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    Macrocyclic chelants for metallopharmaceuticals
    5.
    发明申请
    Macrocyclic chelants for metallopharmaceuticals 失效

    公开(公告)号：US20040067200A1

    公开(公告)日：2004-04-08

    申请号：US10663090

    申请日：2003-09-15

    发明人： Shuang Liu

    IPC分类号： A61K049/00 ,  C07F005/00

    CPC分类号： C07F9/6587 ,  A61K51/04 ,  A61K51/0482 ,  C07F9/6584

    摘要： This invention relates to macrocyclic chelants comprised of one or two heteroatom-containing bridges, compositions containing them and their use in medicine, particularly in diagnostic imaging and radiotherapy. This invention relates especially to the use of metal chelates of the macrocyclic chelants as metallopharmaceuticals in Magnetic Resonance Imaging (MRI) and radiopharmaceuticals. This invention also relates to macrocyclic chelants as bifunctional chelating agents (BFC's) for the labeling of biologically active targeting molecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands, with metal ions and radioisotopes.

    Process of making 3,7,9-trioxa-1-aza-2,8-diphosphaspiro[4,5]decanes
    6.
    发明授权
    Process of making 3,7,9-trioxa-1-aza-2,8-diphosphaspiro[4,5]decanes 失效
    制备3,7,9-三氧杂-1-氮杂-2,8-二磷杂螺[4,5]癸烷的方法

    公开(公告)号：US5239103A

    公开(公告)日：1993-08-24

    申请号：US975043

    申请日：1992-11-12

    申请人： Raymond Seltzer ,  Paul A. Odorisio ,  Sai P. Shum ,  Stephen D. Pastor

    发明人： Raymond Seltzer ,  Paul A. Odorisio ,  Sai P. Shum ,  Stephen D. Pastor

    IPC分类号： C07F9/6584 ,  C07F9/6587 ,  C08K5/5399

    CPC分类号： C08K5/5399 ,  C07F9/65844 ,  C07F9/6587

    摘要： 3,7,9-Trioxa-1-aza-2,8-diphosphaspiro[4.5]decanes of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, alkyl, cycloalkyl, bicycloalkyl, tricycloalkyl or aryl; or can be halogen when n or m is zero,R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently hydrogen, alkyl, aralkyl or aryl;X and Y are independently --O--, --S-- or --NR.sub.16 -- where R.sub.16 is alkyl, cycloalkyl, alkenyl, aryl or aralkyl;W and Z are independently O or S; andn, m, o and p are independently zero or 1, are effective in stabilizing organic materials against the deleterious effects of oxygen, heat and/or actinic radiation.

    摘要翻译： （I）的3,7,9-三氧杂-1-氮杂-2,8-二磷杂螺[4.5]癸烷其中R 1和R 2独立地是氢，烷基，环烷基，双环烷基，三环烷基或芳基; 或当n或m为零时可以为卤素，R3，R4，R5和R6独立地为氢，烷基，芳烷基或芳基; X和Y独立地是-O - ， - S-或-NR 16 - ，其中R 16是烷基，环烷基，烯基，芳基或芳烷基; W和Z独立地为O或S; 并且n，m，o和p独立地为0或1，有效地稳定有机材料以抵抗氧，热和/或光化辐射的有害影响。

    Substituted 3,7,9-trioxa-1-aza-2,8-diphosphaspiro[4.5]decanes and stabilized compositions
    7.
    发明授权
    Substituted 3,7,9-trioxa-1-aza-2,8-diphosphaspiro[4.5]decanes and stabilized compositions 失效
    取代的3,7,9-三氧杂-1-氮杂-2,8-二磷杂螺[4.5]癸烷和稳定组合物

    公开(公告)号：US5075482A

    公开(公告)日：1991-12-24

    申请号：US572728

    申请日：1990-08-23

    申请人： Raymond Seltzer ,  Paul A. Odorisio ,  Sai P. Shum ,  Stephen D. Pastor

    发明人： Raymond Seltzer ,  Paul A. Odorisio ,  Sai P. Shum ,  Stephen D. Pastor

    IPC分类号： C07F9/6587 ,  C08K5/5399

    CPC分类号： C08K5/5399 ,  C07F9/6587

    摘要： 3,7,9-Trioxa-1-aza-2,8-diphosphaspiro[4.5]decanes of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, alkyl, cycloalkyl, bicycloalkyl, tricycloalkyl or aryl; or can be halogen when n or m is zero,R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently hydrogen, alkyl, aralkyl or aryl;X and Y are independently --O-- --S--, or --NR.sub.16 -- where R.sub.16 is alkyl, cycloalkyl, alkenyl, aryl or aralkyl;W and Z are independently O or S; andn, m, o and p are independently zero or 1, are effective in stabilizing organic materials against the deleterious effects of oxygen, heat and/or actinic radiation.

    摘要翻译： （I）的3,7,9-三氧杂-1-氮杂-2,8-二磷杂螺[4.5]癸烷其中R 1和R 2独立地是氢，烷基，环烷基，双环烷基，三环烷基或芳基; 或当n或m为零时可以为卤素，R3，R4，R5和R6独立地为氢，烷基，芳烷基或芳基; X和Y独立地是-O-S-或-NR 16 - ，其中R 16是烷基，环烷基，烯基，芳基或芳烷基; W和Z独立地为O或S; 并且n，m，o和p独立地为0或1，有效地稳定有机材料以抵抗氧，热和/或光化辐射的有害影响。