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    • 2. 发明授权
    • 1,2-Modified fortimicins A and B, intermediates therefor and method for
their manufacture
    • 1,2-改性的fortimicins A和B,其中间体及其制备方法
    • US4340727A
    • 1982-07-20
    • US201651
    • 1980-10-28
    • Jerry R. MartinJohn S. TadanierPaulette Johnson
    • Jerry R. MartinJohn S. TadanierPaulette Johnson
    • C07H15/224C07H15/22
    • C07H15/224
    • A 1,2-modified fortimicin A or B represented by the formulae I, II and III: ##STR1## wherein R is hydrogen or loweralkyl; and R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-lower-alkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, amino hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N-N-diloweralkylaminohydroxyloweralkyl, acyl, aminoacyl, hydroxy-substituted aminoacyl, diaminoacyl, hydroxyacyl, hydroxy-substituted diaminoacyl, N-loweralkylaminoacyl, N, N-diloweralkylaminoacyl, hydroxysubstituted-N-loweralkylaminoacyl and hydroxy-substituted-N, N-diloweralkylaminoacyl, and the pharmaceutically acceptable salts thereof. The compounds are broad spectrum antibiotics.
    • 由式I,II和III表示的1,2-改性的fortimicin A或B:其中R是氢或低级烷基; 其中R 1选自氢,低级烷基,氨基低级烷基,二氨基低级烷基,N-低级烷基氨基低级烷基,N,N-二低级烷基氨基低级烷基,羟基低级烷基,氨基羟基低级烷基,N-低级烷基氨基羟基低级烷基, ,二氨基酰基,羟基酰基,羟基取代的二氨基酰基,N-低级烷基氨基酰基,N,N-二低级烷基氨基酰基,羟基取代的N-低级烷基氨基酰基和羟基取代的N,N-二低级烷基氨基酰基及其药学上可接受的盐。 这些化合物是广谱抗生素。
    • 6. 发明授权
    • 2'N-acyl and alkyl fortimicin B and derivatives, 4,2'-N,N'diacyl and
dialkyl fortimicin B derivatives 4-N-acyl-2'-N-alkyl and
4-N-alkyl-2'-N-acyl fortimicin B derivatives
    • 2'N-酰基和烷基苦味蛋白B及其衍生物,4,2'-N,N'-二酰基和二烷基苦味蛋白B衍生物4-N-酰基-2'-N-烷基和4-N-烷基-2'- -acyl fortimicin B衍生物
    • US4187298A
    • 1980-02-05
    • US863012
    • 1977-12-21
    • Jerry R. MartinJohn S. TadanierPaulette Collum
    • Jerry R. MartinJohn S. TadanierPaulette Collum
    • C07H15/224A61K31/71C07H15/22
    • C07H15/224
    • 2'-N-Acyl and alkyl fortimicin B and fortimicin B derivatives, 4,2'-N,N'-diacyl and dialkyl derivatives, 4-N-acyl-2'-N-alkyl and 4-N-alkyl-2'-N-acyl fortimicin B derivatives represented by the formula ##STR1## wherein: R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, hydroxyacyl, an amino acid residue, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl or N,N-diloweralkylaminohydroxyloweralkyl; and R.sub.1 is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl or hydrogen and the pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds; and methods of making and using the compounds. The compounds are useful as antibiotics, intermediates, and are further useful in making moth proofing agents and pickling inhibitors.
    • 2-N-酰基和烷基维生素B和fortimicin B衍生物,4,2'-N,N'-二酰基和二烷基衍生物,4-N-酰基-2'-N-烷基和4-N-烷基-2 其中:R是酰基,氨基酰基,N-单低级烷基氨基酰基,N,N-二低级烷基氨基酰基,羟基取代的酰基酰基,羟基酰基,氨基酸残基,低级烷基,氨基低级烷基,羟基低级烷基 N,N-二烷基氨基低级烷基,N,N-二烷基氨基低级烷基,氨基羟基低级烷基,N-低级烷基氨基羟基低级烷基或N, 氨基酸残基,羟基酰基,低级烷基,氨基低级烷基,羟基低级烷基,N-低级烷基氨基低级烷基,N,N-二低级烷基氨基低级烷基,氨基羟基低级烷基,N-低级烷基氨基羟基低级烷基,N-低级烷基氨基低级烷基氨基甲酰基, ,N,N-二低级烷基氨基羟基低级烷基或氢及其药学上可接受的盐; 含有这些化合物的药物组合物; 以及制备和使用该化合物的方法。 这些化合物可用作抗生素,中间体,并且还可用于制备防蛀剂和酸洗抑制剂。