Polychelants containing macrocyclic chelant moieties
OwnerPaul F. Sieving, Alan D. Watson +2inventors
InventorsPaul F. Sieving, Alan D. Watson, Steven C. Quay, Scott M. Rocklage
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Abstract
There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g, DOTA residues, conjugated to a polyamine backbone molecule, e.g, polylysine. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein.
Claims33
A polychelant comprising a backbone moiety being the residue of an amine group containing molecule with bonded thereto a plurality of macrocyclic chelant moieties capable of complexing metal ions, and metal chelates and salts thereof.
- (b) bonded to said backbone moiety through its amine groups a plurality of macrocyclic chelant moieties capable of complexing metal ions,
- a metal chelates and salts of said polychelant compound.
A polychelant compound formed by a process comprising the following steps:
- (a) dispersing a carboxylic macrocyclic chelant in a polar anhydrous solvent;
- (b) adding a base with a pKa sufficient to remove all carboxyl protons to create an amine salt of the said chelant soluble in said solvent;
- (c) chilling the reaction mixture to between about 5.degree. C. and 55.degree. C. above the freezing point of the solvent;
- (d) adding a substantially equimolar amount of chilled alkylhaloformate under anhydrous conditions while approximately maintaining the temperature of step (c) for a period of time sufficient for substantially complete reaction to form a slurry containing the mixed carboxycarbonic anhydride of said chelant;
- and
- (e) slowly adding the slurry to a solution of the free base form of a polymer carrying a plurality of free amines.
Dependencies are inferred from the claim text.