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公开(公告)号:US4659812A
公开(公告)日:1987-04-21
申请号:US767562
申请日:1985-08-20
申请人: Shimpei Aburaki , Yukio Narita , Jun Okumura , Takayuki Naito , Donald G. Walker
发明人: Shimpei Aburaki , Yukio Narita , Jun Okumura , Takayuki Naito , Donald G. Walker
IPC分类号: C07D501/18
CPC分类号: C07D501/18
摘要: Temperature stable crystalline mono-hydrochloric and sulfuric acid addition salts of 7-amino-3-(1-methylpyrrolidinio)methyl-3-cephem-4-carboxylate substantially free of .DELTA..sup.2 isomer are intermediates for the preparation of broad spectrum 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoxyiminoacetamido]-3-[(1-methyl-1-pyrrolidinio)methyl]-3-cephem-4-carboxylates. The monohydrochloric acid addition salt intermediate is prepared by a process comprising the steps of (1) neutralizing diphenylmethyl 7-amino-3-chloromethyl-3-cephem-4-carboxylate hydrochloride, (2) reacting the resulting free base with benzaldehyde to produce diphenylmethyl 7-benzylideneamino-3-chloromethyl-3-cephem-4-carboxylate, (3) reacting the resulting product with sodium iodide to convert the chloromethyl group to iodomethyl, (4) reacting the resulting product with N-methylpyrrolidine to give the quaternized product diphenylmethyl 7-benzylideneamino-3-(1-methylpyrrolidinio)methyl-3-cephem-4-carboxylate iodide, and (5) reacting with hydrochloric acid to form said intermediate.
摘要翻译: 基本上不含DELTA 2异构体的7-氨基-3-(1-甲基吡咯烷酮基)甲基-3-头孢烯-4-羧酸酯的温度稳定的结晶一盐酸和硫酸加成盐是用于制备广谱7- [ - (2-氨基噻唑-4-基)-α-(Z) - 甲氧基亚氨基乙酰氨基] -3 - [(1-甲基-1-吡咯烷基)甲基] -3-头孢烯-4-羧酸盐。 通过包括以下步骤的方法制备单盐酸加成盐中间体:(1)中和7-氨基-3-氯甲基-3-头孢烯-4-羧酸二苯甲酯盐酸盐,(2)使所得游离碱与苯甲醛反应,生成二苯基甲基 (3)使所得产物与碘化钠反应,将氯甲基转化为碘甲基,(4)使所得产物与N-甲基吡咯烷反应,得到季铵化产物 (1-甲基吡咯烷基)甲基-3-头孢烯-4-羧酸二苯基酯碘化物,和(5)与盐酸反应形成所述中间体。
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公开(公告)号:US4500526A
公开(公告)日:1985-02-19
申请号:US541593
申请日:1983-10-13
申请人: Kiyoto Imae , Shimpei Aburaki , Yukio Narita , Jun Okumura , Takayuki Naito
发明人: Kiyoto Imae , Shimpei Aburaki , Yukio Narita , Jun Okumura , Takayuki Naito
IPC分类号: C07D277/20 , C07D501/46 , C07D501/36 , A61K31/545
CPC分类号: C07D277/587 , Y02P20/55
摘要: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 is one of various alkyl, alkenyl, alkynyl, cycloalkyl, carboxyalkyl or carboxycycloalkyl moieties described herein, and R.sup.5 is hydrogen, amino, carboxy, formyl, carbamoyl, guanidino, amidino or one of various alkyl, alkoxy, alkylthio or substituted amino moieties described herein, and nontoxic pharmaceutically acceptable acid addition salts, physiologically hydrolyzable esters and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.
摘要翻译: 其中R 1是氢或常规的氨基保护基,R 2是本文所述的各种烷基,烯基,炔基,环烷基,羧基烷基或羧基环烷基部分之一,R 5是氢,氨基, 羧基,甲酰基,氨基甲酰基,胍基,脒基或本文所述的各种烷基,烷氧基,烷硫基或取代的氨基部分之一,以及无毒的药学上可接受的酸加成盐,其生理上可水解的酯和溶剂合物,以及其制备方法 。 其中R1是氢的化合物是有效的抗菌剂。
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公开(公告)号:US4486586A
公开(公告)日:1984-12-04
申请号:US465374
申请日:1983-02-10
申请人: Yukio Narita , Seiji Iimura , Shimpei Aburaki , Jun Okumura , Takayuki Naito
发明人: Yukio Narita , Seiji Iimura , Shimpei Aburaki , Jun Okumura , Takayuki Naito
IPC分类号: A61K20060101 , A61K31/545 , A61K31/546 , A61K31/55 , A61P31/04 , C07D501/20 , C07D501/24 , C07D501/46 , C07D519/00 , C07D519/06
CPC分类号: C07D501/24 , Y02P20/55
摘要: 7-{(Z)-2-(2-Aminothiazol-4-yl)-2-[(substituted)oxyimino]acetamido}-3-[3-(quaternary ammonio)-1-propen-1-yl]-3-cephem-4-carboxylates and salts, esters and solvates thereof, having potent antibacterial activity, are provided. Processes for their preparation and intermediates in their preparation also are disclosed.
摘要翻译: 7 - {(Z)-2-(2-氨基噻唑-4-基)-2 - [(取代的)氧亚氨基]乙酰氨基} -3- [3-(季铵)-1-丙烯-1-基] -3 - 头孢-4-羧酸盐及其具有强力抗菌活性的盐,酯和溶剂合物。 其制备方法及其制备中的中间体也被公开。
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公开(公告)号:US4525473A
公开(公告)日:1985-06-25
申请号:US480602
申请日:1983-03-30
申请人: Shimpei Aburaki , Hajime Kamachi , Yukio Narita , Jun Okumura , Takayuki Naito
发明人: Shimpei Aburaki , Hajime Kamachi , Yukio Narita , Jun Okumura , Takayuki Naito
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/46 , C07D513/04 , C07D519/06
CPC分类号: C07D277/587 , C07D513/04 , Y02P20/55
摘要: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 is a straight or branched chain alkyl, alkenyl or alkynyl containing from 1 to 4 carbon atoms, and ##STR2## is a quaternary ammonio group as described herein, and nontoxic pharmaceutically acceptable salts, physiologically hydrolyzable esters and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.
摘要翻译: 其中R 1是氢或常规氨基保护基的式Ⅺ化合物,R 2是含有1至4个碳原子的直链或支链烷基,烯基或炔基,和 - (+)N 3BOND Q是 公开了本文所述的季铵基和无毒的药学上可接受的盐,其生理上可水解的酯和溶剂化物,以及它们的制备方法。 其中R1是氢的化合物是有效的抗菌剂。
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公开(公告)号:US4406899A
公开(公告)日:1983-09-27
申请号:US354851
申请日:1982-03-04
申请人: Shimpei Aburaki , Hajime Kamachi , Yukio Narita , Jun Okumura , Takayuki Naito
发明人: Shimpei Aburaki , Hajime Kamachi , Yukio Narita , Jun Okumura , Takayuki Naito
IPC分类号: A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/46
CPC分类号: C07D501/46 , Y02P20/55
摘要: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, and R.sup.2 is a straight or branched chain alkyl group containing from 1 to 4 carbon atoms, allyl, 2-butenyl or 3-butenyl, and nontoxic pharmaceutically acceptable salts and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.
摘要翻译: 其中R 1为氢或常规氨基保护基,R 2为含有1至4个碳原子的直链或支链烷基,烯丙基,2-丁烯基或3-丁烯基和无毒的式 公开了其药学上可接受的盐和溶剂化物,以及它们的制备方法。 其中R1是氢的化合物是有效的抗菌剂。
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公开(公告)号:US5475973A
公开(公告)日:1995-12-19
申请号:US316379
申请日:1994-09-30
申请人: Hiroaki Furukawa , Sadahiro Onimaru , Yukio Narita
发明人: Hiroaki Furukawa , Sadahiro Onimaru , Yukio Narita
CPC分类号: D07B1/068 , D07B1/0673 , D07B1/0693 , B60C2009/0014 , D07B2201/102 , D07B2201/1032 , D07B2201/2011 , D07B2201/2024 , D07B2201/2036 , D07B2201/2061 , D07B2205/306 , D07B2205/3071 , D07B2205/3092 , D07B2401/2025
摘要: A rope comprising a plurality of wires (2, 3, 4) made of a steel wire being twisted together; at least the wires which are arranged in such a manner as to be disposed on an outer surface of the rope (1) being made of a plated steel wire wherein a corrosion resistance is superior; at least said wires which are located in a center of the rope not being made of the wire wherein the corrosion resistance is superior.
摘要翻译: 包括由钢绞线制成的多根线(2,3,4)绞合在一起的绳; 至少以布置在绳索(1)的外表面上的方式布置的电线由电镀钢丝制成,其中耐腐蚀性优异; 至少所述位于绳索中心的线不是由电线制成,其中耐腐蚀性优异。
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公开(公告)号:US5802929A
公开(公告)日:1998-09-08
申请号:US855646
申请日:1997-05-13
申请人: Hiroaki Furukawa , Sadahiro Onimaru , Yukio Narita
发明人: Hiroaki Furukawa , Sadahiro Onimaru , Yukio Narita
CPC分类号: F16C1/10 , F16C1/20 , Y10T74/20402 , Y10T74/20408 , Y10T74/20456
摘要: A rope-operated device includes a wire rope and an arrangement for guiding the wire rope. The wire rope itself is a stranded rope having a core strand which is a parallel lay strand. The core strand and the side strands are each composed of 19 wires stranded as Warrington type strands. A silicon lubricant is used for lubricating the wire rope and the arrangement for guiding the wire rope.
摘要翻译: 绳索操作装置包括钢丝绳和用于引导钢丝绳的装置。 钢丝绳本身是具有芯线的绞合绳,其是平行的绞合线。 芯股线和侧股线由绞合为Warrington型股线的19根线组成。 硅润滑剂用于润滑钢丝绳和用于引导钢丝绳的装置。
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