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    Antibiotic FR-900129 substance, a process for the preparation thereof and pharmaceutical compositions containing the same
    3.
    发明授权
    Antibiotic FR-900129 substance, a process for the preparation thereof and pharmaceutical compositions containing the same 失效
    抗生素FR-900129物质，其制备方法和含有它们的药物组合物

    公开(公告)号：US4313935A

    公开(公告)日：1982-02-02

    申请号：US125486

    申请日：1980-02-28

    申请人： Tadaaki Komori ,  Michio Yamashita ,  Eiko Iguchi ,  Masanobu Kohsaka ,  Hatsuo Aoki ,  Hiroshi Imanaka

    发明人： Tadaaki Komori ,  Michio Yamashita ,  Eiko Iguchi ,  Masanobu Kohsaka ,  Hatsuo Aoki ,  Hiroshi Imanaka

    IPC分类号： C07G11/00 ,  C12P1/06 ,  C12R1/465 ,  A61K35/00 ,  C12P13/00

    CPC分类号： C12R1/465 ,  C12P1/06 ,  Y10S435/886

    摘要： Prodn. of FR-900129 comprises culturing a Streptomyces n. 4012 category which is analogous to Streptomyces misakiensis and Steptomyces aburaviensis, i.e. Streptomyces avellaneus No. 4012, at 25.degree. C. to 30.degree. C. during 50 to 100 hours in a culture medium which consists of a carbon source (e.g. glucose, fructose, glycerin, starch, galactose, maltose, dextrin), an organic or inorganic nitrogen source (e.g. yeast extract, peptone, cottonseed cake, soyabean powder, cornsteep liquor, dry yeast, ammonium nitrate, ammonium sulphate, ammonium phosphate, urea and amino acid) and an inorganic salt (e.g. calcium carbonate, sodium phosphate, potassium phosphate, sodium chloride, potassium chloride, magnesium salt and copper salt). The produced FR-900129 is isolated by a collecting step, a purifying step, a vacuum condensation step, a freeze-drying step, a pH adjusting step, a cationic, anionic or nonionic resin treating step, an active carbon adsorption step and a crystallizing and recrystallizing step. The isolated material may then be converted to its adduct salt or its ester conventionally.

    摘要翻译： 产品 的FR-900129包括培养Streptomyces n。 4012类似于Streptomyces misakiensis和Steptomyces aburaviensis（即Streptomyces avellaneus No.4012），在25℃至30℃下在50至100小时内在由碳源（例如葡萄糖，果糖， 甘油，淀粉，半乳糖，麦芽糖，糊精），有机或无机氮源（例如酵母提取物，蛋白胨，棉籽饼，大豆粉，玉米浸液，干酵母，硝酸铵，硫酸铵，磷酸铵，尿素和氨基酸） 和无机盐（例如碳酸钙，磷酸钠，磷酸钾，氯化钠，氯化钾，镁盐和铜盐）。 生产的FR-900129通过收集步骤，纯化步骤，真空冷凝步骤，冷冻干燥步骤，pH调节步骤，阳离子，阴离子或非离子树脂处理步骤，活性炭吸附步骤和结晶 和重结晶步骤。 然后可以将分离的材料通常转化为其加合物盐或其酯。

    Method of treating tumors using tetracyclo compounds
    5.
    发明授权
    Method of treating tumors using tetracyclo compounds 失效
    使用四环化合物治疗肿瘤的方法

    公开(公告)号：US4861774A

    公开(公告)日：1989-08-29

    申请号：US947759

    申请日：1986-12-30

    申请人： Masanobu Kohsaka ,  Hiroshi Terano ,  Tadaaki Komori ,  Morita Iwami ,  Michio Yamashita ,  Masashi Hashimoto ,  Itsuo Uchida ,  Shigehiro Takase

    发明人： Masanobu Kohsaka ,  Hiroshi Terano ,  Tadaaki Komori ,  Morita Iwami ,  Michio Yamashita ,  Masashi Hashimoto ,  Itsuo Uchida ,  Shigehiro Takase

    IPC分类号： A61K31/535 ,  A61P31/04 ,  A61P35/00 ,  C07D498/18 ,  C12P17/18 ,  C12R1/465

    CPC分类号： C07D498/18 ,  C12P17/188 ,  C12R1/465 ,  Y02P20/55

    摘要： The invention relates to a method for treatment of carcinoma or sarcoma tumor in mammals which comprises administering to said mammal an effective amount of a tetracyclo compound of the formula: ##STR1## in which R.sup.1 is formyl, protected formyl, hydroxymethyl, protected hydroxymethyl, arylaminomethyl, carboxy, protected carboxy, aryliminomethyl, hydroxyiminomethyl, alkoxyiminomethyl, acyloxyiminomethyl, semicarbazonomethyl or arylsemicarbazonomethyl,R.sup.2 is hydroxy, alkoxy, or protected hydroxy,R.sup.3 is hydrogen and R.sup.4 is methyl, hydroxymethyl or protected hydroxymethyl, orR.sup.3 and R.sup.4 are combined together to form methylene or oxo,R.sup.5 is hydroxy, alkoxy or protected hydroxy, andR.sup.6 is hydrogen, imino-protective group or alkyl,and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及一种治疗哺乳动物癌或肉瘤肿瘤的方法，包括向所述哺乳动物施用有效量的下式的四环化合物：其中R 1为甲酰基，被保护的甲酰基，羟甲基，保护的羟甲基，芳基氨基甲基 羧基，保护的羧基，芳基亚氨基甲基，羟基亚氨基甲基，烷氧基亚氨基甲基，酰氧基亚氨基甲基，氨基甲酰基甲基或芳基氨基丙基甲基，R2是羟基，烷氧基或被保护的羟基，R3是氢，R4是甲基，羟甲基或保护的羟甲基，或R3和R4组合在一起形成 亚甲基或氧代，R 5为羟基，烷氧基或保护的羟基，R 6为氢，亚氨基保护基或烷基，及其药学上可接受的盐。