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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。

    (Substituted benzyl)-thio heterocyclic compounds having a leukotriene-antagonist activity
    5.
    发明公开
    (Substituted benzyl)-thio heterocyclic compounds having a leukotriene-antagonist activity 失效
    （取代苄基） - 十二烷基杂环化合物具有亮氨酸 - 拮抗剂活性

    公开(公告)号：EP0214732A3

    公开(公告)日：1988-01-13

    申请号：EP86305633

    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.

    Oxazinobenzazole compounds
    7.
    发明公开
    Oxazinobenzazole compounds 失效
    恶嗪苯并唑化合物

    公开(公告)号：EP0500319A1

    公开(公告)日：1992-08-26

    申请号：EP92301320.5

    申请日：1992-02-18

    申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

    发明人： Tsuzuki, Ryuji ,  Matsumoto, Yuzo ,  Matsuhisa, Akira ,  Yoden, Toru ,  Uchida, Wataru ,  Yanagisawa, Isao

    IPC分类号： C07D498/04 ,  C07D513/04 ,  A61K31/535

    CPC分类号： C07D513/04

    摘要： Oxazinobenzazole derivatives represented by the following general formula and salts thereof:
    wherein R 1 , R 2 , R 3 and R 9 are the same or different and selected from hydrogen atoms and C 1 -C 6 alkyl groups ; R 5 and R 6 form, in conjunction with the two adjacent carbon atoms, a 5- or 6-membered heterocyclic ring having at least two nitrogen atoms and optionally a further heteroatom selected from oxygen, sulphur and nitrogen ; and m is 0 or 1.
    The compounds are useful as antispasmodic medicaments.

    摘要翻译： 由以下通式表示的恶嗪并苯并唑衍生物及其盐：其中R1，R2，R3和R9相同或不同并选自氢原子和C1-C6烷基; R5和R6与两个相邻碳原子一起形成具有至少两个氮原子和任选另外的选自氧，硫和氮的杂原子的5-或6-元杂环; 并且m是0或1.该化合物可用作抗痉挛药物。