| abstract |
The invention provides lactam derivatives of the general formula (I) <CHEM> wherein R<1> represents a hydrogen atom or a group selected from C1-6alkyl, C3-6alkenyl, C3-10alkynyl, C3-7cycloalkyl,C3-7cycloalkylC1-4alkyl, phenyl, phenylC1-3alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO2R<3>, -COR<3>, -CONR<3>R<4> or -SO2R<3> (wherein R<3> and R<4>, which may be the same or different each represents a hydrogen atom, a C1-6alkyl or C3-7cycloalkyl group, or a phenyl or phenylC1-4alkyl group, in which the phenyl group is optionally substituted by one or more C1-4alkyl, C1-4alkoxy or hydroxy groups or halogen atoms, with the proviso that R<3> does not represent a hydrogen atom when R<1> represents a group -CO2R<3> or -SO2R<3>); and R<2> represents a group of formula (a), (b) or (c): <CHEM> wherein R<5> represents a hydrogen atom or a C1-6alkyl, C3-7cycloalkyl, C3-6alkenyl or phenylC1-3alkyl group; n represents 2, 3 or 4; Q represents a hydrogen or a halogen atom, or a hydroxy, C1-4alkoxy, phenylC1-3alkoxy or C1-6alkyl group or a group -NR<6>R<7> or -CONR<6>R<7> wherein R<6> and R<7>, which may be the same or different, each represents a hydrogen atom or a C1-4alkyl or C3-4alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring); and physiologically acceptable salts and solvates thereof. The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT3 receptors and are useful, for example in the treatment of psychotic disorders, anxiety and nausea and vomiting. |