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    Antibiotics SF-1771 substance and SF-1771-B substance as well as the production of these substances
    5.
    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。

    "> Antibiotic 9-acyl-3
    9.
    发明授权
    Antibiotic 9-acyl-3"-thiomethoxymethyl-SF-837 composition and process for preparing the same 失效
    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。

    "> 9-O-Alkanoyl-3
    10.
    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。