Use of omeprazole as an antimicrobial agent
    2.
    发明授权
    Use of omeprazole as an antimicrobial agent 失效
    使用奥美拉唑作为抗微生物剂

    公开(公告)号:US5093342A

    公开(公告)日:1992-03-03

    申请号:US572951

    申请日:1990-09-12

    CPC分类号: C07D401/12

    摘要: Use of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-sulfinyl]-1H-benzimidazole or a pharmaceutically acceptable salt thereof in the treatment of infectious diseases, especially such caused by Campylobacter pylori.

    摘要翻译: PCT No.PCT / SE90 / 00070 Sec。 371 1990年9月12日第 102(e)1990年9月12日PCT PCT 1990年2月2日提交PCT公布。 出版物WO90 / 09175 日期为1990年8月23日。使用5-甲氧基-2 [[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基] - 亚磺酰基] -1H-苯并咪唑或其药学上可接受的盐在 传染病,特别是幽门螺杆菌引起的。

    Quinolonecarboxylic acid compounds and pharmaceutical use thereof
    3.
    发明授权
    Quinolonecarboxylic acid compounds and pharmaceutical use thereof 失效
    喹诺酮羧酸化合物及其药物用途

    公开(公告)号:US4889857A

    公开(公告)日:1989-12-26

    申请号:US250634

    申请日:1988-09-29

    IPC分类号: C07D413/04

    CPC分类号: C07D413/04

    摘要: A quinolonecarboxylic acid compound of the formula: ##STR1## wherein R.sup.1 is an alkyl group, a cycloalkyl group, a haloalkyl group, an alkenyl group, mono- or di-alkylamino groups, a phenyl group or a phenyl group substituted by one to three substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group or an amino group, R.sup.2 is a hydrogen atom, an alkyl group, a cycloalkyl group, an acyl group or an alkoxycarbonyl group, R.sup.3 is a hydrogen atom, an alkyl group or an aralkyl group, or R.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a heterocyclic ring, R.sup.4 is a hydrogen atom or an alkyl group, R.sup.5 is a hydrogen atom, an alkyl group, an aralkyl group or an ester residue which is readily hydrolyzable in vivo, X is a hydrogen atom, a halogen atom or an alkyl group, n is interger of 1 to 3, and a salt thereof, and pharmaceutical use thereof.The compounds exhibit antibacterial activites and are useful for the treatment of various infectious diseases.

    Helicobacter pylori-colonized mongolian gerbils, method for preparation
thereof, and method for screening anti-Helicobacter pylori substance
using them
    8.
    发明授权
    Helicobacter pylori-colonized mongolian gerbils, method for preparation thereof, and method for screening anti-Helicobacter pylori substance using them 失效
    幽门螺杆菌定殖的蒙古沙鼠,其制备方法,幽门螺杆菌分离培养基及使用它们的抗幽门螺杆菌物质筛选方法

    公开(公告)号:US5929299A

    公开(公告)日:1999-07-27

    申请号:US693100

    申请日:1996-08-09

    摘要: Helicobacter pylori-colonized Mongolian gerbils prepared by oral inoculation of a broth culture obtained from a liquid culture of Helicobacter pylori, to the Mongolian gerbils for intragastric colonization of Helicobacter pylori. These Mongolian gerbil models are useful for screening the therapeutic efficacies of drugs against Helicobacter pylori, as well as elucidation of pathology of Helicobacter pylori disease in humans. Moreover, the medium of the present invention for isolating Helicobacter pylori, which is supplemented with vancomycin, trimethoprim, amphotericin B, polymyxin B and 2,3,5-triphenyltetrazolium chloride, enables selective and efficient detection of Helicobacter pylori colonized in their Mongolian gerbils which have microorganisms living in stomach. A combined use of the above-mentioned Mongolian gerbil models and the medium for isolating Helicobacter pylori enables screening of an anti-Helicobacter pylori substance at an animal levels thereby enabling accurate prediction of clinical effects of the anti-Helicobacter pylori substance.

    摘要翻译: PCT No.PCT / JP95 / 02531 Sec。 371日期:1996年8月9日 102(e)日期1996年8月9日PCT提交1995年12月8日PCT公布。 第WO96 / 18291号公报 日期1996年6月20日幽门螺杆菌定殖的蒙古沙鼠通过口服接种从幽门螺杆菌液体培养物获得的肉汤培养物制备成蒙古沙鼠用于幽门螺杆菌胃内定殖。 这些蒙古沙鼠模型可用于筛选药物对幽门螺杆菌的治疗功效,以及阐明人幽门螺杆菌病的病理学。 此外,本发明的用于分离补充有万古霉素,甲氧苄氨嘧啶,两性霉素B,多粘菌素B和2,3,5-三苯基四氮唑氯化物的幽门螺杆菌的培养基能够选择性和有效地检测在其蒙古沙鼠中定居的幽门螺杆菌, 有微生物住在胃里。 综合使用上述的蒙古沙鼠模型和用于分离幽门螺杆菌的培养基使得能够以动物水平筛选抗幽门螺杆菌物质,从而能够准确预测抗幽门螺杆菌物质的临床效果。

    8-methoxy-quinolonecarboxylic acid derivatives
    9.
    发明授权
    8-methoxy-quinolonecarboxylic acid derivatives 失效
    8-甲氧基 - 喹啉酮羧酸衍生物

    公开(公告)号:US5677316A

    公开(公告)日:1997-10-14

    申请号:US473357

    申请日:1995-06-07

    CPC分类号: C07D401/04

    摘要: 8-Methoxy-quinolonecarboxylic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl, a phenylalkyl or an ester residue hydrolyzable in the living body, R.sub.2 is a hydrogen atom or methyl and n is an integer of 1, optical isomers thereof, pharmaceutically acceptable salts thereof and hydrates thereof. The 8-methoxy-quinolonecarboxylic acid derivatives of the present invention have enforced and a wide range of in vitro and in vivo antibacterial effects against Gram-positive bacteria, while retaining a strong antibacterial effect against Gram-negative bacteria, that the conventional quinolonecarboxylic acid antibacterial agents have. In addition, the compounds of the present invention scarcely show problematic side-effects and are low toxic. Therefore, they are expected to show superior clinical effects as antibacterial agents.

    摘要翻译: 式(I)的8-甲氧基 - 喹啉酮羧酸衍生物,其中R1是氢原子,低级烷基,苯基烷基或可在生物体中水解的酯残基,R2是氢原子或甲基,n是 1的整数,其光学异构体,其药学上可接受的盐和其水合物。 本发明的8-甲氧基 - 喹诺酮羧酸衍生物对革兰氏阳性细菌的体外和体内抗菌作用具有广泛的应用范围,同时保留对革兰氏阴性细菌的强烈的抗菌作用,常规的喹诺酮羧酸抗菌剂 代理商有。 此外,本发明的化合物几乎不显示有问题的副作用,并且毒性低。 因此,作为抗菌剂,预期其具有优异的临床效果。

    Pharmaceutical use of pyridine compounds
    10.
    发明授权
    Pharmaceutical use of pyridine compounds 失效
    吡啶化合物的药用

    公开(公告)号:US5616581A

    公开(公告)日:1997-04-01

    申请号:US460666

    申请日:1995-06-02

    摘要: A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobacter pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.

    摘要翻译: 式(I)的吡啶化合物其中R 1是氢,卤素,烷基,烷氧基等,R 2和R 3各自是氢,卤素或烷基,-P = Q-是 -CH = CH-,-N = CH-或-CH = N-,A是氧原子,硫原子或其中R4是氢,烷基等的N(R4),n是0,1或2, B是S(O)p,其中p是0,1或2,D是单键,亚烷基等,E是烷氧基烷基或-N(R6)(R7),其药学上可接受的盐具有抗菌性 针对幽门螺杆菌的活性,抗溃疡活性,胃肠细胞保护活性,溃疡复发,复发预防活性和胃酸分泌抑制活性,可用作药物制剂。