Bifunctional tridentate pyrazolyl containing ligands for re...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/14 (2006.01) A61K 51/04 (2006.01) A61P 35/00 (2006.01) C07D 231/12 (2006.01)

Patent

CA 2522326

The present invention relates to a chelating agent of the general formula: (I), wherein m is 0 or 1; X is NR4 or S; Y is SR5, NHR5 or P(R5)2; R1 and R3 are the same or different and are selected from H, alkyl or aryl; R2 is H, COOH, NHR6 or (CH2)nCOOR6; R4 is H, alkyl, aryl, (CH2)nCOOR6 or (CH2)nOR6; R5 is H, alkyl, aryl, (CH2)nCOOR6 or (CH2)nOR6, R6 is H, alkyl or aryl; n is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; and when R1=R3=CH3, R2, R4 and R5 are not all three H. The invention further relates to a method and kit for the preparation of radiolabeled biomolecules while using the chelating agent.

L'invention concerne un agent chélateur de formule générale (I), dans laquelle : m représente 0 ou 1; X représente NR¿4? ou S; Y représente SR¿5?, NHR¿5? ou P(R¿5?)¿2?; R¿1? et R¿3? sont identiques ou différents et sont choisis parmi H, alkyle ou aryle; R¿2? représente H, COOH, NHR¿6? ou (CH¿2?)¿n?COOR¿6?; R¿4? représente H, alkyle, aryle, (CH¿2?)¿n?COOR¿6? ou (CH2)¿n?OR¿6?; R¿5? représente H, alkyle, aryle, (CH¿2?)¿n?COOR¿6? ou (CH¿2?)¿n?OR¿6? ; R¿6? représente H, alkyle ou aryle; n représente 1, 2, 3, 4, 5, 6, 7, 8, 9 ou 10; et lorsque R¿1?=R¿3?=CH¿3?, R¿2?, R¿4? et R¿5? ne représentent pas tous les trois H. L'invention concerne également un procédé et un kit servant à préparer des molécules identifiées à l'aide d'un marqueur radioactif par l'utilisation dudit agent chélateur.

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