Solvay Pharmaceuticals, B.v.

Mayke B Hesselink

Gustaaf J M Van Scharrenburg

Andrew C McCreary

Roelof W Feenstra

Cornelis G Kruse

Wouter I Iwema Bakker

Hein K A C Coolen

Axel Stoit

Bernard J Van Vliet

Jan H Van Maarseveen

Maria L Pras-Raves

Peter H Van Amsterdam

Jan-Willem Terpstra

Gijsbert D Kuil

Theodorus S M Koopman

Hendrink J Koster

Marinus Verhage

Dirk De Boer

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.

[object Object]

The present disclosure relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The disclosure also relates to the use of the compounds for the manufacture of a medicament giving a beneficial effect. The disclosure also relates to the use of the compounds for the manufacture of a medicament for treating a disease or condition. The disclosure further relates to the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

N-oxides as prodrugs of piperazine and piperidine derivatives

The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NKreceptor antagonistic activity represented by the general formula (1) wherein: Rrepresents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1&#x2013;3C), Rand Rindependently represent halogen, H, OCH, CHand CF, R, Rand Rindependently represent H, OH, O-alkyl(1&#x2013;4C), CHOH, NH, dialkyl(1&#x2013;3C)N, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or morpholin-4-yl substituted with one or two methyl or methoxymethyl groups, morpholin-4-ylamino, morpholin-4-ylmethyl, imidazol-1-yl, thiomorpholin-4-yl, 1,1-dioxothiomorpholin-4-yl or 3-oxa-8-azabicyclo[3.2.1]oct-8-yl; Rand Rtogether may represent a keto, a 1,3-dioxan-2-yl or a 1,3-dioxolan-2-yl group, X represents either O or S, n has the value of 1, 2 or 3, a is the asymmetrical carbon atom 8a, 9a or 10a when n equals 1, 2 or 3 respectively The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions containing at least one of these compounds as an active ingredient 

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Weesp, Netherlands

Mayke B Hesselink