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    Novel labdane derivatives, process for the preparation thereof, and pharmaceutical compositions containing labdane derivatives
    2.
    发明公开
    Novel labdane derivatives, process for the preparation thereof, and pharmaceutical compositions containing labdane derivatives 失效
    半日花烷衍生物，它们的制备方法和含有半日花烷衍生物的药物制剂。

    公开(公告)号：EP0116713A1

    公开(公告)日：1984-08-29

    申请号：EP83112756.8

    申请日：1983-12-19

    申请人： SCHERING CORPORATION

    发明人： Kreutner, William ,  Green, Michael John ,  Saksena, Anil Kumar ,  Shue, Ho-Jane

    IPC分类号： C07D311/92 ,  C07D409/04

    CPC分类号： C07D409/04 ,  C07D311/92

    摘要： This invention relates to a pharmaceutical composition eliciting an antiallergic andior bronchodilatory effect, which comprises a compound of general formula I
    including the 5,6 and 6,7 dehydro derivatives, in the free form or in the form of its solvate,

    wherein U is =O or (H,R 1 ) ;
    V is =0 or (H,R 2 );
    wherein R, is H or OR 11 , wherein R 11 is H or acyl, R 2 is H, OR 11 , OSO 2 R' or OR', wherein R' is alkyl; or when R, and R 2 are taken together they may form


    R 3 is hydrogen, alkyl, CH 2 0H, CHO, CO 2 R 15 , -CH=CR 16 R 17 , -C≡C-R 18 , -CHOH-C≡C-R 19 ;
    -CH=C=CHR 19 , -CH=H-OR 19 ,
    wherein Z is O or
    -CH=N-NDE or -CH(ZR 20 ) 2 wherein Z is defined as above;
    R 4 is H or OH;
    R 5 is OH; or when
    R 4 and R 5 are taken together they may form
    wherein Z is defined as above;
    X is 0 or H'OR" wherein R" is H, carboxylic acyl or trifluoroacetyl;
    Q is hydrogen, chlorine or bromine; or Q together with R 3 may form a bond between the carbon atoms of positions 12 and 13; whereby in the 5,6-dehydro-derivatives of formula I R 1 is H and in the 6,7-dehydro-derivatives of formula I R, and R 2 are H;
    and wherein R 11 , R 13 , R 14 , T 15 , R 16 , R 17 . R 18 , R 19 , R 20 , A, B, D, and E are as defined in the claims.
    Part of the compounds of formula I are new compounds.

    摘要翻译： 本发明涉及的药物组合物在抗过敏和/或支气管扩张药的效果，该方法包括通式的化合物引发我... ...包括5.6和6.7脱氢衍生物，在自由形式或形式 其溶剂化物，...其中U是O或（H，R1）; ... V是O或（H，R2）; ...其中R1是H或OR 11，worin R 11是H或酰基，R 2是H，OR 11，OSO 2分钟或 OR分钟，worin R“是烷基; 或当R 1和R 2一起可形成它们... ... R3是氢，烷基，CH 2 OH，CHO，CO2R15， - CH = CR 16 R 17，-C IDENTICAL C-R18，-CHOH-C IDENTICAL C-R19; ... -CH = C = CHR19，-CH = H-OR19，... ... worin Z是O或S，... ... CN = N-NDE或... -CH（ZR20）2 worin Z为定义为 以上; ... R4是H或OH; R 5 ...是OH; 或当... R4和R5结合在一起它们可形成... ... worin Z的定义如上; ... X为O或H /或仲worinř秒为H，羧酸酰基或三氟乙酰基; ... Q是氢，氯 或溴; 或Q与R 3一起可形成位置12和13的碳原子之间的键; 由此式的5,6-脱氢衍生物I R1是H和在式-6,7-脱氢衍生物我R1和R2是H; ...和worin R11，R13，R14，T15，R16，R17， R18，R19，R20，A，B，D，和E如权利要求中限定。 式I的化合物的... 第一部分是新的化合物。