Lactam derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 471/16 (2006.01) A61K 31/475 (2006.01) A61K 31/535 (2006.01) C07D 498/16 (2006.01) C07D 513/16 (2006.01)

Patent

CA 2011107

ABSTRACT LACTAM DERIVATIVES The invention provides lactam derivatives of the general formula (I) (I) Image wherein n represents 2 or 3; Im represents an imidazolyl group of the formula : Image or Image wherein one of the groups represented by R1, R2 and R3 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 of different, represents a hydrogen atom or a C1-6alkyl group: Y represents a group -(CH2)m-, wherein m represents 2, 3 or 4; or Y represents a group -X(CH2)p-, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR4, where R4 is a C1-6alkyl group, and X is attached to the benzene ring moiety of the molecule; 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.

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