Janssen Pharmaceutica Nv

Anne Simone Josephine Lesage

Johannes Wilhelmus John F Thuring

Theodorus Dinklo

Gregor James MacDonald

Dominique Jean-Pierre Mabire

Marcel Frans Leopold De Bruyn

Alain Philippe Poncelet

Sophie Philippe Coupa

Wei Zhuang

Marc Gaston Venet

Yves Emiel Maria Van Roosbroeck

François Paul Bischoff

Frans Alfons Maria Van Den Keybus

Hilde Lavreysen

Cornelus Gerardus Maria Janssen

James Edward Stewart Duffy

Christopher James Grantham

Marc Venet Gaston

This invention concerns the use of a compound of formula (I) 

2-aniline-4-aryl substituted thiazole derivatives

The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).  The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.

Trisubstituted 1,2,4 triazoles

The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy.  The invention particularly relates to a potent positive allosteric modulator of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.

1,3,5-trisubstituted triazole derivative

The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).  The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.

Trisubstituted 1,2,4-triazoles

The present invention concerns compounds of formula. In a preferable embodiment, X represents O; Rrepresents Calkyl; cycloCalkyl or (cycloCalkyl)Calkyl, wherein one or more hydrogen atoms in a Calkyl-moiety or in a cycloCalkyl-moiety optionally may be replaced by Calkyloxy, aryl, halo or thienyl; Rrepresents hydrogen; halo; Calkyl or amino; Rand Reach independently represent hydrogen or Calkyl; or Rand Rmay be taken together to form &#x2014;R&#x2014;R&#x2014;, which represents a bivalent radical of formula -Z-CH&#x2014;CH&#x2014;CH&#x2014; or -Z-CH&#x2014;CH&#x2014; with Zbeing O or NRwherein Ris Calkyl; and wherein each bivalent radical is optionally substituted with Calkyl; or Rand Rmay be taken together to form a bivalent radical of formula &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;; Rrepresents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

Metabotropic glutamate receptor antagonists

The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and their preparation; it further relates to compositions comprising them, as well as their use for marking and identifying metabotropic glutamate receptor sites and for imaging an organ.  In a preferable embodiment, X represents O; Rrepresents Calkyl; cycloCalkyl or (cycloCalkyl)Calkyl, wherein one or more hydrogen atoms in a Calkyl-moiety or in a cycloCalkyl-moiety optionally may be replaced by Calkyloxy, aryl, halo or thienyl; Rrepresents hydrogen; halo; Calkyl or amino; Rand Reach independently represent hydrogen or Calkyl; or Rand Rmay be taken together to form &#x2014;R&#x2014;R&#x2014;, which represents a bivalent radical of formula -Z-CH&#x2014;CH&#x2014;CH&#x2014; or -Z-CH&#x2014;CH&#x2014; with Zbeing O or NRwherein Ris Calkyl; and wherein each bivalent radical is optionally substituted with Calkyl; or Rand Rmay be taken together to form a bivalent radical of formula &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;; Rrepresents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. Most preferred are radiolabelled compounds in which the radioactive isotope is selected from the group of ofH,C andF. The invention also relates to their use in a diagnostic method, in particular for marking and identifying a mGluR1 receptor in biological material, as well as to their use for imaging an organ, in particular using PET.

Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands

The present invention concerns compounds of formula. In a preferable embodiment, X represents O; Rrepresents Calkyl; cycloCalkyl or (cycloCalkyl)Calkyl, wherein one or more hydrogen atoms in a Calkyl-moiety or in a cycloCalkyl-moiety optionally may be replaced by Calkyloxy, aryl, halo or thienyl; Rrepresents hydrogen; halo; Calkyl or amino; Rand Reach independently represent hydrogen or Calkyl; or Rand Rmay be taken together to form &#x2014;R&#x2014;R&#x2014;, which represents a bivalent radical of formula &#x2014;Z&#x2014;CH&#x2014;CH&#x2014;CH&#x2014; or &#x2014;Z&#x2014;CH&#x2014;CH&#x2014; with Zbeing O or NRwherein Ris Calkyl; and wherein each bivalent radical is optionally substituted with Calkyl; or Rand Rmay be taken together to form a bivalent radical of formula &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;; Rrepresents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

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Halle-Zoersel, Belgium

Anne Simone Josephine Lesage