Diagnostic imaging methods using rhenium and technetium complexes containing a hypoxia-localizing moiety
First Claim
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1. 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)p --R2 where (A)p is a linking group and R2 is a nitro-heterocyclic hypoxia localizing moiety; and
wherein the other R'"'"' groups, that are not --(A)p --R2, and the R groups are the same, or different and are independently selected from hydrogen, halogen, hydroxy, alkyl, alkonyl, alkynyl, alkoxy, aryl, --COOR3, ##STR47## --NH2, hydroxyalkyl, alkoxyalkyl, hydroxyaryl, haloalkyl, arylalkyl, alkyl--COOR3, --alkyl--CON(R3)2, --alkyl--N(R3)2, --aryl--COOR3, --aryl--CON(R3)2, --aryl--N(R3)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;
R1 is hydrogen, a thiol protecting group or --(A)p --R2 ;
R3 is hydrogen, alkyl or aryl;
m=2 t5;
p=0 t20; and
where the term aryl denotes phenyl or substituted phenyl, andobtaining a diagnostic image of said hypoxic tissue.
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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.
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Citations
8 Claims
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1. A method for the diagnostic imaging of hypoxic tissue in a mammalian species comprising the steps of:
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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)p --R2 where (A)p is a linking group and R2 is a nitro-heterocyclic hypoxia localizing moiety; and
wherein the other R'"'"' groups, that are not --(A)p --R2, and the R groups are the same, or different and are independently selected from hydrogen, halogen, hydroxy, alkyl, alkonyl, alkynyl, alkoxy, aryl, --COOR3, ##STR47## --NH2, hydroxyalkyl, alkoxyalkyl, hydroxyaryl, haloalkyl, arylalkyl, alkyl--COOR3, --alkyl--CON(R3)2, --alkyl--N(R3)2, --aryl--COOR3, --aryl--CON(R3)2, --aryl--N(R3)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;R1 is hydrogen, a thiol protecting group or --(A)p --R2 ; R3 is hydrogen, alkyl or aryl; m=2 t5; p=0 t20; and
where the term aryl denotes phenyl or substituted phenyl, andobtaining a diagnostic image of said hypoxic tissue. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
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Specification
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Current AssigneeBracco Suisse SA
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Original AssigneeBracco International B.V. (Bracco SPA)
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InventorsNunn, Adrian D., Ramalingam, Kondareddiar, Nowotnik, David P., Linder, Karen, Rumsey, William L., Pirro, John P., DiRocco, Richard J.
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Primary Examiner(s)Kight, John
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Assistant Examiner(s)Kelley, Lara Chapman
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Application NumberUS08/476,604Time in Patent Office896 DaysField of Search424/1.65, 548/327.5, 534/10, 534/14US Class Current424/1.65CPC Class CodesA61K 2123/00 Preparations for testing in...A61K 51/0478 complexes from non-cyclic l...A61K 51/0497 conjugates with a carrier b...C07C 251/38 to carbon atoms of a satura...
