ETHYLENEDIAMINETETRAACETIC ACID BIS(AMIDE) DERIVATIVES AND THEIR RESPECTIVE COMPLEXES WITH MN(II) ION FOR USE AS MRI CONTRAST AGENT

The present invention relates to novel substituted ethylenediaminetetraacetic acid bisamide derivatives, their complexes with Mn(II) ion and the use thereof as contrast agents for Magnetic Resonance Imaging (MRI) analysis. The present invention includes novel substituted ethylenediaminetetraacetic acid bisamide derivatives of general formula I, or a pharmaceutical acceptable salt thereof: wherein: n is 1, 2 or 3; and Ri and R2 are alkyl groups and at least one of them is substituted by a carboxyl group; or Ri and R2, taken together with the adjacent N atom, form a 5-6 membered unsubstituted aromatic ring; or Ri and R2, taken together with the adjacent N atom, form a 6-7 membered unsubstituted saturated ring; or Ri and R2, taken together with the adjacent N atom, form a 5-7 membered saturated ring substituted (i) by one or more hydroxyl and one additional moiety selected from: alkyl, hydroxyalkyl, cycloalkyl-alkyl; or (ii) by one moiety selected from: acyl, carbamoyl substituted at the carbamoyl nitrogen by one polyhydroxyalkyl, Ar, -Y-Ar, wherein Y is a moiety selected from alkyl, acyl, carbamoyl and Ar is aryl optionally substituted; or Ri and R2, taken together with the adjacent N atom, form a 6 membered heterocycloalkyl ring substituted at the heteroatom by -Y-Ar where Y and Ar are as defined above; or Ri and R2, taken together with the adjacent N atom, form a 8-11 membered satured bicyclic ring, optionally containing an heteroatom and optionally substituted. La présente invention concerne de nouveaux dérivés substitués de bisamide d'acide éthylène diaminetétraacétique, leurs complexes avec l'ion Mn(II) et l'utilisation de ceux-ci en tant qu'agents de contraste pour analyse par Imagerie par Résonance Magnétique (IRM).