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    "> Antibiotic 9-acyl-3
    7.
    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
    8.
    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。