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US 5,527,885 AGranted
Bifunctional isothiocyanate derived thiocarbonyls as ligands for metal binding
AssigneeCytogen Corporation
InventorsDaniel J. Coughlin, Benjamin A. Belinka, Jr.
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Abstract
This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.
Claims23
A chelating agent of the formula:
- L-D(NHCSNHR).sub.2
- in which L is a linker;
- D is an alkyl, cyclic alkyl or aryl group substituted with the NHCSNHR groups;
- and R is H or a substituent of the general formula:
- R=--(NH).sub.a (CH.sub.2).sub.b CY(NH).sub.d (CH.sub.2).sub.e --Z
- in which
- a=0 or 1;
- b=0-10;
- CY is C=S, C=O or CH.sub.2 ;
- d=0-2;
- e=1-10;
- and
- Z=is H or a polar group selected from the group consisting of an amine, N(R').sub.3.sup.+ X.sup.-, SO.sub.3 H, CO.sub.2 H, OH, H.sub.2 PO.sub.3 ;
- in which X.sup.- is a counterion and R' is a C.sub.1 to C.sub.4 lower alkyl,
- or a salt thereof.
12 more elements
Dependencies are inferred from the claim text.