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    Rapamycin position 27 conjugates
    2.
    发明授权
    Rapamycin position 27 conjugates 失效
    雷帕霉素27位缀合物

    公开(公告)号：US06328970B1

    公开(公告)日：2001-12-11

    申请号：US09576952

    申请日：2000-05-24

    申请人： Katherine L. Molnar-Kimber ,  Craig E. Caufield ,  Timothy D. Ocain ,  Amadeo A. Failli

    发明人： Katherine L. Molnar-Kimber ,  Craig E. Caufield ,  Timothy D. Ocain ,  Amadeo A. Failli

    IPC分类号： A61K3900

    CPC分类号： G01N33/533 ,  A61K31/435 ,  A61K47/643 ,  A61K47/6835

    摘要： Provided are rapamycin conjugates which are useful as immunogenic molecules for the generation of antibodies specific for rapamycin or a derivative thereof, for measuring levels of rapamycin or derivatives thereof; for isolating rapamycin binding proteins; and detecting antibodies specific for rapamycin or derivatives thereof. This invention also provides monoclonal antibodies specific for rapamycin or a ring opened derivative of rapamycin.

    摘要翻译： 提供雷帕霉素缀合物，其可用作产生雷帕霉素或其衍生物特异性抗体的免疫原性分子，用于测量雷帕霉素或其衍生物的水平; 用于分离雷帕霉素结合蛋白; 并检测对雷帕霉素或其衍生物特异的抗体。 本发明还提供对雷帕霉素特异性的单克隆抗体或雷帕霉素的开环衍生物。

    Biotin esters of rapamycin
    6.
    发明授权
    Biotin esters of rapamycin 失效
    雷帕霉素的生物素酯

    公开(公告)号：US5504091A

    公开(公告)日：1996-04-02

    申请号：US224206

    申请日：1994-04-14

    申请人： Katherine L. Molnar-Kimber ,  Timothy D. Ocain ,  Steven K. Vernon ,  John J. Huang

    发明人： Katherine L. Molnar-Kimber ,  Timothy D. Ocain ,  Steven K. Vernon ,  John J. Huang

    IPC分类号： C07D519/00 ,  G01N33/94 ,  A61K31/395

    CPC分类号： C07D519/00 ,  G01N33/9446 ,  Y10S435/975 ,  Y10T436/141111

    摘要： A compound of the structure ##STR1## R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR2## X is ##STR3## Y is ##STR4## Z is --CH.sub.2 --, --S--S--, or ##STR5## R.sup.3 is hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, --(CH.sub.2).sub.q CO.sub.2 R.sup.5, --(CH.sub.2).sub.r NR.sup.6 R.sup.7, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazoylmethyl, halo, trifluoromethyl, or phenyl which is optionally mono-, di-, or tri-substituted;R.sup.4, R.sup.6, and R.sup.7 are each, independently, hydrogen, alkyl, or arylalkyl;R.sup.5 is hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, or phenyl which is optionally mono-, di-, or tri-substituted;h=0-1;j=0-1;m=0-6;n=0-6;p=0-10;q=0-10;r=0-6;with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, or a pharmaceutically acceptable salt thereof which is useful for inducing immunosuppression; in the treatment of transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, solid tumors, fungal infections, adult T-cell leukemia/lymphoma, and hyperproliferative vascular disorders; for measuring levels of rapamycin; for isolating rapamycin-binding proteins; and detecting monoclonal antibodies specific for rapamycin or derivatives thereof.

    摘要翻译： 结构式I R1和R2的化合物各自独立地为氢或Y是Z，其中Z是-CH 2 - ，-SS-或者R 3是氢， 烷基，芳基烷基，烯基，炔基， - （CH 2）q CO 2 R 5， - （CH 2）r NR 6 R 7，氨基甲酰基烷基，氨基烷基，羟基烷基，脒基烷基，巯基烷基，烷基硫代烷基，吲哚基甲基，羟基苯基甲基，咪唑基甲基，卤素，三氟甲基或苯基， 二取代或三取代的; R4，R6和R7各自独立地为氢，烷基或芳基烷基; R5是氢，烷基，芳基烷基，烯基，炔基或任选被一或二或三取代的苯基; h = 0-1; j = 0-1; m = 0-6; n = 0-6; p = 0-10; q = 0-10; r = 0-6; 条件是R1和R2不同时为氢，或其药学上可接受的盐，可用于诱导免疫抑制; 在移植排斥反应的治疗中，宿主与移植物疾病，自身免疫疾病，炎症疾病，实体瘤，真菌感染，成人T细胞白血病/淋巴瘤和过度增殖性血管疾病; 用于测量雷帕霉素的含量; 用于分离雷帕霉素结合蛋白; 并检测对雷帕霉素或其衍生物特异性的单克隆抗体。