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1. 发明申请

WO2014069649A1 PROCESSES FOR PRODUCTION OF INTERMEDIATES FOR 2-ALKYL CEPHEM COMPOUNDS 审中-公开
标题翻译：用于生产2-烷基丙烯酸酯化合物的中间体的方法
公开(公告)号：WO2014069649A1
公开(公告)日：2014-05-08
申请号：PCT/JP2013/079803
申请日：2013-10-29
申请人： SHIONOGI & CO., LTD.
发明人： YOKOO, Katsuki , HISAKAWA, Shinya , YAMAWAKI, Kenji , AOKI, Toshiaki , YOKOTA, Yutaka , TAKEO, Masatoshi , ASAI, Mikito
IPC分类号： C07D501/14 , C07D501/16
CPC分类号： C07D501/16 , C07B2200/13 , C07D501/59
摘要： The invention relates to processes for the production of intermediates for preparing 2-alkyl cephem compounds useful as antimicrobial drugs. The invention provides a process which comprises oxidating a compound of the formula (I) or a salt thereof to give a compound of the formula (II) or a salt thereof wherein each symbol is as defined in the specification.
摘要翻译：本发明涉及用于制备用作抗微生物药物的2-烷基头孢烯化合物的中间体的方法。本发明提供了一种方法，其包括将式（I）化合物或其盐氧化得到式（II）化合物或其盐，其中每个符号如说明书中所定义。

2. 发明申请

WO2014102594A2 SUBSTITUTED BENZIMIDAZOLE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：取代的苯并咪唑型哌啶化合物及其用途
公开(公告)号：WO2014102594A2
公开(公告)日：2014-07-03
申请号：PCT/IB2013/002884
申请日：2013-12-23
申请人： PURDUE PHARMA L.P. , SHIONOGI & CO., LTD. , TANAKA, Nobuyuki , YAMAWAKI, Kenji , YU, Jianming , ZHOU, Xiaoming , YAO, Jiangchao
发明人： TANAKA, Nobuyuki , YAMAWAKI, Kenji , YU, Jianming , ZHOU, Xiaoming , YAO, Jiangchao
IPC分类号： C07D401/14
CPC分类号： C07D471/08 , C07D401/04
摘要： The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof, e.g., a pharmaceutically acceptable salt or solvate, wherein R 1 , R 2 , R 3 , Q a , W, U, A, B, Z, a, and the dashed lines are as defined herein, compositions comprising an effective amount of a Substituted Benzimidazole-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Benzimidazole-Type Piperidine Compound.
摘要翻译：本公开涉及式（I）的取代的苯并咪唑型哌啶化合物及其药学上可接受的盐或溶剂化物，例如其药学上可接受的盐或溶剂合物，其中R 1，，R 2，R 3，Q a，W，U，A，B，Z，a和虚线如定义本文中，包含有效量的取代的苯并咪唑型哌啶化合物的组合物，以及治疗或预防例如疼痛的病症的方法，所述方法包括向有需要的动物施用有效量的取代的苯并咪唑型哌啶化合物。 / p>

3. 发明申请

WO2014068388A1 2 SUBSTITUTED CEPHEM COMPOUNDS 审中-公开
标题翻译： 2替代CEPHEM化合物
公开(公告)号：WO2014068388A1
公开(公告)日：2014-05-08
申请号：PCT/IB2013/002423
申请日：2013-10-29
申请人： GLAXO GROUP LIMITED , SHIONOGI & CO., LTD.
发明人： LIAO, Xiangmin , PEARSON, Neil, David , PENDRAK, Israil , THALGI, Reema , YAMAWAKI, Kenji , YOKOO, Katsuki , SATO, Jun , KUSANO, Hiroki , AOKI, Toshiaki
IPC分类号： C07D505/24 , A61K31/546 , C07D501/50
CPC分类号： C07D501/48 , A61K9/0019 , C07D501/50 , C07D505/24 , Y02A50/473
摘要： The compounds of formula (I) of the subject invention are related to 2-substituted cephem compounds, which have a wide antimicrobial spectrum, in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical compositions comprising the same.
摘要翻译：本发明的式（I）化合物与具有广谱抗菌谱的2-取代头孢烯化合物有关，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，以及包含该化合物的药物组合物。

4. 发明公开

EP3318567A1 TRICYCLIC COMPOUND HAVING SULFINYL OR SULFONYL 审中-公开
标题翻译：含有磺酰基或磺酰基的三环化合物
公开(公告)号：EP3318567A1
公开(公告)日：2018-05-09
申请号：EP16818011.5
申请日：2016-06-30
申请人： Shionogi & Co., Ltd
发明人： YAMAWAKI, Kenji , KUSANO, Hiroki
IPC分类号： C07D501/14 , A61K31/546 , A61P31/04
CPC分类号： C07D501/14 , A61K31/546 , A61P31/04
摘要： It is intended to provide a compound that exhibits a strong antibacterial spectrum against various bacteria including gram-negative bacteria, or a pharmaceutical composition having an antibacterial activity against carbapenem-resistant bacteria.
The present invention provides a compound represented by formula (I):

wherein -W- is -S(=O)- or -S(=O) 2 -, -T- is -CR 4A R 4B - or -CR 5A R 5B -CR 6A R 6B -, R 4A , R 4B , R 5A , R 5B , R 6A and R 6B are each independently a hydrogen atom or the like, R 1 is substituted or unsubstituted heterocyclyl or the like, R 2A and R 2B are each independently a hydrogen atom or the like, or R 2A and R 2B are taken together to form substituted or unsubstituted methylidene or the like, and R 3 is a hydrogen atom or the like, R 11 is carboxy or the like, R 7A and R 7b are each independently a hydrogen atom or the like, its ester form or a pharmaceutically acceptable salt thereof, or a hydrate thereof.
摘要翻译：旨在提供对包括革兰氏阴性细菌在内的各种细菌或对碳青霉烯抗性细菌具有抗菌活性的药物组合物表现出强抗菌谱的化合物。本发明提供由式（I）表示的化合物：其中-W-是-S（= O） - 或-S（= O）2 - ， - T是-CR4AR4B-或-CR5AR5B-CR6AR6B-，R4A ，R4B，R5A，R5B，R6A和R6B各自独立地为氢原子等，R 1为取代或未取代的杂环基等，R 2A和R 2B各自独立地为氢原子等，或R 2A和R 2B合在一起以形成取代或未取代的亚甲基等，且R 3为氢原子等，R 11为羧基等，R 7A和R 7b各自独立地为氢原子等，其酯形式或其药学上可接受的盐，或其水合物。

5. 发明公开

EP2917223A1 2 SUBSTITUTED CEPHEM COMPOUNDS 审中-公开
标题翻译： 2-SUBSTITUIERTE CEPHEMVERBINDUNGEN
公开(公告)号：EP2917223A1
公开(公告)日：2015-09-16
申请号：EP13820853.3
申请日：2013-10-29
申请人： Glaxo Group Limited , Shionogi & Co., Ltd
发明人： LIAO, Xiangmin , PEARSON, Neil, David , PENDRAK, Israil , THALGI, Reema , YAMAWAKI, Kenji , YOKOO, Katsuki , SATO, Jun , KUSANO, Hiroki , AOKI, Toshiaki
IPC分类号： C07D505/24 , A61K31/546 , C07D501/50
CPC分类号： C07D501/48 , A61K9/0019 , C07D501/50 , C07D505/24 , Y02A50/473
摘要： The present invention relates to 2-substituted cephem compounds of Formula (I) having a quaternary ammonium group on the 3-side chain, preferably together with a cathechol group, or pharmaceutically acceptable salts thereof, which exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and/or Gram positive bacteria, corresponding pharmaceutical compositions, methods of making, treatment methods for bacterial infections or uses thereof.
摘要翻译：本发明涉及在3-侧链上具有季铵基团的式（I）的2-取代头孢烯化合物，优选与导管胆碱基团或其药学上可接受的盐，其表现出针对各种细菌的有效的抗菌谱包括革兰氏阴性细菌和/或革兰氏阳性细菌，相应的药物组合物，制备方法，细菌感染的治疗方法或其用途。

6. 发明公开

EP2912040A1 PROCESSES FOR PRODUCTION OF INTERMEDIATES FOR 2-ALKYL CEPHEM COMPOUNDS 审中-公开
标题翻译：于制备中间体2-烷基头孢
公开(公告)号：EP2912040A1
公开(公告)日：2015-09-02
申请号：EP13851709.9
申请日：2013-10-29
申请人： Shionogi & Co., Ltd.
发明人： YOKOO, Katsuki , HISAKAWA, Shinya , YAMAWAKI, Kenji , AOKI, Toshiaki , YOKOTA, Yutaka , TAKEO, Masatoshi , ASAI, Mikito
IPC分类号： C07D501/14 , C07D501/16
CPC分类号： C07D501/16 , C07B2200/13 , C07D501/59
摘要： The invention relates to processes for the production of intermediates for preparing 2-alkyl cephem compounds useful as antimicrobial drugs. The invention provides a process which comprises oxidating a compound of the formula (I) or a salt thereof to give a compound of the formula (II) or a salt thereof wherein each symbol is as defined in the specification.

7. 发明授权

EP2917223B1 2 SUBSTITUTED CEPHEM COMPOUNDS 有权
公开(公告)号：EP2917223B1
公开(公告)日：2019-01-16
申请号：EP13820853.3
申请日：2013-10-29
申请人： Glaxo Group Limited , Shionogi & Co., Ltd
发明人： LIAO, Xiangmin , PEARSON, Neil, David , PENDRAK, Israil , THALGI, Reema , YAMAWAKI, Kenji , YOKOO, Katsuki , SATO, Jun , KUSANO, Hiroki , AOKI, Toshiaki
IPC分类号： C07D505/24 , A61K31/546 , C07D501/50

8. 发明公开

EP2341053A1 CEPHALOSPORIN HAVING CATECHOL GROUP 无效转让
标题翻译： 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。

9. 发明授权

EP2960244B1 CEPHALOSPORIN HAVING CATECHOL GROUP 有权
标题翻译： CEPHALOSPORIN拥有CATECHOL集团
公开(公告)号：EP2960244B1
公开(公告)日：2016-09-14
申请号：EP15175084.1
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

10. 发明授权

EP2341053B1 CEPHALOSPORIN HAVING CATECHOL GROUP 无效转让
标题翻译：头孢菌素儿茶酚
公开(公告)号：EP2341053B1
公开(公告)日：2016-01-13
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

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