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US 5,659,041 AGranted
Hydrazino-type radionuclide chelators having an N.sub.3 S configuration
AssigneeResolution Pharmaceuticals Inc.
InventorsAlfred Pollak, Robert A. Kirby, Robert Dunn-Dufault
Life of this patent
Estimating the term…
Abstract
Radionuclide chelating compounds are provided for conjugation to targeting molecules such as proteins, peptides or antibodies. The resulting labeled targeting molecules may be used in diagnosis and therapy.
Claims33
A compound of the general formula:
- ##STR4## wherein R.sup.1 is H or a sulfur proteoting group;
- R.sup.2 and R.sup.3 are seleoted independently from H;
- carboxyl;
- lower alkyl;
- and lower alkyl substituted with a group seleoted from hydroxyl, sulfhydryl, halogen, oarboxyl and aminooarbonyl;
- R.sup.4 and R.sup.7 are each H;
- R.sup.5 and R.sup.6 are seleoted independently from H;
- carboxyl;
- lower alkyl;
- lower alkyl substituted with a group seleoted from hydroxyl, sulfhydryl, halogen, carboxyl, lower alkoxycarbonyl and aminocarbonyl;
- and an alpha carbon side ohain of any amino aoid other than proline;
- R.sup.8 is seleoted from H, carboxyl, lower alkyl and lower alkyl substituted with hydroxyl, carboxyl or halogen;
- and
- R.sup.9 and R.sup.10 together form a 5- or 6-membered, saturated or unsaturated heterocyclic ring which is optionally fused to another 5- or 6-membered saturated or unsaturated, heterooyolio or carbocyolio ring wherein either ring is optionally substituted with a group seleoted from halogen, alkyl, hydroxyalkyl, carboxyl, carboxyalkyl, carboxyalkylthio, thiooyanato, amino, hydrazino and a oonjugating group for ooupling a targeting moleoule to said either ring.
11 more elements
Dependencies are inferred from the claim text.