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    • 11. 发明公开
    • Multidentate aza ligands able to complex metal ions and the use thereof in diagnostics and therapy
    • 阿尔法里安·祖尔
    • EP1803711A1
    • 2007-07-04
    • EP07003558.9
    • 2002-07-10
    • BRACCO IMAGING S.p.A.
    • Giovenzana, Giovanni BattistaPalmisano, GiovanniSisti, MassimoCavallotti, CamillaAime, SilvioCalabi, Luisella
    • C07D243/08A61K49/08C07C229/16C07C229/76
    • C07D243/08A61K49/0002A61K49/101
    • Compounds of general formula (I):
      in which: R 1 is hydrogen, C 1 -C 20 alkyl, C 3 -C 10 cycloalkyl, C 4 -C 20 cycloalkylalkyl, aryl, arylalkyl, or two R 1 , taken together, form a straight or cyclic C 2 -C 10 alkylene group or an ortho disubstituted arylene; R 2 is hydrogen, C 1 -C 20 alkyl, C 3 -C 10 cycloalkyl, C 4 -C 20 cycloalkylalkyl, aryl or arylalkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R 3 , R 4 and R 5 are hydrogen, C 1 -C 20 alkyl, C 3 -C 10 cycloalkyl, C 4 -C 20 cycloalkylalkyl, aryl, arylalkyl; FG are carboxy, -PO 3 H 2 or -RP(O)OH groups, wherein R is hydrogen, C 1 -C 20 alkyl, C 3 -C 10 cycloalkyl, C 4 -C 20 cycloalkylalkyl, aryl, arylalkyl; 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 203 Pb, 67 Ga, 68 Ga, 72 As, 111 In, 113 In, 90 Y, 97 Ru, 62 Cu, 64 Cu, 52 Fe, 52m Mn, 140 La, 175 Yb, 153 Sm, 166 Ho, 149 Pm, 177 Lu, 142 Pr, 159 Gd, 212 Bi, 47 Sc, 149 Pm, 67 Cu, 111 Ag, 199 Au, 161 Tb and 51 Cr as well as the salts thereof with physiologically compatible bases or acids.
    • 通式(I)的化合物:其中:R 1为氢,C 1 -C 20烷基,C 3 -C 10环烷基,C 4 -C 20环烷基烷基,芳基,芳基烷基或两个R 1一起形成 直链或环状C 2 -C 10亚烷基或邻二取代亚芳基; R 2是氢,C 1 -C 20烷基,C 3 -C 10环烷基,C 4 -C 20环烷基烷基,任选地被允许与能够与生理系统相互作用的合适分子缀合的官能团取代的芳基或芳烷基; R 3,R 4和R 5是氢,C 1 -C 20烷基,C 3 -C 10环烷基,C 4 -C 20环烷基烷基,芳基,芳基烷基; FG是羧基,-PO 3 H 2或-RP(O)OH基团,其中R是氢,C 1 -C 20烷基,C 3 -C 10环烷基,C 4 -C 20环烷基烷基,芳基,芳基烷基; 其螯合物与金属元素的二价离子的原子序数范围在20,31,39,42,43,44,49和57和83之间,放射性同位素选自203 Pb,67 Ga,68 Ga, 72 As,111 In,113 In,90 Y,97 Ru,62 Cu,64 Cu,52 Fe,52m Mn,140 La,175 Yb,153 Sm,166 Ho,149 Pm,177 Lu,142 Pr,159 Gd ,212 Bi,47 Sc,149 Pm,67 Cu,111 Ag,199 Au,161 Tb和51 Cr以及其与生理相容性碱或酸的盐。