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    • 3. 发明授权
    • Antibiotics
    • 抗生素
    • US5942495A
    • 1999-08-24
    • US857281
    • 1997-05-16
    • Edward BorowskiJolanta GrzybowskaPawel SowinskiJerzy GumieniakAndrzej Czerwinski
    • Edward BorowskiJolanta GrzybowskaPawel SowinskiJerzy GumieniakAndrzej Czerwinski
    • C07H17/08A61K31/71
    • C07H17/08
    • The invention relates to an N-alkyl-N-glycosyl derivative of antifungal antibiotics of the polyene macrolide group of general formula 1(a), wherein M represents polyene macrolide antibiotics residues, R represents a variable part of sugar residue, R.sup.1 represents a C.sub.1-4 alkyl group and R.sup.2 represents hydrogen or a C.sub.1-4 alkyl group; their salts of general formula 2(a), wherein R, R.sup.1, R.sup.2 and M are as herein defined and A represents an anion of organic or inorganic acid. Compounds of formula 1(b) and 2(b) wherein the N-alkyl and alkyl ester groups are represented by methyl are of particular interest.The invention relates also to processes for preparation of the compounds, to compositions containing these compounds and to their use in therapy and the treatment of external and internal fungal infections in humans and animals. ##STR1##
    • 本发明涉及通式1(a)的多烯大环内酯类抗真菌抗生素的N-烷基-N-糖基衍生物,其中M表示多烯大环内酯抗生素残基,R表示糖残基的可变部分,R1表示C1 -4-烷基,R 2表示氢或C 1-4烷基; 其通式2(a)的盐,其中R,R 1,R 2和M如本文所定义,A代表有机或无机酸的阴离子。 特别令人感兴趣的是其中N-烷基和烷基酯基由甲基表示的式1(b)和2(b)的化合物。 本发明还涉及制备化合物的方法,含有这些化合物的组合物及其在治疗和治疗人和动物中的外部和内部真菌感染中的用途。