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    • 4. 发明授权
    • Cationic compounds useful for making radiodiagnostic agents
    • 用于制造放射诊断剂的阳离子化合物
    • US4451450A
    • 1984-05-29
    • US311770
    • 1981-10-15
    • Vinayakam Subramanyam
    • Vinayakam Subramanyam
    • A61K51/00A61K51/04C07F9/50C07F9/54C07F9/66C07F13/00A61K43/00A61K49/00C07F9/90
    • A61Q5/00A61K51/04C07F9/5045C07F9/5449A61K2123/00
    • A normally solid, hydrophilic compound capable of binding with Tc-99m to form a cationic complex is provided. The compound has a formula selected from: ##STR1## wherein: R, R', R", R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently selected from hydrogen; or substituted or unsubstituted alkyl, alkylene, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; and R plus R.sup.i in formula (A) may be taken together to form a cyclic compound;A, A', A", A.sup.1, A.sup.2, A.sup.3, A.sup.4, A.sup.5 and A.sup.6 are independently neutral functional elements, each having a free electron pair available for accepting a proton to provide a charged ligand and having the capability of complexing with Tc-99m to form a cationic complex;Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4, Y.sup.5 and Y.sup.6 are each independently selected from hydrogen; or substituted or unsubstituted alkyl, alkylene, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclin groups;Z is an anion;i is an integer from 0 to 6;j, j' and j" are each independently 0 or 1;k.sup.1, k.sup.2, k.sup.3, k.sup.4, k.sup.5 and k.sup.6 are each independently 0 or 1;n, n' and n" are each independently the integer 1 or 2;n.sub.1, n.sub.2, n.sub.3, n.sub.4, n.sub.5, n.sub.6, are independently 0 or 1; andn.sub.7 and n.sub.8 are each an integer from 1 to 6; andn.sub.9 and n.sub.10 are each an integer from 1 to 3.These compounds are capable of reducing technetium to form stable cationic complexes. Radiolabelled such complexes are useful in connection with radiodiagnostic test of myocardial and/or hepatobiliary tissues.
    • 提供能够与Tc-99m结合以形成阳离子络合物的通常为固体的亲水性化合物。 该化合物具有选自以下的式:其中:R,R',R“,R 1,R 2,R 3,R 4,R 5和R 6各自独立地选自氢; 或取代或未取代的烷基,亚烷基,芳基,烷基芳基,芳基烷基,单环烷基,多环烷基,杂环和碳环基团; 式(A)中的R plus R 1可以一起形成环状化合物; A,A',A“,A1,A2,A3,A4,A5和A6分别是中性功能元件,每个具有可用于接受质子以提供带电配体并具有与Tc络合的能力的自由电子对 -99μm形成阳离子络合物; Y1,Y2,Y3,Y4,Y5和Y6各自独立地选自氢; 或取代或未取代的烷基,亚烷基,芳基,烷基芳基,芳烷基,单环烷基,多环烷基,杂环和碳环基; Z是阴离子; 我是0到6的整数; j,j'和j“各自独立地为0或1; k1,k2,k3,k4,k5和k6各自独立地为0或1; n,n'和n“各自独立地为整数1或2; n1,n2,n3,n4,n5,n6独立地为0或1; n7和n8各自为1〜6的整数, n9和n10各自为1〜3的整数。这些化合物能够还原锝以形成稳定的阳离子络合物。 放射性标记的这种复合物可用于心肌和/或肝胆组织的放射诊断测试。