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US 5,294,717 AGranted
Bifunctional chelating agents, their chelates and process of preparation
OwnerSpyros Theodoropulosinventor
Life of this patent
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Abstract
Bifunctional chelating agents based on substituted 8-hydroxy-2-carboxamidoquinolines and their chelates are provided together with processes for their preparation. The agents can react with a variety of biological substrates and/or chelate with a variety of transition metals providing useflu in vivo agents for localizing radioactivity where needed for diagnostic or therapeutic purposes.
Claims7
An 8-substituted-2-carboxamidoquinoline compound having the structure:
- ##STR14## wherein:
- R.sub.2, R.sub.3 and R.sub.4 are identical or different, and are selected from the group consisting of hydrogen, hydroxyl, halogen, C.sub.1 -C.sub.5 alkyl, nitro, nitroso, --SO.sub.3 H, --PO.sub.3 H, and an aryl up to C.sub.18 ;
- X is selected from the group consisting of OH and SH;
- R.sub.5 and R.sub.6 are identical or different, and are selected from the group consisting of hydrogen, a C.sub.1 -C.sub.18 alkyl group which may be unsubstituted or substituted with a member selected from the group consisting of mercapto, carboxy, hydroxy and dialkylamino;
- an aryl up to C.sub.18 which may be substituted with at least one member selected from the group consisting of hydroxy, carboxy amino and mercapto groups;
- and a pyridyl or 8-quinolyl group which may be substituted with a member selected from the group consisting of hydroxy and carboxy;
- the group Q-L represents a substrate coupling moiety, wherein Q is hydrogen, a C.sub.1 -C.sub.18 alkyl group which may be unsubstituted or substituted with the same substituents as R.sub.5 and R.sub.6 above, an aryl and aralkyl up to C.sub.18 pyridyl or 8-quinolyl;
- with the proviso that when Q is hydrogen, L is nonexistent;
- L is a nitro, or an amino group.
6 more elements
A compound having the chemical structure:
- ##STR16##
- 4.
Dependencies are inferred from the claim text.