Process for production of heterodimers of glutamic acid
    13.
    发明授权
    Process for production of heterodimers of glutamic acid 有权
    谷氨酸异二聚体生产工艺

    公开(公告)号:US08465725B2

    公开(公告)日:2013-06-18

    申请号:US12815637

    申请日:2010-06-15

    IPC分类号: A61K51/00 A61K49/00

    摘要: A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of radionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR′, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR′, S, S(O)2, C(O)2, (CH2)p; R′ is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.

    摘要翻译: 用于制备放射性标记的式(I)化合物的制备方法包括在酸性条件下,在氧化剂存在下使式(II)化合物与卤素的放射性核素源反应,其中:* I为123I,124I,125I 或131I; R是低级烷基,任选被一个或多个氟原子取代; Q是C(O),O,NR',S,S(O)2,C(O)2,(CH 2)p; Y是C(O),O,NR',S,S(O)2,C(O)2,(CH 2)p; R'是H,C(O),S(O)2,C(O)2; Z是H,C 1 -C 4烷基,苄基,取代的苄基或三烷基甲硅烷基; m为0,1,2,3,4或5; n为0,1,2,3,4,5或6; p为0,1,2,3,4,5或6。

    PSMA-targeted dendrimers
    16.
    发明授权

    公开(公告)号:US09687572B2

    公开(公告)日:2017-06-27

    申请号:US13991812

    申请日:2011-12-06

    IPC分类号: A61K51/04 A61K51/06

    CPC分类号: A61K51/0497 A61K51/065

    摘要: A dendrimer conjugate according to Formula (I), or its pharmaceutically acceptable salt, or solvate thereof: and complexes of Formula I conjugates with metals radionuclides of elements such as rhenium, technetium, yttrium, lutetium and others to provide a complex for imaging tissues or for the radiotherapeutic treatment of cancer tissue. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.