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    Cyclopentapeptide derivatives and uses thereof
    3.
    发明授权
    Cyclopentapeptide derivatives and uses thereof 有权
    环戊四肽衍生物及其用途

    公开(公告)号：US09266924B2

    公开(公告)日：2016-02-23

    申请号：US13641947

    申请日：2011-04-20

    申请人： Oliver Demmer ,  Horst Kessler ,  Hans-Jürgen Wester ,  Margret Schottelius ,  Ingrid Dijkgraaf ,  Andreas Konard Buck

    发明人： Oliver Demmer ,  Horst Kessler ,  Hans-Jürgen Wester ,  Margret Schottelius ,  Ingrid Dijkgraaf ,  Andreas Konard Buck

    IPC分类号： A61K51/00 ,  A61M36/14 ,  C07K7/64 ,  A61K51/08

    CPC分类号： C07K7/64 ,  A61K51/088

    摘要： The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa1 to Xaa4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a detectable label; or ii) a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof, with the proviso that -L-Ar-D does not comprise a 18F-benzoyl residue.

    摘要翻译： 本发明尤其涉及具有式（I）结构的化合物或其药学上可接受的盐，其中Xaa1至Xaa4彼此独立，任选N-烷基化天然或非天然氨基酸，R为 H或甲基，L是连接体部分，Ar是包含芳族部分的间隔基，D包括，优选i）有机络合剂和可检测标记的组合; 或ii）可检测标记，有机络合剂或活性物质，所述活性物质特别选自细胞毒性剂，脂质，糖，糖结合物，糖衍生物，蛋白质及其组合，条件是-L-Ar- D不包含18 F-苯甲酰残基。

    Chelating Agent
    5.
    发明申请
    Chelating Agent 审中-公开
    螯合剂

    公开(公告)号：US20100081799A1

    公开(公告)日：2010-04-01

    申请号：US12517206

    申请日：2007-12-10

    申请人： Sebastian Knör ,  Armin Modlinger ,  Hans-Jürgen Wester ,  Horst Kessler

    发明人： Sebastian Knör ,  Armin Modlinger ,  Hans-Jürgen Wester ,  Horst Kessler

    IPC分类号： C07D257/02 ,  C07F5/00

    CPC分类号： C07D257/02 ,  Y02P20/55

    摘要： A compound of the formula: wherein R1 is selected from H, methyl, ethyl, carboxyl protecting groups and hydrophilic moieties, R2 and R3 are independently selected from H, methyl, ethyl and carboxyl protecting groups, R4 is selected from H, methyl, ethyl, hydrophilic moieties and carboxyl protecting groups, and R5 is an aryl, heteroaryl, alkyl or a combination of these groups and is substituted with a carbonyl group, an aminooxy group or a functional group suitable for participating in a cycloaddition reaction. The compounds of the invention may be useful as bifunctional chelating agents which allow chemoselective attachment to targeting molecules.

    摘要翻译： 下式的化合物：其中R1选自H，甲基，乙基，羧基保护基和亲水部分，R2和R3独立地选自H，甲基，乙基和羧基保护基，R4选自H，甲基，乙基 ，亲水部分和羧基保护基，R 5是芳基，杂芳基，烷基或这些基团的组合，并被羰基，氨基氧基或适于参与环加成反应的官能团取代。 本发明的化合物可用作允许化学选择性连接靶向分子的双功能螯合剂。