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    • 47. 发明专利
    • Low toxic derivative of 3-demethoxyistamycin b
    • 低毒性衍生物3-DEMETHOXYISTAMYCIN B
    • JPS59216898A
    • 1984-12-06
    • JP9075283
    • 1983-05-25
    • Microbial Chem Res Found
    • UMEZAWA HAMAOKONDOU SHINICHI
    • A61K31/70A61K31/7028A61K31/7034A61K31/7036A61P31/04C07H15/224
    • C07H15/224
    • NEW MATERIAL:A compound shown by the formula I {1W4 of 4 R' are -CHRS O
      3 M [M is H, ammonium ion, or alkaline (earth) metal], and the rest of R' is H}.
      EXAMPLE: Sodium 4-demethoxyisatmycin B-mono-N-methanesulfonate.
      USE: An antibacterial agent against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.
      PREPARATION: 3-Demethoxyistamycin B (acid addition salt) shown by the formula II is reacted with an aldehyde shown by the formula RCHO [R is H, alkyl, or (substituted)phenyl] and sulfurous acid (hydrogensulfite) shown by the formula MHSO
      3 , to give a compound shown by the formula I wherein methanesulfone group shown by the formula -CHRSO
      3 M is introduced into 1W4 of 3 amino groups and one methylamino group of the compound shown by the formula II.
      COPYRIGHT: (C)1984,JPO&Japio
    • 新材料:由式I {1-4的R'表示的化合物是-CHRS O 3 M [M是H,铵离子或碱土金属],其余的R'是H}。 实施例:4-去甲氧基异霉素B-单-N-甲磺酸钠。 用途:抗革兰氏阳性和革兰氏阴性细菌,包括铜绿假单胞菌。 制备:式II所示的3-去甲氧基霉素B(酸加成盐)与式RCHO [R为H,烷基或(取代的)苯基]所示的醛和式MHSO 3所示的亚硫酸(亚硫酸氢盐)反应 得到式I所示的化合物,其中由式-CHRSO 3 M表示的甲烷基基团被引入式III中所示化合物的3个氨基的1-4个和1个甲基氨基中。
    • 48. 发明专利
    • Novel antibiotic acmimycin and its preparation
    • 新型抗生素ACMIMYCIN及其制备方法
    • JPS5945890A
    • 1984-03-14
    • JP15792182
    • 1982-09-09
    • Toyo Jozo Co Ltd
    • SAKAKIBARA HIDEOKURITA MASASHISATOI SHIYUUZOUMUTOU NAOKITAKADA MASAKIHAYASHI MITSUO
    • C07D493/04A61K31/35A61K35/74A61P31/04C07H15/224C12P1/06C12P17/18C12R1/465
    • C07H15/224
    • NEW MATERIAL:Acmimycin having the following physical and chemical properties. Elementary analysis: shown by the table. Molecular weight: 346. Melting point: 123 deg.C (decomposition). Specific rotatory powder:[alpha] D+44.2 deg. (C=1, water). Ultraviolet absorption spectrum: not showing characteristic absorption at 220-360nm in an aqueous solution, only showing end group absorption. Infrared absorption spectrum: shown by the figure. Solubility: soluble in water, slightly soluble in lower alcohol, insoluble in acetone, benzene, and ethyl acetate. Color reaction, positive in ninhydrin reaction, decoloring reaction of potassium permanganate, negative in Erson-Morgan reaction, Sakaguchi reaction. Classification of basicity, acidity, or neutrality: basicity. Its acid addition salt. USE:An antibiotic having antibacterial activity against Gram-positive and Gram- negative bacteria. PROCESS:A bacterium[e.g., Streptomyces sp. AC 4559(FERM P-6645)] belonging to the genus Streptomyces, capable of producing antibiotic acmimycin, separated from the soil in plowed field of Akiyoshi machi, Minegun, yamaguchi prefecture, is cultivated in a medium.
    • 新材料:具有以下物理和化学性质的阿米霉素。 基本分析:如表所示。 分子量:346.熔点:123℃(分解)。 特殊旋转粉末:α24D+ 44.2度 (C = 1,水)。 紫外吸收光谱:在220-360nm的水溶液中不显示特征吸收,仅显示端基吸收。 红外吸收光谱:如图所示。 溶解性:溶于水,微溶于低级醇,不溶于丙酮,苯和乙酸乙酯。 色素反应,茚三酮反应中阳性,高锰酸钾脱色反应,Erson-Morgan反应阴性,坂口反应。 碱度,酸度或中性分类:碱度。 其酸加成盐。 用途:抗革兰氏阳性和革兰氏阴性细菌具有抗菌活性的抗生素。 方法:细菌[例如,链霉菌属(Streptomyces sp。 在介质中培养属于链霉菌属的AC 4559(FERM P-6645)],其能够生产抗生素阿米霉素,与山药县仁仁秋山町耕地中的土壤分离。