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    3-OXO-1,3-DIHYDRO-INDAZOLE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS PHOSPHOLIPASE INHIBITORS
    118.
    发明授权
    3-OXO-1,3-DIHYDRO-INDAZOLE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS PHOSPHOLIPASE INHIBITORS 有权
    3-氧代-1,3-二氢吲哚-2-碳酸钠衍生物ALS磷脂酰胺抑制剂

    公开(公告)号：EP1610779B1

    公开(公告)日：2009-09-09

    申请号：EP04723448.9

    申请日：2004-03-25

    申请人： ELI LILLY AND COMPANY

    发明人： EACHO, Patrick, Irving ,  FOXWORTHY-MASON, Patricia, Sue ,  LIN, Ho-Shen ,  LOPEZ, Jose, Eduardo ,  MOSIOR, Marian, Kazimierz ,  RICHETT, Michael, Enrico

    IPC分类号： A61K31/416 ,  C07D231/56 ,  C07C275/26 ,  A61P3/06

    CPC分类号： C07D231/56 ,  C07D405/12 ,  C07D409/12

    摘要： The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C5-C13alky1;:C,-C,2haloalkyl, C4­C,2alkenyl, C4-C12alkynyl, or C,- C5alkylcycloalkyl, C3-C8cycloalkyl, C,­ C5alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with onf to three substituents independently selected from C,-C8a)kyl, C,-C8haloalkyl,`C2-CBalkenyl, C2-C8a)kynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (C}12)m000C,-Csalkyl, (CH2)mNRaRb, and C,­C4alkylcycloalkyl; wherein Wand Rb are independently selected from hydrogen, C,­CBalkyl, C2-CBalkenyl, C2-CBalkynyl, and C,- C5alkylcycloalkyl; R2 is hydrogen; R3, R4, R5, and R6, are independently selected from hydrogen, C,-C12alkyl, C2­C,2haloalkyl, C2-C,2 alkenyl, C2-C12alkynyl, C,-Ct2alkylaryl, C,-C12alkylcyclohexyl, C,­ C12alkylcyclopentyl, C,-C1zalkylheterocyclic, (CH2)m000H, (CH2)mC0(C,-C,o)alkyl, (CH2)m COO(C,-C,o)alkyl, (CH2)mCOO(C,-C,o)alkylaryl, C,-C,oalkylamino, halo, (CH2)mCONH2, (CH2)rCONRaRb, phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from CBalkyl, C,-CBhaloalkyl, C2-CBalkenyl, CZ CBalkynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (CH2)m000C,-Csalkyl, and C,-C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,-Cloalkyl, C,­C,ohaloalkyl, C2-C,oalkenyl, C2-C,oalkynyl, C,-C6alkylaryl, C,-C6alkylcyclohexyl, C - C6aikylcyclopentyl, C,-C6alkylheterocyclic, or aryl; or a pharmaceutically acceptable sal lvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.