Multidentate AZA ligands able to complex metal ions and the use thereof in diagnostics and therapy

摘要

Compounds of general formula (I): in which: R₁ through R₅ are as defined in the specification FG, which can be the same or different, are carboxy, -PO₃H₂ or -RP(O)OH groups, wherein R is hydrogen, or an optionally substituted group selected from C₁-C₂₀ alkyl, C₃-C₁₀ cycloalkyl, C₄-C₂₀ cycloalkylalkyl, aryl, arylalkyl, a group bearing an acidic moiety, and a group bearing an amino moiety, each of which may be further optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among ²⁰³Pb, ⁶⁷Ga, ⁶⁸Ga, ⁷²As, ¹¹¹In, ¹¹³In, ⁹⁰Y, ⁹⁷Ru, ⁶²Cu, ⁶⁴Cu, ⁵²Fe, ^52mMn, ¹⁴⁰La, ¹⁷⁵Yb, ¹⁵³Sm, ¹⁶⁶Ho, ¹⁴⁹Pm, ¹⁷⁷Lu, ¹⁴²Pr, ¹⁵⁹Gd, ²¹²Bi, ⁴⁷Sc, ¹⁴⁹Pm, ⁶⁷Cu, ¹¹¹Ag, ¹⁹⁹Au, ¹⁶¹Tb, ⁵¹Cr, ¹⁶⁷Tm, ¹⁴¹Ce, ¹⁶⁸Yb, ⁸⁸Y, ¹⁶⁵Dy, ¹⁶⁶Dy, ⁹⁷Ru, ¹⁰³Ru, ¹⁸⁶Re, ¹⁸⁸Re, ^99mTc, ²¹¹Bi, ²¹²Bi, ²¹³Bi, ²¹⁴Bi, ¹⁰⁵Rh, ¹⁰⁹Pd, ^117mSn, ¹⁷⁷Sn and ¹⁹⁹Au, as well as the salts thereof with physiologically compatible bases or acids.