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    ANTIBIOTIC COMPOUND
    5.
    发明专利
    ANTIBIOTIC COMPOUND 失效

    公开(公告)号：JPS57171925A

    公开(公告)日：1982-10-22

    申请号：JP2757282

    申请日：1982-02-24

    申请人： BRISTOL BANYU RES INST LTD

    发明人： KONISHI MASATAKA ,  MIYAGI TAKEO ,  TSUKIURA HIROSHI ,  KAWAGUCHI HIROSHI

    IPC分类号： C12P21/04 ,  A61K38/00 ,  A61P31/04 ,  C07K1/20 ,  C07K7/60 ,  C07K7/62 ,  C07K14/195 ,  C07K14/41 ,  C12R1/09

    摘要： NEW MATERIAL:A peptide of formulaI(R is H, group of formula II, III or IV; Dab is alpha, gamma-diaminobutyric acid; Leu is leucine; Phe is phenylalanine). EXAMPLE:Bu-2470A ( C41H71N13O8.5HCl.4H2O). USE:Antibiotic. PREPARATION:Bacillus circulans strain G493-B6 (ATCC 31,805) is cultured in an aqueous enriched medium containing assimilable carbon and nitrogen sources under submerged aeration conditions until a practical amount of Bu-2470 complex is accumulated and the Bu-2470 complex is collected from the culture medium without cotamination with other substances simultaneously formed. The cultivation temperature is 20-45 deg.C and fermentation is conducted at 25-35, preferably 27-32 deg.C.

    PREPARATION OF ANTIBIOTIC SUBSTANCE COLISTIN SALT
    6.
    发明专利
    PREPARATION OF ANTIBIOTIC SUBSTANCE COLISTIN SALT 失效

    公开(公告)号：JPS57144250A

    公开(公告)日：1982-09-06

    申请号：JP2937381

    申请日：1981-03-03

    申请人： KAYAKU ANTIBIOTIC RESEARCH CO

    发明人： SATOU HIROYUKI ,  KOYAMA YASUO ,  MIYATA JIYUICHI ,  SATOU TADAAKI

    IPC分类号： C07K7/62 ,  A61K38/00 ,  A61P31/04

    摘要： PURPOSE:To prepare the titled compound useful as an excellent antibiotic agent, capable of increasing the concentration in blood effectively even by the oral administration, easily, by reacting a colistin base with an organic acid in water or in an organic solvent. CONSTITUTION:The objective compound can be prepared by reacting a colistin base with an organic acid of formula (R2 and R3 are H or methy)( e.g. propionic acid, isobutyric acid, pivalic acid, etc.) at 40-60 deg.C in water or a water-miscible organic solvent (e.g. methanol, ethanol, isopropanol, etc.) or a mixture of water and an organic solvent. Since colistin has 5mol of free amino groups originated from the gamma-amino group of alpha,gamma-diaminobutyric acid in the molecule, 5mol equivalent of acid is added to 1mol of the colistin base.

    Preoduction of novel antibiotic derivative
    7.
    发明专利
    Preoduction of novel antibiotic derivative 失效
    引发新型抗生素衍生物

    公开(公告)号：JPS5758655A

    公开(公告)日：1982-04-08

    申请号：JP13238780

    申请日：1980-09-25

    申请人： Kayaku:Kk

    发明人： KURIHARA TOUZABUROU ,  KOYAMA YASUO ,  SATOU HIROYUKI ,  SUZUKI SHIGENORI

    IPC分类号： C07K7/62 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07K1/113

    摘要： PURPOSE: The intermediate, resulting from reaction between colistin and a specific halide or aldehyde, is converted to its methanesulfonate sodium salt to produce an antibiotic derivative with lowered toxicity of colistin and increased antibiotic activity.
    CONSTITUTION: Colistin is made to react with a compound of R
    2 X (R
    2 is alkyl, alkenyl, benzyl; X is halogen or aldehyde) to give an N-substituted colistin of formula I (R
    1 is residual group of colistin). Further, the product is made to react with sodium oxymethanesulfonate to produce an antibiotic derivative of formula II. In the compound of R
    2 X, an example having halogen as the reaction group is methyl halide or ethyl halide and having aldehyde is formaldehyde or acetaldehyde. The reaction readily proceeds when heated to 40W50°C.
    COPYRIGHT: (C)1982,JPO&Japio

    摘要翻译： 目的：由粘菌素与特定的卤化物或醛反应产生的中间体转化为甲磺酸钠盐，产生抗生素衍生物，毒性降低，抗生素活性降低。 构成：使Colistin与R2X（R2是烷基，烯基，苄基; X是卤素或醛）的化合物反应，得到式I的N-取代的粘菌素（R1是粘菌素的残基）。 此外，使产物与羟甲磺酸钠反应以产生式II的抗生素衍生物。 在R2X的化合物中，具有卤素作为反应基团的实例是甲基卤化物或乙基卤化物，并且具有醛是甲醛或乙醛。 当加热至40-50℃时，反应容易进行。

    9.
    发明专利
    失效

    公开(公告)号：JPS4843917B1

    公开(公告)日：1973-12-21

    申请号：JP9138770

    申请日：1970-10-17

    IPC分类号： C07K7/62 ,  A61K38/00 ,  C07K1/113

    10.
    发明专利
    失效

    公开(公告)号：JPS4843753B1

    公开(公告)日：1973-12-20

    申请号：JP9973369

    申请日：1969-12-11

    IPC分类号： C07K7/62 ,  A61K38/00 ,  C07K1/113