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    Process for the production of a 7-methoxycephalosporine derivative
    1.
    发明授权
    Process for the production of a 7-methoxycephalosporine derivative 失效
    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。

    1-Oxadethiacephalosporin derivatives and antibacterial use thereof
    2.
    发明授权
    1-Oxadethiacephalosporin derivatives and antibacterial use thereof 失效
    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。

    Process for the production of a cephamycin derivative
    3.
    发明授权
    Process for the production of a cephamycin derivative 失效
    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。

    "> 9-O-Alkanoyl-3
    4.
    发明授权
    9-O-Alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance and the production thereof 失效
    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。

    5-Substituted picolinic acid derivatives and an anti-hypertensive composition containing the same
    5.
    发明授权
    5-Substituted picolinic acid derivatives and an anti-hypertensive composition containing the same 失效
    5-取代的吡啶甲酸衍生物和含有它们的抗高血压组合物

    公开(公告)号：US4229448A

    公开(公告)日：1980-10-21

    申请号：US23504

    申请日：1979-03-23

    申请人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

    发明人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

    IPC分类号： C07D213/65 ,  C07D213/79 ,  C07D213/81 ,  A61K31/455

    CPC分类号： C07D213/79 ,  C07D213/65 ,  C07D213/81

    摘要： 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.

    摘要翻译： 由式（I）表示的5-取代的吡啶甲酸衍生物：其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基： 其中可以相同或不同的R 3和R 4各自表示氢原子，卤素原子，低级烷基，低级烷氧基，硝基，氨基，N-烷基取代的氨基， 酰氨基，乙酰基，酰氧基，羟基或卤素取代的烷基，或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基，其中M表示氢，钠，钾，钙，铝或镁原子，具有1至6个碳原子的直链或支链或环状烷氧基，氨基烷氧基，苯氧基，取代的 苯氧基，5-茚满氧基，具有式“IMAGE”的酰氧基烷氧基，其中R5表示氢原子或甲基，R6表示碳原子数1〜6的低级烷基，苯基或取代苯基 或由式“IMAGE”表示的氨基，其中R7和R8可以相同或不同，表示可用作抗高血压剂的氢原子，低级烷基或苯基， 制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。

    Process for preparing D,L-2-amino-4-methylphosphinobutyric acid
    6.
    发明授权
    Process for preparing D,L-2-amino-4-methylphosphinobutyric acid 失效
    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。

    Azole derivatives and anti-ulcerative composition containing same
    8.
    发明授权
    Azole derivatives and anti-ulcerative composition containing same 失效
    唑衍生物和含有其的抗溃疡组合物

    公开(公告)号：US5200407A

    公开(公告)日：1993-04-06

    申请号：US716621

    申请日：1991-06-14

    申请人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Naoki Yamazaki ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Motohiro Nishio ,  Tomoya Machinami ,  Seiji Shibahara ,  Takashi Tsuruoka ,  Shigeharu Inouye

    发明人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Naoki Yamazaki ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Motohiro Nishio ,  Tomoya Machinami ,  Seiji Shibahara ,  Takashi Tsuruoka ,  Shigeharu Inouye

    IPC分类号： C07D471/04 ,  C07D498/04 ,  C07D513/04

    CPC分类号： C07D471/04 ,  C07D513/04

    摘要： Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which A, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represents a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-membered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integer from 0 to 2.

    摘要翻译： 通式（I）的化合物：其中A，B，C和D各自表示-CH =或-N =，条件是其中至少一个为 -N =; X表示-NH-，-O-或-S-; Y表示 - （CH 2）p - ，其中p是0至4的整数，-C（CH 3）2 - ， - CH 2 CH = CH - ， - CH 2 CO - ， - CF 2 - 或-CH 2 COCH 2 - R1表示氢原子，C1-4烷基，卤素原子或C1-4烷氧基; R2表示氢原子，羟基，饱和或不饱和的C1-6烷基，C1-6烷氧基，羧基，可以任意取代的饱和或不饱和的C 1-12烷氧基羰基，环烷氧基羰基， 含有至少一个氮原子的饱和或不饱和五元或六元杂环基，任选具有一个或多个氮和/或氧原子，其可以任选地被缩合和/或取代，-CONR 3 R 4，-NR 3 R 4，-OCOR 3或 - NHCONHR 3其中R3和R4可以相同或不同，表示可以被任意取代的C 1-6烷基或环烷基，m和n各自表示0〜2的整数。