Adducts of macrocyclic chelants
US5554748A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 30, 1993 |
| Grant date | Sep 10, 1996 |
| Priority date | — |
| Expiry date | Dec 30, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC08G69/48
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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. For example, adducts of a macrocyclic chelant can be formed by the process of (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 chelant soluble in the solvent, (c) chilling the reaction mixture to between about 5.degree. C. and 55.degree. C. above the freezing point of the solvent, and (d) adding substantial equimolar amount of chilled alkylhaloformate under anhydrous conditions so as to form a slurry containing the mixture carboxycarbonic anhydride of the chelant.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.