Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-08-31
1991-03-05
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514215, 514219, 5142282, 5142295, 514287, 540546, 540555, 544 14, 544 99, 544343, 546 70, C07D47104, A61K 31475
Patent
active
049978314
ABSTRACT:
The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl 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-HT.sub.3 receptors and are useful, for example in the treatment of psychotic disorders, anxiety and nausea and vomiting.
REFERENCES:
patent: 3299078 (1967-01-01), Prachter
patent: 3914421 (1975-10-01), Rajagopalan
patent: 4013652 (1977-03-01), Rajagopalan
patent: 4115577 (1978-09-01), Rajagopalan
patent: 4183936 (1980-01-01), Rajagopalan
patent: 4939136 (1990-07-01), Haeck et al.
Bays David E.
Coates Ian H.
North Peter C.
Oxford Alexander W.
Glaxo Group Limited
Haley Jacqueline
Lee Mary C.
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