Lactam derivatives

Details Lactam derivatives Lactam derivatives

C - Chemistry, Metallurgy

07

D

167/208, 260/276

C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/44 (2006.01) A61K 31/55 (2006.01) C07D 209/00 (2006.01) C07D 221/00 (2006.01) C07D 223/00 (2006.01) C07D 487/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 1339022

The invention relates to tricyclic lactams of the general formula (I) (I) Image wherein Im represents an imidazolyl group of the formula: Image or Image 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, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO2R5, -COR5, -CONR5R6 or -SO2R5 (wherein R5 and R6, 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 R5 does not represent a hydrogen atom when R1 represents a group -CO2R5 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 the same or different, represents a hydrogen atom or a C1-6alkyl group; n represents 2 or 3; and physiologically acceptable salts and solvates thereof. The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.

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