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    • 1. 发明授权
    • Novel compounds of the gentamicin class
    • 庆大霉素类的新型化合物
    • US4412068A
    • 1983-10-25
    • US271552
    • 1981-06-08
    • David Rosi
    • David Rosi
    • C07H15/236C12P19/48C07G11/00C07H15/26C12R1/31
    • C12R1/31C07H15/236C12P19/485Y02P20/55Y10S435/869
    • 5-Deoxygentamicin C.sub.2b and 6'-N-methyl-2-hydroxy- and 6'-N-methyl-5-deoxygentamicins C.sub.2b are prepared, as the major fermentation products, by culturing a nutrient medium containing carbohydrates, a source of assimilable nitrogen, essential salts and either D-streptamine or 2,5-dideoxystreptamine with a mutant of Micromonospora purpurea and isolating the fermentation products from the nutrient medium. The fermentation products are acylated with an ester of an .omega.-[N-(benzyloxycarbonyl)amino]-.alpha.-hydroxy-lower-alkanoic acid after first blocking the primary amino group at the 2'-position with an amine-protecting group, followed by catalytic hydrogenolysis of the benzyloxycarbonyl group and removal of the amine-protecting group to prepare the 1-(.omega.-amino-.alpha.-hydroxy-lower-alkanoyl) derivatives.
    • 通过培养含有碳水化合物的营养培养基,可同化氮源,制备5-脱氧虫酰胺Cbb和6'-N-甲基-2-羟基 - 和6'-N-甲基-5-脱氧阿霉素C2b作为主要的发酵产物 ,必需盐和D-链霉胺或具有小单孢菌突变体的2,5-二隐球菌素,并从营养培养基中分离发酵产物。 在用胺保护基团首先封闭2位上的伯氨基后,将发酵产物用ω-[N-(苄氧基羰基)氨基]-α-羟基 - 低级 - 链烷酸的酯进行酰化,随后 通过催化氢解苄氧羰基并除去胺保护基以制备1-(ω-氨基-α-羟基 - 低级烷酰基)衍生物。
    • 4. 发明授权
    • Everninomicin antibiotics and method for the manufacture thereof
    • 益生菌抗生素及其制备方法
    • US3499078A
    • 1970-03-03
    • US3499078D
    • 1968-09-25
    • SCHERING CORP
    • LUEDEMANN GEORGE MWEINSTEIN MARVIN J
    • A61K36/06C07H15/236C12P1/06C12P17/18C12P19/48A61K21/00C07G11/00C21D9/00
    • C12R1/29C07H15/236C12P1/06C12P17/189C12P19/485Y10S435/863
    • Antibiotic No. 467 is produced by cultivating an antibiotic 467-producing strain of micromonospora halophytica var. nigra, especially NRRL 3097, or a 467-producing mutant thereof in an aqueous nutrient medium containing assimilable sources of carbon and nitrogen under aerobic conditions. Antibiotic No. 467 is found mainly in the clarified broth, from which it may be extracted at pH 2 to 9.5 with a water-immiscible organic solvent, e.g. ethylacetate. The solvent extract is concentrated and the antibiotic precipitated by a non-solvent such as hexane. Antibiotic 467 is insoluble in water, hexane and petroleum ether; soluble in ethyl acetate, methanol, butanol, benzene and ether; it is stable to acid and heat; contains C 60.73%, H 7.53%, N 3.70%, O 27.20%, Cl 0.04% and S 0.80%; U.V. 264 mm E1%=183 and 302 mm E1%=116 (inflection points); I.F. (Fig. 1); negative Ninhydrin and Sakaguchi tests; positive ferricyanide and reducing sugars; Rf values for various systems are specified; active against a wide range of gram-positive organisms. Paper chromatograms indicate the presence of various components of antibiotic No. 467. Therapeutic compositions comprise antibiotic No. 467, or a component thereof, and a carrier.
    • 抗生素号467是通过培养产生抗生素467的小孢子虫菌株变种产生的。 黑质,特别是NRRL 3097,或其在含有营养培养基中的467产生突变体,其在需氧条件下含有可同化的碳和氮源。 抗生素号467主要存在于澄清的肉汤中,可以用pH与水不混溶的有机溶剂例如pH 2至9.5进行萃取。 乙酸乙酯。 浓缩溶剂提取物,用非溶剂如己烷沉淀抗生素。 抗生素467不溶于水,己烷和石油醚; 溶于乙酸乙酯,甲醇,丁醇,苯和乙醚; 对酸和热是稳定的; 含C 60.73%,H 7.53%,N 3.70%,O 27.20%,Cl 0.04%和S 0.80%; U.V. 264毫米E1%= 183和302毫米E1%= 116(拐点); 如果。 (图。1); 负Ninhydrin和Sakaguchi测试; 正铁氰化物和还原糖; 指定各种系统的Rf值; 活跃于广泛的革兰氏阳性生物。 纸张色谱图表明抗生素编号467的各种组分的存在。治疗组合物包含抗生素No.467或其组分和载体。
    • 9. 发明授权
    • 2-Hydroxy gentamicin compounds
    • 2-羟基庆大霉素化合物
    • US4387219A
    • 1983-06-07
    • US209412
    • 1980-11-24
    • Haruo YamamotoSol J. Daum
    • Haruo YamamotoSol J. Daum
    • C07H15/236C12P19/48C07H15/22
    • C12R1/31C07H15/236C12P19/485Y02P20/55
    • 2-Hydroxygentamicins B, B.sub.1 and A.sub.3 and 2-hydroxy antibiotics JI-20A and JI-20B are prepared as fermentation products by culturing a nutrient medium containing carbohydrates, a source of assimilable nitrogen, essential salts and D-streptamine with a mutant of Micromonospora purpurea, and isolating the said fermentation products from the nutrient medium; the fermentation products are acylated with an ester of an .omega.-(N-benzyloxycarbonyl)amino-.alpha.-hydroxy-lower-alkanoic acid, after first blocking the 6'-and/or 2'-amine group with an amine-protecting group, followed by catalytic hydrogenolysis of the benzyloxycarbonyl group and removal of the amine-protecting groups to prepare the 1-N-(.omega.-amino-.alpha.-hydroxy-lower-alkanoyl) derivatives.
    • 通过培养含有碳水化合物,可同化氮源,必需盐和D-链霉素的营养培养基,制备2-羟基阿霉素B,B1和A3和2-羟基抗生素JI-20A和JI-20B作为发酵产物,其具有小单孢菌突变体 紫外线,并从所述营养培养基中分离所述发酵产物; 在用胺保护基团首先封闭6'-和/或2'-胺基团之后,用ω-(N-苄氧基羰基)氨基-α-羟基 - 低级 - 链烷酸的酯将发酵产物酰化, 然后催化氢解苄氧羰基并除去胺保护基以制备1-N-(ω-氨基-α-羟基 - 低级烷酰基)衍生物。