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Title:
6-(4-ARYLALKYLPIPERAZIN-1-YL)BENZODIOXANE AND 6-(4-ARYLALKYLPIPERAZIN-1-YL)CHROMANE DERIVATIVES: DOPAMINE RECEPTOR SUBTYPE SPECIFIC LIGANDS
Document Type and Number:
WIPO Patent Application WO2000000489
Kind Code:
A3
Abstract:
Disclosed are compounds of formula (I) or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 and R5 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, trifluoromethyl or trifluoromethoxy; and X is oxygen, a bond, C1-C2 alkylene or methyleneoxy, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

Inventors:
TRAN JENNIFER N (US)
THURKAUF ANDREW (US)
Application Number:
PCT/US1999/014426
Publication Date:
February 10, 2000
Filing Date:
June 25, 1999
Export Citation:
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Assignee:
NEUROGEN CORP (US)
TRAN JENNIFER N (US)
THURKAUF ANDREW (US)
International Classes:
A61K31/496; A61P25/00; A61P25/16; A61P25/18; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P43/00; C07D307/79; C07D311/58; C07D313/08; C07D319/18; C07D321/10; C07D405/04; (IPC1-7): C07D311/04; C07D307/79; C07D313/08; C07D319/18; C07D321/10; C07D405/04
Domestic Patent References:
WO1998033784A11998-08-06
WO1997045419A11997-12-04
WO1997044334A21997-11-27
WO1997041108A11997-11-06
Foreign References:
US5550129A1996-08-27
Other References:
ALLEN B. REITZ ET AL.: "n-aryl-n'-benzylpiperazines as potential antipsychotic agents", J. MED. CHEM., vol. 38, no. 21, 1995, columbus ohio, pages 4211 - 4222, XP002065378
S. SARATI ET AL.: "kinetics of piribedil and effects on dopamine metabolism: hepatic biotransformation is not a determinant of its dopaminergic action in rats", PSYCHOPHARMACOLOGY, vol. 105, 1991, pages 541 - 545, XP002065935
IZZY BOYFIELD ET AL.: "n-(substituted-phenyl)piperazines: Antagonists with high binding and functional selectivity for dopamine d4 receptors", BIOORGANIC &MEDICINAL CHEMISTRY LETTERS, vol. 6, no. 11, 1996, great britain, pages 1227 - 1232, XP002065936
MICHAEL S. HADLEY: "d4 Receptors and their Antagonists", MEDICINAL RESEARCH REVIEWS, vol. 16, no. 6, 1996, pages 507-526, XP000654693
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