Deuterated 1-piperazino-3-phenyl indanes for treatment of schizophrenia
AssigneeH. Lundbeck A/S
InventorsMorten JORGENSEN, Peter Hongaard ANDERSEN, Klaus Gjervig JENSEN
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Abstract
The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.
Claims11
A process for the preparation of a compound of formula (S)-(XV):
- comprising treatment of a compound of formula (XIV)
- with ((R)-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl)(norbornadiene)rhodium(I)tetrafluoroborate.
A process for the preparation of a compound of formula (1R,3S)-(IV)-tartrate,
- -tartrate comprising treatment of racemic trans-1-(6-chloro-3-phenyl(d5)-indan-1-yl)-1(d3), 2,2-trimethyl piperazine with L-(+)-tartaric acid.
A polymorph of the hydrogen tartrate salt of compound (IV) having the XRPD pattern as shown in FIG. 18.
Dependencies are inferred from the claim text.