Solvay Pharmaceuticals, B.v.

Solvay Pharmaceuticals, Gmbh

Andrew C McCreary

Gustaaf J M Van Scharrenburg

Cornelis G Kruse

Martinus Th M Tulp

Wouter I Iwema Bakker

Roelof W Feenstra

Mayke B Hesselink

Josephus H M Lange

Herman H Van Stuivenberg

Hein K A C Coolen

Arnoldus H J Herremans

Jan H Van Maarseveen

Adrianus Van Den Hoogenband

Axel Stoit

Bernard J Van Vliet

Eric Ronken

Maria L Pras-Raves

Peter H Van Amsterdam

Jan-Willem Terpstra

Hendrink J Koster

Marinus Verhage

Jessica A R Dijksman

Dirk De Boer

Gijsbert D Kuil

Theodorus S M Koopman

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

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]

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

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

Computer game systems respond to the spatial state of a pointing device. Changes in the spatial state of a hand held or mobile unit, or plurality of units drive a game scheme maintained in a computer. Position and attitude of the mobile device cause program branching functions which are bases upon a game rule set. In example, a game scheme executed on a computing apparatus may be incorporated into a mobile telephone having a GPS and electronic compass. Physical states relating to position and pointing attitude of the telephone as described in part by position or attitude parameters, drives computer programming code to takes actions which depend on measured position and attitude values thus making computer games for mobile users are made highly interactive. User gestures including simple pointing actions allow a user to express desires to a computer in an express and direct fashion. These games have many features which cannot be found in more traditional handheld computer games which do not take into consideration the spatial state of an object controlled by a player-user 

The present invention relates to a group of 1H-1,2,4-triazole-3-carboxamide derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing at least one of these compounds as an active ingredient. These 1H-1,2,4-triazole-3-carboxamide derivatives are potent cannabinoid-CBreceptor agonists, partial agonists, inverse agonists or antagonists, useful for the treatment of disorders involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R-Rhave the meanings given in the specification.

The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NKreceptor antagonistic activity. The invention also relates to methods for the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient, as well as to the use of these compositions for the treatment of disorders in which neurokinin receptors are involved. The invention relates to compounds represented by the general formula (1) wherein the symbols have the meanings as given in the description.

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 

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

The invention relates to novel phenylpiperazine derivatives of the formula wherein: &mdash;R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.

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Weesp, Netherlands

Andrew C McCreary