Back to results
US 5,688,487 AGranted
Diagnostic imaging methods using rhenium and technetium complexes containing a hypoxia-localizing moiety
AssigneeBracco International B.V.
InventorsKaren Linder, Adrian D. Nunn, David P. Nowotnik, Kondareddiar Ramalingam, Richard J. DiRocco, William L. Rumsey, John P. Pirro
Life of this patent
Estimating the term…
Abstract
Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprising a metal, preferably radionuclide of rhenium or technetium; a hypoxia-localizing moiety; and, a complexing ligand, wherein said ligand and said radionuclide combined have cell membrane permeabilities greater than that of sucrose, are disclosed.
Claims8
A method for the diagnostic imaging of hypoxic tissue in a mammalian species comprising the steps of:
- administering a pharmaceutical formulation comprising a metal complex, said metal complex comprising a radionuclide of technetium and a ligand of either formula Ia or Ib:
- ##STR46## wherein at least one R' is --(A).sub.p --R.sub.2 where (A).sub.p is a linking group and R.sub.2 is a nitro-heterocyclic hypoxia localizing moiety;
- and wherein the other R' groups, that are not --(A).sub.p --R.sup.2, and the R groups are the same, or different and are independently selected from hydrogen, halogen, hydroxy, alkyl, alkonyl, alkynyl, alkoxy, aryl, --COOR.sub.3, ##STR47## --NH.sub.2, hydroxyalkyl, alkoxyalkyl, hydroxyaryl, haloalkyl, arylalkyl, alkyl--COOR.sub.3, --alkyl--CON(R.sub.3).sub.2, --alkyl--N(R.sub.3).sub.2, --aryl--COOR.sub.3, --aryl--CON(R.sub.3).sub.2, --aryl--N(R.sub.3).sub.2, 5- or 6-membered nitrogen- or oxygen-containing heterocycle;
- or two groups taken together with the one or more atoms to which they are attached form a carbocyclic or heterocyclic, saturated or unsaturated spiro or fused ring which may be substituted with R groups;
- R.sub.1 is hydrogen, a thiol protecting group or --(A).sub.p --R.sub.2 ;
- R.sub.3 is hydrogen, alkyl or aryl;
- m=2 t5;
- p=0 t20;
- and where the term aryl denotes phenyl or substituted phenyl, and
- obtaining a diagnostic image of said hypoxic tissue.
7 more elements
Dependencies are inferred from the claim text.