C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/208, 260/276
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.
Bays David E.
Coates Ian H.
North Peter C.
Oxford Alexander W.
Bays David E.
Coates Ian H.
Glaxo Group Limited
North Peter C.
Oxford Alexander W.
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