The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Apr. 14, 2009
Filed:
Mar. 26, 2003
Anne Simone Josephine Lesage, Halle-Zoersel, BE;
François Paul Bischoff, Vosselaar, BE;
Cornelus Gerardus Maria Janssen, Vosselaar, BE;
Hilde Lavreysen, Lommel, BE;
Anne Simone Josephine Lesage, Halle-Zoersel, BE;
François Paul Bischoff, Vosselaar, BE;
Cornelus Gerardus Maria Janssen, Vosselaar, BE;
Hilde Lavreysen, Lommel, BE;
Janssen Pharmaceutica N.V., Beerse, BE;
Abstract
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 —R—R—, which represents a bivalent radical of formula -Z-CH—CH—CH— or -Z-CH—CH— 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 —CH—CH—CH—CH—; 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.