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|Title:||Tricyclic 5-HT.sub.3 receptor antagonists|
|Abstract:||The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond; n is 1, 2 or 3; p is 0, 1, 2 or 3; q is 0, 1 or 2; each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino; each R.sup.2 is lower alkyl; and R.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1; z is 1, 2 or 3; and R.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.|
|Inventor(s):||Berger; Jacob (Los Altos Hills, CA), Clark; Robin D. (Palo Alto, CA), Eglen; Richard M. (Mountain View, CA), Smith; William L. (Sunnyvale, CA), Weinhardt; Klaus K. (San Francisco, CA)|
|Assignee:||Syntex (U.S.A.) Inc. (Palo Alto, CA)|
Patent Claim Types:|
see list of patent claims
|Compound; Use; Composition;|
|Country||Document Number||Estimated Expiration||Supplementary Protection Certificate||SPC Country||SPC Expiration|
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