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206 条记录 (耗时 0.025 秒)

    1-N-isoserylkanamycins and the production thereof
    43.
    发明授权
    1-N-isoserylkanamycins and the production thereof 失效
    1-N-异辛基卡那霉素及其制备

    公开(公告)号：US3939143A

    公开(公告)日：1976-02-17

    申请号：US466053

    申请日：1974-05-01

    申请人： Hamao Umezawa ,  Kenji Maeda ,  Shinichi Kondo ,  Sumio Umezawa

    发明人： Hamao Umezawa ,  Kenji Maeda ,  Shinichi Kondo ,  Sumio Umezawa

    IPC分类号： C07H15/236 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： 1-N-isoseryl derivatives of kanamycin A, kanamycin B and 3',4'-dideoxykanamycin B are now synthesized, which are new and useful compounds active against gram-negative and gram-positive bacteria and also against drug-resistant strains of these bacteria. The production of the 1-N-isoserylkanamycins is made by reacting isoserine with the 1-N-amino group of kanamycin with the functional amino group(s) being protected, following by removal of the amino-protecting groups and by chromatographic separation of the desired 1-N-isoserylation product.

    摘要翻译： 现在合成了卡那霉素A，卡那霉素B和3'，4'-双脱氧卡那霉素B的1-N-异丝氨酰基衍生物，它们是对革兰氏阴性和革兰氏阳性细菌有活性的新的和有用的化合物，也是针对这些的抗药性菌株 菌。 通过使异丝氨酸与卡那霉素的1-N-氨基与被保护的官能氨基反应，然后除去氨基保护基，并通过色谱分离来制备1-N-异丝氨酰卡那霉素 所需的1-N-异山梨酰化产物。

    3',4'-Diedeoxykanamycin B derivatives
    44.
    发明授权
    3',4'-Diedeoxykanamycin B derivatives 失效
    3'，4'-脱氧卡那霉素B衍生物

    公开(公告)号：US4357465A

    公开(公告)日：1982-11-02

    申请号：US187014

    申请日：1980-09-15

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Shigeo Seki ,  Shunzo Fukatsu ,  Shuntaro Yasuda

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Shigeo Seki ,  Shunzo Fukatsu ,  Shuntaro Yasuda

    IPC分类号： C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.

    摘要翻译： 提供了用于合成3'，4'-双脱氧卡那霉素B的新途径，其通过新的中间体有效抑制卡那霉素B的卡那霉素抗性生物，其中基本方法包括3'，4'-环氧基 氨基和羟基保护的卡那霉素B与黄原酸酯的衍生物形成相应的3'，4'-二脱氧-3'-烯衍生物，然后除去其氨基和羟基保护基团，并通过氢化得到的3 '，4'-二脱氧-3'-烯 - 卡那霉素B.对应于3'，4'-环氧衍生物的3'，4'-环硫化物衍生物，其在3'，4' 含有黄原酸酯的环氧衍生物也用作制备3'，4'-双脱氧卡那霉素B的中间体。

    Novel macrolactone derivatives and process of producing them
    45.
    发明授权
    Novel macrolactone derivatives and process of producing them 失效
    新型大分子内酯衍生物及其制备方法

    公开(公告)号：US4255564A

    公开(公告)日：1981-03-10

    申请号：US75036

    申请日：1979-09-12

    申请人： Sumio Umezawa ,  Hamao Umezawa ,  Kuniaki Tatsuta

    发明人： Sumio Umezawa ,  Hamao Umezawa ,  Kuniaki Tatsuta

    IPC分类号： C07D313/00 ,  C07D407/06 ,  C07H15/04 ,  C07H17/08

    CPC分类号： C07H15/04 ,  C07D313/00 ,  C07D407/06 ,  C07H17/08

    摘要： By protecting the aldehyde group of a macrolide series antibiotics with a cyclic acetal or thioacetal, novel macrolide derivatives can be produced from the macrolide series antibiotics by releasing successively, the sugar moieties bonded to the macrolide antibiotics.The novel marcolide derivatives obtained by this invention, that is, the derivatives of a macrolide series antibiotics produced by releasing partially or wholly the sugar moieties bonded are useful as intermediates for producing novel macrolide series antibiotics.

    摘要翻译： 通过用环缩醛或硫缩醛保护大环内酯类抗生素的醛基，可以通过依次释放大环内酯类抗生素，与大环内酯类抗生素结合的糖部分，产生新型大环内酯衍生物。 通过本发明获得的新型海藻糖衍生物，即通过部分或全部释放部分键合产生的大环内酯类抗生素的衍生物，可用作生产新型大环内酯类抗生素的中间体。