PROCESS FOR PRODUCING LACTAM DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS

The invention provides potent and selective antagonists of 5-HT at 5-HT3 receptors which are tricyclic lactams of the formula (I) (I) wherein Im represents an imidazolyl group of the formula: and R1 represents a hydrogen atom or a group selected from C1-6alkyl, C3-6alkenyl, C3-10alkynyl, C3-7cycloal...

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Bibliographische Detailangaben
Hauptverfasser: COATES,IAN HAROLD,GB, OXFORD,ALEXANDER WILLIAM,GB, PRICE,BARRY JOHN,GB, NORTH,PETER CHARLES,GB
Format: Patent
Sprache:eng
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Zusammenfassung:The invention provides potent and selective antagonists of 5-HT at 5-HT3 receptors which are tricyclic lactams of the formula (I) (I) wherein Im represents an imidazolyl group of the formula: and R1 represents a hydrogen atom or a group selected from C1-6alkyl, C3-6alkenyl, C3-10alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, phenylC1-3alkyl, -CO2R5, -COR5, -CONR5R6 or -SO2R5; one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6alkyl, C3-7cycloalkyl, C3-6alkenyl, phenyl or phenylC1-3alkyl group, and each of the other two groups, which may be same or different, represents a hydrogen atom or a C1-6alkyl group; Y represents the group CH=CH or (CH2)n, wherein n represents 2 or 3; Q represents a halogen atom, or a group selected from hydroxy, C1-4alkoxy, phenylC1-3alkoxy, C1-6alkyl, cyano, phenyl which may be unsubstituted or substituted by one or more C1-4alkyl, C1-4alkoxy or hydroxy groups or halogen atoms, -NR7R8, -CONR7R8 , -(CH2)pCONR7R8, -(CH2)qNR9R10 or -(CH2)2CO2R11; Q' represents a hydrogen or a fluorine atom; and physiologically acceptable salts and solvates thereof.