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    Oligomer-Protease Inhibitor Conjugates
    73.
    发明申请
    Oligomer-Protease Inhibitor Conjugates 审中-公开
    低聚物 - 蛋​​白酶抑制剂缀合物

    公开(公告)号：US20110195912A1

    公开(公告)日：2011-08-11

    申请号：US13119107

    申请日：2009-09-17

    申请人： Jennifer Riggs-Sauthier ,  Laurie A. Vander Veen

    发明人： Jennifer Riggs-Sauthier ,  Laurie A. Vander Veen

    IPC分类号： A61K38/55 ,  C07K5/10 ,  C07K5/08 ,  A61P31/20 ,  A61P31/14

    CPC分类号： A61K47/60

    摘要： Provided are small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the small molecule drug not attached to the water soluble oligomer.

    摘要翻译： 提供通过共价连接水溶性寡聚物进行化学修饰的小分子药物。 本发明的缀合物当通过多种施用途径中的任一种施用时，显示出与未附着于水溶性低聚物的小分子药物不同的特征。

    Synthesis of Azo Bonded Immunoregulatory Compounds
    79.
    发明申请
    Synthesis of Azo Bonded Immunoregulatory Compounds 有权
    偶氮键合的免疫调节化合物的合成

    公开(公告)号：US20080033153A1

    公开(公告)日：2008-02-07

    申请号：US11631582

    申请日：2005-07-07

    申请人： Jennifer Riggs-Sauthier ,  Nnochiri Ekwuribe

    发明人： Jennifer Riggs-Sauthier ,  Nnochiri Ekwuribe

    IPC分类号： C07C245/08

    CPC分类号： C07C245/08

    摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.

    摘要翻译： 公开了制备式I化合物的方法：其中R 1，R 3和R 4独立地是氢或C 1 C 1至C 4烷基，R 2是：其中R 5选自氢和C C 1至C 4烷基，或其中R 6，R 7和R 8是 独立地是氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。 该方法可以包括将适当官能化的苯胺化合物转化为重氮盐（可以首先通过还原硝基苯形成苯胺化合物）并将重氮盐与适当官能化的苯化合物偶联。 适当官能化的苯胺化合物包括伯醇或醛基，然后将其氧化成羧酸基团，或包括被水解成羧酸基团的腈或酰胺基团。 所述方法还可以涉及适当官能化的硝基苯的直接偶联（通过还原硝基以形成偶氮键）。 化合物及其代谢物可用于治疗或预防各种疾病，特别是胃肠道的炎性病症。