Methods for preparing perfluorinated [ 18 f]-radiolabelled...

Drug – bio-affecting and body treating compositions – In vivo diagnosis or in vivo testing – Magnetic imaging agent

Reexamination Certificate

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C424S181100, C424S001890, C548S338100

Reexamination Certificate

active

07108846

ABSTRACT:
The present invention relates to chemical synthesis of radiolabelled perfluorinated bioactive compounds. More particularly, the present invention relates to radiolabelled compounds to be used as indicators for tissue hypoxia. More particularly, the present invention relates to the synthesis and the use of [18F] labelled perfluorinated nitroimidazole compounds having an incorporation of [18F] atoms characterized by a specific radioactivity of the compound comprised between 1 and 30 Ci/mmol, preferably between 1 and 20 Ci/mmol, preferably 1 and 10 Ci/mmol. More particularly to [18F] labelled EF3 or [18F] labelled EF5. The present invention also relates to a method for the detection of tissue hypoxia in a patient comprising introducing an [18F] labelled nitroimidazole compound into said patient, imaging tissue hypoxia in said patient, and, quantifying tissue hypoxia in said patient.

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Kachur AV, et al. Synthesis of new hypoxia markers EF1 and [18F]-EF1. Applied Radiation and Isotopes. 1999;51:643-50.
J.B. Dickey et al., Fluorinated Aminoanthraquinon Dyes, Industrial and Engineering Chemistry, vol. 48, 1956, 209-213, XP-000874162, USA.
Olivier Josse et al, A Convenient Synthesis of Ethyl 3-Aminopropanedithioate (Beta-Alanine Ethyl Dithioester) Synthesis, Mar. 1999, 404-406, XP-002129104, Germany and USA.

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