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    NOVEL PROCESS
    5.
    发明公开
    NOVEL PROCESS 有权
    新工艺

    公开(公告)号：EP2496945A1

    公开(公告)日：2012-09-12

    申请号：EP10776336.9

    申请日：2010-11-03

    申请人： GlaxoSmithKline LLC

    发明人： BAMBOROUGH, Paul ,  CHUNG, Chun-Wa

    IPC分类号： G01N33/68 ,  C12N9/12

    CPC分类号： G01N33/566 ,  C12N9/1205 ,  G01N33/6803 ,  G01N2500/02 ,  G01N2500/10 ,  Y02A50/58

    摘要： A compound or a pharmaceutically acceptable salt or solvate thereof with a molecular weight in the range 100 to 750 which inhibits the binding of the first and/or second bromodomains of human BRD-2 to 4 to acetylated lysine residues of their physiological partner which is able to: a) form a hydrogen bonding interaction in which the compound accepts a hydrogen bond from the sidechain NH2 group of the asparagine residue found at: or b) accept a water-mediated hydrogen bond in which the compound accepts a hydrogen bond from a water that is itself hydrogen-bonded to the sidechain hydroxyl of the tyrosine residue found at and c) which are also able to form a Van der Waals interaction with a lipophilic binding region of a binding pocket such that one or more heavy atoms of the said compounds lie within a 5A range of any of the heavy atoms of the following bromodomain residues which define the binding pocket: for use in the treatment of chronic autoimmune and inflammatory conditions, acute inflammatory conditions or cancer.

    NOVEL sEH INHIBITORS AND THEIR USE
    6.
    发明公开
    NOVEL sEH INHIBITORS AND THEIR USE 审中-公开
    新型的抑制剂及其用途

    公开(公告)号：EP2217068A1

    公开(公告)日：2010-08-18

    申请号：EP08837193.5

    申请日：2008-10-10

    申请人： GlaxoSmithKline LLC

    发明人： DING, Yun ,  LONDREGAN, Allyn, T. ,  MARINO, Joseph Paul, Jr.

    IPC分类号： A01N43/66 ,  A61K31/53

    CPC分类号： C07D403/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

    摘要： The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R5a, R6a, A, B, Y, I, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

    摘要翻译： 本发明涉及新型sEH抑制剂及其在治疗由sEH酶介导的疾病中的用途。 具体而言，本发明涉及根据式I的化合物：其中R 1，R 2，R 5a，R 6a，A，B，Y，I和m如下定义，及其药学上可接受的盐。 本发明的化合物是sEH抑制剂并且可以用于治疗由sEH酶介导的疾病，例如高血压。 因此，本发明还涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制sEH和治疗与之相关的病症的方法。