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US 6,719,958 B1Granted
Polychelants, their complexes with metal ions, their preparation and their uses
AssigneeDibra S.p.A.
InventorsLuigia Gozzini, Federico Maisano, Marcella Murru
Life of this patent
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Abstract
A new class of polychelants, their chelates with metal ions and their physiologically acceptable salts, useful, either as they are or in association or formulation with other components, for diagnostic imaging as general or specific contrast agents for specific tissues, organs or body compartments.
Claims16
A compound of formula (I):
- L[NH2]p[NHF]z[N[F]2]x (I),
- in which
- L is a polyaminic organic moiety;
- F is a —CH2—T—K group, representing a chelant/chelate residue, where
- T is a C2-C5 aliphatic chain, interrupted or not by one or more heteroatoms selected from O, N, S or by functional groups selected from carbonyl, thiocarbonyl, amide, ester, thiourea, thioamide groups, said chain being linked covalently to an atom of a residue K,
- K is a tetraazacyclododecyl containing group, or one of its metal chelates, or one of its salts and where
- the total number of the F groups is 3 to 2 m;
- p is a number from 0 to m − 2, z is a number from 0 to m− 1, and x is a number from 1 to m,
- where m is a number from 2 to 1000, m being the total number of the primary amino groups originally present on L and where
- p+x+z=m, with the proviso that, when x=1, then z≠0, and in which the chelated metal ions are bi- or trivalent paramagnetic ions or radioisotopes.
7 more elements
A compound of formula (I):
- L[NH2]p[NHF]z[N[F]2]x (I),
- in which:
- L is selected from a group consisting of spermidine, norspermidine, spermine, 4,9-dioxadodecandiamine, 3,6-dioxaoctandiamine, an alkylenediamine, diethylenetriamine, triethylenetetramine, tris-(2-aminoethyl)amine, jeffamine, N-glucosamine, lysine and its derivatives, ornithine and diamino sugars;
- F is a —CH2—T—K group, representing a chelant residue, where
- T is a C2-C5 aliphatic chain, containing an amido or carbonylamino group, said chain being linked covalently to a nitrogen atom of a K residue,
- K is a tetraazacyclododecyl containing group a tetraazacyclododecyl containing group, its derivatives, metal chelates or salts, in which
- the metal ion chelates are selected from the bi- or trivalent ions of elements having atomic numbers between 20 and 31, or 39, 42, 43, 44, 49, or between 57 and 83 or the ions of the following radioisotopes 51Cr, 67Ga, 68Ga, 111In, 99mTc 40La, 175Yb, 153Sm, 166Ho, 90Y, 149Pm 177Lu 47Sc 142Pr, 159Gd and 212Bi and where
- the total number of the F groups is 3 to 2 m;
- p is a number from 0 to m − 2, z is a number from 0 to m − 1, and x is a number from 1 to m,
- where m is a number from 2 to 1000, m being the total number of the primary amino groups originally present on L and where
- p+x+z=m, with the proviso that, when x=1, then z≠0, and in which the chelated metal ions are bi- or trivalent paramagnetic ions or radioisotopes.
8 more elements
Dependencies are inferred from the claim text.