Chemical product usable as a non-radioactive carrier
    1.
    发明授权
    Chemical product usable as a non-radioactive carrier 失效
    可用作非放射性载体的化学产品

    公开(公告)号:US5077389A

    公开(公告)日:1991-12-31

    申请号:US947093

    申请日:1986-12-29

    摘要: The present invention relates to a chemical product usable as a non-radioactive carrier which comprises (1) a unit of a polyformyl compound having at least three formyl groups per molecule, (2) at least two units of an amino group-containing chelating compound bonded to the polyformyl compound by a methyleneimine linkage (--CH.dbd.N--) or a methyleneamine linkage (--CH.sub.2 NH--) between a formyl group in the polyformy compound and an amino group in the chelating compound, optionally followed by reduction, (3) at least one unit of an amino group-containing physiologically active substance bonded to the polyformyl compound by a methyleneimine linkage or a methyleneamine linkage between a formyl group in the polyformyl compound and the amino group in the physiologically active substance, optionally followed by reduction.

    Chemical product usable as a non-radioactive carrier
    3.
    发明授权
    Chemical product usable as a non-radioactive carrier 失效
    可用作非放射性载体的化学产品

    公开(公告)号:US5384401A

    公开(公告)日:1995-01-24

    申请号:US215671

    申请日:1994-03-22

    摘要: A radioactive diagnostic agent which comprises (1) the unit of a polyformyl compound having at least three formyl groups per molecule, (2) at least two units of an amino group-containing chelating compound bonded to the polyformyl compound with intervention of a methyleneimine linkage (--CH.dbd.N--) or a methyleneamine linkage (--CH.sub.2 NH--) formed by the condensation between the formyl group in the polyformyl compound and the amino group in the chelating compound, optionally followed by reduction, (3) at least one unit of an amino group-containing physiologically active substance bonded to the polyformyl compound with intervention of a methyleneimine linkage or a methyleneamine linkage formed by the condensation between the formyl group in the polyformyl compound and the amino group in the physiologically active substance, optionally followed by reduction, and (4) at least two radioactive metallic elements of which each is bonded to the chelating compound through a chelating bond.

    摘要翻译: 一种放射性诊断剂,其包含(1)每分子具有至少三个甲酰基的聚甲基化合物的单元,(2)至少两个与聚甲酰基化合物结合的含氨基的螯合化合物的单元, (-CH = N-)或通过聚甲酰基化合物中的甲酰基与螯合化合物中的氨基之间的缩合形成的亚甲基胺键(-CH 2 NH-),任选地随后还原,(3)至少一个单元 与聚甲酰基化合物结合的含氨基的生理活性物质通过由聚甲酰基化合物中的甲酰基与生理活性物质中的氨基之间的缩合形成的亚甲基亚胺键或亚甲基胺键介导,任选地随后还原, 和(4)至少两个放射性金属元素,其各自通过螯合键与螯合化合物键合。

    Radioactive diagnostic agent
    4.
    发明授权
    Radioactive diagnostic agent 失效
    放射性诊断剂

    公开(公告)号:US4666697A

    公开(公告)日:1987-05-19

    申请号:US558333

    申请日:1983-12-05

    摘要: A radioactive diagnostic agent which comprises (1) a unit of a polyformyl compound having at least three formyl groups per molecule, (2) at least two units of an amino group-containing chelating compound bonded to the polyformyl compound a methyleneimine linkage (--CH.dbd.N--) or a methyleneamine linkage (--.sub.2 NH--) formed by the condensation between the formyl group in the polyformyl compound and the amino group in the chelating compound, optionally followed by reduction, (3) at least one unit of an amino group-containing physiologically active substance bonded to the polyformyl compound by a methyleneimine linkage or a methyleneamine linkage formed by the condensation between the formyl group in the polyformyl compound and the amino group in the physiologically active substance, optionally followed by reduction, and (4) at least two radioactive metallic elements of which each is bonded to the chelating compound through a chelating bond.

    摘要翻译: 一种放射性诊断剂,其包含(1)每分子具有至少三个甲酰基的聚甲基化合物的单元,(2)至少两个与所述聚甲基化合物结合的含氨基的螯合化合物的单元,亚甲基亚胺键(-CH = N-)或通过聚甲酰基化合物中的甲酰基与螯合化合物中的氨基之间的缩合形成的亚甲基胺键(-2NH-),任选地随后还原,(3)至少一个氨基单元 通过由聚甲酰基化合物中的甲酰基与生理活性物质中的氨基之间的缩合形成的亚甲基亚胺键或亚甲基键连接到聚甲基化合物上的生理活性物质,任选地随后还原,和(4)在 至少两个放射性金属元素各自通过螯合键与螯合化合物结合。

    Porphyrin derivatives
    7.
    发明授权
    Porphyrin derivatives 失效
    卟啉衍生物

    公开(公告)号:US4849207A

    公开(公告)日:1989-07-18

    申请号:US922492

    申请日:1986-10-23

    CPC分类号: C07D487/22

    摘要: A porphyrin compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each --CH.dbd.CH.sub.2, --CH.sub.2 CH.sub.3, --CH(O-lower alkanoyl)CH.sub.3, --CH(OR)CH.sub.3 or --CH(O-lower alkylene-OR)CH.sub.3 ; R.sub.3 is --H, --COOH, --COO-lower alkyl, --COO-lower alkylene-OR or --COO-lower alkylene-OOC-Z; R.sub.4 is --H, -lower alkyl or -lower alkylene-OR; R is --H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R.sub.3 therefrom; A is --CH.sub.2 -- or --CO--; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfuntional carboxyl compound, at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R.sub.1 being capable of representing 1-iodoethyl in addition to said meanings when R.sub.3 is --COO-lower alkylene-OOC-Z, which shows a high accumulation in the locus of cancer with quick excretion from normal tissues.

    摘要翻译: 一种下式的卟啉化合物:其中R 1和R 2各自为-CH = CH 2,-CH 2 CH 3,-CH(O-低级烷酰基)CH 3,-CH(OR)CH 3或-CH(O-低级) 亚烷基-OR)CH 3; R3是-H,-COOH,-COO-低级烷基,-COO-低级亚烷基-OR或-COO-低级亚烷基-OOC-Z; R4是-H-低级烷基或 - 低级亚烷基-OR; R是-H,低级烷基或除了氢原子以外的多官能羧基化合物的残基; Z是除了R3之外的式(I)化合物的残基; A是-CH2-或-CO-; 并且来自γ位置的虚线表示没有键合或单个直接键合; 7位和8位之间的虚线表示存在单键或双键; 其与卟啉骨架中的金属和/或多官能羧基化合物的残基的络合物,R 1,R 2,R 3和R 4中的至少一个为含有R的基团,其表示多官能羧基化合物的残基 当R 3为-COO-低级亚烷基-OOC-Z时,R 1除了所述含义之外,还能够表示1-碘乙基,其在正常组织中快速排出的癌症基因座中表现出高度的积累。

    3-Aminomethylene-2,4-pentanedione bis(thiosemicarbazone) derivatives
    9.
    发明授权
    3-Aminomethylene-2,4-pentanedione bis(thiosemicarbazone) derivatives 失效
    3-氨基亚甲基-2,4-戊二酮双(缩氨基硫脲)衍生物

    公开(公告)号:US4474984A

    公开(公告)日:1984-10-02

    申请号:US332152

    申请日:1981-12-18

    摘要: A radioactive diagnostic agent which comprises a physiologically active substance and a radioactive metallic element combined with a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, C.sub.1 -C.sub.3 alkyl or phenyl. The agent is characteristic in having a high stability even after being administered into a human body and showing the substantially the same behavior as the physiologically active substance itself in a human body.

    摘要翻译: 一种放射性诊断剂,其包含与下式化合物组合的生理活性物质和放射性金属元素:其中R 1和R 2各自为氢,C 1 -C 3烷基或苯基。 即使在施用于人体后也具有高稳定性,并且在人体内表现出与生理活性物质本身基本相同的作用。