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1. 发明公开

EP2960244A1 CEPHALOSPORIN HAVING CATECHOL GROUP 有权
标题翻译： CEPHALOSPORIN MIT CATECHOLGRUPPE
公开(公告)号：EP2960244A1
公开(公告)日：2015-12-30
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
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:

or its 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，如下所示：下式化合物或其酯，在7环上的环上的氨基保护的化合物侧链，其药学上可接受的盐或其溶剂化物。

2. 发明授权

EP0893446B1 CEPHEM COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS 失效
标题翻译：头孢类及药物含有这些化合物
公开(公告)号：EP0893446B1
公开(公告)日：2006-10-04
申请号：EP97914600.8
申请日：1997-04-04
申请人： SHIONOGI & CO., LTD.
发明人： NISHITANI, Yasuhiro , ISHIKURA, Koji
IPC分类号： C07D501/38 , C07D401/04 , C07D409/04 , A61K31/545
CPC分类号： C07D401/04 , C07D409/04 , C07D501/00
摘要： Cephem compounds having groups of general formula (II) at the 3-position of the cephem ring, or salts or hydrates thereof, wherein Het is a mono- or poly-cyclic hetero-ring having one or more atoms selected from among N, O and S which may be the same or different from each other; R1 is hydrogen, optionally substituted lower alkyl or lower alkenyl; A is optionally substituted lower alkylene, lower alkenylene or a single bond while B is optionally substituted imino or a single bond, or alternatively A and B may be united to form a single bond; and D is a single bond or group (a).

3. 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

4. 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

5. 发明公开

EP2703406A1 NOVEL CEPHEM COMPOUND HAVING CATECHOL OR PSEUDO-CATECHOL STRUCTURE 审中-公开
标题翻译： 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。

6. 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。

7. 发明公开

EP2030982A1 GLYCOPEPTIDE ANTIBIOTIC DERIVATIVE 审中-公开
标题翻译：抗生素治疗糖尿病
公开(公告)号：EP2030982A1
公开(公告)日：2009-03-04
申请号：EP07744107.9
申请日：2007-05-25
申请人： SHIONOGI & CO., LTD.
发明人： NISHITANI, Yasuhiro , YOSHIDA, Osamu , IWAKI, Tsutomu , KATO, Issei
IPC分类号： C07K9/00 , A61K38/00 , A61P31/04 , C07K7/06 , C07K14/36
CPC分类号： C07K9/008 , A61K38/00 , A61K38/04
摘要： The present invention provides a novel glycopeptide antibiotic derivative.
These derivatives are represented by the formula (I)

or a pharmaceutically acceptable salt or solvate thereof,
wherein
R A is

-X 1 -Ar 1 -X 2 -Y-X 3 -Ar 2

wherein
X 1 , X 2 and X 3 are single bond; heteroatom-containing group selected from the group consisting of -N=, =N-, - NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group;
Y is -NR 2 CO-, -CONR 2 - (R 2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R 3 is alkylene;
Ar 1 and Ar 2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond;
R B is

-NHNR X R Y or -NR Z OR W

wherein
R X is hydrogen or lower alkyl;
R Y is hydrogen, optionally substituted lower alkyl, C(=NH)NH 2 , CSNH 2 , COCONH 2 , CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl;
R Z is hydrogen or lower alkyl;
R W is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl;
R C is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N=, =N-, -NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -; and
R is optionally substituted alkyl.
摘要翻译：本发明提供了一种新型糖肽抗生素衍生物。这些衍生物由式（I）表示或其药学上可接受的盐或溶剂化物，其中RA为€ƒ€ƒ€ƒ€ƒ€ƒ-X 1 -Ar 1 -X 2 -YX 3 -Ar 2其中X 1，X 2和X 3为单键; 选自-N =，= N - ， - NR 1 - （R 1为氢或低级烷基）， - O - ， - S - ， - SO-和-SO 2 - 的含杂原子的基团，或其联系; 或任选被取代并任选被一个或多个所述含杂原子基团中断的亚烷基或亚烯基; Y是-NR 2 CO-，-CONR 2 - （R 2是氢或低级烷基）或式（II）的基团，其中R 3是亚烷基; Ar 1和Ar 2是任选被取代并可具有不饱和键的碳环或杂环; R B是€ƒ€ƒ€ƒ€ƒ€ƒ-NHNR X R Y或-NR Z OR W其中R X是氢或低级烷基; R Y是氢，任选取代的低级烷基，C（= NH）NH 2，CSNH 2，COCONH 2，CN，任选取代的杂环基和任选取代的氨基甲酰基; R Z是氢或低级烷基; R W是氢，任选取代的低级烷基，任选取代的低级烯基，任选取代的杂环基，任选取代的杂环羰基或任选取代的氨基甲酰基; RC是氢或任选取代的烷基，其中所述烷基可以被选自N =，N-，-NR 1 - （R 1是氢或低级烷基），-O-，-S- ，-SO-和-SO 2 - ; 和R是任选取代的烷基。

8. 发明公开

EP0893446A1 CEPHEM COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS 失效
标题翻译： CEPHEMVERBINDUNGEN UND MEDIKAMENTE DIE DIESE VERBINDUNGEN ENTHALTEN
公开(公告)号：EP0893446A1
公开(公告)日：1999-01-27
申请号：EP97914600.8
申请日：1997-04-04
申请人： SHIONOGI & CO., LTD.
发明人： NISHITANI, Yasuhiro , ISHIKURA, Koji
IPC分类号： C07D501/38 , C07D401/04 , C07D409/04 , A61K31/545
CPC分类号： C07D401/04 , C07D409/04 , C07D501/00
摘要： A cephem compound, wherein the cephem ring has a substituent at the 3-position, which substituent is shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R 1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):
摘要翻译：头孢烯化合物，其中头孢烯环在3位上具有取代基，该取代基由式II表示，其中Het是包含一个或多个选自N， O和S可以相同或不同; R 1是氢，任选取代的低级烷基或任选取代的低级烯基; A是任选取代的低级亚烷基，任选取代的低级亚烯基或单键; B是任选取代的亚氨基或单键; 或A和B组合在一起可形成单一债券; 和D是单键或式（a）的基团：

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