DEPSIPEPTIDE AND CONGENERS THEREOF FOR USE AS IMMUNOSUPPRESSANTS
    94.
    发明授权
    DEPSIPEPTIDE AND CONGENERS THEREOF FOR USE AS IMMUNOSUPPRESSANTS 无效
    酯肽及其类似物对使用免疫抑制剂

    公开(公告)号:EP1246839B1

    公开(公告)日:2004-06-16

    申请号:EP00983997.8

    申请日:2000-12-06

    IPC分类号: C07K11/00 C07K5/10 A61K38/15

    摘要: Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.

    NUCLEIC ACIDS, PROTEINS, AND ANTIBODIES
    96.
    发明公开

    公开(公告)号:EP1254165A2

    公开(公告)日:2002-11-06

    申请号:EP01946887.5

    申请日:2001-01-17

    摘要: The present invention relates to novel proteins. More specifically, isolated nucleic acid molecules are provided encoding novel polypeptides. Novel polypeptides and antibodies that bind to these polypeptides are provided. Also provided are vectors, host cells, and recombinant and synthetic methods for producing human polynucleotides and/or polypeptides, and antibodies. The invention further relates to diagnostic and therapeutic methods useful for diagnosing, treating, preventing and/or prognosing disorders related to these novel polypeptides. The invention further relates to screening methods for identifying agonists and antagonists of polynucleotides and polypeptides of the invention. The present invention further relates to methods and/or compositions for inhibiting or enhancing the production and function of the polypeptides of the present invention.

    NOVEL PROCESS FOR THE SYNTHESIS OF EXOCHELINS
    99.
    发明公开
    NOVEL PROCESS FOR THE SYNTHESIS OF EXOCHELINS 审中-公开
    新工艺HEXOCHELINE的制备

    公开(公告)号:EP1105416A1

    公开(公告)日:2001-06-13

    申请号:EP99941047.5

    申请日:1999-08-11

    IPC分类号: C07K11/00

    CPC分类号: C07K11/00 Y02P20/55

    摘要: A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)]serine or L-N-[2-benzyloxy(benzoyl)] threonine, creating L-N-t-Boc-εhydroxynorleucine and reacting same to produce L-N-Boc-ε-bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc-ε-bromonorleucine trimethylsilylethyl ester to give an L-N?2-Boc-N6¿-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N?2-Boc-N6¿-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy(benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid , preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.