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17 条记录 (耗时 0.032 秒)

    Gem-distributed esters of rapamycin
    1.
    发明授权
    Gem-distributed esters of rapamycin 失效
    雷公藤分泌的酯

    公开(公告)号：US5385910A

    公开(公告)日：1995-01-31

    申请号：US156334

    申请日：1993-11-22

    申请人： Timothy D. Ocain ,  Guy A. Schiehser

    发明人： Timothy D. Ocain ,  Guy A. Schiehser

    IPC分类号： C07D498/18 ,  A61K31/445 ,  C07D471/04

    CPC分类号： C07D498/18

    摘要： Compounds of the structure ##STR1## R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a saturated heterocycle wherein the heterocyclic ring may be optionally mono-, di-, or tri-substituted;m=0-1; andn=0-6;with the proviso that R and R.sup.1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, and ##STR3## R.sup.1 is ##STR4## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a saturated heterocycle wherein the heterocyclic ring may be optionally mono-, di-, or tri-substituted;m=0-1; andn=0-6;or a pharmaceutically acceptable salt thereof which are useful as immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agents.

    摘要翻译： 结构式I R和R 1的化合物各自独立地为氢，或者R 2和R 3各自独立地为烷基，芳基烷基，或者可以一起形成环烷基环; R 4和R 5各自独立地为氢，烷基，芳基烷基，或者可以一起形成饱和杂环，其中杂环可以是任选的单，二或三取代; m = 0-1; 并且n = 0-6; 条件是R和R 1不是氢或其药学上可接受的盐，而R 2和R 3各自独立地为氢，烷基，芳基烷基，或者可以一起形成 环烷基环; R 4和R 5各自独立地为氢，烷基，芳基烷基，或者可以一起形成饱和杂环，其中杂环可以是任选的单，二或三取代; m = 0-1; 并且n = 0-6; 或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

    Rapamycin position 27 conjugates
    3.
    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
    4.
    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。

    Method for inhibiting immune response
    6.
    发明授权
    Method for inhibiting immune response 失效
    抑制免疫反应的方法

    公开(公告)号：US5708022A

    公开(公告)日：1998-01-13

    申请号：US482308

    申请日：1995-06-07

    申请人： Cecilia M. Bastos ,  Timothy D. Ocain

    发明人： Cecilia M. Bastos ,  Timothy D. Ocain

    IPC分类号： C07F15/00 ,  A61K31/28

    CPC分类号： C07F15/0053

    摘要： Use of ruthenium complexes as immunosuppressive agents to prevent or significantly reduce graft rejection in organ and bone marrow transplantation is described. The ruthenium complexes can also be used as immunosuppressant drugs for T-lymphocyte mediated autoimmune diseases, such as diabetes, and may be useful in alleviating psoriasis and contact dermatitis. The ruthenium complexes can also be used therapeutically in the treatment of hyperproliferative vascular disease.

    摘要翻译： 描述了使用钌络合物作为免疫抑制剂以预防或显着降低器官和骨髓移植中的移植排斥反应。 钌络合物也可用作T淋巴细胞介导的自身免疫疾病如糖尿病的免疫抑制药物，可用于缓解牛皮癣和接触性皮炎。 钌络合物也可用于治疗过度增生性血管疾病。

    Aromatic compounds for inhibiting immune response
    9.
    发明授权
    Aromatic compounds for inhibiting immune response 失效
    用于抑制免疫反应的芳香族化合物

    公开(公告)号：US5739169A

    公开(公告)日：1998-04-14

    申请号：US656468

    申请日：1996-05-31

    申请人： Timothy D. Ocain ,  Huai Gao ,  Jeffrey I. Krieger ,  Theresa M. Sampo

    发明人： Timothy D. Ocain ,  Huai Gao ,  Jeffrey I. Krieger ,  Theresa M. Sampo

    IPC分类号： C07C229/58 ,  C07C233/43 ,  C07D257/04 ,  A61K31/135 ,  A01N33/02 ,  C07C229/00

    CPC分类号： C07D257/04 ,  C07C229/58 ,  C07C233/43

    摘要： Novel compounds ##STR1## wherein R.sup.1 to R.sup.13 are independently selected from C.sub.2 -C.sub.4 linear and branched alkyls, H, NH.sub.2, CH.sub.3, OR.sup.14, fluorine, chlorine, iodine, NO.sub.2, CF.sub.3, NHCOCH.sub.3, NHCOOtBu, NHR.sup.15, NR.sup.16 R.sup.17 and phenyl, for use as immunosuppressive agents to prevent or significantly reduce graft rejection in organ and bone marrow transplantation are described. The novel compounds can also be used as an immunosuppressant drug for T-lymphocyte mediated autoimmune diseases, such as diabetes, and may be useful in alleviating psoriasis and contact dermatitis. Additionally, the novel compounds can be used for antiproliferation and gene therapy.

    摘要翻译： 其中R 1至R 13独立地选自C 2 -C 4直链和支链烷基，H，NH 2，CH 3，OR 14，氟，氯，碘，NO 2，CF 3，NHCOCH 3，NHCOOtBu，NHR 15，NR 16 R 17和苯基， 用作免疫抑制剂以预防或显着降低器官和骨髓移植中的移植物排斥。 新型化合物也可用作T淋巴细胞介导的自身免疫性疾病如糖尿病的免疫抑制药物，可用于缓解牛皮癣和接触性皮炎。 另外，新型化合物可用于抗增殖和基因治疗。