Pyrimidine derivatives, a process for preparing them and a pharmaceutical composition containing them.

摘要

ew 4-anilinopyrimidine derivatives of formula (I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="28" wi="67" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>(wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>R' and R<Sup>2</Sup> are the same or different and each represents a C<Sub>1</Sub> - C<Sub>6</Sub> alkyl group or R<Sup>1</Sup> and R<Sup>2</Sup> together represent a C<Sub>3 </Sub>- C<Sub>5</Sub> alkylene group;</ListItem><ListItem>R<Sup>3</Sup> represents a hydrogen atom or a C<Sub>1</Sub> - C<Sub>6</Sub> alkyl group;</ListItem><ListItem>n is 0, 1 or 2; and</ListItem><ListItem>R<Sup>4</Sup> represents a C, - C<Sub>6</Sub> alkyl group, a C<Sub>1</Sub> - C<Sub>6</Sub> alkoxy group, a C, - C<Sub>6</Sub> haloalkyl group, a halogen atom, a nitro group, a C<Sub>1</Sub> - C<Sub>6</Sub> alkanesulphonyl group, a cyano group, a carboxy group or a C<Sub>2</Sub>- C<Sub>7</Sub> alkoxycarbonyl group and, when n is 2, the two groups represented by R<Sup>4</Sup> may be the same or different or they may together represent a methylenedioxy group)</ListItem></UnorderedLists>
and pharmaceutically acceptable acid addition salts thereof have been found to have strong antidepressant activity, with low toxicity and very few side-effects. The compounds may be formulated in conventional pharmaceutical compositions for administration by various routes and may be prepared by reacting a 4-halopyrimidine with aniline or an aniline derivative.