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    Substituted 2-hydroxyphenyl cycloalkanes and pharmaceutical compositions thereof
    3.
    发明公开
    Substituted 2-hydroxyphenyl cycloalkanes and pharmaceutical compositions thereof 失效
    取代基2-羟基苯基 - 环烷烃和灭菌药物制剂Zusammensetzungen。

    公开(公告)号：EP0048572A2

    公开(公告)日：1982-03-31

    申请号：EP81304139.9

    申请日：1981-09-10

    申请人： PFIZER INC.

    发明人： Johnson, Michael Ross ,  Melvin, Jr., Lawrence Sherman

    IPC分类号： C07C43/23 ,  C07C39/17 ,  A61K31/00 ,  C07C39/42 ,  C07C39/23 ,  C07C37/00 ,  C07C49/00 ,  C07C45/00 ,  C07C47/00 ,  C07C91/23 ,  C07C131/04

    CPC分类号： C07D209/48 ,  C07B2200/07 ,  C07C39/17 ,  C07C39/23 ,  C07C39/42 ,  C07C45/44 ,  C07C45/515 ,  C07C45/59 ,  C07C45/60 ,  C07C45/64 ,  C07C45/673 ,  C07C45/69 ,  C07C47/27 ,  C07C47/277 ,  C07C47/46 ,  C07C47/47 ,  C07C49/245 ,  C07C49/255 ,  C07C49/747 ,  C07C49/753 ,  C07C49/757 ,  C07C403/02 ,  C07C403/08 ,  C07C2601/14 ,  C07D303/32 ,  Y02P20/55

    摘要： Compounds are disclosed having the formula
    wherein



    R 1 is hydrogen, benzyl or an ester moiety;
    Y is -CH(R 2 ")CH(R 2 )- or -CH(R 3 )CH 2 -;
    R 2 " is hydrogen or methyl;
    R 2 is OH or X-substituted (C 1-6 )alkyl;
    R 3 is OH, cyano or X-substituted (C 1-3 )alkyl;
    X is -OR 6 , -SR 6 , -S(O)R 6 , -S(O) 2 R 6 , -NR 6 R 7 , -COOR 7 , -CONR 7 R 8 or oxo;
    with the proviso that when X is -NR 6 R 7 , -COOR 7 or -CONR 7 R 8 , said group is located on the terminal carbon atom of R 2 or R 3 ;
    R e is hydrogen, (C 1-6 )alkyl or acetyl, with the provisos that, when R 6 in -NR 6 R 7 is acetyl, R 7 is hydrogen, and R 6 in S(O)R 6 and S(O) 2 R 6 cannot be acetyl;
    each of R 7 and R 8 is hydrogen or (C 1-6 )alkyl;
    s is an integer of 1 or 2; and Z-W is alkyl or oxaalkyl having 5 to 13 carbon atoms, or phenyl- or pyridyl-alkyl or -oxaalkyl having 3 to 8 carbon atoms in the alkyl or oxaalkyl group.
    Pharmaceutical compositions of such compounds, other than those in which
    is mandeloyl or R 1 is benzyl, are useful as analgesic or CNS agents and as anti-emetic agents.

    摘要翻译： 公开了具有下式的化合物：CH 2 R 1是氢，苄基或酯部分; Y是-CH（R2sec）CH（R2） - 或-CH（R3）CH2-; R2 sec为氢或甲基; R2是OH或X取代的（C1-6）烷基; R3是OH，氰基或X取代（C1-3）烷基; X是-OR 6，-SR 6，-S（O）R 6，-S（O）2 R 6，-NR 6 R 7，-COOR 7，-CONR 7 R 8或氧代; 条件是当X是-NR 6 R 7，-COOR 7或-CONR 7 R 8时，所述基团位于R 2或R 3的末端碳原子上; R 6为氢，（C 1-6）烷基或乙酰基，条件是当-NR 6 R 7中的R 6为乙酰基时，R 7为氢，S（O）R 6和S（O） R 7和R 8各自为氢或（C 1-6）烷基; s是1或2的整数; 并且Z-W是具有5至13个碳原子的烷基或氧杂烷基，或在烷基或氧杂烷基中具有3至8个碳原子的苯基或吡啶基 - 烷基或 - 氧杂烷基。 这些化合物的药物组合物除了是戊二酰基或R1是苄基之外，可​​用作镇痛药或CNS药剂和作为止吐剂。