利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

8 条记录 (耗时 0.012 秒)

    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。

    Imidazole guanidines, their preparation and compositions containing them
    3.
    发明公开
    Imidazole guanidines, their preparation and compositions containing them 失效
    咪唑胍，维他命Zu ihrer Herstellung und diese enthaltende Zusammensetzungen。

    公开(公告)号：EP0020173A1

    公开(公告)日：1980-12-10

    申请号：EP80301833.2

    申请日：1980-06-02

    申请人： Merck & Co., Inc.

    发明人： Bolhofer, William A. ,  Cragoe, Edward J. ,  Hoffman, Jacob M.

    IPC分类号： C07D233/64 ,  C07D409/04 ,  C07D409/06 ,  A61K31/415

    CPC分类号： C07D233/64 ,  A61K31/415 ,  C07C45/63 ,  C07C205/45 ,  C07D233/90 ,  C07D333/42 ,  C07C49/233

    摘要： Imidazole cyanoguanidines of formula
    where

    R 1 is hydrogen or methyl;
    R 2 is lower alkyl; each of m and n independently of the other, is 0, 1, 2 or 3;
    A is a phenylene, cyclohexylene, thienylene, tetrahydro- thienylene, or 1,3-dithianylene radical and is optionally substituted with a halogen;
    Y is oxygen, sulfur, =NR 3 or = CHR 4 where R 3 is hydrogen, cyano, lower alkyl, phenyl, lower alkylsulfonyl, or phenylsulfonyl; and
    R 4 is nitro, phenylsulfonyl, or lower alkylsulfonyl, and their pharmaceutically acceptable salts, are novel and are useful for the suppression of gastric acid secretion in mammals. Compositions for such uses containing the compounds are also disclosed. The compounds are made by introducing the of formula
    group into an amine

    摘要翻译： 咪唑氰基氰胺类化合物... ...其中R1是氢或甲基; R2是低级烷基; m和n彼此独立地是0,1,2或3; A是亚苯基，亚环己基，亚噻吩基，四氢噻吩基或1,3-二噻吩基，任选被卤素取代; Y是 氧，硫，= NR 3或= CHR 4，其中R 3是氢，氰基，低级烷基，苯基，低级烷基磺酰基或苯磺酰基; 和R4是硝基，苯基磺酰基或低级烷基磺酰基及其药学上可接受的盐是新颖的，可用于抑制哺乳动物中的胃酸分泌。 还公开了含有这些化合物的用途的组合物。 该化合物是通过将...... NHR 2 - 基团引入到式...的胺中而制成的... ...

    4-(2-methyl-2-hydroxypropyl-amino)-5,6-dihydrothieno-2(2,3-B)thiopyran-2-sulfonamide-7,7-dioxide
    7.
    发明公开
    4-(2-methyl-2-hydroxypropyl-amino)-5,6-dihydrothieno-2(2,3-B)thiopyran-2-sulfonamide-7,7-dioxide 失效
    4-（2-甲基-2- hydrooxypropylamino）-5,6- dihydrothieno-（2,3- B）噻喃-2-磺酰胺-7,7-二dioxid。

    公开(公告)号：EP0411702A1

    公开(公告)日：1991-02-06

    申请号：EP90202066.8

    申请日：1990-07-27

    申请人： MERCK & CO. INC.

    发明人： Hoffman, Jacob M. ,  Zacchei, Antony G. ,  Lee, Ling L. ,  Varga, Sandor L.

    IPC分类号： C07D495/04 ,  A61K31/38

    CPC分类号： C07D495/04

    摘要： 4-(2-Methyl-2-hydroxypropylamino)-5,6-dihy­drothieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide is a major mammalian metabolite of 4-(2-methylpropyl­amino)-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfon­amide-7,7-dioxide and is itself an active carbonic anhydrase inhibitor useful in the treatment of ocular hypertension by topical administration.

    摘要翻译： 4-（2-甲基-2-羟丙基氨基）-5,6-二氢噻吩并[2,3-b]噻喃-2-磺酰胺-7,7-二氧化物是主要的4-（2-甲基丙基氨基） -5,6-二氢噻吩并[2,3-b]噻喃-2-磺酰胺e-7,7-二氧化物，其本身是用于通过局部给药治疗高眼压症的活性碳酸酐酶抑制剂。