Duphar International Research Bv

Johannes Mos

Jan Hartog

Cornelis G Kruse

Gustaaf J M Van Scharrenburg

Roelof W Feenstra

Gerben M Visser

Johannes A M Van Der Heijden

Stephen K Long

Bartholomeus J Van Steen

Gerrit P Toorop

Jacques Schipper

The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S is hydrogen, halogen, alkyl (1-3C), CN, CF , OCF , SCF , alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR , S, CH , O, SO or SO , wherein R is H or alkyl (1-3C); . . . Z represents &boxH;C or &mdash;N; &mdash;R independently represent H or alkyl (1-3C), or R and R together can form a bridge 2 or 3 C-atoms; R is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl&mdash;methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D -receptor agonism and partial serotonin 5-HT -receptor agonism mediated activities.

Piperazine and piperidine compounds

The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 ##STR1## wherein R.sub.1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano,

2,3-dihydro-1,4-benzodioxin-5-yl-piperazine derivatives having 5-HT

It has been found that a group of piperazine derivatives known to have blood-pressure lowering properties possess good anxiolytic properties. In two well known animal test models the compounds are active when used intraperitoneally in dosages of 0.3 mg/kg.

Anxiolytically active piperazine derivatives

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Weesp, Netherlands

Johannes Mos