Troponyl piperazines as dopamine D4 receptor ligands

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United States of America Patent

PATENT NO 5998414
SERIAL NO

08907672

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Described herein are compounds of the general formula: ##STR1## a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, wherein: R.sub.1 is H, halo, aryl or aryl substituted with one or two groups independently selected from halo, C.sub.1-4 alkyl, C.sub.1-4 -alkoxy, nitro, trifluoromethyl, trifluoromethoxy or cyano; R.sub.2 is C.sub.4-9 alkyl; phenyl or phenyl substituted with one or two groups selected independently from OH, cyano, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, trifluoromethyl, trifluoromethoxy, nitro or phenyl; naphthyl; phenyl fused to a 5 or 6-membered heterocycle; the coumarin moiety ##STR2## wherein R.sub.3 and R.sub.4 are selected independently from H, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; or 1,2-methylenedioxy phenyl; with the proviso that R.sub.2 is not phenyl or 3,4-dimethoxyphenyl when R.sub.1 is H. Also described is their use as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia and anxiety.

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Patent Owner(s)

Patent OwnerAddress
HOECHST MARION ROUSSEL INC2110 E GALBRAITH ROAD - P O BOX 156300 CINCINNATI OH 45215

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Fu, Jian-min Elmsford, NY 56 520
Treasurywala, Adi M Mississauga, CA 1 3
Wang, Xin Kirkland, CA 1487 14353

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