Radiolabeled neuropeptide y y5 receptor antagonists

Details Radiolabeled neuropeptide y y5 receptor antagonists Radiolabeled neuropeptide y y5 receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 491/048 (2006.01) A61K 31/506 (2006.01) A61K 51/00 (2006.01) A61K 51/04 (2006.01) C07D 491/04 (2006.01) G01N 33/566 (2006.01) G01N 33/60 (2006.01)

Patent

CA 2454228

The present invention is directed to radiolabeled neuropeptide Y Y5 receptor antagonists of the formula: (see above formula) which can be labeled with a radionuclide selected from the group consisting of: 3H, 11C, 18F, 15O and 13 N; analogs of this compound could be labeled with 1251, 123I, 131I, 75Br, 15O, 13N, 211At, 82Br, 77Br or 76Br; particular antagonists include [11C] trans-N-[5-(2-fluorophenyl)-2-pyrimidinyl]-3-oxospiro[5- azaisobenzofurane-1(3H),1'-cyclohexane]-4'-carboxamide and [18F] trans-N-[5-(2- fluorophenyl)-2-pyrimidinyl]-3-oxospiro[5-azaisobenzofurane-1(3H),1'- cyclohexane]- 4'-carboxamide and pharmaceutically acceptable salts thereof; the antagonists are useful for the labeling and diagnostic imaging of neuropeptide Y Y5 receptors in mammals.

L'invention concerne des antagonistes radiomarqués du récepteur Y5 du neuropeptide Y, qui sont utiles pour le marquage et l'imagerie de diagnostic des récepteurs Y5 du neuropeptide Y chez les mammifères.

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