发明名称 KANAMYCIN-B DERIVATIVES
摘要 1-N-(alpha-hydroxy-omega-aminoalkanoyl)-6'-N-methyl-3',4'-dideoxyka namycins B or pharmaceutically acceptable acid addition salts thereof are prepared by selective acylation of the 1-amino group of an amino-protected derivative of the formula <IMAGE> in which R1 is a monovalent amino protective group and R2 is hydrogen or a monovalent amino protective group, with an alpha -hydroxyomega -amino acid of the formula V or with a functional derivative thereof, in which n is 1, 2 or 3, R3 is an amino protective group and R4 is hydrogen, or R3 and R4 together are a divalent amino protective group, after which the amino protective groups are eliminated from the 1-N-acylated product obtained in this way. The prepared compounds are effective not only against Gram-negative and Gram-positive bacteria with the usual kanamycin sensitivity but also against kanamycin-resistant bacteria. <IMAGE>
申请公布号 AU8518975(A) 申请公布日期 1977.03.31
申请号 AU19750085189 申请日期 1975.09.25
申请人 BRISTOL-MYERS CO. 发明人 HAMAO UMEZAWA;KENJI MAEDA;SHINICHI KONDO;KANAGAWA-KEN
分类号 C07H15/234;A61K31/70;A61K31/7008;A61K31/7028;A61K31/7034;A61K31/7036;A61P31/04;C07H15/236 主分类号 C07H15/234
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