Duphar International Research Bv

U.S. Philips Corporation

Jan Hartog

Johannes M Zwagemakers

Ineke Van Wijngaarden

Berend Olivier

Cornelis G Kruse

Johannes A Van Der Heyden

Johannes Mos

Roelof Van Hes

Wouter Wouters

Bartholomeus J Van Steen

Jacques Schipper

Dirkje A Van Dalen-Van Der Aa

Lneke Van Wijngaarden

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

The invention relates to new compositions with pyschotropic activity which comprise a compound of formula 1 of the formula sheet as the active substance. The compounds of formula 1 are for the greater part new compounds. The invention therefore also relates to these new compounds and to the preparation thereof in a manner known for the synthesis of analogous compounds.

Bibyclic heteroacrylpiperazine derivatives having psychotropic activity,

The invention relates to 3,4-dehydropiperidine derivatives having psychotropic activity, which compounds are represented by the general formula 1 ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.3 alkyl;

3,4-dehydropiperidine derivatives having psychotropic activity

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

Blood-pressure lowering compounds having a structure as shown in the accompanying formula sheets.

Blood-pressure lowering 4-bicyclic-1-piperazinyl-alkyl amides

The invention relates to a group of new bicyclic heteroarylpiperazine derivatives of formula 1. It was found that these compounds have interesting psychotropic in particular anti-psychotic properties. The compounds can be prepared according to methods known for the synthesis of analogous compounds.

Method of treating psychotropic conditions employing substituted

Tertiary amines of formula 3 have a strong and prolonged spasmolytic effect, also after oral administration, on the smooth musculature of the tractus gastrointestinalis, the tractus urogenitalis and the bronchial system and have a low toxicity. The compounds can be synthetized according to methods known per se and been formulated to pharmaceutical compositions.

Spasmolytics

Novel substituted aromatic aliphatic amino carboxylic acids containing a tertiary nitrogen atom such as 3-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)] ethylamino] -1-propane carboxylic acid ethyl ester or 7-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)] ethylamino] -1-heptane carboxylic acid ethyl ester have been found to be useful spasmolytic agents.

Aralkylamino carboxylic acids and derivatives having spasmolytic activity

An aralkylamino sulfone such as 4- [n-ethyl -[1-methyl-2-(4-methoxy-phenyl)] ethylamino] -butyl sulfone is useful as a spasmolytic for the smooth muscle system.

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Weesp, Netherlands

Jan Hartog