| 摘要 |
<p>Compounds of formula (I)
<Chemistry id="chema01" num="0001"><Image id="ia01" he="35" wi="58" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>R is hydrogen or C<Sub>1-6</Sub> alkyl;</ListItem><ListItem>R, and R<Sub>2</Sub> are both hydrogen; or</ListItem><ListItem>R<Sub>1</Sub> is hydrogen, 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>5</Sub> and R<Sub>e</Sub> are independently selected from hydrogen and C<Sub>1-4</Sub> alkyl and Y is sel lected from hydrogen OR<Sub>7</Sub> or SR<Sub>7</Sub> where R<Sub>7</Sub> is hydrogen, C<Sub>1-4</Sub> alkyl or C<Sub>2-4</Sub> alkanoyl, and NR<Sub>8</Sub>R<Sub>9</Sub> where R<Sub>e</Sub> and R<Sub>9</Sub> are independently hydrogen, C<Sub>1-4</Sub> alkyl, C<Sub>2-4</Sub> alkenyl or C<Sub>2-4</Sub> alkanoyl or togemer are C<Sub>4-6</Sub> polymethylene, or COR<Sub>10</Sub> where R<Sub>10</Sub> is OH or C<Sub>1-4</Sub> alkyl, or COR<Sub>10</Sub> is a pharmaceutically acceptable ester or am de. 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>o</Sub> as defined for R<Sub>2</Sub> above;</ListItem><ListItem>or R, 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 a mono- or fused bi-cyclic heteroaryl group having up to ten atoms in the aromatic ring(s), not more than two of which are selected from nitrogen, oxygen or sulphur, other than those containing basic nitrogen, optionally substituted by one or two substituents selected from halogen, CF<Sub>3</Sub>, C<Sub>1-4</Sub> alkoxy, C<Sub>1-4</Sub> alkyl, hydroxy, nitro, cyano, C<Sub>2-10</Sub> acyloxy, NR<Sub>11</Sub> R<Sub>12</Sub> wherein R<Sub>11</Sub> and R<Sub>12</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>13</Sub> wherein R<Sub>13</Sub> is hydroxy, C<Sub>1-6</Sub> alkoxy or NR<Sup>14</Sup> R<Sub>16</Sub> wherein R<Sub>15</Sub> and R<Sub>14</Sub> are independently selected from hydrogen or C<Sub>1-6</Sub> aklyl; 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 more of halogen, CF<Sub>3</Sub>, C<Sub>1-4</Sub> alkyl, and is attached at nitrogen atom 1 or 2; show anti-inflammatory and anti-allergy activity.</ListItem></UnorderedLists></p> |
