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1. 发明授权

US06174877B1 Carbapenem compound, their production and use 失效
标题翻译：碳青霉烯化合物，其生产和使用
公开(公告)号：US06174877B1
公开(公告)日：2001-01-16
申请号：US09101470
申请日：1998-07-10
申请人： Yukio Ishibashi , Shinichi Imamura , Tetsuo Miwa
发明人： Yukio Ishibashi , Shinichi Imamura , Tetsuo Miwa
IPC分类号： A61K3140
CPC分类号： C07D477/20
摘要： A cephem compound of the formula: wherein R1 stands for an optionally substituted lower alkyl group, R2 stands for H or a lower alkyl group, R3 stands for H, an optionally substituted hydrocarbon group, cyano group, a lower alkyloxy group or a lower alkylthio group, and the ring A stands for an optionally substituted non-quaternarized nitrogen-containing heterocyclic ring, provided that, when A is unsubstituted 2-pyridyl group, R3 stands for a group other than hydrogen, or their esters or salts, has excellent antibacterial activities, oral absorbability and stability, and is useful as an antibacterial agent.
摘要翻译：下式的头孢烯化合物：其中R1代表任意取代的低级烷基，R2代表H或低级烷基，R3代表H，任意取代的烃基，氰基，低级烷氧基或低级烷硫基并且环A代表任选取代的非季铵化含氮杂环，条件是当A是未取代的2-吡啶基时，R 3代表氢以外的基团或其酯或盐，具有优异的抗菌性活性，口服吸收性和稳定性，可用作抗菌剂。

2. 发明授权

US4845257A 4-halogeno-2-oxyimino-3-oxobutyric acids and derivatives 失效
标题翻译： 4-卤代-2-氧代亚氨基-3-氧代丁酸及其衍生物
公开(公告)号：US4845257A
公开(公告)日：1989-07-04
申请号：US50332
申请日：1987-05-18
申请人： Kenzo Naito , Yukio Ishibashi
发明人： Kenzo Naito , Yukio Ishibashi
IPC分类号： C07C67/00 , C07C239/00 , C07C249/12 , C07C251/32 , C07C251/38 , C07F7/18
CPC分类号： C07F7/1852
摘要： A method of producing a 4-halo-2-(substituted or unsubstituted)hydroxyimino-3-oxobutyric acid ester or amide, which is a synthetic intermediate of value for the production of cephalosporins containing an aminothiazole group, characterized by reacting a 2-(substituted or unsubstituted)-hydroxyimino-3-oxobutyric acid or an ester or amide thereof with a silylating agent and reacting the resulting novel 2-(substituted)hydroxyimino-3-silyloxy-3-butenoic acid ester or amide with a halogenating agent.
摘要翻译：制备4-卤代-2-（取代或未取代的）肟基-3-氧代丁酸酯或酰胺的方法，其是含有氨基噻唑基团的头孢菌素的合成中间值，其特征在于使2-（取代或未取代的） - 羟基亚氨基-3-氧代丁酸或其酯或酰胺与甲硅烷基化剂反应，并使所得新的2-（取代的）肟基-3-甲硅烷氧基-3-丁烯酸酯或酰胺与卤化剂反应。

3. 发明授权

US4980464A Method for production of cephalosporin compounds 失效
标题翻译：生产头孢菌素化合物的方法
公开(公告)号：US4980464A
公开(公告)日：1990-12-25
申请号：US373594
申请日：1989-06-30
申请人： Kenzo Naito , Yukio Ishibashi
发明人： Kenzo Naito , Yukio Ishibashi
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04 , C07D501/18 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/46 , C07D519/06 , C07F7/10
CPC分类号： C07D501/20 , C07D501/04 , C07D501/18 , C07D501/46 , Y02P20/55
摘要： A method for producing a compound of the formula; ##STR1## wherein R stands for a hydrogen atom, an acyl group or a protective group other than acyl groups, Q stands for a hydrogen atom or an ester residue, Y stands for the residue of a nucleophilic compound and the dotted line shows the double bond at 2- or 3- position of the cephem ring or a salt thereof, characterized by allowing a compound of the formula; ##STR2## [R, Q and the dotted line are of the same meaning as above] or a salt thereof to react with a nucleophilic compound or a salt thereof and a compound of the formula; ##STR3## wherein R.sup.1, R.sup.2, R.sup.3 independently stand for a hydrocarbon group having not more than 8 carbon atoms, or R.sup.1 and R.sup.2, R.sup.1 and R.sup.3 or R.sup.2 and R.sup.3 may be combined to form polymethylene group, according to which the end product [I] of high quality can be provided in a high yield by one reaction step by using the compound [III] of relatively low cost, thus the method of this invention is advantageous for mass-producing the compound [I] on an industrial scale from the compound [II] and a nucleophilic compound.
摘要翻译：一种制备式的化合物的方法; 其中R表示氢原子，酰基或除酰基以外的保护基，Q表示氢原子或酯残基，Y表示亲核性化合物的残基，虚线表示表示头孢烯环的2-或3-位上的双键或其盐，其特征在于允许下式的化合物： [II] [R，Q和虚线具有与上述相同的含义]或其盐与亲核化合物或其盐和下式化合物反应; 其中R 1，R 2，R 3独立地表示不多于8个碳原子的烃基，或者R 1和R 2，R 1和R 3或R 2和R 3可以组合形成多亚甲基，其中通过使用相对低成本的化合物[III]，可以通过一次反应步骤以高产率提供高质量的最终产物[I]，因此本发明的方法有利于大量生产化合物[I] 化合物[II]和亲核化合物的工业规模。

4. 发明授权

US5492903A Crystalline esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo[3.2.0]h e 失效
标题翻译：（+） - （5R，6S）-6 - [（R）-1-羟乙基] -3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷 -2-烯-2-羧酸
公开(公告)号：US5492903A
公开(公告)日：1996-02-20
申请号：US112072
申请日：1993-08-26
申请人： Yoshiharu Maeda , Yukio Ishibashi , Tetsuya Tsukamoto , Masahiro Mizuno
发明人： Yoshiharu Maeda , Yukio Ishibashi , Tetsuya Tsukamoto , Masahiro Mizuno
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： Crystalline acetoxymethyl and pivaloyloxymethyl esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0]hept-2-ene-carboxylic acid can be obtained by adding a poor solvent to a solution of acetoxymethyl or pivaloyloxymethyl ester of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0]hept-2-ene-carboxylic acid in a good solvent. The crystalline penem compounds obtained show improved stability and are useful antibacterial agents.
摘要翻译：（+） - （5R，6S）-6 - [（R）-1-羟乙基] -3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2 通过向（+） - （5R，6S）-6 - [（R）-1-羟乙基] - （（R）-1-羟乙基）-6 - [（R）-1-羟基乙基） - 乙酰氧基甲基酯的乙酰氧基甲基或新戊酰氧基甲基酯的溶液中加入不良溶剂， 3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚-2-烯羧酸在良溶剂中反应。获得的结晶青枯烯化合物显示出改进的稳定性，并且是有用的抗菌剂。

5. 发明授权

US5162522A Method for producing cephem compounds 失效
标题翻译：头孢烯化合物的制备方法
公开(公告)号：US5162522A
公开(公告)日：1992-11-10
申请号：US691307
申请日：1991-04-25
申请人： Kenzo Naito , Yukio Ishibashi , Toshihiko Fujitani
发明人： Kenzo Naito , Yukio Ishibashi , Toshihiko Fujitani
IPC分类号： A61K31/545 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/26
CPC分类号： C07D501/04 , C07D501/18 , C07D501/26
摘要： A method for producing 3-(3-oxobutyryloxymethyl)-3-cepham-4-carboxylic acids which are antibiotics or intermediates for the synthesis of antibiotics, at a low temperature in a very short period of time and in good yield, characterized by reacting a 3-hydroxylmethyl-3-cephem-4-carboxylic acid with diketene in the presence of a 4-(tertiary-amino)pyridine and if necessary, when a 7-acylamino-3-(3-oxobutyryloxymethyl)-3-cephem-4-carboxylic acid is obtained, subjecting it to deacylation at the 7-position thereof.
摘要翻译：一种生产3-（3-氧代丁酰氧基甲基）-3-头孢烯-4-羧酸的方法，它是抗生素或用于合成抗生素的中间体，在非常短的时间内以低的温度和良好的产率，其特征在于反应 3-羟基甲基-3-头孢烯-4-羧酸与4-（叔 - 氨基）吡啶存在下的双烯酮，如果需要，当7-酰基氨基-3-（3-氧代丁酰氧基甲基）-3-头孢烯-4-羧酸得到4-羧酸，使其在其7-位脱羟基。

6. 发明授权

US4927964A Method for production of 2-oxyimino-3-oxobutyric acids 失效
标题翻译： 2-氧亚氨基-3-氧代丁酸的生产方法
公开(公告)号：US4927964A
公开(公告)日：1990-05-22
申请号：US295510
申请日：1989-01-11
申请人： Kenzo Naito , Yukio Ishibashi , Haruo Shinbo
发明人： Kenzo Naito , Yukio Ishibashi , Haruo Shinbo
IPC分类号： C07C251/34 , C07C67/00 , C07C239/00 , C07C249/14 , C07C251/38 , C07C251/60
CPC分类号： C07C251/60
摘要： An advantageous method of producing in large amounts on a commercial scale 2-substituted oxyimino-3-oxobutyric acids, which are useful as intermediates in the synthesis of e.g. aminothiazole cephalosporins, is characterized by reacting a tert-butyl 2-substituted oxyimino-3-oxobutyrate with a hydrogen halide in an anhydrous organic solvent.

7. 发明授权

US5183929A Method for production of T-butyl 3-oxobutyrates and their use 失效
标题翻译： 3-氧代丁酸叔丁酯的制备方法及其用途
公开(公告)号：US5183929A
公开(公告)日：1993-02-02
申请号：US770333
申请日：1991-10-03
申请人： Kenzo Naito , Yukio Ishibashi , Haruo Shinbo
发明人： Kenzo Naito , Yukio Ishibashi , Haruo Shinbo
IPC分类号： B01J31/02 , C07B61/00 , C07C67/03 , C07C67/46 , C07C69/24 , C07C69/675 , C07C69/72 , C07D501/04 , C07D501/20 , C07D501/36
CPC分类号： C07D501/20 , C07C69/72 , C07D501/04
摘要： Disclosed are an advantageous method of industrial production of tert-butyl 3-oxobutylate, which is a useful intermediate for synthesis, characterized by reacting tert-butyl alcohol with diketene in the presence of 4-(tertiary amino) pyridine, and an industrially advantageous method of producing cephalosporin compounds or pharmaceutically acceptable salts thereof, using tert-butyl 3-oxobutylate as an intermediate.
摘要翻译：公开了工业生产3-氧代丁酸叔丁酯的有利方法，其是合成的有用中间体，其特征在于在4-（叔氨基）吡啶存在下使叔丁醇与双烯酮反应，工业上有利的方法使用3-氧代丁酸叔丁酯作为中间体生产头孢菌素化合物或其药学上可接受的盐。

8. 发明授权

US5109131A Method for production of t-butyl 3-oxobutyrates and their use 失效
标题翻译： 3-丁氧基-3-丁酮的生产方法及其用途
公开(公告)号：US5109131A
公开(公告)日：1992-04-28
申请号：US295516
申请日：1989-01-11
申请人： Kenzo Naito , Yukio Ishibashi , Haruo Shinbo
发明人： Kenzo Naito , Yukio Ishibashi , Haruo Shinbo
IPC分类号： B01J31/02 , C07B61/00 , C07C67/03 , C07C67/46 , C07C69/24 , C07C69/675 , C07C69/72 , C07D501/04 , C07D501/20 , C07D501/36
CPC分类号： C07D501/20 , C07C69/72 , C07D501/04
摘要： Disclosed are an advantageous method of industrial production of tert-butyl 3-oxobutylate, which is a useful intermediate for synthesis, characterized by reacting tert-butyl alcohol with diketene in the presence of 4-(tertiary amino) pyridine, and an industrially advantageous method of producing cephalosporin compounds or pharmaceutically acceptable salts thereof, using tert-butyl 3-oxobutylate as an intermediate.

9. 发明授权

US4908444A Method of producing cephem compounds 失效
标题翻译：头孢烯化合物的制备方法
公开(公告)号：US4908444A
公开(公告)日：1990-03-13
申请号：US3286
申请日：1987-01-14
申请人： Kenzo Naito , Yukio Ishibashi
发明人： Kenzo Naito , Yukio Ishibashi
IPC分类号： C07D501/04 , A61K31/545 , C07D501/06 , C07D501/16 , C07D501/18 , C07D501/24 , C07D501/26 , C07D501/28 , C07D501/34 , C07D501/57
CPC分类号： C07D501/04 , C07D501/34
摘要： A method of producing 3-alkanoyloxymethyl-3-cephem-4-carboxylic acids, which are useful as antibiotics or as intermediates in the synthesis of antibiotics, by reacting a 3-hydroxymethyl-3-cephem-4-carboxylic acid with a saturated fatty acid anhydride in an aqueous medium in the presence of an acid-acceptor base and a 4-(tertiary amino)pyridine.
摘要翻译：通过使3-羟甲基-3-头孢烯-4-羧酸与饱和脂肪酸反应，制备3-烷酰氧基甲基-3-头孢烯-4-羧酸的方法，其可用作抗生素或合成抗生素中的中间体酸酐在酸性受体碱和4-（叔氨基）吡啶的存在下在水性介质中反应。

10. 发明授权

US4592974A Active material for negative poles of alkaline dry cells, and method for making said material 失效
标题翻译：碱性干细胞负极活性物质及其制备方法
公开(公告)号：US4592974A
公开(公告)日：1986-06-03
申请号：US687369
申请日：1984-12-28
申请人： Ryuzo Takeda , Shigeru Ooyama , Yukio Ishibashi
发明人： Ryuzo Takeda , Shigeru Ooyama , Yukio Ishibashi
IPC分类号： C22C30/00 , H01M4/42
CPC分类号： H01M4/42 , C22C30/00
摘要： Novel active materials for negative poles in alkaline dry cells, and method of preparing the same are disclosed. Said materials and method do not employ harmful Hg. In place of Hg, an alloy containing at least three elements selected from Bi, Pb, In, Cd, and Ga is used to have a zinc dust alloyed at its outer surfaces with said alloy elements which are afforded with a high hydrogen overvoltage effective to retard the generation of hydrogen due to self erosion of the zinc dust in an alkaline solution of the dry cells.
摘要翻译：公开了碱性干细胞中负极的新型活性物质及其制备方法。所述材料和方法不使用有害汞。代替Hg，使用含有选自Bi，Pb，In，Cd和Ga中的至少三种元素的合金，在其外表面上合金化锌粉，所述合金元素具有高的氢过电压，阻止由于干细胞的碱性溶液中锌粉的自身侵蚀而产生氢。

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