Substituted thioureas as bifunctional chelators

Details Substituted thioureas as bifunctional chelators Substituted thioureas as bifunctional chelators

C - Chemistry, Metallurgy

07

K

C07K 16/00 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 51/08 (2006.01) A61K 51/10 (2006.01) C07B 59/00 (2006.01) C07C 335/22 (2006.01) C07C 337/06 (2006.01) C07D 207/452 (2006.01) C07D 213/71 (2006.01) C07F 3/12 (2006.01) C07F 13/00 (2006.01) C07K 1/13 (2006.01) C07K 2/00 (2006.01)

Patent

CA 2117770

2117770 9321151 PCTABS00027 This invention relates to chelating agents of formula (I), in which L is a linker; D is an alkyl backbone, cyclic alkyl backbone or aryl backbone group substituted with the NHCSNHR groups: and R is hydrogen or a substituent of general formula (1) in which a = 0 or 1; b = 0-10; c = 0 or 1; if c = 1, Y = S, O or H2; d = 0-2; e = 0-10; and Z = H, N+(R')3X-, SO3H, CO2H, OH, H2PO3; in which X- is a counterion such as a halide or an acid anion and R' is a C1 to C4 lower alkyl, useful for coupling metal ions to biologically active molecules. In particular, substantial thioureas 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.

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