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    3-oxo-1, 3-dihydro-indazole-2-carboxylic acid amide derivatives as phospholipase inhibitors
    3.
    发明申请
    3-oxo-1, 3-dihydro-indazole-2-carboxylic acid amide derivatives as phospholipase inhibitors 审中-公开

    公开(公告)号：US20060211755A1

    公开(公告)日：2006-09-21

    申请号：US10544910

    申请日：2004-03-25

    申请人： Patrick Eacho ,  Patricia Foxworthy-Mason ,  Ho-Shen Lin ,  Jose Lopez ,  Marian Mosior ,  Michael Richett

    发明人： Patrick Eacho ,  Patricia Foxworthy-Mason ,  Ho-Shen Lin ,  Jose Lopez ,  Marian Mosior ,  Michael Richett

    IPC分类号： A61K31/416 ,  C07D231/56

    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-C13alkyl; 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 one 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 W and 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,—C12alkylaryl, C,—C12alkylcyclohexyl, C, C12alkylcyclopentyl, C,—C12alkylheterocyclic, (CH2)m000H, (CH2)mC0(C,—C,o)alkyl, (CH2)m COO(C,—C,o)alkyl, (CH2)mCOO(C1-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, CZCBalkynyl, 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 sallvate 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.