Aphidicolane derivatives, their preparation and pharmaceutical compositions comprising them.

摘要

Aphidicolane derivatives of the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="43" wi="45" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R<Sup>1</Sup> stands for hydrogen or a hydroxy radical, R<Sup>2</Sup> stands for a hydroxy or methyl radical, or the group CR<Sup>1</Sup> R<Sup>2 </Sup>stands for a keto group; R<Sup>3</Sup> stands for a formyl or hydroxymethyl radical, or for the group -CH<Sub>2</Sub>0.CO.OR<Sup>6</Sup>, wherein R<Sup>6</Sup> stands for a defined radical or R<Sup>2</Sup> and R<Sup>3</Sup> are joined together to form the group -O.CO.OCH<Sub>2</Sub>-; R<Sup>4</Sup> stands for a hydroxy radical; R<Sup>5</Sup> stands for a formyl radical, a hydroxyalkyl radical -(CH<Sub>2</Sub>)<Sub>1-3</Sub>OH, a radical -CHR<Sup>7</Sup>OH, wherein R<Sup>7</Sup> stands for a defined radical, or R<Sup>5</Sup> stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group -CH<Sub>2</Sub>0.CO.OR<Sup>8</Sup>, wherein R<Sup>8</Sup> stands for a defined radical, or R<Sup>5</Sup> stands for the group -CH<Sub>2</Sub>O.CO.(CH<Sub>2</Sub>)m.CR<Sup>11</Sup>R<Sup>12</Sup>.(CH<Sub>2</Sub>)<Sub>n</Sub>.NR<Sup>9</Sup>R<Sup>10</Sup>. wherein m, n, R<Sup>9,</Sup> R<Sup>10</Sup>, R<Sup>11</Sup> and R<Sup>12</Sup> have defined values, or R<Sup>5</Sup> stands for the group -CH<Sub>2</Sub>O.SO<Sub>2</Sub>.R<Sup>13</Sup>, wherein R<Sup>13</Sup> stands for a defined radical; or R<Sup>4</Sup> and R<Sup>5</Sup> are joined together to form the group -O.CH<Sub>2</Sub>- or -O.CO.OCH<Sub>2</Sub>-; and, where appropriate, pharmaceutically acceptable salts thereof. Processes for the preparation of said aphidicolane derivatives. Pharmaceutical compositions comprising one of thecompounds and a pharmaceutical diluent or carrier. The compounds exhibit inhibitory activity against DNA-containing viruses and they inhibit the growth of some tumours.