Kefalas A/s

H. Lundbeck A/s

Niels Lassen

Jorn Lasse Buus

Allan J Bigler

Klaus P Bogeso

Peter Bregnedal Hansen

Klaus Gjervig Jensen

Klaus P Boges

The present invention relates to novel amino alkyl substituted urea derivatives as well as their acid addition salts with pharmaceutically acceptable acids, to methods for the preparation of said derivatives and pharmaceutical compositions containing same, and a method for the treatment of tumors therewith. The novel urea derivatives have shown pronounced anti-neoplastic activity when tested against various tumor models in animals. The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different and are selected from the group consisting of a phenyl group, each of said phenyl groups being optionally substituted with one or two groups selected from halogen, CF.sub.3, OH, or alkoxy (1-4 C-atoms); and R.sup.1 and R.sup.2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring; R.sup.3 and R.sup.4 are each selected from hydrogen, lower alkyl or alkenyl groups with from 1-6 carbon atoms inclusive, cyclopentyl or cyclohexyl; and n is 0 or 1, as well as pharmaceutically acceptable acid addition salts thereof. When X is different from Y and/or R.sup.3 is different from R.sup.4 the compounds of Formula I exist as optical isomers, which may be separated in the individual enantiomers, which often show the activity in different degree. These individual isomers as well as their isolation fall within the scope of the present invention.

Aminoalkyl substituted urea derivatives and method of treatment

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;

Xanthene and thioxanthene derivatives, compositions thereof, and

Xanthene and thioxanthene derivatives, compositions thereof and

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 corresponds 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;

Xanthene and thioxanthene derivatives

The present invention relates to novel behenic acid esters of the following general formula: ##STR1## wherein X is 'N' or 'CH,' the non-toxic acid addition salts thereof, a method for the preparation of said esters and therapeutic compositions thereof having prolonged effect.

Behenic acid esters, compositions thereof and a method of  preparation

Fluoro-substituted thiaxanthene derivatives as well as their non-toxic pharmaceutically acceptable acid addition salts having pronounced neuroleptic properties and a relatively low degree of undesired side effects, methods of preparation of said derivatives, pharmaceutical compositions containing same which may be administered to animals, including human beings, orally or parenterally.

Thiaxanthene derivatives

Thiaxanthene derivatives, compositions thereof and methods of treating

The present invention relates to the novel alpha-isomer of 2-chloro-9-[3'-(N'-2-hydroxyethylpiperazino-N)-propylidene]-thiaxanthene, carboxylic acid esters thereof, the non-toxic acid addition salts of these compounds, methods of preparing and purifying the said compounds, therapeutic compositions thereof and a method of treating psychotic patients therewith.

Compositions of and method of treating with the alpha-isomer of

Alpha-isomer of

Fluoro-substituted phenothiazine derivatives as well as their non-toxic pharmaceutically acceptable acid addition salts having pronounced neuroleptic properties and a relatively low degree of undesired side effects, a method for the preparation of said derivatives, pharmaceutical compositions containing same which may be administered to animals, including human beings, orally or parenterally.

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Gentofte, Denmark

Niels Lassen