Isoquinolinone and dihydroisoquinolinone 5-HT.sub.3 receptor ant

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514307, 546126, 546133, 546137, 546141, 546142, A61K 3144, C07D45302

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active

054911486

ABSTRACT:
5-HT.sub.3 receptor antagonist compounds of Formula I: ##STR1## in which X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino;
R.sup.1 is hydrogen, lower alkyl, phenyl or halogen;
R.sup.2 is a group selected from Formulae (a), (b), (c) and (d): ##STR2##

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Scholtysik, et al., 5-Hydroxytryptamine Antagonist ICS 205-930 Blocks Cardiac Potassium, Sodium and Calcium Currents.sup.1, J. Pharmacol. Exp. Ther., 1988, vol. 245, No. 3, pp. 773-778.
Salituro, et al., Benzotriazinones as "Virtual Ring" Mimics of o-Methoxybenzamides: Novel and Potent 5-HT.sub.3 Receptor Antagonists, J. Med. Chem., 1990, vol. 33, pp. 2942-2944.
Berger, et al., U.S. patent application Ser. No. 07/704,565.
Berger, et al., U.S. patent application Ser. No. 07/442,082.

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