Solvay Pharmaceuticals, B.v.

Solvay Pharmaceuticals, Gmbh

Duphar International Research Bv

Abbvie B.v.

Abbott Healthcare Products B.v.

Herman H Van Stuivenberg

Josephus H M Lange

Cornelis G Kruse

Arnoldus H J Herremans

Jacobus Tipker

Hiskias G Keizer

Tinka Tuinstra

Ineke Van Wijngaarden

Gustaaf J M Van Scharrenburg

Andrew C McCreary

Jacobus A J Den Hartog

Jacobus A Den Hartog

Roelof W Feenstra

Bernard J Van Vliet

Maria L Pras-Raves

Jan-Willem Terpstra

Samuel David

Daniel Jasserand

Jessica A R Dijksman

Josephus HM Lange

Leonardus AJM Sliedregt

Andrew C Mccreary

The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CBreceptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CBreceptors are involved. The compounds have the general formula (I) wherein R-Rhave the meanings given in the specification.

1H-imidazole derivatives as cannabinoid CB2 receptor modulators

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 invention relates to a group of novel benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these imidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1): wherein the symbols have the meanings as given in the description.

Benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors

The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.

Hydronopol substituted benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors

The present invention relates to 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives as CBantagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said pyrazole derivatives. 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 (I) wherein the symbols have the meanings given in the specification.

1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives having CB1-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.

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.

The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R-Rand X have the meanings given in the specification.

1 H-imidazole derivatives as cannabinoid receptor modulators

The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

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.

1H-imidazole derivatives as cannabinoid receptor modulators

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

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.

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Weesp, Netherlands

Herman H Van Stuivenberg