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    CEPHALOSPORIN HAVING CATECHOL GROUP
    1.
    发明公开
    CEPHALOSPORIN HAVING CATECHOL GROUP 有权
    CEPHALOSPORIN MIT CATECHOLGRUPPE

    公开(公告)号：EP2341053A1

    公开(公告)日：2011-07-06

    申请号：EP09823578.1

    申请日：2009-10-27

    申请人： Shionogi&Co., Ltd.

    发明人： NISHITANI, Yasuhiro ,  YAMAWAKI, Kenji ,  TAKEOKA, Yusuke ,  SUGIMOTO, Hideki ,  HISAKAWA, Shinya ,  AOKI, Toshiaki

    IPC分类号： C07D505/24 ,  A61K31/5365 ,  A61K31/546 ,  A61K31/55 ,  A61P31/04 ,  C07D501/46 ,  C07D519/06

    CPC分类号： C07D501/46 ,  C07D505/24 ,  C07D519/06

    摘要： The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows:
    A compound of the formula:

    wherein,
    X is N, CH or C-Cl;
    T is S or the like;
    A and G are lower alkylene or the like;
    B is a single bond or the like;
    D is a single bond, -NR 7 -, -CO-, -CO-NR 7 -, -NR 7 -CO-, -NR 7 -CO-NR 7 -, or the like;
    E is optionally substituted lower alkylene;
    F is a single bond or optionally substituted phenylene;
    R 3 , R 4 , R 5 and R 6 each is independently hydrogen, halogene, nitrile, or the like;

    or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

    摘要翻译： 本发明提供了具有广谱抗菌谱的Cephem化合物，对β-内酰胺酶产生革兰氏阴性细菌具有强力的抗微生物活性，如下所示：其中X为N，CH或C-Cl; T是S等; A和G是低级亚烷基等; B是单键等; D是单键，-NR 7 - ， - CO - ， - CO - NR 7 - ， - NR 7 -CO - ， - NR 7 -CO-NR 7 - 等; E是任选取代的低级亚烷基; F是单键或任选取代的亚苯基; R 3，R 4，R 5和R 6各自独立地为氢，卤素，腈等; 或酯，在7-侧链的环上的氨基保护的化合物，其药学上可接受的盐或溶剂合物。

    NOVEL CEPHEM COMPOUND HAVING CATECHOL OR PSEUDO-CATECHOL STRUCTURE
    6.
    发明公开
    NOVEL CEPHEM COMPOUND HAVING CATECHOL OR PSEUDO-CATECHOL STRUCTURE 审中-公开
    NEE CEPHEMVERBINDUNG MIT EINER CATECHOL- ODER PSEUDO-CATECHOL-STRUKTUR

    公开(公告)号：EP2703406A1

    公开(公告)日：2014-03-05

    申请号：EP12777752.2

    申请日：2012-04-25

    申请人： Shionogi & Co., Ltd.

    发明人： NISHITANI, Yasuhiro ,  AOKI, Toshiaki ,  SATO, Jun ,  YAMAWAKI, Kenji ,  YOKOO, Katsuki ,  SANO, Masayuki

    IPC分类号： C07D501/46 ,  A61K31/546 ,  A61P31/04 ,  C07D501/18 ,  C07D519/06

    CPC分类号： C07D501/60 ,  C07D501/18 ,  C07D501/46 ,  C07D519/00 ,  C07D519/06

    摘要： The present invention provides a novel compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria. Specifically, the present invention provides a compound of the formula (I):

    wherein each symbol is as defined in the specification,
    or an amino-protected compound when the amino group is present on the ring in the 7-side chain, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.

    摘要翻译： 本发明提供了具有广谱抗菌谱的新型化合物，特别是对产生β-内酰胺酶的革兰氏阴性细菌表现出有效的抗微生物活性。 具体而言，本发明提供式（I）化合物：其中各符号如说明书中所定义，或氨基保护的化合物，当氨基存在于7-侧链的环上时，或药学上 其可接受的盐和包含其的药物组合物。

    C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    10.
    发明公开
    C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    C5-C6稠合的三环亚胺二氮嗪二氧化物化合物作为基础缓蚀剂，组合物及其使用

    公开(公告)号：EP3201204A1

    公开(公告)日：2017-08-09

    申请号：EP15846682.1

    申请日：2015-09-28

    申请人： Merck Sharp & Dohme Corp.

    发明人： HE, Shuwen ,  CUMMING, Jared N. ,  SCOTT, Jack D.

    IPC分类号： C07D513/14

    CPC分类号： A61K45/06 ,  A61K31/54 ,  A61K31/549 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04 ,  C07D519/00 ,  C07D519/06

    摘要： In its many embodiments, the present invention provides certain C5-C6 fused tricyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R2, R3, RA, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

    摘要翻译： 在其许多实施方案中，本发明提供了某些C 5 -C 6稠合的三环亚胺基噻二嗪化合物，包括式（I）化合物或其互变异构体，以及所述化合物和所述互变异构体的药学上可接受的盐，其中R 1A，R 2，R 3， 环A，RA，m，-L 1 - 和RL如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其有关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其他活性剂组合）的药物组合物，以及它们的制备和使用方法，包括用于可能治疗阿尔茨海默氏病。