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    Tri-aza macrocycles and processes for their preparation
    2.
    发明授权
    Tri-aza macrocycles and processes for their preparation 失效
    三环大环化合物及其制备方法

    公开(公告)号：US5247077A

    公开(公告)日：1993-09-21

    申请号：US865816

    申请日：1992-03-31

    申请人： David Parker ,  Michael A. W. Eaton

    发明人： David Parker ,  Michael A. W. Eaton

    IPC分类号： C07D255/02 ,  C07F9/6515

    CPC分类号： C07F9/6515 ,  C07D255/02

    摘要： ##STR1## Tri-aza macrocycles of formula (I), wherein m and n, which may be the same or different, is each zero or an integer 1, 2, or 3; p is zero or an integer 1 or 2; q is zero or an integer from 1 to 6 inclusive; R
    1 , R
    2 and R
    3 , which may be the same or different, is each a hydrogen atom or a group --CO
    2 H or --P(O)(XH)R
    4 (where X is an oxygen or sulpher atom and R
    4 is a hydrogen atom or an alkyl or alkoxy group), with the proviso that at least one of R
    1 , R
    2 and R
    3 is a --P(O)(XH)R
    4 group; L is a covalent bond or a linker group; Z is a hydrogen atom or a reactive functional group; and metal complexes and/or salts thereof; are described together with processes for their preparation and compositions containing them. The compounds are useful as imaging agents, and in the treatment of abnormal cell disorders, such as in the treatment of tumours, and may be coupled to other molecules, such as proteins, for use in diagnosis and therapy.

    摘要翻译： （1）式（I）的三氮杂大环，其中m和n可以相同或不同，分别为零或整数1,2或3; p为零或整数1或2; q为0或1〜6的整数; R 1，R 2和R 3可以相同或不同，分别为氢原子或-CO 2 H或-P（O）（XH）R 4（其中X为氧或硫原子，R4为氢原子或 烷基或烷氧基），条件是R 1，R 2和R 3中的至少一个是-P（O）（XH）R 4基团; L是共价键或连接基团; Z是氢原子或反应性官能团; 和金属络合物和/或其盐; 与其制备方法和含有它们的组合物一起描述。 这些化合物可用作显像剂，以及用于治疗异常细胞疾病，例如治疗肿瘤，并且可以与其它分子例如蛋白质偶联用于诊断和治疗。

    Tetra-aza macrocycles and processes for their preparation
    4.
    发明授权
    Tetra-aza macrocycles and processes for their preparation 失效
    四环大环化合物及其制备方法

    公开(公告)号：US5342936A

    公开(公告)日：1994-08-30

    申请号：US964117

    申请日：1992-10-02

    申请人： David Parker ,  Michael A. W. Eaton

    发明人： David Parker ,  Michael A. W. Eaton

    IPC分类号： A61K51/04 ,  A61K51/10 ,  C07F9/6524 ,  C07D255/02

    CPC分类号： C07F9/6524 ,  A61K51/0482 ,  A61K51/1093 ,  A61K2123/00

    摘要： (1) Tetra-aza macrocycles of formula (I), wherein m and n, which may be the same or different, is each zero or an integer 1,2, or 3; d is zero or an integer 1, 2 or 3; q is zero or an integer from 1 to 6 inclusive; R, R1, R2 and R3, which may be the same or different, is each a hydrogen atom or a group -P(O)(XH)R4 (where X is an oxygen or sulphur atom and R4 is a hydrogen atom or an alkyl or alkoxy group), with the proviso that at least one of R, R1, R2 and R3 is a -P(O)(XH)R4 group; L is a covalent bond or a linker group; Z is a hydrogen atom or a reactive functional group; and metal complexes and/or salts thereof; are described together with processes for their preparation and compositions containing them. The compounds are useful for imaging and in the treatment of abnormal cell disorders, such as in the treatment of tumours, and may be coupled to other molecules, such as proteins for use in diagnosis and therapy.

    摘要翻译： （1）式（I）的四氮杂大环，其中m和n可以相同或不同，分别为零或整数1,2或3; d为零或整数1,2或3; q为0或1〜6的整数; R，R 1，R 2和R 3可以相同或不同，分别为氢原子或基团-P（O）（XH）R4（其中X为氧或硫原子，R4为氢原子或 烷基或烷氧基），条件是R，R 1，R 2和R 3中的至少一个是-P（O）（XH）R 4基团; L是共价键或连接基团; Z是氢原子或反应性官能团; 和金属络合物和/或其盐; 与其制备方法和含有它们的组合物一起描述。 所述化合物可用于成像和治疗异常细胞病症，例如治疗肿瘤，并且可以与其它分子（例如用于诊断和治疗的蛋白质）偶联。