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Last Updated: April 26, 2024

Claims for Patent: 5,158,952


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Summary for Patent: 5,158,952
Title: 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
Abstract:The present invention relates to novel 3-piperidinyl-1,2-benzisoxazoles having long-acting antipsychotic properties and which are useful in the treatment of warm-blooded animals suffering from psychotic diseases. Methods of preparing said compounds and compositions containing the same.
Inventor(s): Janssen; Cornelus G. M. (Vosselaar, BE), Knaeps; Alfonsus G. (Herentals, BE), Kennis; Ludo E. J. (Turnhout, BE), Vandenberk; Jan (Beerse, BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Application Number:07/422,847
Patent Claims: 1. A compound selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetr ahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, a pharmaceutically acceptable acid addition salt thereof, and an enantiomeric form thereof.

2. An antipsychotic composition comprising an inert carrier and as active ingredient an antipsychotic effective amount of a compound selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetr ahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, a pharmaceutically acceptable acid addition salt thereof, and an enantiomeric form thereof.

3. A method of treating warm-blooded animals suffering from psychotic diseases, which method comprises the administration to said warm-blooded animals of an antipsychotic effective amount of a compound selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetr ahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, a pharmaceutically acceptable acid addition salt thereof, and an enantiomeric form thereof.

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