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Complexes with .sup.99m Tc suitable for radiolabelling monoclonal antibodies or other macro molecules

机译:99m Tc的复合物适用于放射性标记单克隆抗体或其他大分子

摘要

The ligand L, (R.sup.3)(R.sup.4)(R.sup.5)C--N(R)--C(R.sup.1)(R. sup.2)-- (CH.sub.2).sub.n --COOH L where R is hydrogen, hydroxy, alkyl, hydroxyalkyl, or alkylcarboxy, or R and R.sup.1 together may form a mono-, di-, tri-, or tetra-methylene radical, or R and R.sup.3 together may form a mono-, di-, tri-, or tetra-methylene radical, and R.sup.1 and R. sub.2 may be the same or different and are selected from hydrogen, hydroxy, alkyl, hydroxyalkyl, carboxy, alkylcarboxy, alkylamine, alkylthiol, aryl or R.sup.1 and R.sup.2 together may form a tetra- or penta-methylene radical, and R.sup.3 and R.sup.4 and R.sup.5 may be the same or different and are selected from hydrogen, hydroxy, alkyl, hydroxyalkyl, carboxy, alkylcarboxy, provided that at least one of R.sup. 3, R.sup.4 and R.sup.5 is hydroxyalkyl, and n is equal to 0, 1 or 2, for example tricine, form useful complexes with .sup.99m Tc, for radiolabelling macromolecules such as monoclonal antibodies.
机译:配体L,(R.sup.3)(R.sup.4)(R.sup.5)C--N(R)-C(R.sup.1)(R。sup.2)- -(CH 2)n -COOH L,其中R为氢,羟基,烷基,羟烷基或烷基羧基,或R和Rupup.1可以一起形成单,二,三- ,或四亚甲基,或R和R 3一起可以形成一,二,三或四亚甲基,并且R 1和R.sub.2可以相同R 1或R 2选自氢,羟基,烷基,羟烷基,羧基,烷基羧基,烷基胺,烷基硫醇,芳基或R 1和R 2一起可形成四-或五-亚甲基,R 3 sup.3和R.4和R.5可以相同或不同,并且选自氢,羟基,烷基,羟烷基,羧基,烷基羧基,条件是R.sup.3中的至少一个。在图3中,R 4和R 5是羟烷基,并且n等于0、1或2,例如三辛胺,与99m Tc形成有用的配合物,用于放射性标记大分子,例如单克隆抗体。

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