Xanthene and thioxanthene derivatives, compositions thereof and treatment therewith
AssigneeKefalas A/S
InventorsNiels Lassen, Klaus P. Boges, Peter B. Hansen, Jorn L. M. Buus, Allan J. Bigler
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AssigneeKefalas A/S
InventorsNiels Lassen, Klaus P. Boges, Peter B. Hansen, Jorn L. M. Buus, Allan J. Bigler
Estimating the term…
The present invention relates to novel thioxanthene and xanthene derivatives which have useful pharmacodynamic activity, such as neuroleptic activity and antiemetic activity, methods for the preparation of said derivatives, pharmaceutical compositions containing same, and a method for the treatment of psychic disorders by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings. The new compounds of the present invention correspond to the Formula I: ##STR1## wherein X is a halogen atom, an alkyl group with from one to four carbon atoms inclusive, an alkyloxy group with from one to four carbon atoms inclusive, a methylthio group, a methylsulphonyl group, a dimethylsulfamoyl group, a trifluoromethyl group or an acetyl group; Y is hydrogen, fluorine or a methyl group; Z is oxygen or sulphur; n is an integer from zero to three inclusive, and R is a cycloalkyl group with from four to six carbon atoms inclusive in the ring substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amino groups, acetamido groups, mesylamino groups or oxo groups, a five- or six-: membered saturated heterocyclic ring having one or two heteroatoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group or oxo group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twentytwo carbon atoms inclusive, as well as their non-toxic pharmaceutically acceptable acid addition salts with the proviso that methyl is present only when one of the other named substituents is also present.
A compound selected from the group consisting of
1-(Trans-4-hydr oxycyclohexylmethyl)-4-(2-trifluoromethyl-6-fluoro-9-thioxanthenylidene)pip eridine.
1-(Ci s-3,4,5-trihydroxycyclohexylmethyl)-4-(2-trifluoromethyl-6-fluoro-9-thioxan thenylidene)piperidine.
1-(Trans-4-aminocycl ohexylmethyl)-4-(2-trifluoromethyl-6-fluoro-9-thioxanthenylidene)piperidine
Dependencies are inferred from the claim text.