Solvay Pharmaceuticals, B.v.

Arqule, Inc.

Maria L Pras-Raves

Roelof W Feenstra

Cornelis G Kruse

Gustaaf J M Van Scharrenburg

Bernard J Van Vliet

Hiskias G Keizer

Josephus H M Lange

Herman H Van Stuivenberg

Axel Stoit

Gary R Gustafson

Andrew C McCreary

Jan H Reinders

Tinka Tuinstra

Mayke B Hesselink

Jan-Willem Terpstra

Jacobus Aj Den Hartog

Guustaaf Jm Van Scharrenburg

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 present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): whereinwherein the symbols have the meanings given in the specification.

[1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-S-transferase and NADPH quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular

The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-Areceptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient. The invention relates to compounds of the general formula (1) wherein Y represents a group of the general formula (A), (B) or (C) and all other symbols have the meanings as given in the description.

1,3,5-Triazine derivatives as ligands for human adenosine-A3 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

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Weesp, Netherlands

Maria L Pras-Raves