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    THIAZOLO-PYRIDINE COMPOUNDS AS HIF MODULATORS
    7.
    发明公开
    THIAZOLO-PYRIDINE COMPOUNDS AS HIF MODULATORS 审中-公开
    三唑并嘧啶二酮类化合物

    公开(公告)号：EP3124489A1

    公开(公告)日：2017-02-01

    申请号：EP16174358.8

    申请日：2007-04-04

    申请人： Fibrogen, Inc.

    发明人： DENG, Shaojiang ,  WU, Min ,  TURTLE, Eric D. ,  HO, Wen-Bin ,  AREND, Michael P. ,  CHENG, Heng ,  FLIPPIN, Lee A.

    IPC分类号： C07D513/04 ,  A61K31/4365 ,  A61P7/06 ,  A61P9/10

    摘要： The present invention relates to novel compounds of formula I

    wherein:
    q is 0 or 1;
    • A is -S- and B is =N-; or
    • A is =N- and B is -S-;
    one of -A≃C(R 6 )- or -B≃C(R 6 )- is a double bond and the other is a single bond;
    R 1 is selected from the group consisting of hydroxyl, alkoxy, substituted alkoxy, acyloxy, cycloalkoxy, substituted cycloalkoxy, aryloxy, substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, heterocyclyloxy, substituted heterocyclyloxy, mercapto, thioether, sustituted alkylthio, arylsulfanyl, heteroarylsulfanyl, amino, substituted amino, acylamino, and aminoacyl;
    R 2 is selected from the group consisting of hydrogen, deuterium, and methyl;
    R 3 is selected from the group consisting of hydrogen, deuterium, alkyl, and substituted alkyl;
    R 4 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; and
    R 5 and R 6 are as defined in claim 1;
    capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).

    摘要翻译： 本发明涉及新的式I化合物，其中：q为0或1; ¢A是-S-，B是= N-; 或¢A为= N-和B为-S-; -A‰ƒC（R 6） - 或-B‰ƒC（R 6） - 是双键，另一个是单键; R 1选自羟基，烷氧基，取代的烷氧基，酰氧基，环烷氧基，取代的环烷氧基，芳氧基，取代的芳氧基，杂芳氧基，取代的杂芳氧基，杂环氧基，取代的杂环氧基，巯基，硫醚，取代的烷硫基，芳基硫烷基，杂芳基硫烷基，氨基 取代氨基，酰氨基和氨酰基; R 2选自氢，氘和甲基; R 3选自氢，氘，烷基和取代的烷基; R 4选自氢，烷基和取代的烷基; R 5和R 6如权利要求1所定义; 能够调节缺氧诱导因子（HIF）的稳定性和/或活性。

    TREATMENT FOR HIGH CHOLESTEROL
    9.
    发明公开
    TREATMENT FOR HIGH CHOLESTEROL 审中-公开
    治疗高胆固醇VALUES

    公开(公告)号：EP2822545A2

    公开(公告)日：2015-01-14

    申请号：EP13758366.2

    申请日：2013-03-08

    申请人： Fibrogen, Inc.

    发明人： LIN, Al, Y. ,  NEFF, Thomas, B. ,  YU, Kin-Hung

    IPC分类号： A61K31/00

    CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/472 ,  A61K45/06 ,  C07D217/26 ,  A61K2300/00

    摘要： The present invention provides a method for treatment of high cholesterol by reducing low density lipoprotein cholesterol (LDL-C) and/or very low density Opoproiein cholesterol (VLDL-C) in subjects In need thereof by administering a compound that inhibits HIF hydroxylase activity. The method is useful, for reducing LDL cholesterol levels and total cholesterol levels even In subjects already undergoing treatment with other cholesterol-lowering medications, for example statins, fibrates, nicotinic acids and bile acid-binding resins, and in patients having chronic kidney disease or end stage renal disease,
    inter alia.