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    Antibiotic FR-900129 substance, a process for the preparation thereof and pharmaceutical compositions containing the same
    11.
    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。

    N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof
    15.
    发明授权
    N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof 失效
    N-酰基肽，其制备方法及其药物组合物

    公开(公告)号：US4643990A

    公开(公告)日：1987-02-17

    申请号：US452827

    申请日：1982-12-23

    申请人： Kazuyoshi Umehara ,  Keizo Yoshida ,  Hirokazu Tanaka ,  Itsuo Uchida ,  Masanobu Kohsaka ,  Hiroshi Imanaka

    发明人： Kazuyoshi Umehara ,  Keizo Yoshida ,  Hirokazu Tanaka ,  Itsuo Uchida ,  Masanobu Kohsaka ,  Hiroshi Imanaka

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  A61K37/43 ,  C07C67/02 ,  C07C69/52 ,  C07C101/26 ,  C07C101/30 ,  C07C143/12 ,  C07K5/08

    CPC分类号： C07K5/06104 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06086 ,  A61K38/00

    摘要： N-acylpeptides are disclosed of the formula: ##STR1## wherein R.sup.1 is alkanoyloxy or alkenoyloxy; R.sup.2 is alkyl or alkenyl; R.sup.3 and R.sup.4 are each lower alkyl, hydroxy(lower)alkyl, ar(lower)alkyl, esterified carboxy(lower)alkyl, carboxy(lower)alkyl, protected amino(lower)alkyl or amino(lower)alkyl; R.sup.5 is hydrogen, hydroxy(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl; R.sup.6 is carboxy, esterified carboxy or sulfo(lower)alkyl; A.sup.1, A.sup.2 and A.sup.3 are each bond or lower alkylene; and m and n are each an integer of 0 or 1; or its pharmaceutically acceptable salt. These compounds have anti-complementary activity and fibrinolytic activity, and are useful as therapeutic agents for immune-complex diseases or autoimmune diseases such as nephritis, rheumatic diseases, systemic lupus erythematosus, etc. and thrombosis such as cerebral apoplexy, coronary insufficiency, pulmonary embolism, etc.

    摘要翻译： N-酰基肽公开于下式：其中R 1是烷酰氧基或烯酰基氧基; R2是烷基或烯基; R 3和R 4各自为低级烷基，羟基（低级）烷基，芳（低级）烷基，酯化羧基（低级）烷基，羧基（低级）烷基，被保护的氨基（低级）烷基或氨基（低级） R5是氢，羟基（低级）烷基，被保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基或酯化羧基（低级）烷基; R6是羧基，酯化的羧基或磺基（低级）烷基; A1，A2和A3各自为键或低级亚烷基; m和n分别为0或1的整数; 或其药学上可接受的盐。 这些化合物具有抗互补活性和纤维蛋白溶解活性，并且可用作免疫复合物疾病或自身免疫性疾病如肾炎，风湿性疾病，系统性红斑狼疮等的治疗剂，以及血栓形成如脑中风，冠状动脉功能不全，肺栓塞 等等