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    (Substituted benzyl)-thio heterocyclic compounds having a leukotriene-antagonist activity
    2.
    发明公开
    (Substituted benzyl)-thio heterocyclic compounds having a leukotriene-antagonist activity 失效
    （取代苄基） - 硫代杂环维生素，死亡白细胞素拮抗剂 - 维尔京。

    公开(公告)号：EP0214732A2

    公开(公告)日：1987-03-18

    申请号：EP86305633.9

    申请日：1986-07-22

    申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

    发明人： Mase, Toshiyasu ,  Murase, Kiyoshi ,  Tsuzuki, Ryuji ,  Tomioka, Kenichi ,  Hara, Hiromu

    IPC分类号： C07D285/12 ,  C07D239/56 ,  C07D213/70 ,  C07D249/12 ,  C07D275/02 ,  A61K31/41 ,  A61K31/44 ,  A61K31/505

    CPC分类号： C07D213/70 ,  C07D239/56 ,  C07D249/12 ,  C07D275/03 ,  C07D285/125 ,  C07D285/135

    摘要： Heterocyclic compound of formula (I) and salts thereof are SRS-A antagonists:
    wherein R' is a C 1 to C 8 acyl group; R 2 is a C 1 to C a alkyl group; Het- is a 5- or 6-membered heterocyclic ring which contains 1 to 3 nitrogen atoms and may additionally contain a sulfur atom or an oxygen atom; R 3 is a carboxy group, an amino group, a C 1 to C 8 alkylamino group which may be carboxy-substituted, a C, to C 8 alkanoylamino group which may be carboxy-substituted, a di-(C 1 -C 8 alkyl) amino group, a hydroxy group, a C 1 to C 8 alkoxy group which may be carboxy-substituted, a mercapto group, a C 1 -C 8 alkylthio group which may be carboxy-substituted, a group of formula:
    or formula:
    (wherein p is integer of 1 to 5, q is 0, 1 or 2, r is an integer of 1 to 5; R 4 is a carboxy group, a C 1 -C 8 alkoxy group which may be carboxy-substituted or a C 1 -C 8 alkyl group which may be carboxy-substituted and optionally additionally contain a sulfur atom or an oxygen atom in the carbon chain thereof); and n is 0 or an integer of to 3; provided that when the compound is substituted by a carboxy group, said carboxy group may be in the form of an ester, and when n is 2 or 3 different R 3 's is may be present.

    摘要翻译： 式（I）的杂环化合物及其盐是SRS-A拮抗剂：... 其中R 1是C 1至C 8酰基; R 2是C 1至C 8烷基; Het是含有1至3个氮原子并可另外含有硫原子或氧原子的5-或6-元杂环; R 3是羧基，氨基，可被羧基取代的C1〜C8烷基氨基，可以被羧基取代的C1〜C8烷酰基氨基，二 - （C1-C8烷基）氨基， 羟基，可以被羧基取代的C1〜C8烷氧基，巯基，可以被羧基取代的C1-C8烷硫基，式：...... ...或式：...... ...（其中p为1至5的整数，q为0,1或2，r为1至5的整数; R 4为羧基，可为羧基的C 1 -C 8烷氧基 或可被羧基取代的C 1 -C 8烷基，并且任选地在其碳链中另外含有硫原子或氧原子）; n为0或1〜3的整数， 条件是当化合物被羧基取代时，所述羧基可以是酯的形式，当n是2或3个不同的R 3时，可以存在分子s。