NEW 3,6,9, 15-TETRAAZA-BICYCLO 9.3.1 PENTADECA- 1(14), 11(15), 12-TRIENE BASED COMPOUNDS AND THEIR APPLICATION AS LIGANDS OF ESSENTIAL METAL ION BASED MRI AND ⁵²MN BASED PET CONTRAST AGENTS

摘要

The one subject of the invention is the compounds of general formula (I), their isomers, their physiologically acceptable salts and/or Mn(II), Fe(II), Fe(III), Co(II) and Ni(II) complexes. The other subject of the invention is the application of the above compounds. The compounds of general formula (I): wherein R_a refers to -OH group or -NR₃R₄ group and -NR₃R₄ group may refer to: a) -NR₃R₄ with N atom in the ring means a ring of 4 to 7, that in certain cases may contain another heteroatom, and in specific cases the ring may be replaced with an aryl group (of 5 to 7 carbon atoms) substituted with -COOH, -OH, -OCH₃, -NO₂, -NH₂, -NCS, -NHS- activated ester, aryl (of 5 to 7 carbon atoms), or nitro-, amino- or isothiocyanate group, or b) in the -NR₃R₄ group R₃ means a H atom, alkyl, aryl, nitroaryl, aminoaryl or isothiocyanate-aryl group (of 1 to 6 carbon atoms) and R4 is a H atom, alkyl (of 1 to 6 carbon atoms) or -(CH₂)_n-COOH group, whereas n=1 to 10 integer, or c) -NR₃R₄ group is one of the below groups: whereas R₁ is a H atom, carboxyl or alkyl-carbonyl group (of 1 to 4 carbon atoms); and R_b is a H atom or alkyl group (of 1 to 6 carbon atoms), and X means independently from one another H atom, -CH₃, -COOH, -OH, -OCH₃, alkoxy- (of 2 to 6 carbon atoms), -NO2, -NH2, -NCS, -NHS-activated ester, alkyl (of 2 to 12 carbon atoms) or aryl (of 5 to 7 carbon atoms) group, in certain cases the latter may be substituted with hydroxyl, hydroxyalkyl (of 1 to 6 carbon atoms), nitro, amino or isothiocyanate group; and Y means: -NH- or NCH₂-Z group, whereas in the CH₂-Z group Z refers to one selected group of the below: -C(O)NR₃R₄ group, in which -NR₃R4 means as referred to above, whereas z= 0- 18 integer, whereas z=0-18 integer, whereas z=0-18 integer, whereas z=0-18 integer and H atom, alkyl (of 1 to 6 carbon atoms) or -(CH₂)_n-COOH group, whereas n=l to 10 integer, or, whereas z= 0-18 integer, whereas z=0-18 integer and R_2a refers to H atom, -OCH₃, or -CF₃ group, whereas R_2b refers to H atom, -CH₃, -OCH₃.CF₃; - COOH, -COON(CO)₂(CH₂)₂, -NO₂, -NH₂ or -NCS- group, whereas z= 0-18 integer and R₂c refers to H atom, NO₂, -NH₂ or -NCS- group, whereas ζ=0-18, -and x=l-5 integer, whereas z=0-18,, and x=1.5 integer; whereas z=1-5, and x=1-5 integer, R_2d refers to H atom, -CH₃, -OCH₃;.CF₃, -COOH, - COON(CO)₂(CH₂)₂, -NO₂, -NH₂ or -NCS group,