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21. 发明申请

US20070042974A1 Nozel azalide and azalactam derivatives and method for producing the same 失效
标题翻译：诺贝尔氮杂和吖内酰胺衍生物及其制备方法
公开(公告)号：US20070042974A1
公开(公告)日：2007-02-22
申请号：US10569063
申请日：2004-08-20
申请人： Tomoaki Miura , Kenichi Kanemoto , Satomi Natsume , Naoto Ohkura , Yumiko Fujihira , Takashi Watanabe , Hideki Fushimi , Kunio Atsumi , Keiichi Ajito
发明人： Tomoaki Miura , Kenichi Kanemoto , Satomi Natsume , Naoto Ohkura , Yumiko Fujihira , Takashi Watanabe , Hideki Fushimi , Kunio Atsumi , Keiichi Ajito
IPC分类号： A61K31/7052 , C07H17/08
CPC分类号： A61K31/7052 , C07H15/04 , C07H17/00
摘要： A compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, which is useful for a prophylactic and/or therapeutic treatment of a microbial infectious disease. [R1 is hydrogen atom, or a linear C1-6 alkylcarbonyl group; R2 is hydrogen atom, or a C1-6 alkylcarbonyl group; R3 is hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkenyl group, a C2-6 alkenylcarbonyl group, a C2-6 alkynyl group, or an Ar—B— group (Ar represents an aryl group, or a heterocyclic group, and B is a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C2-6 alkenyl group, a C2-6 alkenylcarbonyl group, or a C2-6 alkynyl group); R5, R6, R7, and R8 represent hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or an Ar—B′— group (B′ is a C1-6 alkyl group, a C2-6 alkenyl group, or a C2-6 alkynyl group); X is oxygen atom, or an —NR4— group (R4 is hydrogen atom, a C1-6 alkyl group, or a C1-6 alkyl group which may be substituted with an Ar group); and R4′ is hydrogen atom, or a group represented by the aforementioned formula (a) (R3″ and R4″ represent hydrogen atom, or a linear or branched C1-6 alkylcarbonyl group)]
摘要翻译：由以下通式（1）表示的化合物或其药学上可接受的盐，其可用于预防和/或治疗微生物感染性疾病。 R 1是氢原子或直链C 1-6烷基羰基; R 2是氢原子或C 1-6烷基羰基; R 3是氢原子，C 1-6烷基，C 1-6烷基羰基，C 1-6烯基，C 2-6烯基羰基，C 2-6炔基或 Ar-B-基（Ar表示芳基或杂环基，B为C1-6烷基，C1-6烷基羰基，C2-6烯基，C2-6链烯基羰基或 C 2-6炔基）; R 5，R 6，R 7和R 8表示氢原子，C 1-6烷基，C2-6烯基，C2-6炔基或Ar-B'-基（B'是C1-6烷基，C2-6链烯基或C2-6炔基）; X是氧原子或-NR 4 - 基团（R 4）是氢原子，C 1-6烷基或可以是C 1-6烷基的C 1-6烷基被Ar基团取代）; 和R 4'是氢原子，或由上述式（a）表示的基团（R 3'和R 4“ 代表氢原子，或直链或支链C 1-6烷基羰基）]

22. 发明授权

US06908913B2 Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US06908913B2
公开(公告)日：2005-06-21
申请号：US10344729
申请日：2001-11-22
申请人： Yuko Kano , Yasuo Yamamoto , Takahisa Maruyama , Takehiko Sawabe , Eiki Shitara , Kazuhiro Aihara , Kunio Atsumi , Takashi Ida
发明人： Yuko Kano , Yasuo Yamamoto , Takahisa Maruyama , Takehiko Sawabe , Eiki Shitara , Kazuhiro Aihara , Kunio Atsumi , Takashi Ida
IPC分类号： A61P31/04 , C07D477/14 , C07D519/00 , A61K31/429 , C07D519/06
CPC分类号： C07D477/14
摘要： An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and β-lactamase producing bacteria and are stable to DHP-1. The carbapenem derivatives according to the present invention are compounds represented by formulae (I) and (II) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl, R2 and R3 each independently represent H; halogen; substituted or unsubstituted alkyl; cycloalkyl; substituted or unsubstituted alkylcarbonyl; carbamoyl; substituted or unsubstituted aryl; substituted or unsubstituted alkylthio; morpholinyl; alkylsulfonyl; or formyl, n is 0 (zero) to 4, and Hy represents a substituted or unsubstituted monocyclic or bicyclic heterocyclic group.
摘要翻译：本发明的目的是提供对MRSA，PRSP，流感病毒和产生β-内酰胺酶的细菌具有强抗生素活性并且对DHP-1稳定的碳青霉烯衍生物。根据本发明的碳青霉烯衍生物是由式（I）和（II）表示的化合物或其药学上可接受的盐：其中R 1表示H或甲基，R 2，和R 3各自独立地表示H; 卤素; 取代或未取代的烷基; 环烷基取代或未取代的烷基羰基; 氨基甲酰基; 取代或未取代的芳基; 取代或未取代的烷硫基; 吗啉基烷基磺酰基; 或甲酰基，n为0（零）至4，Hy表示取代或未取代的单环或双环杂环基。

23. 发明授权

US4839350A Cephalosporin compounds and the production thereof 失效
标题翻译：头孢菌素化合物及其生产
公开(公告)号：US4839350A
公开(公告)日：1989-06-13
申请号：US36124
申请日：1987-04-07
申请人： Kunio Atsumi , Kenji Sakagami , Yuichi Yamamoto , Takashi Yoshida , Ken Nishihata , Shinichi Kondo , Shunzo Fukatsu
发明人： Kunio Atsumi , Kenji Sakagami , Yuichi Yamamoto , Takashi Yoshida , Ken Nishihata , Shinichi Kondo , Shunzo Fukatsu
IPC分类号： C07D277/32 , C07D501/22 , C07D501/24
CPC分类号： C07D277/32 , Y02P20/55
摘要： A class of new caphalosporin compounds (syn-isomer) is now provided, which is useful as antibacterial agent and is represented by the general formula (I) ##STR1## wherein R.sup.1 is an amino group or a protected amino group; R.sup.2 is a lower alkyl group, a carboxymethyl group or a protected carboxymethyl group; R.sup.3 is a hydrogen atom, a salt-forming cation or a carboxyl-protecting group; A is an unsubstituted or substituted phenyl group, an unsubstituted or substituted furyl group, an unsubstituted or substituted thiazolyl group or an unsubstituted or substituted 3-lower-alkylthiazolio group, and a pharmaceutically acceptable salt or ester thereof.
摘要翻译：现在提供一类新的头孢菌素化合物（顺式异构体），其可用作抗菌剂并由通式（I）表示，其中R 1是氨基或被保护的氨基; R2是低级烷基，羧甲基或受保护的羧甲基; R3是氢原子，成盐阳离子或羧基保护基; A是未取代或取代的苯基，未取代或取代的呋喃基，未取代或取代的噻唑基或未取代或取代的3-低级烷基噻唑基及其药学上可接受的盐或酯。

24. 发明授权

US07524951B2 Intermediates of 2-substituted carbapenem derivatives and process for production thereof 失效
公开(公告)号：US07524951B2
公开(公告)日：2009-04-28
申请号：US10538466
申请日：2003-12-15
申请人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
发明人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
IPC分类号： C07D519/06 , C07D513/04
CPC分类号： C07D513/04 , C07F9/6561 , Y02P20/55
摘要： The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.

25. 发明授权

US5232947A Oxamic acid compounds and pharmaceutical composition for use in improvement of damaged cerebral functions of brain 失效
标题翻译：用于改善脑损伤脑功能的恶唑酸化合物和药物组合物
公开(公告)号：US5232947A
公开(公告)日：1993-08-03
申请号：US754393
申请日：1991-09-04
申请人： Yasuo Sato , Shinsuke Katoh , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
发明人： Yasuo Sato , Shinsuke Katoh , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
IPC分类号： A61K31/19 , C07C233/56
CPC分类号： C07C233/56 , A61K31/19 , Y10S514/921
摘要： New N,N-di-alkyl- or alkenyl-substituted derivatives of oxamic acid of which the two alkyl or alkenyl groups are different from each other are now produced and found to exhibit the cerebral protective effect against cerebral anoxia in the brain of a mammalian animal, including human, and to be useful as an agent for improving or ameliorating the damaged or disturbed functions of the brain. Some known N,N-di-alkyl-substituted derivatives of oxamic acid or which the two alkyl groups are identical to each other are now also found to have similar, cerebral protective effect against cerebral anoxia and to be useful as an agent for improving the damaged functions of the brain.
摘要翻译：现在产生两个烷基或链烯基彼此不同的新的N，N-二 - 烷基 - 或链烯基取代的衍生物，并发现它们在哺乳动物脑中表现出对脑缺氧的脑保护作用动物，包括人类，并且可用作改善或改善大脑受损或紊乱功能的药剂。现在还发现一些已知的氧杂酸的N，N-二烷基取代的衍生物或两个烷基彼此相同，对脑缺氧具有相似的脑保护作用，并且可用作改善损坏大脑功能。

26. 发明授权

US5132454A Oxamic acid compounds and pharmaceutical compositions for use in improvement of damaged cerebral functions of brain 失效
标题翻译：用于改善脑损伤的神经功能的含氧化合物和药物组合物
公开(公告)号：US5132454A
公开(公告)日：1992-07-21
申请号：US662192
申请日：1991-02-28
申请人： Yasuo Sato , Shinsuke Kato , Takako Taniguchi , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
发明人： Yasuo Sato , Shinsuke Kato , Takako Taniguchi , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
IPC分类号： A61K31/19 , A61P9/00 , A61P25/28 , C07C231/12 , C07C233/36 , C07C233/56
CPC分类号： C07C233/56
摘要： A method of inhibiting the abnormal postnatal axial growth of the eye of a maturing animal during conditions ordinarily leading to said abnormal growth, which comprises (1) determining the neurochemical present in the retina of said eye, e.g., dopamine, the concentration of which is reduced during said conditions, and (2) administering to said eye during postnatal maturation effective amounts of said neurochemical, its agonist or its antagonist.

27. 发明授权

US07662841B2 Imidazothiazole derivatives and process for producing the same 失效
标题翻译：咪唑并噻唑衍生物及其制备方法
公开(公告)号：US07662841B2
公开(公告)日：2010-02-16
申请号：US11795522
申请日：2006-01-19
申请人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
发明人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
IPC分类号： A61K31/429 , C07D235/02
CPC分类号： C07D513/04
摘要： The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.
摘要翻译：本发明涉及式（I）化合物及其制备方法。在式（I）中，X表示卤素原子，R1表示-COR2基团，其中R2表示基团OM或C1-12烷氧基，其中M表示氢原子，碱金属，碱土金属或季铵。使用该化合物作为合成中间体可以以低成本实现以高效安全的方式生产具有强效抗菌活性的碳青霉烯衍生物。

28. 发明申请

US20080114164A1 Imidazothiazole Derivatives and Process for Producing the Same 失效
标题翻译：咪唑噻唑衍生物及其制备方法
公开(公告)号：US20080114164A1
公开(公告)日：2008-05-15
申请号：US11795522
申请日：2006-01-19
申请人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
发明人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
IPC分类号： C07D513/02
CPC分类号： C07D513/04
摘要： The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.
摘要翻译：本发明涉及式（I）化合物及其制备方法。在式（I）中，X表示卤素原子，R 1表示基团-COR 2，其中R 2表示基团OM或C1- 12烷氧基，其中M表示氢原子，碱金属，碱土金属或季铵。使用该化合物作为合成中间体可以以低成本实现以高效安全的方式生产具有强效抗菌活性的碳青霉烯衍生物。

29. 发明申请

US20080076917A1 Intermediates of 2-Substituted Carbapenem Derivatives and Process for Production Thereof 失效
标题翻译： 2-取代的碳青霉烯衍生物的中间体及其制备方法
公开(公告)号：US20080076917A1
公开(公告)日：2008-03-27
申请号：US10538466
申请日：2003-12-15
申请人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
发明人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
IPC分类号： C07D205/00 , C07D487/00
CPC分类号： C07D513/04 , C07F9/6561 , Y02P20/55
摘要： The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.
摘要翻译：本发明涉及由式（1）表示的化合物及其制备方法。这些化合物的使用可以以安全和成本有效的方式实现具有有效抗微生物活性和广谱抗菌谱的碳青霉烯衍生物的生产。

30. 发明申请

US20070167620A1 Crystalline carbapenem intermediate 失效
标题翻译：结晶碳青霉烯中间体
公开(公告)号：US20070167620A1
公开(公告)日：2007-07-19
申请号：US10561200
申请日：2004-06-18
申请人： Kazuhiro Aihara , Toshifumi Hasegawa , Shinichi Kitahara , Takashi Watanabe , Takashi Ando , Takehiko Sawabe , Eiki Shitara , Kunio Atsumi , Kazumi Ota
发明人： Kazuhiro Aihara , Toshifumi Hasegawa , Shinichi Kitahara , Takashi Watanabe , Takashi Ando , Takehiko Sawabe , Eiki Shitara , Kunio Atsumi , Kazumi Ota
IPC分类号： C07D205/02
CPC分类号： C07F9/568
摘要： This invention relates to crystals of compounds of formula (I), wherein TBS represents t-butyldimethylsilyl, and Ph represents phenyl, or its salt or solvate. Compounds of formula (I) are synthesis intermediates of 2-substituted-1β-methyl carbapenem compounds useful as antimicrobial agents. The crystals of the present invention have excellent handleability and can realize the production of carbapenem compounds having excellent antimicrobial actibity in a simpler manner with improved yield and purity.
摘要翻译：本发明涉及式（I）化合物的晶体，其中TBS代表叔丁基二甲基甲硅烷基，Ph代表苯基或其盐或溶剂合物。式（I）化合物是可用作抗微生物剂的2-取代的-1β-甲基碳青霉烯化合物的合成中间体。本发明的晶体具有优异的可操作性，并且可以以更简单的方式实现具有优异的抗微生物活性的碳青霉烯化合物的生产和提高产率和纯度。

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