Substituted imidazolylmethyltetrahydro-carbazolones.

摘要

The invention relates to compounds of the general formula (I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="27" wi="83" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>R' represents a group CO<Sub>2</Sub>R<Sup>5</Sup>, COR<Sup>5</Sup>, CONR<Sup>5</Sup>R<Sup>6</Sup> or SO<Sub>2R</Sub><Sup>5</Sup> (wherein R<Sup>5</Sup> and R<Sup>6</Sup>, which may be the same or different, each represents a hydrogen atom, a C<Sub>1-6</Sub> alkyl or C<Sub>3</Sub>.<Sub>7</Sub> cycloalkyl group, or a phenyl or phenyl- (C<Sub>1-4</Sub>) alkyl group in which the phenyl group is optionally substituted by one or more C<Sub>1-4</Sub> alkyl, C<Sub>1-4</Sub>, alkoxy or hydroxy groups or halogen atoms, with the proviso that R<Sup>5</Sup> does not represent a hydrogen atom when R' represents a group CO<Sub>2</Sub>R<Sup>5</Sup> or SO<Sub>2</Sub>R<Sup>5</Sup>); and one of the groups represented by R<Sup>2</Sup>, R<Sup>3</Sup> and R<Sup>4</Sup> is a hydrogen atom or a C<Sub>1-6</Sub> alkyl, C<Sub>3-7</Sub> cycloalkyl, C<Sub>2-6</Sub> alkenyl or phenyl-(C<Sub>1-3</Sub>)alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C<Sub>1-6</Sub> alkyl group; and physiologically acceptable salts and solvates thereof.</ListItem></UnorderedLists>

The compounds are potent and selective antagonists of "neuronal" 5-hydroxytryptamine receptors and are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania); anxiety; pain; gastric stasis; symptoms of gastrointestinal dysfunction such as occur with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence; migraine; and nausea and vomiting.