Solvay Pharmaceuticals, B.v.

Tinka Tuinstra

Herman H Van Stuivenberg

Gustaaf J M Van Scharrenburg

Jacobus A J Den Hartog

Cornelis G Kruse

Josephus H M Lange

Roelof W Feenstra

Hiskias G Keizer

Maria L Pras-Raves

Jan-Willem Terpstra

Samuel David

Daniel Jasserand

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

The invention relates to a group of hydronopol substituted 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 novel benzimidazolone 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.

Hydronopol substituted benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors

The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission. 

Neurotensin active 2,3,diaryl-pyrazolidine derivatives

Growing community of inventors

Weesp, Netherlands

Tinka Tuinstra