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    PHTHALAZINE-CONTAINING ANTIDIABETIC COMPOUNDS
    5.
    发明公开
    PHTHALAZINE-CONTAINING ANTIDIABETIC COMPOUNDS 审中-公开
    PHTHALAZINHALTIGE抗糖尿病化合物

    公开(公告)号：EP2393810A1

    公开(公告)日：2011-12-14

    申请号：EP10703404.3

    申请日：2010-02-04

    申请人： Schering Corporation

    发明人： DAVIS, Jason, L. ,  MAYER, Michael, John ,  JOSIEN, Hubert, B.

    IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  A61K31/50 ,  A61P3/10

    CPC分类号： C07D417/12 ,  C07D417/14 ,  C07D487/04

    摘要： This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N-N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.

    NOVEL GAMMA SECRETASE INHIBITORS
    8.
    发明公开
    NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
    新的抑制剂GAMMASEKRETASE

    公开(公告)号：EP1740570A2

    公开(公告)日：2007-01-10

    申请号：EP05733367.6

    申请日：2005-04-04

    申请人： SCHERING CORPORATION

    发明人： ASBEROM, Theodros ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  PISSARNITSKI, Dmitri, A. ,  ZHAO, Zhiqiang ,  MCBRIAR, Mark, D.

    IPC分类号： C07D401/06 ,  C07D401/14 ,  C07D471/04 ,  A61K31/44 ,  A61P25/28

    CPC分类号： C07D451/04 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

    摘要： Gamma-secretase inhibitors of the formula: Chemical formula should be inserted here as it appears on the abstract in paper form. are useful in treating various neurodegenerative diseases, wherein, for example: R1 includes unsubstituted or substituted aryl or heteroaryl groups; R2 includes -C(O)-Y, alkylene-C(O)-Y, alkylene-cycloalkylene-C(O)-Y, cycloalkylene-alkylene-C(O)-Y, alkylene cycloalkylene-alkylene-C(O)-Y, cycloalkylene-C(O)-Y, -S(O)-Y, alkylene-S(O)-Y, alkylene-cycloalkylene-S(O)-Y, cycloalkylene-alkylene-S(O)-Y, alkylene cycloalkylene-alkylene-S(O)-Y, cycloalkylene-S(O)-Y, -S(O2)-Y, alkylene-S(O2)-Y, alkylene cycloalkylene S(O2)-Y, cycloalkylene alkylene S(O2)-Y, alkylene cycloalkylene-alkylene-S(O2)-Y, and cycloalkylene-S(O2)-Y, wherein Y is as defined herein, and each of said alkylene or cycloalkylene may be unsubstituted or substituted as provided herein; each R3 is independently includes H, alkyl, O alkyl, OH, N(R9)2, acyl, and aroyl; or the moiety (R3)2, together with the ring carbon atom to which it is shown attached in formula I, defines a carbonyl group, -C(O)-; each R3A and R3B independently includes H, or alkyl; R11 includes aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. One or more of the compounds of formula I, or pharmaceutically acceptable salts, solvates, and/or esters, or compositions comprised thereof, may be used to treat, e.g., Alzheimer's Disease.