Solvay Pharmaceuticals, B.v.

Solvay Pharmaceuticals, Gmbh

Arnoldus H J Herremans

Cornelis G Kruse

Josephus H M Lange

Herman H Van Stuivenberg

Jacobus Tipker

Andrew C McCreary

Wouter I Iwema Bakker

Hein K A C Coolen

Gustaaf J M Van Scharrenburg

Martinus Th M Tulp

Jan H Van Maarseveen

Adrianus Van Den Hoogenband

Jessica A R Dijksman

The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CBreceptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I), wherein R and R-Rhave the meanings given in the specification. 

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The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.

The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.

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 novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CBreceptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R&#x2013;Rhave the meanings given in the specification.

1H-imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity

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 present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component

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Weesp, Netherlands

Arnoldus H J Herremans