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1. 发明公开

EP0747381A1 CARBAPENEM DERIVATIVE 失效
标题翻译：碳青霉烯衍生物
公开(公告)号：EP0747381A1
公开(公告)日：1996-12-11
申请号：EP95909978.9
申请日：1995-02-24
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAKAGAWA, Susumu, Banyu Pharmaceutical Co., Ltd. , FUKATSU, Hiroshi, Banyu Pharmaceutical Co., Ltd. , USHIJIMA, Ryosuke, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07D477/00
CPC分类号： C07D477/20
摘要： A compound of the formula:
wherein R 1 is a hydrogen atom or a lower alkyl group, R 2 is a hydrogen atom or a negative charge, R 3 is a hydrogen atom or a lower alkyl group, Ar is a phenyl group, a naphthyl group or a group of:
(wherein each of A 4 and A 5 is a single bond, -NHSO 2 - or the like, and Het is a pyrrolinyl group, a 1,4-diazabicyclo[2.2.2]octanyl group or the like which may be substituted with a hydroxyl group, a carbamoyl lower alkyl group or the like) which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfonyl group or the like; a hydroxyl group; a di-lower alkylsulfamoyl group or the like, each of A 1 , A 2 and A 3 is a single bond or a lower alkylene group which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfamoyl group or the like; a pyridyl group or a pyridinio group or the like which may be substituted with a lower alkyl group, a carbamoyl lower alkyl group or the like, and W is a sulfur atom, a single bond or the like; or a pharmaceutically acceptable salt or ester thereof, a process for its production and an antibacterial agent containing it as an active ingredient.
摘要翻译：下式化合物：其中R 1为氢原子或低级烷基，R 2为氢原子或负电荷，R 3为氢原子或低级烷基中，Ar为苯基，萘基或下述基团：其中A4和A5各自为单键，-NHSO2-等，Het为吡咯啉基，1,4-二氮杂双环[ 可以被可被羟基取代的低级烷基，低级烷基氨磺酰基等取代的可以被羟基，氨基甲酰基低级烷基等取代的2-辛基或其类似物），二低级烷基磺酰基等; 羟基; 二低级烷基氨磺酰基等，A1，A2和A3各自为可以被羟基取代的低级烷基，低级烷基氨磺酰基等取代的单键或低级亚烷基基，二低级烷基氨磺酰基等; 可以被低级烷基，氨基甲酰基低级烷基等取代的吡啶基或吡啶基等，W是硫原子，单键等; 或其药学上可接受的盐或酯，其生产方法和含有它作为活性成分的抗菌剂。

2. 发明授权

EP0747381B1 CARBAPENEM DERIVATIVE 失效
标题翻译：碳青霉烯衍生物
公开(公告)号：EP0747381B1
公开(公告)日：2001-10-31
申请号：EP95909978.9
申请日：1995-02-24
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAKAGAWA, Susumu, Banyu Pharmaceutical Co., Ltd. , FUKATSU, Hiroshi, Banyu Pharmaceutical Co., Ltd. , USHIJIMA, Ryosuke, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07D477/00
CPC分类号： C07D477/20
摘要： A compound represented by general formula (I), a medicinally acceptable salt or ester thereof, a process for producing the same, and an antibacterial containing the same as the active ingredient: wherein R1 represents hydrogen or lower alkyl; R2 represents hydrogen or a negative charge; R3 represents hydrogen or lower alkyl; Ar represents lower alkyl, lower alkylsulfamoyl, etc. (each of which may be substituted by hydroxyl, di (lower alkyl) sulfonyl, etc.), or phenyl, naphthyl or a group of formula α or β (each of which may be substituted by hydroxyl, di (lower alkyl) sulfamoyl, etc.), wherein A¿4? and A5 represent each a single bond, -NHSO2-, etc., and Het represents pyrrolinyl, 1,4-diazabicyclo[2.2.2]octanyl, etc. (each of which may be substituted by hydroxyl, carbamoylated lower alkyl, etc.); A1, A2 and A3 represent each a single bond or lower alkylene which may be substituted by lower alkyl, lower alkylsulfamoyl, etc. (each of which may be substituted by hydroxyl, di(lower alkyl)sulfamoyl, etc.) or may be substituted by pyridyl, pyridinio, etc. (each of which may be substituted by lower alkyl, carbamoylated lower alkyl, etc.); and W represents sulfur, a single bond, etc.

3. 发明公开

EP0453574A1 CEPHALOSPORIN DERIVATIVE 失效
标题翻译： CEPHALOSPORINDERIVAT。
公开(公告)号：EP0453574A1
公开(公告)日：1991-10-30
申请号：EP90916366.9
申请日：1990-11-13
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAKAGAWA, Susumu, Banyu Pharmaceutical Co., Ltd. , MITOMO, Ryuji, c/o Banyu Pharmaceutical Co., Ltd. , USHIJIMA, Ryosuke, Banyu Pharmaceutical Co., Ltd. , ASAI, Akira, c/o Banyu Pharmaceutical Co., Ltd. , KUROYANAGI, Satoru, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： A novel, optically active compound of formula (I) which is useful as a remedy for bacterial infection, a pharmaceutically acceptable salt or ester thereof, a crystal thereof, and production and uses thereof.
摘要翻译：具有下式的化合物：其中R是可被取代的乙烯基，苯基或芳烷基; 或其药学上可接受的盐，生理上可水解的酯或其溶剂合物。

4. 发明公开

EP1048669A1 CARBAPENEM DERIVATIVES 审中-公开
标题翻译：碳青霉烯衍生物
公开(公告)号：EP1048669A1
公开(公告)日：2000-11-02
申请号：EP98961372.4
申请日：1998-12-16
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAKANO, Masato , KIYONAGA, Hideo, Banyu Pharm. Co., Ltd. , IMAMURA, Hideaki, Banyu Pharm. Co., Ltd. , MITSUYA, Aya, Banyu Pharm. Co., Ltd. , SATO, Hiroki, Banyu Pharmaceutical Co., Ltd. , SUGIMOTO, Yuichi, Banyu Pharmaceutical Co., Ltd. , SAKURABA, Shunji, Banyu Pharmaceutical Co., Ltd. , NAKAGAWA, Susumu, 32-1, Aza Gomae , FUKATSU, Hiroshi, Banyu Pharmaceutical Co., Ltd. , USHIJIMA, Ryosuke, Banyu Pharmaceutical Co., Ltd. , HASHIZUME, Terutaka, Banyu Pharm. Co., Ltd. , NAGANO, Rie, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07D477/20 , A61K31/40
CPC分类号： C07D477/20
摘要： Compounds represented by general formula (I); a process for producing the same; and utilization thereof as antimicrobial agents and metallo-β-lactamase inhibitors, wherein R 1 represents hydrogen or lower alkyl; R 2 represents hydrogen, an ester residue, etc.; R 3 and R 4 are the same or different and each represents hydrogen, halogeno, etc.; R 5 and R 6 are the same or different and each represents hydrogen, lower alkoxy, etc., or lower alkyl optionally having one or two substituents selected from the group consisting of carbamoyl, carboxy and hydroxy; group (a) represents aryl selected from the group consisting of benzene and naphthalene rings, etc.; and Y represents a single bond, linear C 1-4 alkylene, etc. (provided that the case where R 3 and R 4 are hydrogen, (a) is benzene, Y is methylene and R 5 and R 6 are hydrogen is excluded).
摘要翻译：由通式（I）表示的化合物; 其制造方法; 其作为抗微生物剂和金属β-内酰胺酶抑制剂的用途，其中R 1表示氢或低级烷基; R 2表示氢，酯残基等; R 3和R 4相同或不同，各自表示氢，卤素等; R 5和R 6相同或不同，各自表示氢，低级烷氧基等，或任选具有一个或两个选自氨基甲酰基，羧基和羟基的取代基的低级烷基; 基团（a）表示选自苯和萘环等的芳基; 并且Y表示单键，线性C 1-4亚烷基等（条件是R 3和R 4为氢，（a）为苯，Y为亚甲基，R 5和R 5为氢， 6>是氢被排除）。

5. 发明公开

EP0516861A1 PYRIDONECARBOXYLIC ACID DERIVATIVE 失效
标题翻译： PYRIDONCARBONSÄUREDERIVAT。
公开(公告)号：EP0516861A1
公开(公告)日：1992-12-09
申请号：EP91920828.0
申请日：1991-11-29
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： OKURA, Akira, Banyu Pharmaceutical Co., Ltd. , YOSHINARI, Tomoko, Banyu Pharmaceutical Co., Ltd. , NAKAGAWA, Susumu, Banyu Pharmaceutical Co., Ltd. , MANO, Eiichi, Banyu Pharmaceutical Co., Ltd. , ARAKAWA, Hiroharu, Banyu Pharmaceutical Co., Ltd. , USHIJIMA, Ryosuke, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04 , C07D471/04
摘要： A compound represented by general formula (I), a pharmaceutically acceptable salt of ester thereof, a process for the production thereof, and an antitumor agent containing the same as the active ingredient. In formula (I), R¹ represents linear, branched or cyclic lower alkyl, or optionally fluorinated phenyl; R² and R³ represent each hydrogen, or linear, branched or cyclic lower alkyl; R⁴ represents hydrogen or N(R⁵)R⁶, wherein R⁵ and R⁶ represent each hydrogen, or linear, branched or cyclic lower alkyl; X represents nitrogen or C-Y, wherein Y represents hydrogen, halogen, methyl or methoxy; m and n represent each an integer of 0 or 1; and represents a single or double bond.
摘要翻译：由通式（I）表示的化合物，其药学上可接受的酯，其制备方法和含有该活性成分的抗肿瘤剂。在式（I）中，R 1表示直链，支链或环状低级烷基或任选氟化苯基; R 2和R 3代表每个氢或直链，支链或环状低级烷基; R 4表示氢或N（R 5）R 6，其中R 5和R 6表示每个氢或直链，支链或环状低级烷基; X表示氮或C-Y，其中Y表示氢，卤素，甲基或甲氧基; m和n表示0或1的整数; 和@表示单键或双键。

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