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31. 发明授权

US4466913A 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：US4466913A
公开(公告)日：1984-08-21
申请号：US388209
申请日：1982-06-14
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 , C07C103/52
CPC分类号： C07K5/0827 , C07F9/4816 , C12P13/04 , C12R1/465 , C12R1/55
摘要： 2-Amino-4-(hydroxy)phosphinoylbutyryl-L-alanyl-L-alanine.
摘要翻译： 2-氨基-4-（羟基）膦酰基丁酰基-L-丙氨酰-L-丙氨酸。

32. 发明授权

US4302580A Process for the production of a cephamycin derivative 失效
标题翻译：生产头孢霉素衍生物的方法
公开(公告)号：US4302580A
公开(公告)日：1981-11-24
申请号：US185594
申请日：1980-09-09
申请人： Katsuyoshi Iwamatsu , Jiro Itoh , Shoji Omoto , Takashi Tsuruoka , Shigeharu Inouye
发明人： Katsuyoshi Iwamatsu , Jiro Itoh , Shoji Omoto , Takashi Tsuruoka , Shigeharu Inouye
IPC分类号： C07D501/04 , C07D501/36 , C07D501/57 , C12P35/08
CPC分类号： C12P35/08
摘要： A chemotherapeutic, antibacterial agent, 7.beta.-[(2D-2-amino-2-carboxy)ethylthioacetamido]-7.alpha.-methoxy-3-[(1-methyl-1H-tetrazole-5-yl)thiomethyl]-3-cephem-4-carboxylic acid is produced economically and efficiently starting from cephamycin A and/or B by a "new route" process comprising the consecutive steps of reaction of cephamycin with 5-mercapto-1-methyl-1H-tetrazole; protection of the terminal amino group thereof by acylation; protection of the two carboxyl groups thereof by esterification; replacement of the acyl group initially having attached to the 7-amino group by a halogenoacetyl group; deprotection of the blocked 4-carboxyl group; and condensation of D-cysteine with the halogenoacetyl group attaching to the 7-amino group.
摘要翻译： 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- 头孢霉素-4-羧酸从头孢霉素A和/或B开始通过包含头孢霉素与5-巯基-1-甲基-1H-四唑的连续步骤的“新途径”方法经济有效地产生; 通过酰化保护其末端氨基; 通过酯化保护其两个羧基; 用卤代乙酰基取代最初连接在7-氨基上的酰基; 封闭的4-羧基脱保护; 和D-半胱氨酸与连接于7-氨基的卤代乙酰基缩合。

33. 发明授权

US4264532A Process for preparing D,L-2-amino-4-methylphosphinobutyric acid 失效
标题翻译：制备D，L-2-氨基-4-甲基膦酰基丁酸的方法
公开(公告)号：US4264532A
公开(公告)日：1981-04-28
申请号：US140198
申请日：1979-06-15
申请人： Takashi Tsuruoka , Akira Suzuki , Kunitaka Tachibana , Kazuko Mizutani , Yasuharu Sekizawa , Shigeharu Inouye , Tetsuo Takematsu
发明人： Takashi Tsuruoka , Akira Suzuki , Kunitaka Tachibana , Kazuko Mizutani , Yasuharu Sekizawa , Shigeharu Inouye , Tetsuo Takematsu
IPC分类号： A01N57/20 , C07F9/30 , C07F9/32
CPC分类号： C07F9/3211 , A01N57/20 , C07F9/301
摘要： PCT No. PCT/JP78/00058 Sec. 371 Date June 15, 1979 Sec. 102(e) Date June 15, 1979 PCT Field Dec. 18, 1978 PCT Pub. No. WO79/00405 PCT Pub. Date July 12, 1979This invention relates to a novel process for preparing D,L-2-amino-4-methylphosphinobutyric acid having herbicidal and antifungicidal activities which comprises subjecting acrolein to reaction with a dialkyl phosphonite to synthesize an acetal of an ester of 3-oxopropylmethylphosphinic acid; treating the thus obtained compound with an acid for deacetalization to obtain an ester of 3-oxopropylmethylphosphinic acid and then applying the Strecker's process used for amino synthesis to the thus obtained ester.
摘要翻译： PCT No.PCT / JP78 / 00058 Sec。 371日期1979年6月15日 102（e）日期1979年6月15日PCT领域1978年12月18日PCT公布。公开号WO79 / 00405 日期1979年7月12日本发明涉及一种具有除草和杀真菌活性的D，L-2-氨基-4-甲基膦酰基丁酸的新方法，该方法包括使丙烯醛与二烷基亚膦酸酯反应，合成3 - 氧代丙基甲基次膦酸用酸脱乙酰化处理得到的化合物，得到3-氧代丙基甲基次膦酸的酯，然后将用于氨基合成的斯特雷克氏法用于得到的酯。

34. 发明授权

US4220639A Antibiotics SF-2050 and SF-2050B substances and production and use thereof 失效
标题翻译：抗生素SF-2050和SF-2050B物质及其生产和使用
公开(公告)号：US4220639A
公开(公告)日：1980-09-02
申请号：US006873
申请日：1979-01-26
申请人： Kazunori Ohba , Chuhei Nojiri , Yasuaki Ogawa , Jiro Itoh , Kunikazu Totsugawa , Norio Ezaki , Takashi Shomura , Tomizo Niwa , Shigeharu Inouye , Yujiro Yamada
发明人： Kazunori Ohba , Chuhei Nojiri , Yasuaki Ogawa , Jiro Itoh , Kunikazu Totsugawa , Norio Ezaki , Takashi Shomura , Tomizo Niwa , Shigeharu Inouye , Yujiro Yamada
IPC分类号： C12N9/99 , C12P1/06 , C12D9/14 , A61K35/00
CPC分类号： C12N9/99 , C12P1/06 , Y10S435/886
摘要： New antibiotics, SF-2050 substance and SF-2050B substance are produced by cultivating a microorganism Streptomyces sp. SF-2050 now deposited under FERM-P 4358 and under ATCC. 31450 in a liquid culture medium under aerobic conditions, and these antibiotics may be isolated from the fermentation broth and useful as an antibacterial agent. These antibiotics have an activity inhibitory to .beta.-lactamase.
摘要翻译：新型抗生素SF-2050物质和SF-2050B物质是通过培养微生物Streptomyces sp。 SF-2050现在以FERM-P 4358和ATCC保藏。 31450在有氧条件下在液体培养基中，这些抗生素可以从发酵液中分离并用作抗菌剂。这些抗生素具有抑制β-内酰胺酶的活性。

35. 发明授权

US4189489A 5-Alkoxy-picolinic acid calcium salts and anti-hypertensive composition containing 5-alkoxy-picolinic acid calcium salts and anti-hypertensive composition thereof 失效
标题翻译：含有5-烷氧基 - 吡啶甲酸钙盐及其抗高血压组合物的5-烷氧基 - 吡啶甲酸钙盐和抗高血压组合物
公开(公告)号：US4189489A
公开(公告)日：1980-02-19
申请号：US838180
申请日：1977-09-30
申请人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
发明人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
IPC分类号： A61K31/44 , A61P9/12 , C07D213/65 , C07D213/79 , A61K31/445 , C07D213/89
CPC分类号： C07D213/79 , C07D213/65
摘要： 5-Alkoxy-picolinic acids and the salts and the esters thereof represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and M represents a hydrogen atom; a calcium atom; a sodium atom; a potassium atom; an aluminum atom; an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom); a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic acids and the salts and the esters thereof, and anti-hypertensive compositions containing the 5-alkoxy-picolinic acids and the salts and the esters thereof.
摘要翻译： 5-烷氧基 - 吡啶甲酸及其由式（I）表示的盐及其酯：其中R表示具有1至6个碳原子的烷基，M表示氢原子; 钙原子; 一个钠原子; 钾原子; 铝原子; 未取代的苯基; 被一个或多个具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基或卤素原子（例如氯，溴，碘等）原子取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 或具有式“IMAGE”的酰氧基烷基，其中R 2表示氢原子或甲基，R 3表示具有1至5个碳原子的烷基（例如甲基，正丙基，异丁基，叔丁基等），基团），具有1至4个碳原子的烷氧基，苯基，被一个或多个具有1至4个碳原子的烷基取代的苯基，具有1至4个碳原子的烷氧基或卤素原子（例如氯，溴，碘等原子）或其中烷基部分具有1至3个碳原子的芳烷基，其可用作抗高血压剂，制备5-烷氧基 - 吡啶甲酸的方法和其盐和酯，以及含有5-烷氧基 - 吡啶甲酸及其盐及其酯的抗高血压组合物。

36. 发明授权

US4029881A Antibiotic 9-acyl-3"-thiomethoxymethyl-SF-837 composition and process for preparing the same 失效
标题翻译：抗生素9-酰基-3 {41-甲氧基甲基-SF-837组合物及其制备方法
公开(公告)号：US4029881A
公开(公告)日：1977-06-14
申请号：US345752
申请日：1973-03-28
申请人： Shigeharu Inouye , Shoji Omoto , Taro Niida , Bunzo Nomiya
发明人： Shigeharu Inouye , Shoji Omoto , Taro Niida , Bunzo Nomiya
IPC分类号： A01N43/22 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08 , A01N43/22
摘要： A new derivative of the macrolide antibiotic SF-837 substance is manufactured by treating a 9,2'-diacyl- or 9-acyl-SF-837 composition with dimethylsulfoxide and acetic anhydride, and, subsequently, with an alcohol or water-containing solvent to yield the novel compound, 9-Acyl-3"-thiomethoxymethyl-SF-837 composition. In addition to high therapeutic effectiveness and low acute toxicity, this novel compound of the present invention has the great advantages that it does not have the bitter taste originally accompanying the parent compounds, and the further advantage that it is suitable for pediatric and veterinary use.
摘要翻译：通过用二甲基亚砜和乙酸酐处理9,2'-二酰基或9-酰基-SF-837组合物，然后用醇或含水溶剂来制备大环内酯类抗生素SF-837物质的新衍生物得到新的化合物9-酰基-3“ - 硫代甲氧基甲基-SF-837组合物。本发明的新型化合物除了具有高治疗效果和低急性毒性外，还具有不具有原始伴随母体化合物的苦味的优点，其优点在于适合于儿科和兽医用途。

37. 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。

38. 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。

39. 发明授权

US5190952A 4-acyloxyquinoline derivatives and insecticidal or acaricidal compositions containing same 失效
标题翻译： 4-氰基喹啉衍生物和含有它的杀虫剂或杀胡萝卜素组合物
公开(公告)号：US5190952A
公开(公告)日：1993-03-02
申请号：US549136
申请日：1990-07-05
申请人： Nobuto Minowa , Tomoya Machinami , Seiji Shibahara , Keiichi Imamura , Michiaki Iwata , Masaru Shimura , Shigeharu Inouye
发明人： Nobuto Minowa , Tomoya Machinami , Seiji Shibahara , Keiichi Imamura , Michiaki Iwata , Masaru Shimura , Shigeharu Inouye
IPC分类号： C07D215/22 , A01N43/42 , A01N47/06 , A01N53/00 , C07D215/233 , C07D215/56 , C07D219/06 , C07D405/12 , C07D409/12
CPC分类号： C07D215/233 , A01N43/42 , A01N47/06 , A01N53/00 , C07D215/56 , C07D219/06 , C07D405/12 , C07D409/12
摘要： A 4-acyloxyquinoline derivative represented by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.3 -C.sub.10 cycloalkyl which may be optionally substituted, phenylloweralkyl, phenoxyloweralkyl, aryl group, a group OR.sup.4, where R.sup.4 represents a lower alkyl or aryl group, or a group ##STR2## where X represents an oxygen or a sulphur atom; R.sup.2 represents a hydrogen atom, a lower alkyl alkyl group or a group --COOR.sup.5 where R.sup.5 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl or C.sub.2 -C.sub.10 alkenyl group, provided that R.sup.1 does not represent OR.sup.4 when R.sup.2 is a hydrogen atom and R.sup.3 is methyl; R.sup.2 and R.sup.3 together represent a group (CH.sub.2).sub.m, wherein m is 3 or 4, and W represents a hydrogen atom, 1 to 4 halogen atoms, a lower alkyl or lower alkoxy group which may be the same or different and with which the left-hand nucleus is substituted, provided that the compound wherein R.sup.1 represents methyl, R.sup.2, R.sup.3 and W each represent a hydrogen atom is excluded.

40. 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。

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