Complexes possessing ortho ligating functionality
AssigneeThe Dow Chemical Company
InventorsDavid A. Wilson, Joseph R. Garlich, R. Keith Frank, Kenneth McMillan, Jaime Simon
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Abstract
A group of functionalized amine chelants having ortho ligating functionality that form complexes with rare-earth type metal ions are disclosed. The chelants possess the general formula ##STR1## wherein R.sup.'1, R.sup.'2, R.sup.'3, R.sup.'4, R.sup.'5 and R.sup.'6, Z' and X are all defined in the specification. In addition certain of the chelant-radionuclide complexes can be effectively employed in compositions useful as therapeutic and/or diagnostic agents for calcific tumors and/or relief of bone pain.
Claims8
A complex comprising a chelant possessing ortho ligating functionality having the formula ##STR31## wherein Z' is selected from the group consisting of hydrogen, NH.sub.2, NO.sub.2, NHC(O)CH.sub.3 or N(R').sub.2, where R' is hydrogen and C.sub.1 -C.sub.3 alkyl;
- X is selected from the group consisting of hydrogen, C.sub.1 -C.sub.3 alkyl and CR.sub.3 R.sub.4 COOH;
- R.sub.3 and R.sub.4 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.3 alkyl and COOH;
- R'.sub.1 and R'.sub.2 each are independently selected from the group consisting of hydrogen and COOH, with the proviso that at least one is COOH;
- R'.sub.3, R'4, R'.sub.5 and R'.sub.6 are independently selected from the group consisting of hydrogen and CR.sub.3 R.sub.4 COOH, with the proviso that at least three are CR.sub.3 R.sub.4 COOH;
- or
- a pharmaceutically acceptable salt thereof;
- and complexed with a radionuclide metal ion selected from the group consisting of .sup.153 Sm, .sup.166 Ho, .sup.90 y, .sup.149 pm, .sup.159 Gd, .sup.0 La, .sup.177 Lu, .sup.175 Yb, .sup.47 Sc and .sup.142 Pr.
A complex of claim 27 wherein the metal ion is .sup.153 Sm, .sup.166 Ho, .sup.90 y, .sup.159 Gd or .sup.177 Lu.
Dependencies are inferred from the claim text.