Alkyne derivatives as tracers for metabotropic glutamate...

C - Chemistry – Metallurgy – 07 – D

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C07D 417/06 (2006.01) A61K 51/04 (2006.01) C07B 59/00 (2006.01) C07D 213/06 (2006.01) C07D 213/65 (2006.01) C07D 277/22 (2006.01)

Patent

CA 2503245

The present invention is directed to isotopically labeled alkyne derivative compounds, particularly 11C, 13C,14C, 18F, 15O, 13N, 35S, 2H, and 3H labeled compounds. In particular, the present invention is directed to 11C, 13C, 14C, 18F, 15O, 13N, 35S, 2H, and 3H labeled heterocyclic alkynes and methods of their preparation. The present invention further includes a method of use of the 11C, 18F, 15O, or 13N labeled heterocyclic alkyne compounds as tracers in positron emission tomography (PET) imaging, particularly in the study of metabolic conditions in mammals, specifically conditions modulated by metabotropic glutamate receptors subtype 5 (mGluR5).

La présente invention concerne des composés dérivées d'alcyne marqués isotopiquement, en particulier des composés marqués au ?11¿C, ?13¿C, ?14¿C, ?18¿F, ?15¿O, ?13¿N, ?35¿S, ?2¿H, et au ?3¿H. La présente invention concerne plus particulièrement des alcynes hétérocycliques marqués au ?11¿C, ?13¿C, ?14¿C, ?18¿F, ?15¿O, ?13¿N, ?35¿S, ?2¿H, et au ?3¿H et leurs procédés de préparation. La présente invention concerne également un procédé d'utilisation des composés d'alcyne hétérocycliques marqués au ?11¿C, ?18¿F, ?15¿O, ou au ?13¿N comme marqueurs en imagerie tomographique par émission de positions (TEP), en particulier dans l'étude de troubles métaboliques chez les mammifères, et plus précisément de troubles modulés par les récepteurs du glutamate métabotropique de type 5 (mGluR5).

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