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    PEG conjugates of NK4
    3.
    发明授权
    PEG conjugates of NK4 有权
    NK4的PEG缀合物

    公开(公告)号：US07846896B2

    公开(公告)日：2010-12-07

    申请号：US11869797

    申请日：2007-10-10

    申请人： Michael Brandt ,  Apollon Papdimitriou

    发明人： Michael Brandt ,  Apollon Papdimitriou

    IPC分类号： A61K38/18 ,  C07K38/00

    CPC分类号： A61K47/60

    摘要： The present invention provides a conjugate consisting essentially of a NK4 molecule and a polyethylene glycol group having a molecular weight of from about 20 to about 40 kDa. The invention also provides a composition in which the monoPEGylated conjugates comprise at least 90% of the total of pegylated NK4 molecules and unpegylated NK4 molecules in the composition. Also provided is a composition in which the monoPEGylated conjugates comprise conjugates in which the PEG groups are attached to groups randomly selected from the lysine side chains of NK4 molecules and the N-terminal amino groups of NK4 molecules. A method for the treatment of cancer by administering 1 to 30 mg monoPEGylated NK4 per kg per day is further provided.

    摘要翻译： 本发明提供了基本上由NK4分子和分子量为约20至约40kDa的聚乙二醇基团组成的缀合物。 本发明还提供了一种组合物，其中单聚乙二醇化缀合物包含组合物中聚乙二醇化NK4分子和未聚乙二醇化NK4分子总数的至少90％。 还提供了其中单PEG化缀合物包含缀合物的组合物，其中PEG基团连接到随机选自NK4分子的赖氨酸侧链和NK4分子的N-末端氨基的基团。 进一步提供通过每公斤施用1至30mg单PEG化的NK4来治疗癌症的方法。

    Tripeptides and tripeptide derivatives for the treatment of postlesional disease of the nervous system
    8.
    发明授权
    Tripeptides and tripeptide derivatives for the treatment of postlesional disease of the nervous system 失效
    用于治疗神经系统疾病的三肽和三肽衍生物

    公开(公告)号：US07122524B2

    公开(公告)日：2006-10-17

    申请号：US10635805

    申请日：2003-08-05

    申请人： Jean Rapin ,  Hans Klaus Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

    发明人： Jean Rapin ,  Hans Klaus Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

    IPC分类号： A61K38/00 ,  A61K38/06 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07K38/00

    CPC分类号： A61K38/06

    摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy the following formula (I): (see formula I as in paper form) wherein X represents OH, (C1-5) alkoxy, NH2, NH—C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C1-5) alkoxy groups, (C1-5) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, and Pro; Y1 and Y2 independently from each other represent H or (C1-5) alkyl; R3 and R4 independently from each other represent H, OH, (C1-5) alkyl or (C1-5) alkoxy, provided that R3 and R4 are not both OH or (C1-5) alkoxy; and R5 represents H, OH, (C1-5) alkyl or (C1-5) alkoxy; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及特异性三肽用于治疗缺血性，创伤性或毒性起源性的postsional疾病的用途。 三肽衍生物满足下列通式（I）：（参见纸上形式的式I）其中X表示OH，（C 1-5 - ）烷氧基，NH 2， NH-C 1-5 - 烷基，N（C 1-5烷基）亚烷基。 R 1是衍生自氨基酸Phe，Tyr，Trp，Pro之一的残基，其各自可以任选地被一个或多个（C 1-5 - （C 1-5）烷基或卤素原子，以及Ala，Val，Leu或Ile; R 2是来源于氨基酸Gly，Ala，Ile，Val，Ser，Thr和Pro之一的残基; Y 1和Y 2彼此独立地表示H或（C 1-5烷基）烷基; R 3和R 4彼此独立地表示H，OH，（C 1-5烷基）烷基或（C 1〜 5 S）烷氧基，条件是R 3和R 4不同时为OH或（C 1-5）烷氧基; 和R 5表示H，OH，（C 1-5烷基）烷基或（C 1-5 H 5）烷氧基; 或其药学上可接受的盐。