of inflammatory and allergic disorders.</ListItem></UnorderedLists>