利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

206 条记录 (耗时 0.023 秒)

    Process for production of anthracycline compound R20X2
    65.
    发明授权
    Process for production of anthracycline compound R20X2 失效
    生产蒽环类化合物R20X2的方法

    公开(公告)号：US4855414A

    公开(公告)日：1989-08-08

    申请号：US68627

    申请日：1987-06-30

    申请人： Hamao Umezawa ,  Atsuo Odagawa ,  Shiro Kataoka ,  Shohachi Nakajima

    发明人： Hamao Umezawa ,  Atsuo Odagawa ,  Shiro Kataoka ,  Shohachi Nakajima

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252

    CPC分类号： C07H15/252

    摘要： An anthracycline compound, R20X2, of the following formula (II) is produced by a process which comprises subjecting an anthracycline compound, R20X3, of the following formula (I) or a salt thereof to reaction in the co-presence of (1) acetone and/or dimethylformamide and (2) an aqueous solution containing ammonium ion and/or trialkylamine. ##STR1## The anthracycline compound, R20X2, can be produced not only by the cultivation of actinomycetes but also, in accordance with the process as shown above, by chemical conversion of the anthracycline compound, R20X3, in a high yield.

    摘要翻译： 通过以下方法制备下式（II）的蒽环类化合物R20X2：将下式（I）的蒽环类化合物R20X3或其盐在（1）丙酮共存下进行反应 和/或二甲基甲酰胺和（2）含有铵离子和/或三烷基胺的水溶液。 （II）蒽环类化合物R20X2不仅可以通过放线菌的培养产生，而且可以根据上述方法通过蒽环类化合物R20X3的化学转化产生， 以高收益。

    N-Methanesulfonic acid derivatives of 3-demethoxyistamycin B
    66.
    发明授权
    N-Methanesulfonic acid derivatives of 3-demethoxyistamycin B 失效
    N-脱甲氧基霉素B的N-甲磺酸衍生物

    公开(公告)号：US4567165A

    公开(公告)日：1986-01-28

    申请号：US608213

    申请日：1984-05-08

    申请人： Hamao Umezawa ,  Shinichi Kondo

    发明人： Hamao Umezawa ,  Shinichi Kondo

    IPC分类号： C07H15/224 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/224

    摘要： As new semi-synthetic antibiotic derivatives are provided N-methanesulfonic acid derivatives of 3-demethoxyistamycin B which are less toxic than the parent 3-demethoxyistamycin B but retain usefully high antibacterial activity of the parent antibiotic. The new derivatives are produced by a method of N-sulfomethylation where 3-demethoxyistamycin B is reacted with an aldehyde such as paraformaldehyde and sulfurous acid or sulfite reagent.

    摘要翻译： 由于新的半合成抗生素衍生物提供3-脱甲氧基霉素B的N-甲磺酸衍生物，其比亲本3-脱甲氧基霉素B毒性低，但保留了有效的抗生素抗菌活性。 新衍生物通过N-甲基磺酰化方法制备，其中3-脱甲氧基霉素B与醛如多聚甲醛和亚硫酸或亚硫酸盐试剂反应。

    Anthracycline compounds
    68.
    发明授权
    Anthracycline compounds 失效
    蒽环类化合物

    公开(公告)号：US4550159A

    公开(公告)日：1985-10-29

    申请号：US545137

    申请日：1983-10-25

    申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Takeshi Uchida ,  Masaya Imoto

    发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Hiroshi Naganawa ,  Tsutomu Sawa ,  Takeshi Uchida ,  Masaya Imoto

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252 ,  C12P19/56 ,  C12R1/465 ,  A61K31/71 ,  C07H15/24

    CPC分类号： C07H15/252 ,  C12P19/56 ,  C12R1/465

    摘要： An anthracycline compound, ditrisarubicin, of the formula: ##STR1## wherein R represents one of the following substituents (A), (B), and (C): ##STR2## is produced by a process which comprises cultivating a strain of Streptomyces in a suitable culture medium under aerobic conditions, said strain having the ability to produce the anthracycline compound, ditrisarubicin, and then recovering the anthracycline compound, ditrisarubicin, from the cultured medium. This ditrisarubicin, or an acid addition salt of the ditrisarubicin, can be contained as the active ingredient in antitumor agents and in pharmaceutical compositions for treatment of infections induced by gram-positive microorganisms, whereby good results are attainable.

    摘要翻译： 其中R代表以下取代基之一（A），（B）和（C）的蒽环类化合物，二硝基菌素：其中R代表下列取代基之一：（A） C）是通过包括在有氧条件下在合适的培养基中培养链霉菌菌株的方法生产的，所述菌株具有生产蒽环类化合物，二硝酸菌素的能力，然后从培养基中回收蒽环类化合物二硝酸菌素。 这种二硝维菌素或二硝基阿霉素的酸加成盐可以作为活性成分包含在抗肿瘤剂和用于治疗由革兰氏阳性微生物诱导的感染的药物组合物中，从而获得良好的结果。

    3-O-Demethyl derivatives of the istamycin B series of compounds
    70.
    发明授权
    3-O-Demethyl derivatives of the istamycin B series of compounds 失效
    伊曲霉素B系列化合物的3-O-去甲基衍生物

    公开(公告)号：US4499083A

    公开(公告)日：1985-02-12

    申请号：US298844

    申请日：1981-09-03

    申请人： Hamao Umezawa ,  Yoshiro Okami ,  Shinichi Kondo

    发明人： Hamao Umezawa ,  Yoshiro Okami ,  Shinichi Kondo

    IPC分类号： C12P19/48 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/00 ,  C07H15/224 ,  C12R1/465 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/224 ,  Y02P20/55

    摘要： New derivatives of the istamycin B series of compounds are provided, which are 3-O-demethylistamycin B.sub.O, 3-O-demethylistamycin B and 3-O-demethyl-2"-N-formimidoylistamycin B represented generally by Formula I or specifically by Formulae Ia, Ib and Ic, respectively. Compound Ia is useful as an intermediate for the preparation of Compounds Ib and Ic and the latter two compounds exhibit a high antibacterial activity against a wide variety of Gram-positive and Gram-negative bacteria and are useful antibiotics. Also provided are processes for the preparation of the new derivatives starting from istamycin B.sub.O.

    摘要翻译： 提供了伊曲霉素B系列化合物的新衍生物，它们是通常由式I表示的3-O-脱甲基霉素B B，3-O-脱甲基霉素B和3-O-脱甲基-2'-N-甲亚氨基硫杆菌素B. 式Ia，Ib和Ic。 化合物Ia可用作制备化合物Ib和Ic的中间体，后两种化合物对各种革兰氏阳性和革兰氏阴性细菌表现出高抗菌活性，并且是有用的抗生素。 还提供了从伊曲霉素BO开始制备新衍生物的方法。