Oxa-, thia- and diazabicycloalkane derivatives, process for their preparation and their use as pharmaceuticals.

摘要

Compounds of formula (I) or a pharmaceutically acceptable salt thereof:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="28" wi="81" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein:
<UnorderedLists id="ula01" listStyle="none"><ListItem>j is 0 or 1;</ListItem><ListItem>q is 0, 1 or 2;</ListItem><ListItem>p is 0 and r is 2 or 3, or</ListItem><ListItem>p is 1 and r is 2;</ListItem><ListItem>X is 0, S, SO or NR where R is hydrogen, C<Sub>1-6</Sub> alkyl or C<Sub>1-10</Sub> carboxylic acyl;</ListItem><ListItem>Y is NH; or 0 when R, is hydrogen; either R, is C<Sub>1-6</Sub> alkoxy and one of R<Sub>2</Sub>, R<Sub>3</Sub> and R<Sub>4</Sub> is hydrogen and the other two are selected from hydrogen, halogen, CF<Sub>3</Sub>, C<Sub>1-6</Sub> alkylthio, C<Sub>1-7</Sub> acyl, C<Sub>1-10</Sub> carboxylic acyiamino, C<Sub>1-6</Sub>
alkyl S(O)n wherein n is 0, or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C<Sub>1-6</Sub> alkyl, C<Sub>3-8</Sub> cycloalkyl, C<Sub>3-8</Sub> cycloalkyl, C<Sub>3-8</Sub> cycloalkyl C<Sub>1-4</Sub> alkyl or phenyl C<Sub>1-4</Sub> alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF<Sub>3</Sub>, C<Sub>1-6</Sub> alkyl or C<Sub>1-6</Sub> alkoxy; or R, is hydrogen and R<Sub>2</Sub>, R<Sub>3</Sub> and R<Sub>4</Sub> are independently selected from hydrogen; C<Sub>1-6</Sub> alkyl. hydroxy, C<Sub>1-6</Sub> alkoxy, C<Sub>1-6</Sub> alkylthio or halo; or any two on adjacent carbon atoms together are C<Sub>1-2</Sub> alkylenedioxy and the third is hydrogen, C<Sub>1-6</Sub> alkyl, C<Sub>1-6</Sub> alkoxy or halo; one of R<Sub>5</Sub> and R<Sub>6</Sub> is hydrogen, C<Sub>1-6</Sub> alkyl, phenyl or phenyl-C<Sub>1-6</Sub> alkyl, which phenyl moieties may be substituted by C<Sub>1-6</Sub> alkyl, C<Sub>1-6</Sub> alkoxy or haiogen; and the other is hydrogen or C<Sub>1-6</Sub> alkyl; and</ListItem><ListItem>R<Sub>7</Sub> is hydrogen, C, alkyl, phenyl or phenyl-C<Sub>1-3</Sub> alkyl, which phenyl moieties may be substituted by C<Sub>1-6</Sub> alkyl, <!-- EPO <DP n="2"> -->C<Sub>1-6</Sub> alkoxy, CF<Sub>3</Sub> or halogen having gastric motility enhancing activity, anti-emetic activity and/or 5-HT receptor ant. agonist activity, a process and intermediates for their preparation and their use as pharmaceuticals.</ListItem></UnorderedLists>