Solvay Pharmaceuticals, B.v.

Jan-Willem Terpstra

Gustaaf J M Van Scharrenburg

Cornelis G Kruse

Herman H Van Stuivenberg

Axel Stoit

Roelof W Feenstra

Andrew C McCreary

Bernard J Van Vliet

Jacobus A J Den Hartog

Maria L Pras-Raves

Tinka Tuinstra

Mayke B Hesselink

The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-Dreceptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification,and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.

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The invention relates to a group of novel benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these imidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1): wherein the symbols have the meanings as given in the description.

Benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors

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Weesp, Netherlands

Jan-Willem Terpstra