Solvay Pharmaceuticals, B.v.

Martinus Th M Tulp

Gustaaf J M Van Scharrenburg

Andrew C McCreary

Cornelis G Kruse

Wouter I Iwema Bakker

Hein K A C Coolen

Axel Stoit

Roelof Van Hes

Arnoldus H J Herremans

Jan H Van Maarseveen

Lechoslaw A Turski

Pieter Smid

Adrianus Van Den Hoogenband

Sander Vader

The present invention relates to a composition containing bifeprunox or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, including Parkinson's disease and restless leg syndrome.

Combination preparations comprising bifeprunox and a dopamine agonist

A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.

Combination preparations comprising SLV308 and a dopamine agonist

Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein Ris H or CH. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.

N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs

The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-Dreceptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof,wherein:

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The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH, CF, OCH, halogen, cyano and 5-CF-tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1&#x2013;3C); n has the value 0&#x2013;3; m has the value 0&#x2013;2; Rrepresents NH, NH-alkyl (1&#x2013;3C), dialkyl (1&#x2013;3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH-piperazinyl; Ris hydrogen, alkyl (1&#x2013;4C) or phenyl, or Rtogether with (CH)wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; Rand Rindependently represent hydrogen or methyl, or Rand Rtogether are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved 

Piperazine oxime dervatives having NK-1 receptor antagonistic activity

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Weesp, Netherlands

Martinus Th M Tulp