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1. 发明授权

US5698544A Cephem compound, process for producing the compound, and antimicrobial composition containing the same 失效
标题翻译：头孢烯化合物，制备该化合物的方法和含有该化合物的抗微生物组合物
公开(公告)号：US5698544A
公开(公告)日：1997-12-16
申请号：US537856
申请日：1995-11-16
申请人： Hiroshi Akagi , Masaru Yasui , Takae Yamada , Masahiro Ito , Akio Hyodo , Hideaki Hanaki
发明人： Hiroshi Akagi , Masaru Yasui , Takae Yamada , Masahiro Ito , Akio Hyodo , Hideaki Hanaki
IPC分类号： C07D501/00 , C07D501/24 , C07D501/57 , A61K31/545
CPC分类号： C07D501/00
摘要： The present invention provides a cephem compound having a high antimicrobial activity against various pathogenic bacteria. The cephem compound of the invention is represented by the formula ##STR1## wherein Q represents CH or N, R.sup.1 represents a carboxylate or the like, R.sup.2 represents a hydrogen atom, and R represents ##STR2## wherein R.sup.3 represents a group --(CH.sub.2).sub.m --Y (wherein m is an integer of 1 to 5, and Y represents a quaternary ammonium group) or the like, n is an integer of 0 to 4, B.sup.- represents an anion, f is 0 or 1 when R.sup.1 represents a carboxylate, and 2 when R.sup.1 represents a carboxyl group, and the ring C represents a 5-membered heterocyclic group of not more than 4 nitrogen atoms, which may be substituted by a lower alkyl group.
摘要翻译： PCT No.PCT / JP95 / 00471 Sec。 371日期：1995年11月16日 102（e）日期1995年11月16日PCT 1995年3月17日PCT公布。出版物WO95 / 25109 日期1995年9月21日本发明提供了一种对各种病原菌具有高抗微生物活性的头孢烯化合物。本发明的头孢烯化合物由下式表示，其中Q表示CH或N，R 1表示羧酸酯等，R 2表示氢原子，R表示其中R 3表示基团 - （CH 2）m Y（其中m为1〜5的整数，Y为季铵基）等，n为0〜4的整数，B为阴离子，f为0或1，羧酸酯，当R1表示羧基时为2，环C表示可以被低级烷基取代的不大于4个氮原子的5元杂环基。

2. 发明授权

US5635500A Cephem compound and pharmaceutical composition containing the compound 失效
标题翻译： Cephem化合物和含有该化合物的药物组合物
公开(公告)号：US5635500A
公开(公告)日：1997-06-03
申请号：US240663
申请日：1994-05-16
申请人： Hiroshi Akagi , Masaru Yasui , Yoshifumi Hara , Hideaki Hanaki , Akio Hyodo
发明人： Hiroshi Akagi , Masaru Yasui , Yoshifumi Hara , Hideaki Hanaki , Akio Hyodo
IPC分类号： C07D501/00 , C07D501/04 , C07D501/06 , C07D501/24 , C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： The object of the present invention is to provide a cephem compound having high activity against various pathogenic microorganisms. The cephem compound of this invention is represented by the general formula ##STR1## wherein Q represents CH or N; R.sup.1 represents a carboxylate etc; and R represents ##STR2## or the group ##STR3## where R.sup.2 represents a lower alkyl group etc, n represents an integer of 0 or 1 through 3, B.sup.- represents an anion, f is equal to 0 when R.sup.1 represents a carboxylate and 1 where R.sup.1 represents a carboxyl group, and the ring C represents a 5-membered heterocyclic group of not more than 4 nitrogen atoms, which may be substituted by lower alkyls.
摘要翻译： PCT No.PCT / JP93 / 01326 Sec。 371日期1994年5月16日 102（e）日期1994年5月16日PCT提交1993年9月16日PCT公布。出版物WO94 / 06804 日期1994年3月31日本发明的目的是提供对各种病原微生物具有高活性的头孢烯化合物。本发明的头孢烯化合物由通式表示，其中Q表示CH或N; R1代表羧酸盐等; R表示或R2表示低级烷基等基团，n表示0或1〜3的整数，B-表示阴离子，当R1表示羧酸酯时，f等于0，其中R 1表示羧基，并且环C表示不超过4个氮原子的5元杂环基，其可以被低级烷基取代。

3. 发明授权

US07973147B2 K04-0144 substance and a process for production thereof 有权
标题翻译： K04-0144物质及其生产方法
公开(公告)号：US07973147B2
公开(公告)日：2011-07-05
申请号：US12084878
申请日：2006-05-16
申请人： Satoshi Omura , Hiroshi Tomoda , Yong-pil Kim , Hideaki Hanaki , Atsuko Matsumoto , Yoko Takahashi
发明人： Satoshi Omura , Hiroshi Tomoda , Yong-pil Kim , Hideaki Hanaki , Atsuko Matsumoto , Yoko Takahashi
IPC分类号： C07H15/20 , C07H15/22 , C07C61/12
CPC分类号： C07H11/04 , C07C323/59 , C12P13/02 , C12P19/26 , C12P19/44 , C12R1/465
摘要： A microorganism represented by a strain K04-0144 belonging to Streptomyces sp. having ability to produce K04-0144 substance is cultured in the medium, and the isolated K04-0144A substance, K04-0144B substance and K04-0144C substance therefrom have strong antibacterial activities against Gram-positive bacteria including methicillin-resistant Streptococcus aureus (MRSA), consequently these are useful as the therapeutic agents for infectious disease caused by MRSA as well as infectious diseases caused by multidrug including β-lactam antibiotics resistant bacteria. Further, similarly, since the novel K04-0144D substance isolated from the cultured liquid has the action for enhancing the effect of β-lactam antibiotics, which are utilized as the antibacterial agents, in combination with them, it is useful as the therapeutic agent for infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and multidrug including β-lactam antibiotics resistant bacteria.
摘要翻译：属于Streptomyces sp。的菌株K04-0144所代表的微生物在培养基中培养生产K04-0144物质的能力，分离的K04-0144A物质，K04-0144B物质和K04-0144C物质对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌（MRSA））具有很强的抗菌活性，因此，这些可用作由MRSA引起的感染性疾病的治疗剂以及由多种药物（包括β-内酰胺抗生素抗性细菌）引起的感染性疾病。此外，类似地，由于从培养液中分离的新型K04-0144D物质具有增强作为抗菌剂的β-内酰胺抗生素与其组合的作用，因此可用作治疗剂用于由耐甲氧西林金黄色葡萄球菌（MRSA）引起的感染性疾病和包含β-内酰胺抗生素抗性细菌的多药物。

4. 发明授权

US06294527B1 Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US06294527B1
公开(公告)日：2001-09-25
申请号：US09331183
申请日：1999-07-20
申请人： Hideaki Hanaki , Hiroaki Yamazaki , Yoshio Tsuchida , Hideki Sato , Keiichi Hiramatsu , Seiichiro Kawashima
发明人： Hideaki Hanaki , Hiroaki Yamazaki , Yoshio Tsuchida , Hideki Sato , Keiichi Hiramatsu , Seiichiro Kawashima
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： An antibacterial compound wherein represents benzene ring, pyridine ring, pyrazine ring or 5-membered aromatic neterocycle (having one oxygen or sulfur atom as ring-constituting atom), there being no R4 where represents 5-membered aromatic heterocycle; X and Y respectively represent hydrogen atom or CXY represents C═N—OR5 wherein R5 represents hydrogen atom, halo C1-C6 alkyl or C3-C7 cycloalkyl; R1 represents phenyl, furyl, thienyl, thiazolyl (which may be substituted by amino group), tetrazolyl or thiadiazolyl, R2, R3 and R4 respectively represent hydrogen atom, halogen, hydroxyl group, nitro, C1-C6 alkoxy, trifluoromethyl, isothiuronium C1-C6 alkyl, amino C1-C6 alkyl, halo C1-C6 alkyl, morpholino, piperidino or piperazinyl.
摘要翻译：一种抗菌化合物，其代表苯环，吡啶环，吡嗪环或5元芳族杂环（具有一个氧或硫原子作为构成环的原子），不存在表示5元芳族杂环的R 4，X和Y分别表示氢原子或CXY表示C = N-OR5，其中R5表示氢原子，卤代C1-C6烷基或C3-C7环烷基; R1表示苯基，呋喃基，噻吩基，噻唑基（其可被氨基取代），四唑基或噻二唑基， R 3和R 4分别表示氢原子，卤素，羟基，硝基，C 1 -C 6烷氧基，三氟甲基，异硫脲C 1 -C 6烷基，氨基C 1 -C 6烷基，卤代C 1 -C 6烷基，吗啉代，哌啶子基或哌嗪基。

5. 发明申请

US20090130717A1 Novel K04-0144 Substance and a Process for Production Thereof 有权
标题翻译：新型K04-0144物质及其生产工艺
公开(公告)号：US20090130717A1
公开(公告)日：2009-05-21
申请号：US12084878
申请日：2006-05-16
申请人： Satoshi Omura , Hiroshi Tomoda , Yong-pil Kim , Hideaki Hanaki , Atsuko Matsumoto , Yoko Takahashi
发明人： Satoshi Omura , Hiroshi Tomoda , Yong-pil Kim , Hideaki Hanaki , Atsuko Matsumoto , Yoko Takahashi
IPC分类号： C12P19/44 , C07H15/10 , C12P13/02 , C12N1/20 , C07C59/62
CPC分类号： C07H11/04 , C07C323/59 , C12P13/02 , C12P19/26 , C12P19/44 , C12R1/465
摘要： A microorganism represented by a strain K04-0144 belonging to Streptomyces sp. having ability to produce K04-0144 substance is cultured in the medium, and the isolated K04-0144A substance, K04-0144B substance and K04-0144C substance therefrom have strong antibacterial activities against Gram-positive bacteria including methicillin-resistant Streptococcus aureus (MRSA), consequently these are useful as the therapeutic agents for infectious disease caused by MRSA as well as infectious diseases caused by multidrug including β-lactam antibiotics resistant bacteria. Further, similarly, since the novel K04-0144D substance isolated from the cultured liquid has the action for enhancing the effect of β-lactam antibiotics, which are utilized as the antibacterial agents, in combination with them, it is useful as the therapeutic agent for infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and multidrug including β-lactam antibiotics resistant bacteria.
摘要翻译：属于Streptomyces sp。的菌株K04-0144所代表的微生物在培养基中培养生产K04-0144物质的能力，分离的K04-0144A物质，K04-0144B物质和K04-0144C物质对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌（MRSA））具有很强的抗菌活性，因此，这些可用作由MRSA引起的感染性疾病的治疗剂以及由多种药物（包括β-内酰胺抗生素抗性细菌）引起的感染性疾病。此外，类似地，由于从培养液体中分离的新型K04-0144D物质具有增强作为抗菌剂的β-内酰胺抗生素与其组合的作用，因此可用作治疗剂由耐甲氧西林金黄色葡萄球菌（MRSA）引起的感染性疾病和包括β-内酰胺抗生素抗性细菌在内的多种药物。

6. 发明授权

US06897304B2 Cephem compounds and ESBL-detecting reagents containing the same 失效
标题翻译： Cephem化合物和含有该化合物的ESBL检测试剂
公开(公告)号：US06897304B2
公开(公告)日：2005-05-24
申请号：US10380628
申请日：2001-09-21
申请人： Seiichiro Kawashima , Keiichi Hiramatsu , Hideaki Hanaki , Hiroaki Yamazaki , Hidenori Harada
发明人： Seiichiro Kawashima , Keiichi Hiramatsu , Hideaki Hanaki , Hiroaki Yamazaki , Hidenori Harada
IPC分类号： C07D501/00 , C07D501/14 , C07D501/24 , G01N21/78 , C07D501/22 , C12Q1/34
CPC分类号： C07D501/00 , G01N21/78
摘要： A cephem compound or pharmaceutically acceptable salt thereof represented by the formula I: wherein R1 and R2 may be the same or different and each represent hydrogen atom, nitro or cyano; R3 represents C1-C6 alkyl which may be substituted with carboxyl; R4 represents hydrogen atom or amino; X represents —S— or —SO—, there being no case where both of R1 and R2 are simultaneously hydrogen atom.
摘要翻译：由式I表示的头孢烯化合物或其药学上可接受的盐：其中R 1和R 2可以相同或不同，各自代表氢原子，硝基或氰基; R 3表示可以被羧基取代的C 1 -C 6 -C 6烷基; R 4表示氢原子或氨基; X表示-S-或-SO-，不存在R 1和R 2两者同时为氢原子的情况。

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