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    Method of identifying glycosyl transferase binding compounds
    1.
    发明申请
    Method of identifying glycosyl transferase binding compounds 审中-公开
    鉴定糖基转移酶结合化合物的方法

    公开(公告)号：US20050026214A1

    公开(公告)日：2005-02-03

    申请号：US10489034

    申请日：2002-09-02

    申请人： Jacques Biton ,  Francois Michoux ,  Jean-Noel Veltz ,  Jacques Dumas

    发明人： Jacques Biton ,  Francois Michoux ,  Jean-Noel Veltz ,  Jacques Dumas

    IPC分类号： G01N33/50 ,  A61K45/00 ,  A61P31/04 ,  C12N9/10 ,  C12N15/09 ,  C12Q1/48 ,  G01N33/15 ,  G01N33/573 ,  G01N33/68 ,  G01N33/53

    CPC分类号： G01N33/6845 ,  C12Q1/48 ,  G01N33/68

    摘要： The present invention relates to a method of identifying, screening or selecting a compound which binds to the transglycosylation site of a recombinant glycosyl transferase, comprising the steps consisting in: a) bringing said compound into contact with said recombinant protein before, after or at the same time as said recombinant protein is brought into contact with a transglycosylation activity inhibitor, said inhibitor being labeled with a label that generates a direct or indirect signal, b) studying said signal linked to said recombinant protein, the binding of said compound to the transglycosylation site being deduced from the difference between the signal obtained in step b) and the signal obtained in the absence of said compound.

    摘要翻译： 本发明涉及鉴定，筛选或选择与重组糖基转移酶的转糖基化位点结合的化合物的方法，其包括以下步骤：a）使所述化合物与所述重组蛋白质在之前或之后接触 与所述重组蛋白质与转糖基化活性抑制剂接触的同时，所述抑制剂用产生直接或间接信号的标记进行标记，b）研究与所述重组蛋白相连的所述信号，所述化合物与转糖基化的结合 从步骤b）中获得的信号与在不存在所述化合物的情况下获得的信号之间的差异推断出位点。

    Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
    4.
    发明授权
    Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors 有权
    吡啶，喹啉和异喹啉N-氧化物作为激酶抑制剂

    公开(公告)号：US07678811B2

    公开(公告)日：2010-03-16

    申请号：US11775457

    申请日：2007-07-10

    申请人： Jacques Dumas ,  William J. Scott ,  Bernd Riedl

    发明人： Jacques Dumas ,  William J. Scott ,  Bernd Riedl

    IPC分类号： C07D401/02 ,  A61K31/44 ,  A61K31/47

    CPC分类号： C07D213/89 ,  C07D215/60 ,  C07D217/08

    摘要： This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angogenesis disorders.

    摘要翻译： 本发明涉及含有吡啶，喹啉或异喹啉官能团的脲化合物，其在氮杂原子处被氧化并且可用于治疗（i）raf介导的疾病，例如癌症，（ii）p38介导的疾病，例如 炎症和骨质疏松症，和（iii）VEGF介导的疾病，如血管发生障碍。