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    Antibiotics SF-1771 substance and SF-1771-B substance as well as the production of these substances
    3.
    发明授权
    Antibiotics SF-1771 substance and SF-1771-B substance as well as the production of these substances 失效
    抗生素SF-1771物质和SF-1771-B物质以及这些物质的生产

    公开(公告)号：US4169140A

    公开(公告)日：1979-09-25

    申请号：US736143

    申请日：1976-10-27

    申请人： Kazunori Ohba ,  Takashi Shomura ,  Hiroshi Watanabe ,  Kunikazu Totsukawa ,  Michio Kojima ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inoue ,  Taro Niida

    发明人： Kazunori Ohba ,  Takashi Shomura ,  Hiroshi Watanabe ,  Kunikazu Totsukawa ,  Michio Kojima ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inoue ,  Taro Niida

    IPC分类号： A61K35/74 ,  A61P31/04 ,  C07G11/00 ,  C12P1/06 ,  C12R1/465 ,  A61K35/00

    CPC分类号： C12P1/06

    摘要： A new antibiotic SF-1771 substance is produced by cultivating a new strain, Streptomyces toyocaensis SF-1771, in a liquid culture medium under aerobic conditions. This antibiotic may be isolated from the fermentation broth by treating the broth filtrate with a synthetic adsorbent resin for adsorption of the active compound and eluting the resin with an aqueous alcohol or aqueous acetone, followed by chromatographic purification. SF-1771 substance is a copper-containing antibiotic which shows antibacterial activity against Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis. Removal of the copper component from SF-1771 substance by treatment with hydrogen sulfide, an alkali metal sulfide or a copper-chelating agent gives SF-1771-B substance containing no copper component which shows antibacterial activity as high as but a toxicity lower than SF-1771 substance.

    摘要翻译： 通过在有氧条件下在液体培养基中培养新的菌株Streptomyces toyocaensis SF-1771来生产新的抗生素SF-1771物质。 通过用合成吸附剂树脂处理肉汤滤液以吸附活性化合物并用含水醇或丙酮水溶液洗脱树脂，然后进行色谱纯化，从发酵液中分离出该抗生素。 SF-1771物质是对大肠杆菌，伤寒沙门氏菌，铜绿假单胞菌，金黄色葡萄球菌和枯草芽孢杆菌具有抗菌活性的含铜抗生素。 通过用硫化氢，碱金属硫化物或铜螯合剂处理从SF-1771物质中除去铜成分得到不含铜成分的SF-1771-B物质，其抗菌活性高于但低于SF的毒性 -1771物质。

    "> 9,3
    8.
    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。

    "> 9-O-Alkanoyl-3
    9.
    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。