LABELLED PYRROLYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR USE IN DIAGNOSTIC METHODS
The present invention relates to certain labelled pyrrolyl-oxadizolyl-diazabicyclononane derivatives. Furthermore, the present invention relates to the use of said derivatives in their labelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).
1 . A labelled pyrrolyl-oxadiazole-diazabicyclononane derivative represented by Formula I
or a pharmaceutically acceptable salt thereof, wherein R represents a labelled C 1-6 -alkyl group.
2 . The labelled pyrrolyl-oxadiazole-diazabicyclononane derivative of claim 1 , wherein the C 1-6 -alkyl group is labelled by incorporation of one or more 11 C, 13 C or 14 C.
3 . The labelled pyrrolyl-oxadiazole-diazabicyclononane derivative of claim 1 , wherein R represents a labelled methyl or ethyl group.
4 . The labelled pyrrolyl-oxadiazole-diazabicyclononane derivative of claim 1 , which is
2-(1,4-Diazabicyclo[3.2.2]nonan-4-yl)-5-(1-[ 11 C]methylpyrrol-2-yl)-1,3,4-oxadiazole;
or a pharmaceutically acceptable salt thereof.
5 . A pharmaceutical composition comprising a diagnostically effective amount of a labelled pyrrolyl-oxadiazole-diazabicyclononane derivative of claim 1 , or a pharmaceutically acceptable addition salt thereof; together with at least one pharmaceutically acceptable carrier or diluent.
6 . The labelled pyrrolyl-oxadiazole-diazabicyclononane derivative of claim 1 , for use as a radiotracer to monitor in vivo and in vitro levels of nicotinic acetylcholine receptors, by way of non-invasive determination of the localisation of such receptors (neuroimaging).
7 . The use according to claim 6 , wherein the nicotinic acetylcholine receptor is of the nicotinic α7 receptor subtype.
8 . A method for the non-invasive determination of the distribution of a tracer compound inside a whole, intact living animal or human body, using a physical detection method, wherein the tracer compound is a labelled pyrrolyl-oxadiazole-diazabicyclononane derivative according to claim 1 , or a pharmaceutically acceptable salt thereof.
9 . The method of claim 8 , wherein the compound is labelled by incorporation of 11 C, 13 C or 14 C, and the isotope incorporation is measured by Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
10 . The method of claim 9 , wherein the compound is labelled by incorporation of 11 C, and the isotope incorporation is measured by Positron Emission Tomography (PET).
11 . The method of claim 8 , wherein the compound is 2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-(1-[ 11 C]methylpyrrol-2-yl)-1,3,4-oxadiazole.