C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/237, 260/305
C07D 403/06 (2006.01) A61K 31/415 (2006.01) C07D 403/14 (2006.01)
Patent
CA 1326032
ABSTRACT Tricyclic Ketones The invention relates to compounds of the general formula (I): Image (I) wherein Im represents an imidazolyl group of the formula: Image or Image 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; 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 C1-4 alkyl, 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; Q represents a hydrogen or a halogen atom, or a hydroxy, C1-4alkoxy, phenylC1-3alkoxy or C1-6alkyl group or a group -NR7R8 or -CONR7R8; R7 and R8, which may be the same or 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; n represents 1, 2 or 3; and A-B represents the group CH-CH2 or C=CH; 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.
552963
Bell James Angus
Bradshaw John
Coates Ian Harold
Ewan George Blanch
Humber David Cedric
Glaxo Group Limited
Riches Mckenzie & Herbert Llp
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