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1. 发明申请

WO1998023623A1 CARBAPENEM DERIVATIVES AND ANTIMICROBIALS 审中-公开
标题翻译：卡巴因衍生物和抗生素
公开(公告)号：WO1998023623A1
公开(公告)日：1998-06-04
申请号：PCT/JP1997004270
申请日：1997-11-25
申请人： MEIJI SEIKA KAISHA, LTD. , AIHARA, Kazuhiro , SASAKI, Toshiro , TOYOOKA, Yumiko , KANO, Yuko , ATSUMI, Kunio , IWAMATSU, Katsuyoshi , IDA, Takashi
发明人： MEIJI SEIKA KAISHA, LTD.
IPC分类号： C07D519/06
CPC分类号： C07D477/20
摘要： Compounds exhibiting a wide and potent antimicrobial activity against gram-positive and gram-negative bacteria, a potent antimicrobial activity against various beta -lactamase producing bacteria, MRSA and resistant Pseudomonas aeruginosa, and an extremely high stability to DHP-I. The compounds are presented by general formulae (I) and (II).
摘要翻译：对革兰氏阳性和革兰氏阴性细菌表现出广泛有效的抗微生物活性的化合物，对各种β-内酰胺酶生产细菌，MRSA和耐药铜绿假单胞菌的有效抗微生物活性，以及对DHP-1极高的稳定性。化合物由通式（I）和（II）表示。

2. 发明申请

WO1998022469A1 CEPHEM INTERMEDIATES AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译： CEPHEM中间件及其生产方法
公开(公告)号：WO1998022469A1
公开(公告)日：1998-05-28
申请号：PCT/JP1997004226
申请日：1997-11-20
申请人： MEIJI SEIKA KAISHA, LTD. , FUSHIHARA, Kenichi , SETSU, Fumihito , UMEMURA, Eijirou , ATSUMI, Kunio
发明人： MEIJI SEIKA KAISHA, LTD.
IPC分类号： C07D501/56
CPC分类号： C07D501/02 , C07D501/24 , C07D501/56 , Y02P20/55
摘要： A process for efficiently and economically producing cephem intermediates wherein the side chain at the 7-position is fluorinated and cephem antibiotics wherein the side chain at the 7-position is fluorinated and the side chain at the 3-position is substituted by formylamino. This process comprises reacting a compound of general formula (II), its derivative reactive at the carboxyl group or its salt with a compound of general formula (III), and deblocking the protected functional group, if necessary or desired, to thereby give a compound of general formula (I).
摘要翻译：一种有效和经济地生产头孢烯中间体的方法，其中7-位的侧链是氟化的，并且其中7-位的侧链被氟化并且3-位的侧链被甲酰氨基取代的头孢烯抗生素。该方法包括使通式（II）的化合物，其在羧基或其盐上的反应性衍生物与通式（III）的化合物反应，如果需要或需要，将保护的官能团解封，由此得到化合物的通式（I）。

3. 发明申请

WO1996028455A1 NOVEL CARBAPENEM DERIVATIVES 审中-公开
标题翻译：新卡巴衍生物衍生物
公开(公告)号：WO1996028455A1
公开(公告)日：1996-09-19
申请号：PCT/JP1996000573
申请日：1996-03-08
申请人： MEIJI SEIKA KABUSHIKI KAISHA , AIHARA, Kazuhiro , KANO, Yuko , SHIOKAWA, Sohjiro , SASAKI, Toshiro , SETSU, Fumihito , TOYOOKA, Yumiko , ISHII, Miyuki , ATSUMI, Kunio , IWAMATSU, Katsuyoshi , TAMURA, Atsushi
发明人： MEIJI SEIKA KABUSHIKI KAISHA
IPC分类号： C07D519/00
CPC分类号： C07D477/14
摘要： Novel carbapenem derivatives represented by general formula (I) which have an optionally substituted imidazo[5,1-b]thiazolium-6-ylmethyl group at the 2-position. The compounds have a broad and potent antibacterial activity on Gram-positive bacteria and Gram-negative bacteria including Pseudomonas aeruginosa and show a potent antibacterial effect on various beta -lactamase-producing bacteria and MRSA and an extremely high DHP-1 stability.
摘要翻译：由通式（I）表示的新的碳青霉烯衍生物，其在2-位具有任选取代的咪唑并[5,1-b]噻唑鎓-6-基甲基。该化合物对革兰氏阳性菌和革兰氏阴性细菌（包括铜绿假单胞菌）具有广泛有效的抗菌活性，对各种β-内酰胺酶生产细菌和MRSA具有强力的抗菌作用，并具有极高的DHP-1稳定性。

4. 发明申请

WO1998025935A1 NOVEL CEPHEM DERIVATIVES 审中-公开
标题翻译：新CEPHEM衍生物
公开(公告)号：WO1998025935A1
公开(公告)日：1998-06-18
申请号：PCT/JP1997004489
申请日：1997-12-08
申请人： MEIJI SEIKA KAISHA, LTD. , KOBAYASHI, Kazuko , UMEMURA, Eijirou , ATSUMI, Kunio , IDA, Takashi
发明人： MEIJI SEIKA KAISHA, LTD.
IPC分类号： C07D519/06
CPC分类号： C07D519/00
摘要： Compounds represented by general formula (I). These compounds have broad and potent antibacterial activities on gram-positive bacteria including those producing beta -lactamase and gram-negative bacteria. In particular, these compounds are superior to the existing cephem derivatives of the onium salt type in the antibacterial activities on methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP) and imipenem-resistant Pseudomonas aeruginosa, which makes them highly useful as remedies for infectious diseases caused by various pathogenic bacteria. In said formula, X represents CH or N; R represents hydrogen, optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or cycloalkyl; one of R , R , R and R R NSO2NHC1-6 (wherein R and R may be the same or different from each other and each represents hydrogen or C1-6 alkyl); and n is 0 or 1.
摘要翻译：由通式（I）表示的化合物。这些化合物对革兰氏阳性细菌具有广泛有效的抗菌活性，包括那些产生β-内酰胺酶和革兰氏阴性细菌的抗菌活性。特别地，这些化合物优于现有的鎓盐型头孢烯衍生物对耐甲氧西林金黄色葡萄球菌（MRSA），青霉素耐药性肺炎链球菌（PRSP）和亚胺培南耐药铜绿假单胞菌的抗菌活性，使其高度可用作各种病原菌引起的传染病的补救措施。在所述式中，X表示CH或N; R 1表示氢，任选取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或环烷基; R 2，R 3，R 4，R 5，表示R 6> R 7 NSO 2 NHC 1-6（其中R 6和R 7可以相同或不同，各自表示氢或C 1-6烷基）。 n为0或1。

5. 发明申请

WO1996037499A1 NOVEL CEPHEM DERIVATIVES 审中-公开
标题翻译：新的CEPHEM衍生物
公开(公告)号：WO1996037499A1
公开(公告)日：1996-11-28
申请号：PCT/JP1996001406
申请日：1996-05-24
申请人： MEIJI SEIKA KABUSHIKI KAISHA , UMEMURA, Eijiro , ATSUMI, Kunio , IWAMATSU, Katsuyoshi , TAMURA, Atsushi
发明人： MEIJI SEIKA KABUSHIKI KAISHA
IPC分类号： C07D519/00
CPC分类号： C07D501/00 , Y02P20/55
摘要： Compounds represented by general formula (I) and having a beta -(optionally substituted imidazo[5,1-b]thiazolyl)vinyl group at the 3-position of the cephem ring, and salts and esters thereof. These compounds have an extremely broad antimicrobial spectrum and exerts potent antimicrobial effects on Gram-positive bacteria, Gram-negative bacteria and even resistant bacteria. In formula (I) X represents CH or N; R represents hydrogen or an amino protecting group; R represents hydrogen, C1-6 alkyl, C3-7 cycloalkyl or a hydroxy protecting group; R is not present or represents hydrogen, a cation forming a salt or a carboxy protecting group; R , R and R may be the same or different and each represents hydrogen or C1-6 alkyl; R is not present or represents a cation of C1-6 alkyl; and n is an integer of 0 or 1.
摘要翻译：由通式（I）表示并在头孢烯环的3位具有β-（任选取代的咪唑并[5,1-b]噻唑基）乙烯基的化合物及其盐和酯。这些化合物具有非常宽的抗菌谱，对革兰氏阳性菌，革兰氏阴性细菌甚至抗性细菌都发挥有力的抗菌作用。在式（I）中，X表示CH或N; R 1表示氢或氨基保护基; R 2表示氢，C 1-6烷基，C 3-7环烷基或羟基保护基; R 3不存在或表示氢，形成盐或羧基保护基的阳离子; R 4，R 5和R 6可以相同或不同，各自表示氢或C 1-6烷基; R 7+不存在或表示C 1-6烷基的阳离子; n为0或1的整数。

6. 发明申请

WO1996005205A1 NOVEL CEPHEM DERIVATIVE 审中-公开
标题翻译：新闻CEPHEM DERIVATIVE
公开(公告)号：WO1996005205A1
公开(公告)日：1996-02-22
申请号：PCT/JP1995001627
申请日：1995-08-16
申请人： MEIJI SEIKA KABUSHIKI KAISHA , TSUSHIMA, Masaki , ATSUMI, Kunio , IWAMATSU, Katsuyoshi , TAMURA, Atsushi
发明人： MEIJI SEIKA KABUSHIKI KAISHA
IPC分类号： C07D519/381
CPC分类号： C07D501/00
摘要： A cephalosporin derivative represented by general formula (I) wherein an (un)substituted 3-(imidazo[5,1-b]thiazolium-6-yl)-1-propenyl group is present as a substituent at the 3-position of the cephem ring, having an excellent antibacterial activity, and being useful as a remedy for various microbisms.
摘要翻译：由通式（I）表示的头孢菌素衍生物，其中（（un）取代的3-（咪唑并[5,1-b]噻唑鎓-6-基）-1-丙烯基作为取代基在3- 头孢烯环，具有优异的抗菌活性，可用作各种微生物的补救剂。

7. 发明申请

WO1995009171A1 NOVEL CEPHALOSPORIN DERIVATIVE 审中-公开
标题翻译：新CEPHALOSPORIN衍生物
公开(公告)号：WO1995009171A1
公开(公告)日：1995-04-06
申请号：PCT/JP1994001618
申请日：1994-09-29
申请人： MEIJI SEIKA KAISHA, LTD. , SHIOKAWA, Sohjiro , ATSUMI, Kunio , IWAMATSU, Katsuyoshi , TAMURA, Atsushi , SHIBAHARA, Seiji
发明人： MEIJI SEIKA KAISHA, LTD.
IPC分类号： C07D501/24
CPC分类号： C07D501/00 , Y02P20/55
摘要： A cephalosporin derivative as a cephem compound having an excellent antibacterial activity and being useful as a remedy for various bacterial infections. It has an (un)substituted 2-(5-thiazolyl)vinyl group at the 3-position and is represented by general formula (I) wherein X represents CH or N; R represents amino which may be protected; R represents hydrogen or a hydroxyimino-protecting group; R represents hydrogen, salt-forming cation or a carboxyl-protecting group; R represents hydrogen; and R represents hydrogen, lower alkyl, halogenated (lower) alkyl or halogen.
摘要翻译：作为起始化合物的头孢菌素衍生物具有优异的抗菌活性，可用作各种细菌感染的补救剂。它在3-位具有（未取代的）2-（5-噻唑基）乙烯基，由通式（I）表示，其中X代表CH或N; R 1表示可被保护的氨基; R 2表示氢或羟基亚氨基保护基; R 3表示氢，成盐阳离子或羧基保护基; R 4表示氢; 和R 5代表氢，低级烷基，卤代（低级）烷基或卤素。

8. 发明申请

WO1995007912A1 NOVEL CEPHEM DERIVATIVE 审中-公开
标题翻译：新CEPHEM DERIVATIVE
公开(公告)号：WO1995007912A1
公开(公告)日：1995-03-23
申请号：PCT/JP1994001529
申请日：1994-09-16
申请人： MEIJI SEIKA KABUSHIKI KAISHA , ATSUMI, Kunio , UMEMURA, Eijiro , KANO, Yuko , SHIOKAWA, Sohjiro , KUDO, Toshiaki , TSUSHIMA, Masaki , IWAMATSU, Katsuyoshi , TAMURA, Atsushi , SHIBAHARA, Seiji
发明人： MEIJI SEIKA KABUSHIKI KAISHA
IPC分类号： C07D519/00
CPC分类号： C07D501/00
摘要： A compound represented by general formula (I), i.e., a cephem derivative having an (un)substituted imidazo[5,1-b]thiazolium-6-yl group at the 3-position of the ring, wherein X represents CH or N; R represents H, alkyl, alkenyl, etc.; and R , R , R and R represent each H, alkyl, carbamoyl, amino, etc. This compound has an excellent antibacterial activity and is useful as a remedy for various types of microbism.
摘要翻译：由通式（I）表示的化合物，即在环的3位具有（未）取代的咪唑并[5,1-b]噻唑鎓-6-基的头孢烯衍生物，其中X表示CH或N ; R 1表示H，烷基，烯基等; R 2，R 3，R 4和R 5分别表示H，烷基，氨基甲酰基，氨基等。该化合物具有优异的抗菌活性，可用于各种微生物的补救。

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