发明名称 Aryl piperidine derivatives as inducers of ldl-receptor expression
摘要 The invention concerns a compound of formula (I), wherein Ar1 represents phenyl, naphthyl or phenyl fused by a C3-8cycloalkyl, where each group is substituted by a group -O-Z and optionally one to three further groups independently represented by R<1>; Ar2 represents phenyl or 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C1-4 alkyl and C1-4 alkoxy; Ar3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkenyloxy, C1-4 perfluoroalkoxy, C1-4 acylamino or an electron withdrawing group; A represents -C(H)-; E represents -C1-6alkylene-; X represents -CON(H or C1-4alkyl)- or -N(H or C1-4alkyl)CO-; Y represents a direct link, -N(H or C1-4alkyl)CO- or -CON(H or C1-4alkyl)-; Z represents a metabolically labile group; R<1 >represents halogen, -S(C1-4alkyl), -O-(C0-4 alkylene)-R<2 >or -(C0-4alkylene)-R<2>, where each alkylene group may additionally incorporate an oxygen in the chain, with the proviso that there are at least two carbon atoms between any chain heteroatoms; R<2 >represents: i) hydrogen, C1-4 perfluoroalkyl, C2-3alkenyl, ii) phenyl, naphthyl, a 5- or 6-membered heteroaromatic group or 1,2,3,4-tetrahydronaphthyl, optionally substituted by one or two halogen, hydroxy, C1-4 alkyl, C1-4 alkoxy groups, iii) C3-8cycloalkyl, a 3-7 membered heterocycloalkyl, iv) amino, C1-4 alkylamino or di-C1-4alkylamino, with the proviso that there are at least two carbon atoms between any chain heteroatoms; and physiologically acceptable salts, solvates and pharmaceutical compositions thereof and their use in treating disorders associated with elevated circulating levels of LDL-cholesterol.
申请公布号 US2004072865(A1) 申请公布日期 2004.04.15
申请号 US20030250711 申请日期 2003.10.20
申请人 BOUILLOT ANNE MARIE JEANNE;BOMBRUN AGNES;ANDRE DUMAITRE BERNARD;GOSMINI RONTAIN LUC;CONGREVE MILES STUART;RAMSDEN NIGEL GRAHAME 发明人 BOUILLOT ANNE MARIE JEANNE;BOMBRUN AGNES;ANDRE DUMAITRE BERNARD;GOSMINI RONTAIN LUC;CONGREVE MILES STUART;RAMSDEN NIGEL GRAHAME
分类号 C07D211/14;A61K31/445;A61P1/18;A61P3/06;A61P3/10;A61P9/00;A61P9/10;A61P43/00;C07D211/22;C07D211/34;C07D401/06;C07F9/59;(IPC1-7):A61K31/454;A61K31/454;C07D211/06;C0741/02 主分类号 C07D211/14
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