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31. 发明授权

US3959256A 9-O-Alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance and the production thereof 失效
标题翻译： 9-O-烷酰基-3 {41-烷酰氧基甲基-SF-837物质及其制备
公开(公告)号：US3959256A
公开(公告)日：1976-05-25
申请号：US505310
申请日：1974-09-12
申请人： Shigeharu Inouye , Shoji Omoto , Katsuyoshi Iwamatsu , Taro Niida , Toyoaki Kawasaki , Takashi Tsuruoka
发明人： Shigeharu Inouye , Shoji Omoto , Katsuyoshi Iwamatsu , Taro Niida , Toyoaki Kawasaki , Takashi Tsuruoka
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： A 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is now synthetized, which is a new compound useful in that this new 9-O-alkanoyl-3"-O-alkanoyloxymethyl derivative of the SF-837 substance exhibits an antibacterial activity comparable to that of the parent SF-837 substance but is advantageously free from the unpleasant bitter taste inherent to the SF-837 substance and is hence adapted for oral administration. A process of producing the 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is also provided, which comprises hydrolysing partially and selectively a 9,2'-di-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance in an aqueous alkanol or aqueous acetone. The 9,2'-di-O-alkanoyl-3"-O-alkanopyloxymethyl-SF-837 substance may be prepared by reacting a 9,2'-di-alkanoyl- or O-mono-O-alkanoyl-3"-O-thiomethoxymethyl-SF-837 substance with an alkanoic anhydride which is exemplified by acetic anhydride or propionic anhydride in the specification.
摘要翻译：现在合成了9-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质，这是一种新的化合物，有用的是这种新型的9-O-烷酰基-3'-O-烷酰氧基甲基衍生物 -837物质表现出与母体SF-837物质相当的抗菌活性，但有利地没有SF-837物质固有的不愉快的苦味，因此适于口服给药。还提供了制备9-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质的方法，其包括部分和选择性地水解9,2'-二-O-烷酰基-3'-O - 烷酰氧基甲基-SF-837物质在链烷醇水溶液或丙酮水溶液中。 9,2'-二-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质可以通过使9,2'-二烷酰基或O-单-O-烷酰基-3' 具有链烷酸酐的“-O-硫代甲氧基甲基-SF-837”物质，其例示在说明书中的乙酸酐或丙酸酐。

32. 发明授权

US4325951A 1-Oxadethiacephalosporin derivatives and antibacterial use thereof 失效
标题翻译： 1-硫代十八烷基醚衍生物及其抗菌用途
公开(公告)号：US4325951A
公开(公告)日：1982-04-20
申请号：US200410
申请日：1980-10-24
申请人： Shigeharu Inouye , Takashi Tsuruoka , Katsuyoshi Iwamatsu
发明人： Shigeharu Inouye , Takashi Tsuruoka , Katsuyoshi Iwamatsu
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00 , Y02P20/55
摘要： New antibacterial 1-oxadethiacephalosporin derivatives of the general formula ##STR1## wherein R is a heterocyclic group or a group --S--Het where Het denotes a heterocyclic group, Y is a hydrogen atom or a methoxy group; x and y are each an integer of 1 to 3 is produced by a process comprising condensing a 1-oxacephem compound of the formula ##STR2## wherein R, Y, y are as defined above; R' is a hydrogen atom or a carboxyl-protecting group; and Z is a halo group, with a sulfur-containing amino acid of the formula ##STR3## wherein x is as defined above, in a solvent and removing, if necessary, the residual protective group from the resultant condensation product. The new 1-oxadethiacephalosporin derivatives and the pharmaceutically acceptable salts and esters thereof exhibit high and broad "in vitro" and "in vivo" antibacterial activity, particularly against .beta.-lactamase-producing strains of gram-negative bacteria.
摘要翻译：其中R是杂环基的新型抗菌1-恶二硫醚类衍生物或其中Het表示杂环基的基团-S-Het，Y是氢原子或甲氧基; x和y各自为1〜3的整数，是通过下列方法制备的：其中R 1，Y，y如上所定义的式 R'是氢原子或羧基保护基; Z为卤素基，其中x如上定义，其中x如上所定义，并且如有必要，从所得缩合产物中除去残留的保护基团，其中含有式“IMAGE”的含硫氨基酸。新的1-羟基乙硫菌醚衍生物及其药学上可接受的盐和酯在革兰氏阴性菌的β-内酰胺酶生产菌株中表现出高且广泛的“体外”和“体内”抗菌活性。

33. 发明授权

US4324891A Process for the production of a 7-methoxycephalosporine derivative 失效
标题翻译：生产7-甲氧基头孢菌素衍生物的方法
公开(公告)号：US4324891A
公开(公告)日：1982-04-13
申请号：US178604
申请日：1980-08-15
申请人： Katsuyoshi Iwamatsu , Takashi Tsuruoka , Kazuko Mizutani , Katsumi Kawaharajyo , Tadahiro Watanabe , Shigeharu Inouye
发明人： Katsuyoshi Iwamatsu , Takashi Tsuruoka , Kazuko Mizutani , Katsumi Kawaharajyo , Tadahiro Watanabe , Shigeharu Inouye
IPC分类号： C07D501/04 , C07D501/57
CPC分类号： C07D501/57 , Y02P20/55
摘要： A new, efficient process is provided for the production of 7.beta.-[(2D-2-amino-2-carboxy)-ethylthio-acetamido]-7.alpha.-methoxy-3-[(1-methyl-1H-tetrazole-5-yl) thiomethyl]-3-cephem-4-carboxylic acid useful as new antibacterial agent. This process is economic in using as the starting material the inexpensive, corresponding cephem compound containing no 7.alpha.-methoxy group on the cephem nucleus and comprises 7.alpha.-methoxylation of a protected derivative of the starting cephem compound with t-butyl hypochlorite and lithium methoxide, followed by inactivation of the excessive methoxylation reagents with a trialkyl phosphite and acetic acid to prevent undesired side-reactions such as oxidation of the alkylthioacetyl group of the product, and further by conventional removal of the protecting groups.
摘要翻译：提供了一种新的，有效的方法，用于生产7β - [（2D-2-氨基-2-羧基） - 乙硫基 - 乙酰氨基]-7α-甲氧基-3 - [（1-甲基-1H-四唑-5 - 基）硫代甲基] -3-头孢烯-4-羧酸，可用作新的抗菌剂。该方法在起始物质中是经济的，其是在头孢烯核上不含有7个α-甲氧基的廉价相应的头孢烯化合物，并且包括起始头孢烯化合物与叔丁基次氯酸盐和甲醇锂的保护的衍生物的7α-甲氧基化然后用亚磷酸三烷基酯和乙酸使过量的甲氧基化试剂失活，以防止不期望的副反应如产物的烷基硫代乙酰基氧化，并进一步通过常规除去保护基。

34. 发明授权

US4258184A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4258184A
公开(公告)日：1981-03-24
申请号：US020224
申请日：1979-03-13
申请人： Fumio Kai , Takashi Tsuruoka , Osamu Makabe , Shigeharu Inouye , Hitoshi Ikeda , Yuzo Kazuno , Shokichi Nakajima , Shigeo Seki , Taro Niida
发明人： Fumio Kai , Takashi Tsuruoka , Osamu Makabe , Shigeharu Inouye , Hitoshi Ikeda , Yuzo Kazuno , Shokichi Nakajima , Shigeo Seki , Taro Niida
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D501/56
CPC分类号： C07D501/36 , A61K31/545
摘要： Novel cephalosporin derivatives having formulae (V) and (III): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.8 and A are defined as in the specification.
摘要翻译：具有式（V）和（III）的新型头孢菌素衍生物：其中R 1，R 2，R 3，R 4，R 8和A如说明书中所定义。

35. 发明授权

US5250545A Cancer cell metastasis inhibitor methods 失效
标题翻译：癌细胞转移抑制剂方法
公开(公告)号：US5250545A
公开(公告)日：1993-10-05
申请号：US621699
申请日：1990-12-03
申请人： Tsutomu Tsuruoka , Satoru Nakabayashi , Harumi Fukuyasu , Yuuko Ishii , Takashi Tsuruoka , Haruo Yamamoto , Shigeharu Inouye , Shinichi Kondo
发明人： Tsutomu Tsuruoka , Satoru Nakabayashi , Harumi Fukuyasu , Yuuko Ishii , Takashi Tsuruoka , Haruo Yamamoto , Shigeharu Inouye , Shinichi Kondo
IPC分类号： A61K31/445 , C07D211/76 , C07D211/06 , A61K31/70
CPC分类号： C07D211/76 , A61K31/445
摘要： Sugar lactams such as N-(3-phenylpropyl)-1-deoxynojirimycin, 1-deoxynojirimycin, D-glucaro-.delta.-lactam, 6-O-triphenylmethyl-D-gluco-.delta.-lactam, etc., and new derivatives thereof which inhibit metastasis of cancer cells.
摘要翻译：糖内酰胺如N-（3-苯基丙基）-1-脱氧野尻霉素，1-脱氧野尻霉素，D-葡萄糖内酯-δ-内酰胺，6-O-三苯基甲基-D-葡萄糖-δ-内酰胺等，及其新衍生物抑制癌细胞的转移。

36. 发明授权

US4495358A Antibiotic pyrrolomycin E 失效
标题翻译：抗生素吡咯霉素E
公开(公告)号：US4495358A
公开(公告)日：1985-01-22
申请号：US438658
申请日：1982-11-02
申请人： Masao Koyama , Takashi Tsuruoka , Norio Ezaki , Keinosuke Miyauchi , Shigeharu Inouye
发明人： Masao Koyama , Takashi Tsuruoka , Norio Ezaki , Keinosuke Miyauchi , Shigeharu Inouye
IPC分类号： C07G11/00 , A61K35/74 , A61P31/04 , C07D207/42 , C12P1/06 , C12P17/10 , C12R1/465 , C07D205/10 , A61K31/40
CPC分类号： C12R1/465 , C07D207/42 , C12P17/10
摘要： Antibiotic, designated as pyrrolomycin E is described, and which is obtained by cultivating an pyrrolomycin E - producing strain belonging to the genus Streptomyces, for example, Streptomyces sp. SF-2080 (FERM-P No. 5072, ATCC No. 31673), in a nutrient medium, and recovering pyrrolomycin E from the culture which contains also other antibiotic substances (pyrrolomycin A, B, C and D) together with the desired substance.
摘要翻译：描述了称为吡罗美霉素E的抗生素，其是通过培养属于链霉菌属的吡罗马霉素E产生菌株，例如链霉菌属（Streptomyces sp。 SF-2080（FERM-P No.5072，ATCC No.31673）中，并在还含有其他抗生素物质（吡咯霉素A，B，C和D）的培养物中回收吡罗洛霉素E以及所需物质。

37. 发明授权

US4469643A Phosphorus-containing compounds and process for producing the same 失效
标题翻译：含磷化合物及其制备方法
公开(公告)号：US4469643A
公开(公告)日：1984-09-04
申请号：US550750
申请日：1983-11-10
申请人： Takashi Tsuruoka , Satoshi Imai , Atsuyuki Satoh , Tetsuro Watanabe , Koji Watanabe , Shigeharu Inouye , Taro Niida
发明人： Takashi Tsuruoka , Satoshi Imai , Atsuyuki Satoh , Tetsuro Watanabe , Koji Watanabe , Shigeharu Inouye , Taro Niida
IPC分类号： C07F9/48 , C07K5/08 , C12P13/04 , A61K31/13 , A61K31/66
CPC分类号： C07K5/0827 , C07F9/4816 , C12P13/04 , C12R1/465 , C12R1/55
摘要： Disclosed are compounds having the following general formula: ##STR1## wherein n is an integer of 1 or 2; R.sup.1 is an amino group when n is 2, or an amino group or a hydroxyl group when n is 1; and R.sup.2 is a hydroxyl group when n is 1, or a hydroxyl group or a group of the formula ##STR2## when n is 2; and microbiological process for producing the same. The compounds are useful as precursors for raising the production rate of SF-1293 substance. Some of the compounds are also useful as intermediates for synthesis of 2-amino-4-(hydroxy)(methyl)phosphinoylbutyric acid and the SF-1293 substance.

38. 发明授权

US4455163A Herbicidal compositions and herbicidal processes 失效
公开(公告)号：US4455163A
公开(公告)日：1984-06-19
申请号：US263454
申请日：1981-05-15
申请人： Tetsuo Takematsu , Makoto Konnai , Kunitaka Tachibana , Takashi Tsuruoka , Shigeharu Inouye , Tetsuro Watanabe
发明人： Tetsuo Takematsu , Makoto Konnai , Kunitaka Tachibana , Takashi Tsuruoka , Shigeharu Inouye , Tetsuro Watanabe
IPC分类号： A01N33/26 , A01N37/32 , A01N39/04 , A01N57/20 , A01P13/00 , C07F9/32 , A01N57/00 , A01N37/38
CPC分类号： A01N57/20
摘要： A known antibiotic, SF-1293 substance and salts thereof have now been found to exhibit high herbicidal effects against a wide variety of herbaceous and woody plants, but they are non-phytotoxic particularly to a useful woody plant, Chamaecyparis obtusa. The herbicidal effects of these SF-1293 substances can be noticeably enhanced by applying in combination with certain known herbicides or compounds having biological activities.

39. 发明授权

US4382812A Herbicidal compositions 失效
标题翻译：除草成分
公开(公告)号：US4382812A
公开(公告)日：1983-05-10
申请号：US68185
申请日：1979-08-20
申请人： Tetsuo Takematsu , Makoto Konnai , Kunitaka Tachibana , Takashi Tsuruoka , Shigeharu Inouye , Tetsuro Watanabe
发明人： Tetsuo Takematsu , Makoto Konnai , Kunitaka Tachibana , Takashi Tsuruoka , Shigeharu Inouye , Tetsuro Watanabe
IPC分类号： A01N57/20 , C07F9/30 , A01N57/12
CPC分类号： C07F9/301 , A01N57/20
摘要： 2-Amino-4-(hydroxy) (methyl)phosphinoylbutyric acid, which earlier nomenclature referred to as 2-amino-4-methylphosphinobutyric acid or its metal salts, or acid-addition salts thereof are used as perennial weeds and brush controlling agents. The L-isomer is twice effective than the racemic acid. The perennial weeds and brush controlling effect may be obtained by foliar application over a prolonged period and may be surprisingly enhanced by using the compound with a herbicide or synergist selected from the group consisting of choline salt of maleic hydrazide, a phenoxy series herbicide, a benzoic acid series herbicide, 2,3,6-trichlorophenylacetic acid or a salt thereof, (3,5,6-trichloro-2-pyridyl)oxyacetic acid or a salt thereof, N-phosphonomethylglycine or a salt thereof, ethylcarbamoylphosphoric acid or a salt thereof, 2-(1-allyloxyaminobutylidene)-5,5-dimethyl-4-methoxycarbonyl-cyclohexane-1,3-dione, 3-(3,4-dichlorophenyl)-1-methoxy-1-methylurea,3-amino-1,2,4-triazole, choline or a salt thereof, and diethylamine or a salt thereof.
摘要翻译： 2-氨基-4-（羟基）（甲基）膦酰基丁酸，其较早命名称为2-氨基-4-甲基膦酰基丁酸或其金属盐，或其酸加成盐用作多年生杂草和刷控制剂。 L-异构体比外消旋酸有效两倍。多年生杂草和刷子控制效果可以通过长时间的叶面施用获得，并且可以通过使用化合物与除草剂或增效剂来选择马来酰肼的胆碱盐，苯氧基系列除草剂，苯甲酸酸系除草剂，2,3,6-三氯苯乙酸或其盐，（3,5,6-三氯-2-吡啶基）氧基乙酸或其盐，N-膦酰甲基甘氨酸或其盐，乙基氨基甲酰基磷酸或其盐其中，2-（1-烯丙氧基氨基亚丁基）-5,5-二甲基-4-甲氧基羰基 - 环己烷-1,3-二酮，3-（3,4-二氯苯基）-1-甲氧基-1-甲基脲，3-氨基 -1,2,4-三唑，胆碱或其盐，以及二乙胺或其盐。

40. 发明授权

US4309208A Herbicidal compositions and herbicidal processes 失效
标题翻译：除草组合物和除草过程
公开(公告)号：US4309208A
公开(公告)日：1982-01-05
申请号：US959838
申请日：1978-11-13
申请人： Tetsuo Takematsu , Makoto Konnai , Kunitaka Tachibana , Takashi Tsuruoka , Shigeharu Inouye , Tetsuro Watanabe
发明人： Tetsuo Takematsu , Makoto Konnai , Kunitaka Tachibana , Takashi Tsuruoka , Shigeharu Inouye , Tetsuro Watanabe
IPC分类号： A01N57/20 , A01N57/00
CPC分类号： A01N57/20
摘要： A known antibiotic, SF-1293 substance and salts thereof have now been found to exhibit high herbicidal effects against a wide variety of herbaceous and woody plants, but they are non-phytotoxic particularly to a useful woody plant, Chamaecyparis obtusa. The herbicidal effects of these SF-1293 substances can be noticeably enhanced by applying in combination with certain known herbicides or compounds having biological activities.
摘要翻译：现已发现已知的抗生素SF-1293物质及其盐对各种草本植物和木本植物表现出高除草效果，但特别是对有用的木本植物Chamaecyparis obtusa而言是非植物毒性。通过与某些已知的具有生物活性的除草剂或化合物组合使用，可以显着提高这些SF-1293物质的除草效果。

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