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    Substances having antibiotic activity, processes for their preparation, pharmaceutical compositions containing them, their use in medicaments and microorganisms
    3.
    发明公开
    Substances having antibiotic activity, processes for their preparation, pharmaceutical compositions containing them, their use in medicaments and microorganisms 失效
    具有物质的抗菌活性，它们的制备方法，药物组合物含有它们，它们在医药和微生物的用途。

    公开(公告)号：EP0029309A1

    公开(公告)日：1981-05-27

    申请号：EP80303807.4

    申请日：1980-10-27

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Tomita, Fusao ,  Tamaoki, Tatsuya ,  Shirahata, Kunikatsu ,  Iida, Takao ,  Morimoto, Makoto ,  Fujimoto, Kazuhisa

    IPC分类号： A61K35/66 ,  C12P1/06 ,  C07G11/00

    CPC分类号： C12R1/465 ,  C12P1/06

    摘要： Substances having respectively an elemental analysis of C:55.11%; H:5.74%, a molecular weight of 864-958 a melting point of 180±3°C (decomp); an elemental analysis of C:54.20%; H:6.15%, a molecular weight of 826-1004 and a melting point of 193-194°C (decomp); and an elemental analysis of C:54.34%, H:6.03%, a molecular weight of 822-960 and a melting point of 181-182°C (decomp), have been found to possess antibiotic activity. These substances have been prepared by culturing microorganisms of the genus Streptomyces. A preferred strain is Streptomyces ochraceus DC-45 (FERM-P No. 5219 NRRL 12051). The substances have a pale yellowish colour, have activity against Bacillus subtilis No. 10707 and are soluble in methanol, ethanol and chloroform and insoluble in n-hexane. These substances are of potential interest as medicaments for use against bacteria such as Bacillus subtilis No.10707 and for use as anti-tumour agents.

    摘要翻译： 分别具有C个的元素分析的物质：55.11％; H：5.74％，的864-958的180 +/- 3℃（分解）的熔点的分子量; 的的C元素分析：54.20％; H：6.15％，826的分子量为1004和193-194℃（分解）的熔点 和至C的元素分析：54.34％，H：6.03％，的一个822-960分子量和181-182℃（分解）的熔点，已被发现具有抗菌活性。 这些物质已经制备通过培养链霉菌属的微生物。 优选的菌株是链霉菌赭DC-45（FERM-P 5219号NRRL 12051）。 该物质具有浅黄色颜色，具有对抗枯草芽孢杆菌活动号 10707和可溶于甲醇，乙醇和氯仿，不溶于正己烷。 这些物质是潜在的利益作为药物用于对抗细菌的使用：如枯草芽孢杆菌号 10707和用作抗肿瘤剂。

    Antibiotic compounds, pharmaceutical compositions containing such compounds, process for production thereof
    4.
    发明公开
    Antibiotic compounds, pharmaceutical compositions containing such compounds, process for production thereof 失效
    抗生素化合物，它们的药物组合物和它们的制备方法。

    公开(公告)号：EP0042172A1

    公开(公告)日：1981-12-23

    申请号：EP81104619.2

    申请日：1981-06-15

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Tomita, Fusao ,  Tamaoki, Tatsuya ,  Shirahata, Kunikatsu ,  Kasai, Masaji ,  Hirayama, Noriaki ,  Morimoto, Makoto ,  Fukui, Masanori

    IPC分类号： C07D407/12 ,  C12P17/16 ,  C12P19/60 ,  C07H17/04 ,  A61K31/365

    CPC分类号： C07H17/08 ,  C07D307/60 ,  C07H15/26 ,  C12P17/162 ,  C12P19/60 ,  C12R1/30

    摘要： Antibacterial tetronolide compounds F-1 and F-2 are produced by fermentation of a microorganism belonging to the genus Micromonospora. The antibiotics F-1 and F-2 are accumulated in the culture liquor and are isolated therefrom, respectively. The acyl derivatives of F-1 and F-2, that is F-1-21-0 acetate, F-1-21-0 propionate, F-1-21-0-n butylate, F-1 diacetate, F-1 dipropionate, F-2 triacetate, F-2 tripropionate and F-2 tri-n-butylate, etc., are chemically synthesized from F-1 and F-2, respectively (Fig. 1).
    Their formula :
    wherein R 1 and R 2 may be the same or different substituents and represent a hydrogen atom or an acyl group and R 3 represents a hydrogen atom, an acyl group or a tetronitrose represented by the formula (2)
    and the pharmaceutically acceptable salts thereof.

    摘要翻译： Antibacteriai tetronolide化合物F-1和F-2是由属于埃希孢微生物的发酵生产。 抗生素的F-1和F-2被累积在培养液和从分别分离在那里。 F-1和F-2的酰基衍生物F-确实是1-21-0乙酸，丙酸F-1-21-0，1-21-0 F-Ñ丁醇，F-1二乙酸，F- 1个二丙酸酯，F-2三乙酸酯，F-2和F-2三丙三正丁醇等，从化学F-1和F-2分别合成。 ... 他们的公式：... ...