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US 5,858,327 AGranted
Hydrazino-type N.sub.2 S.sub.2 radionuclide chelating compounds
AssigneeResolutions Pharmaceuticals, Inc.
InventorsAlfred Pollak, Robert Kirby, Robert Dunn-Dufault
Life of this patent
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Abstract
Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targetting molecules may be used in diagnosis and therapy.
Claims19
A compound of the general formula:
- ##STR6## wherein R.sub.1, R.sub.2, R.sub.5 and R.sub.6 are independently selected from the group consisting of H;
- carboxyl;
- lower alkyl;
- lower alkyl substituted with a group selected from the group consisting of hydroxyl, sulfhydryl, halogen, carboxyl and aminocarbonyl;
- R.sub.8 ;
- or R.sub.9 ;
- R.sub.3 and R.sub.4 are independently selected from the group consisting of H or a sulfur protecting group;
- --X is selected from the group consisting of .dbd.O, .dbd.S, .dbd.CH.sub.2, .dbd.NH.sub.2, --NHR.sub.8, or NHR.sub.9 ;
- Y and Z are both NR.sub.7 ;
- R.sub.7 is selected from the group consisting of H, carboxyl, C.sub.1-3 alkyl or C.sub.1-3 alkyl substituted with a group selected from the group consisting of hydroxyl, carboxyl, or halogen;
- R.sub.8 is a conjugating molecule;
- and
- R.sub.9 is a targeting molecule.
10 more elements
A compound of the general formula:
- ##STR7## wherein R.sub.1, R.sub.2, R.sub.5 and R.sub.6 are independently selected from the group consisting of H;
- carboxyl;
- lower alkyl;
- lower alkyl substituted with a group selected from the group consisting of hydroxyl, sulfhydryl, halogen, carboxyl and aminocarbonyl;
- R.sub.8 ;
- or R.sub.9 ;
- R.sub.3 and R.sub.4 are independently selected from the group consisting of H or a sulfur protecting group;
- --X is selected from the group consisting of .dbd.O, .dbd.S, .dbd.CH.sub.2, .dbd.NH.sub.2, --NHR.sub.8, or NHR.sub.9 ;
- Y and Z are both NR.sub.7 ;
- R.sub.7 is selected from the group consisting of H, carboxyl, C.sub.1-3 alkyl or C.sub.1-3 alkyl substituted with a group selected from the group consisting of hydroxyl, carboxyl, or halogen;
- R.sub.8 is a conjugating molecule;
- and
- R.sub.9 is a targeting molecule,
- wherein at least one of R.sub.1, R.sub.2, R.sub.5, or R.sub.6 is R.sub.8 or R.sub.3 or X is --NH--R.sub.8 or --NH--R.sub.9.
11 more elements
A compound of the general formula:
- ##STR8## wherein R.sub.1, R.sub.2, R.sub.5 and R.sub.6 are independently selected from H;
- carboxyl;
- lower alkyl;
- and lower alkyl substituted with a group selected from hydroxyl, sulfhydryl, halogen, carboxyl and aminocarbonyl;
- or R.sub.8 ;
- or R.sub.9 ;
- R.sub.3 and R.sub.4 are independently selected from H and a sulfur protecting group;
- --X is selected from .dbd.O, .dbd.S, .dbd.CH.sub.2, .dbd.NH.sub.2 or --NHR.sub.8 or --NHR.sub.9 ;
- Y and Z are both NR.sub.7 ;
- R.sub.7 is selected from H, carboxyl, C.sub.1-3 alkyl and C.sub.1-3 alkyl substituted hydroxyl, carboxyl and halogen;
- R.sub.8 is a conjugating group;
- and
- R.sub.9 is a targeting molecule;
- wherein at least one of R.sub.1, R.sub.2, R.sub.5 and R.sub.6 is R.sub.9 or X is --NHR.sub.9.
11 more elements
Dependencies are inferred from the claim text.