3,4,5,6-Tetrahydro-2,6-methano-4 beta-amino-1-benzoxocin derivatives, process for their preparation and compositions containing them.

摘要

Compounds are disclosed of general formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="32" wi="53" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>R<Sub>1</Sub> represents a hydrogen atom or C<Sub>1-4</Sub> alkyl or C<Sub>2</Sub>-<Sub>4</Sub> alkenyl group, or the group COANH<Sub>2</Sub>, CSANH<Sub>2</Sub>, or COANHCOCH<Sub>2</Sub>NH<Sub>2</Sub> in which A is methylene optionally substituted by a C<Sub>1-3</Sub> alkyl group; and R<Sub>2</Sub> represents a hydrogen atom or a C<Sub>1-4</Sub> alkyl group; or NR<Sub>1</Sub>R<Sub>2</Sub> forms a piperidino, piperazino or N-methylpiperazino group;</ListItem><ListItem>R<Sub>3</Sub> represents a C<Sub>1-4</Sub> alkyl group or a benzyl group;</ListItem><ListItem>R<Sub>4</Sub> represents a hydrogen or halogen atom; and</ListItem><ListItem>R<Sub>5</Sub> represents a hydrogen atom or a C<Sub>1-4</Sub> alkyl or C<Sub>1-4</Sub> alkoxy group, with the proviso that one of R<Sub>4</Sub> and R<Sub>s</Sub> is a hydrogen atom and physiologically acceptable salts and bioprecursors thereof.</ListItem></UnorderedLists>

The compounds exert efforts on the central nervous system and, in particular exhibit anxiolytic and anti-convulsant activity. The compounds may be formulated with pharmaceutically acceptable carriers or diluents for administration in conventional manner.