Duphar International Research Bv

Other

Ineke Van Wijngaarden

Derk Hamminga

Wouter Wouters

Hans H Haeck

Cornelis G Kruse

Johannes A Van Der Heyden

Jacobus A Den Hartog

Roelof Van Hes

Jan Hartog

Johannes W Jansen

Martinus T Tulp

Berend Olivier

Antonius Hulkenberg

Herman H Van Stuivenberg

Jan Van Dijk

Johannes M Zwagemakers

Maurits E Vandewalle

Josephus H Lange

Raghunathan V Nair

Dirkje A Van Dalen-Van Der Aa

Karin J Van Charldorp

Johan T Van Der Eycken

Rolf Van Hes

Christophorus M Keet

Donald T Witiak

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 a group of new 3,4-dehydropiperidine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1-3 carbon atoms;

3,4-dehydropiperidine derivatives

The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.

Phenylalkyl amine derivatives having anti-ischaemic activity

The invention relates to a group of new 8,9-annelated-.beta.-carbolines and 8,9-annelated-3,4-dihydro-.beta.-carbolines having interesting fibrinolytic properties. In particular the compounds can be used as orally active fibrinolytics. The compounds have the general formulae 1 and 2 ##STR1## wherein R.sub.2 +R.sub.3 together with the carbon atom and the nitrogen atom to which they are bound and the intermediate carbon atom constitute a heterocyclic group consisting of 5-10 ring atoms.

8,9-annelated-.beta.-carbolines and 8,9-annelated

New 8,9-annelated-1,2,3,4-tetrahydro-.beta.-carboline derivatives of the formula ##STR1## wherein R.sub.1 -R.sub.7 are as defined herein; and pharmaceutically acceptable salts and prodrugs thereof. A method of dissolving blood clots using this compound and a pharmaceutical composition having fibrinolytic activity comprising this compound are also part of the present invention.

8,9-anellated-1,2,3,4-tetrahydro-.beta.-carboline derivatives

The present invention concerns 3,4-annelated benzimidazol-2(1H)-one 1-carboxylic acid derivatives of the formula ##STR1## wherein R.sub.0, Z, A, B and C are as defined herein. Such derivatives are useful in the treatment of symptoms which are caused by over-excitation of 5-hydroxytryptamine receptors.

3,4-annelated benzimidazol-2-(1H)-one 1-carboxylic acid derivatives

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

The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.

Annelated indolo [3,2,-C]lactams

1,7-Annelated esters and amides of indolecarboxylic acids having formula 2, ##STR1## wherein R.sub.1 is halogen;

1,7-annelated indolecarboxylic acid esters and amides

The present invention is concerned with compounds of formula 1 ##STR1## wherein R.sub.0 is alkyl, alkoxy or alkylthio having 1-4 carbon atoms, hydroxy, halogen,

Substituted 3,4-annelated benzimidazol-2(1H)-ones

The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.

Di- and tetrahydroisoquinoline derivatives

The invention relates to a group of new 1,4-diazepine derivatives of the formula ##STR1## wherein A represents a group of the formulae 2-10 ##STR2## These compounds have a strong anti-ulcer activity after oral administration.

1,4-diazepine derivatives having anti-ulcer activity

The invention relates to a group of new 3-N substituted carbamoyl-indole derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.

New 3-N substituted carbamoyl-indole derivatives

The invention relates to a group of new .beta.-carbolines, their bio-isosteric benzofuran and benzothiophene analogues, and to the preparation of these compounds. The new compounds can be represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are hydrogen, or R+R.sub.1 or R.sub.1 +R.sub.2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms;

Cytostatic beta-carbolines

The invention relates to a group of tertiary 2,5-dialkyl-3-phenylpiperidine derivatives, having opiate-antagonistic activity represented by general formula 4, ##STR1## wherein A.sub.1 is hydrogen, an optionally esterified hydroxyl group or mercapto group, a group NHA.sub.8 or --CONHA.sub.8, wherein A.sub.8 is hydrogen, alkyl having 1-6 C-atoms or alkylcarbonyl having 2-7 C-atoms;

Growing community of inventors

Weesp, Netherlands

Ineke Van Wijngaarden