公开(公告)号：US4552583A

公开(公告)日：1985-11-12

申请号：US420929

申请日：1982-09-21

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，并且通过使用化合物与除草剂或增效剂，选自马来酰肼的胆碱盐，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。

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。

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。

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。

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。

公开(公告)号：US4083850A

公开(公告)日：1978-04-11

申请号：US700340

申请日：1976-06-28

申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

IPC分类号： C07D213/79 ,  C07D213/55

CPC分类号： C07D213/79

摘要： Novel compounds useful as hypotensive agents are presented having the general formula I ##STR1## wherein R.sub.1 represents a lower aliphatic acyl group, a straight or branched chain alkyl or alkenyl group or an aralkyl group of the general formula ##STR2## wherein R.sub.2 represents hydrogen, a lower alkyl group or a halogen atom. Furthermore, new therapeutic compositions of matter are also described incorporating the above novel 3-substituted-2(1H)pyridone-6-carboxylic acids (I) as an active ingredient with carriers and showing uses as hypotensive agents. These new compounds of the formula I are prepared either by reacting D-glucaro-.delta.-lactam or its salt with an acid anhydride or by reacting 3-hydroxy-2(1H)pyridone-6-carboxylic acid with an acyl anhydride or alkyl halide, aralkyl halide and an alkenyl halide.

摘要翻译： 提供了可用作降压剂的新型化合物，其具有通式I（I），其中R 1表示低级脂族酰基，直链或支链烷基或烯基或通式为“IMAGE”的芳烷基，其中R 2 表示氢，低级烷基或卤素原子。 此外，还描述了新型的物质治疗组合物，其结合上述新型3-取代-2（1H）吡啶酮-6-羧酸（I）作为活性成分与载体并用作降压剂。 式I的这些新化合物通过D-葡聚糖-δ-内酰胺或其盐与酸酐反应或通过使3-羟基-2（1H）吡啶酮-6-羧酸与酰基酸酐或烷基卤化物 芳烷基卤化物和烯基卤化物。

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。

公开(公告)号：US06417362B1

公开(公告)日：2002-07-09

申请号：US09424708

申请日：1999-11-30

申请人： Naoto Ohkura ,  Takashi Tsuruoka ,  Takayuki Usui ,  Yukiko Hiraiwa ,  Tetsuya Matsushima ,  Masaharu Shiotani ,  Tetsutaro Niizato ,  Yuuko Nakatani ,  Shigeki Suzuki ,  Chidsuko Kuroda ,  Kiyoaki Katano

发明人： Naoto Ohkura ,  Takashi Tsuruoka ,  Takayuki Usui ,  Yukiko Hiraiwa ,  Tetsuya Matsushima ,  Masaharu Shiotani ,  Tetsutaro Niizato ,  Yuuko Nakatani ,  Shigeki Suzuki ,  Chidsuko Kuroda ,  Kiyoaki Katano

IPC分类号： C07D24104

CPC分类号： C07D409/12 ,  C07D209/46 ,  C07D217/24 ,  C07D265/22 ,  C07D279/08 ,  G03F7/2049 ,  Y10S977/915

摘要： Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia. wherein A represents group —CR1R2—(CH2)i— where R1 and R2 each represent a hydrogen atom or alkyl, —CH═CH—, —O—CH2—, or —S(O)j—CH2—; B represents a hydrogen or halogen atom; X represents —CR3R4R5, —NR6R7, —(CH2—CH═C(CH3)—CH2)p—CH2CH═C(CH3)2, alkyl, cycloalkyl, phenyl, cinnamyl, or heteroaromatic ring; Y represents —(CH2)q—, —CH═CH—, —NR8—, an oxygen atom, or a bond; Z represents carbonyl or a bond; K represents alkylene or a bond; L represents —CH═CH— or a bond; and M represents a hydrogen atom, alkyl, cycloalkyl, phenyl, heterocyclic ring, biphenyl, or diphenylmethyl.

摘要翻译： 公开了由式（I）表示的化合物及其药学上可接受的盐和溶剂化物。 该化合物可以抑制肝脏中甘油三酯的生物合成，并可以抑制含有载脂蛋白B的脂蛋白从肝脏的分泌。 因此，它们可用于预防或治疗由高脂血症引起的高脂血症（特别是超低密度脂蛋白血症）和动脉硬化疾病如心肌梗死或胰腺炎。其中A代表基团-CR1R2-（CH2）i - 其中R1和R2各自表示氢原子或烷基，-CH = CH-，-O-CH2-或-S（O）j-CH2-; B表示氢或卤素原子; X代表-CR3R4R5，-NR6R7， - （CH2-CH = C（CH3）-CH2）p-CH2CH = C（CH3）2，烷基，环烷基，苯基，肉桂基或杂芳族环; Y表示 - （CH 2）q - ， - CH = CH - ， - NR 8 - ，氧原子或键; Z表示羰基或键; K表示亚烷基或键; L表示-CH = CH-或键; M代表氢原子，烷基，环烷基，苯基，杂环，联苯基或二苯基甲基。

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。

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。