A. H. Robins Company, Incorporated

Robert F Boswell

Harry R Munson, Jr

William J Welstead, Jr

William L Smith

Reevis S Alphin

Robert Louis Duncan, Jr

Derivatives of 2-amino-1-phenylethanol were prepared from substituted amines and benzoin, stilbene oxide or styrene oxide to give compounds of Formula: ##STR1## where R is H or (un)substituted phenyl and C is a linking group or terminal group. The compounds of this invention can inhibit ulceration in in-vivo studies in rats.

Derivatives of 2-amino-1-phenylethanol having antiulcer activity

A method of controlling emesis caused by non-platinum anti-cancer drugs with 2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is loweralkyl; and R.sub.2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, methylsulfonyl, loweralkoxy or Am and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof is disclosed.

2-alkoxy-N-(1-azabicyclo(2.2.2)oct-3-yl) benzamides and thiobenzamides

2-Alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is loweralkyl; and R.sub.2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, alkoxy or Am and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof having gastrokinetic and anti-emetic activity are disclosed.

2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides

1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones of the formula ##STR1## wherein R is hydrogen or fluoro, R.sup.1 is hydrogen, fluoro chloro, bromo or trifluoromethyl, and n is 2 to 4, having anticonvulsant activity and useful as anti-anxiety agents, are disclosed.

1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones

1-Substituted-3-aminoethoxypyrrolidines having the formula ##STR1## WHEREIN R is benzyl, 2-ethoxyphenoxylower-alkyl, 2-propionyloxy-ethyl, 2-methoxy-4-acetylphenoxylower-alkyl, 4-fluorophenoxy lower alkyl, benzoyloxylower-alkyl, 3,4,5-trimethoxybenzoyloxylower-alkyl, 3,4,5-trimethoxybenzoyl, N-(4-methoxyphenyl) carbamoyl, 2-methoxyphenoxylower-alkyl, 3,4,5-trimethoxyphenyl-acetyl, 2-piperidinoethyl or carbamoyl, and Am is dilower-alkylamino, morpholino or piperidino having hypotensive properties are disclosed.

1-Substituted-3-aminoethoxypyrrolidines and use thereof

10-[.omega.-(Benzoylpiperidinyl)alkyl]phenothiazines having the formula ##STR1## wherein R is hydrogen, chloro, bromo, trifluoromethyl, lower alkoxy, acetyl, sulfamoyl, or dimethylsulfamoyl, R.sup.1 is hydrogen, chloro, bromo, fluoro, trifluoromethyl, lower alkyl or lower alkoxy and n is 2, 3 or 4 are disclosed. Methods for the preparation of the compounds are described. The compounds possess tranquilizing activity and are useful as tranquilizing agents in mammals.

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Richmond, VA, United States of America

Robert F Boswell