Lactam derivatives

Details Lactam derivatives Lactam derivatives

C - Chemistry, Metallurgy

07

D

167/209, 167/231

C07D 471/04 (2006.01) A61K 31/44 (2006.01) C07D 487/04 (2006.01)

Patent

CA 1336906

The invention relates to tricyclic lactams of the general formula (I) Image (I) 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-, -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; 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 or -(CH2)pCONR7R8 (wherein R7 and R8, which may be the same of 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 p represents 1,2 or 3), -(CH2)qNR9R10 (wherein R9 represents a hydrogen atom or a C1-4alkyl group, and R10 represents a group -COR11 or -502R11 wherein R11 represents a C1-4alkyl group; and q represents 0, 1, 2 or 3), or -(CH2)2C02R11(R11 being as defined previously); Q' represents a hydrogen or a fluorine atom; 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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