Imidazollyl containing ketone derivatives

Details Imidazollyl containing ketone derivatives Imidazollyl containing ketone derivatives

1988-04-13

1990-04-17

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514397, 546113, 546168, 548336, 548342, 540524, A61K311415, A61K 3144, C07D46306, C07D47104

Patent

active

049180800

ABSTRACT:
The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group; Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.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; and an aromatic or heteroaromatic group as defined in the specification.
The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.

REFERENCES:
patent: 4006137 (1977-02-01), Haugwitz et al.
patent: 4808581 (1989-02-01), Oxford et al.
Fludzinski et al., "Indazoles as Indole Bioisosteres: Synthesis and Evaluation of the Tropanyl Ester and Amide of Indazole-3-carboxylate as Antagonists at the Serotonin 5HT.sub.3 Receptor", Journal of Medicinal Chemistry, vol. 30, No. 9 (Sep., 1987).

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