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    "> 9-O-Alkanoyl-3
    3.
    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。

    "> 9,3
    4.
    发明授权
    9,3",4"-Triacyl ester of the antibiotic SF-837 M.sub.1 substance and the production thereof 失效
    9,3 {41,4 {41-抗生素SF-837M {HD 1 {B物质及其制备的三

    公开(公告)号：US4017607A

    公开(公告)日：1977-04-12

    申请号：US597188

    申请日：1975-07-18

    申请人： Shigeharo Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Taro Niida ,  Toyoaki Kawasaki

    发明人： Shigeharo Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Taro Niida ,  Toyoaki Kawasaki

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： As new compounds are provided 9,3",4"-trialkanoyl SF-837 M.sub.1 substances which have therapeutically useful antibacterial activity and do not show any objectionable long-lasting bitter taste upon its oral administration. These 9,3",4"-trialkanoyl SF-837 M.sub.1 substances may be prepared from SF-837 substance, 9,2',3"-tri-acetyl SF-837 M.sub.1 substance, 9,2'-di-acetyl SF-837 substance, 9-propionyl SF-837 substance or 9,2'-dipropionyl SF-837 substance by acylating the latter with an alkanoic acid anhydride at 50.degree.-120.degree. C to produce the corresponding 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and occasionally the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance, with involving the shift of the 4"-alkanoyl group to the 3"-hydroxyl group. Partial and selective hydrolysis of the 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and/or the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance so produced gives the desired 9,3",4"-tri-alkanoyl SF-837 M.sub.1 substance.

    摘要翻译： 当新化合物被提供具有治疗上有用的抗菌活性的9,3“，4” - 三烷酰基SF-837M1物质，并且在其口服给药时不显示任何令人不快的持久苦味。 这些9,3“，4” - 三烷酰基SF-837 M1物质可以由SF-837物质，9,2'，3“ - 三乙酰基SF-837M1物质，9,2'-二 - 乙酰基SF-837物质，9-丙酰基SF-837物质或9,2'-二丙酰基SF-837物质，通过用烷基酸酐在50°-120℃下酰化后者，产生相应的9,2' 3“，4” - 四烷酰基SF-837 M1物质，偶尔有9,18,2'，3“，4” - 五烷酰基SF-837 M1物质，涉及4 “ - 烷酰基与3” - 羟基。 9,2'，3“，4” - 四烷酰基SF-837 M1物质和/或9,18,2'，3“，”4“ - 五烷酰基SF- 837如此生产的M1物质得到所需的9,3“，”4“ - 三烷酰基SF-837 M1物质。

    Process for the production of a cephamycin derivative
    5.
    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。

    Cephalosporin derivatives
    7.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4785090A

    公开(公告)日：1988-11-15

    申请号：US704077

    申请日：1985-02-21

    申请人： Takashi Tsuruoka ,  Seiji Shibahara ,  Katsuyoshi Iwamatsu ,  Tsuneo Okonogi ,  Satoru Nakabayashi ,  Yasushi Murai ,  Hiroko Ogino ,  Kiyoaki Katano ,  Takashi Yoshida ,  Shigeharu Inoue ,  Shunzo Fukatsu ,  Shinichi Kondo

    发明人： Takashi Tsuruoka ,  Seiji Shibahara ,  Katsuyoshi Iwamatsu ,  Tsuneo Okonogi ,  Satoru Nakabayashi ,  Yasushi Murai ,  Hiroko Ogino ,  Kiyoaki Katano ,  Takashi Yoshida ,  Shigeharu Inoue ,  Shunzo Fukatsu ,  Shinichi Kondo

    IPC分类号： C07D213/64 ,  C07D213/68 ,  C07D221/04 ,  C07D501/36 ,  C07D501/38 ,  A61K31/545

    CPC分类号： C07D221/04 ,  C07D213/64 ,  C07D213/68

    摘要： This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.

    摘要翻译： 这是一类具有下式的抗菌化合物：其中Y是直链或支链烷基或烯基链，3-6个碳原子的环烷基甲基，每个基团任选被卤素取代，或基团< 其中n为0或1-3的整数，A为基团-COR 3，其中R 3为羟基，其中R 4和R 5可以相同或不同，为氢或1-5碳的烷基 原子，基团或含有氮和/或硫的5-或6-元杂环基，R 1和R 2可以相同或不同，为氢，1-5个碳原子的烷基或R1 并且R 2可以组合在一起形成3-5个碳原子的亚烷基，Z是下式的基团：其中m是0或3-5的整数，R6是氢或1-3个碳的烷基 原子和R 7，当m是3-5的整数时，是1-5个碳原子的烷基，烯基，环丙基，基团 - （CH 2）pB，其中p是0或1-3的整数，B是氨基 ，烷基取代的氨基 羟基，羧基，氨基甲酰基，三氟甲基，磺酸，磺酸酰胺，烷硫基或氰基，或当m为0时，其为1-5个碳原子的烷基，其可任选被卤素，链烯基，基团 其中R8是氢，1-4个碳原子的烷基或苯基，或环丙基及其盐。

    7.alpha.Methoxycephalosporin derivatives
    8.
    发明授权
    7.alpha.Methoxycephalosporin derivatives 失效
    7α甲氧头孢菌素衍生物

    公开(公告)号：US4357331A

    公开(公告)日：1982-11-02

    申请号：US104220

    申请日：1979-12-17

    申请人： Katsuyoshi Iwamatsu ,  Shigeharu Inoue ,  Keinosuke Miyauchi ,  Shinichi Kondo ,  Shigeo Seki ,  Yujiro Yamada

    发明人： Katsuyoshi Iwamatsu ,  Shigeharu Inoue ,  Keinosuke Miyauchi ,  Shinichi Kondo ,  Shigeo Seki ,  Yujiro Yamada

    IPC分类号： A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/36 ,  C07D501/40 ,  C07D501/57 ,  C07D501/60

    CPC分类号： C07D501/57

    摘要： A 7.alpha.-methoxycephalosporin derivative represented by the formula (I): ##STR1## wherein R.sub.1 represents a heterocyclic ring or an --S-- heterocyclic ring; R.sub.2 represents a hydrogen atom, a carboxy group or a --COOR.sub.5 group wherein R.sub.5 represents a lower alkyl group, a dialkylamino-lower alkyl group or a ##STR2## group wherein R.sub.6 represents a lower alkyl group, a lower acyl group or a lower alkoxycarbonyl group and Y represents a hydrogen atom or a lower alkyl group; R.sub.3 represents a hydrogen atom, a carbamoyl group or a lower acyl group; R.sub.4 represents a hydrogen atom, a lower alkyl group, a dialkylamino-lower alkyl group or a ##STR3## group wherein R.sub.6 and Y are defined as above; A and B, which may be the same or different, each represents a straight chain or branched chain alkylene group having 1 to 5 carbon atoms; and x represents 0 or 1; or a pharmaceutically acceptable salt thereof and a process for producing the same.

    摘要翻译： 由式（I）表示的7α-甲氧头孢菌素衍生物：其中R 1表示杂环或-S-杂环; R2表示氢原子，羧基或-COOR5基团，其中R5表示低级烷基，二烷基氨基 - 低级烷基或其中R6表示低级烷基，低级酰基或低级烷氧基羰基 基团，Y表示氢原子或低级烷基; R3表示氢原子，氨基甲酰基或低级酰基; R4表示氢原子，低级烷基，二烷基氨基 - 低级烷基或基团，其中R6和Y如上定义; A和B可以相同或不同，各自表示具有1至5个碳原子的直链或支链亚烷基; x表示0或1; 或其药学上可接受的盐及其制备方法。

    Serotonin 5-HT3 receptor partial activator
    9.
    发明授权
    Serotonin 5-HT3 receptor partial activator 失效
    5-羟色胺5-HT3受体部分激活剂

    公开(公告)号：US06867226B2

    公开(公告)日：2005-03-15

    申请号：US10219496

    申请日：2002-08-16

    申请人： Yasuo Sato ,  Megumi Yamada ,  Kazuko Kobayashi ,  Katsuyoshi Iwamatsu ,  Fukio Konno ,  Koichi Shudo

    发明人： Yasuo Sato ,  Megumi Yamada ,  Kazuko Kobayashi ,  Katsuyoshi Iwamatsu ,  Fukio Konno ,  Koichi Shudo

    IPC分类号： A61K31/42 ,  A61K31/423 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/55 ,  A61K31/5513 ,  A61P1/00 ,  A61P1/08 ,  A61P1/12 ,  A61P1/14 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D263/30 ,  C07D263/58 ,  C07D263/60 ,  C07D413/04 ,  A61K31/50

    CPC分类号： C07D263/58 ,  A61K31/496 ,  C07D263/30 ,  C07D413/04

    摘要： This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect.Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.

    摘要翻译： 本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂，并且不引起便秘作为副作用。特别地，基于以下发现： 以下式（2）化合物为代表的新合成苯并恶唑衍生物具有强烈的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体激活作用，本发明提供了这些苯并恶唑衍生物作为5-羟色胺5-HT 3受体部分活化剂。 式中，R 1〜R 4可以相同或不同，表示氢原子，卤素原子，取代或未取代的低级烷基，取代或未取代的低级烯基或取代或未取代的氨基，或二 R1和R2的基团可以连接在一起形成环结构，即苯环; R5表示氢原子，取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。