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    Diamino isothiazole -1-oxides and -1,1-dioxides as gastric secretion inhibitors
    2.
    发明公开
    Diamino isothiazole -1-oxides and -1,1-dioxides as gastric secretion inhibitors 失效
    二氨基噻唑-1-氧化物和-1,1-二氧杂环己烷抑制剂。

    公开(公告)号：EP0067436A2

    公开(公告)日：1982-12-22

    申请号：EP82105169.5

    申请日：1982-06-14

    申请人： Merck & Co., Inc.

    发明人： Britcher, Susan F. ,  Lumma, William C., Jr. ,  Habecker, Charles N. ,  Baldwin, John J. ,  Hoffman, Jacob M.

    IPC分类号： C07D275/02 ,  C07D417/12 ,  A61K31/425

    CPC分类号： C07D275/03 ,  C07C255/00 ,  C07D277/48 ,  C07F7/10 ,  C07F7/1896

    摘要： Novel diamino isothiazote-1-oxides and -1,1-dioxides having the formulae:
    and
    are disclosed wherein:

    R is e.g. hydrogen, loweralkyl;
    p is 1 or 2;
    n is 0 or 1;
    m is 2 to 4;
    X is oxygen, sulfur or methylene;
    R 2 is e.g. hydrogen, halogen or loweralkyl;
    R 3 and R 4 are e.g. independently hydrogen or loweralkyl; and
    Ⓐ is phenylene or a 5- or 6-membered heterocycle containing one to three heteroatoms selected from oxygen, sulfur or nitrogen, which may optionally have a benzo ring fused thereon; and, a substituted 5-membered heterocycle wherein the substituents are loweralkyl, loweralkoxy, carbonyl, halo, carbamoyl, substituted carbamoyl;

    provided that when Ⓐ in Formulae la and Ib above is a 5-membered heterocycle, or a benzo fused 5-membered heterocycle containing one heteroatom, n is 1; and, the physiologically acceptable salts and N-oxides thereof. Processes for preparing such compounds are also disclosed. The compounds are useful for suppressing gastric acid secretions in mammals.

    摘要翻译： 公开了具有下式的新型二氨基异噻唑-1-氧化物和-1,1-二氧化物：其中：R为例如 氢，低级烷基; p为1或2; n为0或1; m为2〜4; X是氧，硫或亚甲基; R 2是例如。 氢，卤素或低级烷基; R 3和R 4是例如。 独立地是氢或低级烷基; 并且芳基是亚苯基或含有一至三个选自氧，硫或氮的杂原子的5-或6-元杂环，其可任选地具有稠合在其上的苯并环; 和取代的5元杂环，其中取代基是低级烷基，低级烷氧基，羰基，卤素，氨基甲酰基，取代的氨基甲酰基; 条件是当上述式Ⅰa和Ib为5元杂环或含有一个杂原子的苯并稠合的5元杂环时，n为1; 及其生理上可接受的盐和N-氧化物。 还公开了制备这些化合物的方法。 该化合物可用于抑制哺乳动物中的胃酸分泌。

    Thiadiazole oxides as gastric antisecretory agents
    4.
    发明公开
    Thiadiazole oxides as gastric antisecretory agents 失效
    噻二唑Oxyde mit antisekretorischer Wirkung。

    公开(公告)号：EP0073971A1

    公开(公告)日：1983-03-16

    申请号：EP82107483.8

    申请日：1982-08-17

    申请人： Merck & Co., Inc.

    发明人： Baldwin, John J. ,  Bolhofer, William A. ,  Lumma, William C., Jr.

    IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D285/10 ,  A61K31/33

    CPC分类号： C07D285/10 ,  C07D417/12 ,  C07D417/14

    摘要： There are disclosed novel thiadiazole oxide compounds having the formula:
    wherein: B ' is R Ⓐ (CH 2 ) n X (CH 2 ) m , -,
    wherein:

    R is hydrogen, loweralkyl:
    wherein R 1 and R 2 are independently e.g. hydrogen, loweralkyl, cycloloweralkyl, or phenylloweralkyl, or R 1 and R 2 may be joined to form, along with the nitrogen to which they are attached, a 5- or 6-membered heterocycle; R 3 and R 4 are independently hydrogen or loweralkyl;
    n is 0 or 1;
    m is 2 to 4;
    k is 1 to 4;
    X is oxygen, sulfur or methylene;
    p is 1 or 2;
    Ⓐ is phenylene or a 5- or 6-membered heterocycle containing one to three heteroatoms selected from oxygen, sulfur or nitrogen, which may optionally have a benzo ring fused thereon; provided that when @ is a 5-membered heterocycle or benzo fused 5-membered heterocycle, n is 1 and processes for the preparation of such compounds. The compounds are useful for the suppression of gastric acid secretions in mammals.

    摘要翻译： 公开了具有下式的新型噻二唑氧化物化合物：其中：B 1是R A / C n和（CH 2）n X（CH 2）m - ; 并且，B 2是R CHEM，其中：R是氢，低级烷基：CHEM，其中R 1和R 2独立地是例如。 氢，低级烷基，环低级烷基或苯基低级烷基，或者R 1和R 2可以与它们所连接的氮连接形成5-或6-元杂环; R3和R4独立地是氢或低级烷基; n为0或1; m为2〜4; k为1〜4; X是氧，硫或亚甲基; p为1或2; 芳基是亚苯基或含有一至三个选自氧，硫或氮的杂原子的5-或6-元杂环，其可以任选地具有稠合在其上的苯并环; 条件是当A和C 5'是5元杂环或苯并稠合的5元杂环时，n为1，并且用于制备这些化合物的方法。 该化合物可用于抑制哺乳动物的胃酸分泌。