公开(公告)号：US09238657B2

公开(公告)日：2016-01-19

申请号：US13063878

申请日：2009-10-27

申请人： Yasuhiro Nishitani ,  Kenji Yamawaki ,  Yusuke Takeoka ,  Hideki Sugimoto ,  Shinya Hisakawa ,  Toshiaki Aoki

发明人： Yasuhiro Nishitani ,  Kenji Yamawaki ,  Yusuke Takeoka ,  Hideki Sugimoto ,  Shinya Hisakawa ,  Toshiaki Aoki

IPC分类号： C07D501/46 ,  C07D505/24 ,  C07D519/06 ,  A61K31/546

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

摘要： The present disclosure describes Cephem compounds 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 optionally present, and when present is, —NR7—, —CO—, —CO—NR7—, —NR7—CO—, —NR7—CO—NR7—, or the like; F is optionally present, and when present is or phenylene; R3 and R4 are —OR8; R5 and R6 each is independently hydrogen, halogen, nitrile, or —OR8; or an ester at the carboxyl at the 7-position side chain or at the 4-position, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof, which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria.

摘要翻译： 本公开内容描述了具有下式的Cephem化合物：其中X是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是任选存在的，并且当存在时为-NR 7 - ， - CO - ， - CO-NR 7 - ， - NR 7 -CO-，-NR 7 -CO-NR 7 - 等; F任选存在，当存在时为或亚苯基; R3和R4是-OR8; R5和R6各自独立地为氢，卤素，腈或-OR8; 或在7-位侧链或4-位的羧基处的酯，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，其具有宽的 抗菌谱，对抗β-内酰胺酶产生革兰氏阴性细菌具有有效的抗菌活性。

公开(公告)号：US20110190254A1

公开(公告)日：2011-08-04

申请号：US13063878

申请日：2009-10-27

申请人： Yasuhiro Nishitani ,  Kenji Yamawaki ,  Yusuke Takeoka ,  Hideki Sugimoto ,  Shinya Hisakawa ,  Toshiaki Aoki

发明人： Yasuhiro Nishitani ,  Kenji Yamawaki ,  Yusuke Takeoka ,  Hideki Sugimoto ,  Shinya Hisakawa ,  Toshiaki Aoki

IPC分类号： A61K31/546 ,  C07D501/60 ,  A61P31/00

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, —NR7—, —CO—, —CO—NR7—, —NR7—CO—, —NR7—CO—NR7—, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 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泛抗微生物谱并且对产生β-内酰胺酶的革兰氏阴性细菌具有强效抗微生物活性的Cephem化合物，如下式所示：其中X是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其溶剂合物。