Hydrazino-type n2s2 chelators

Details Hydrazino-type n2s2 chelators Hydrazino-type n2s2 chelators

C - Chemistry, Metallurgy

07

K

C07K 2/00 (2006.01) A61K 51/00 (2006.01) A61K 51/08 (2006.01) C07C 323/48 (2006.01) C07C 323/60 (2006.01) C07C 327/30 (2006.01) C07C 327/32 (2006.01) C07D 309/08 (2006.01) C07F 13/00 (2006.01) G01N 33/534 (2006.01) G01N 33/60 (2006.01)

Patent

CA 2169269

Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting radiolabelled compounds are useful in diagnosis and therapy. In formula (I) R1, R2, R5 and R6 are independently selected from H; carboxyl; C1-3alkyl; and C1-3alkyl substituted with a group selected from hydroxyl, sulfhydryl, halogen, carboxyl and aminocarbonyl, R3 and R4 are independently selected from H and a sulfur protecting group; X is selected from O, the group NH2+, and the group CH2; Y and Z are independently selected from the group CR1R2 and NR7; and R7 is selected from H, carboxyl, C1-3alkyl and C1-3alkyl substituted with a group selected from hydroxyl, carboxyl and halogen.

L'invention concerne des composés de chélation de radionucléides destinés à se conjuguer à des molécules de ciblage telles que des protéines, des peptides ou des anticorps. Les composés radiomarqués en résultant sont utiles dans le diagnostic ainsi qu'en thérapie et répondent à la formule (I), dans laquelle R1, R2, R5 et R6 sont choisis indépendamment parmi H, carboxyle, alkyle C1-3, et alkyle C1-3 substitué par un groupe choisi parmi hydroxyle, sulfhydryle, halogène, carboxyle et aminocarbonyle; R3 et R4 sont choisis indépendamment parmi H et un groupe protecteur de soufre; X est choisi parmi O, le groupe NH2<+> et le groupe CH2; Y et Z sont choisis indépendamment parmi le groupe CR1R2 et NR7 est choisi parmi H, carboxyle, alkyle C1-3 et alkyle C1-3 substitué par un groupe choisi parmi hydroxyle, carboxyle et halogène.

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