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    • 2. 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。
    • 5. 发明授权
    • 3-De-O-methyl-2-N-acyl and alkyl fortimicins A and B
    • 3-脱-O-甲基-2-N-酰基和烷基fortimicins A和B
    • US4187297A
    • 1980-02-05
    • US863014
    • 1977-12-21
    • Jerry R. MartinJohn S. TadanierPaulette Collum
    • Jerry R. MartinJohn S. TadanierPaulette Collum
    • A01N43/14C07H15/224A61K31/71C07H15/22
    • C07H15/224
    • 3-De-O-methyl-2'-N-acyl and alkyl 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 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, hydrogen; the pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds; and methods of making and using the compounds. The compounds are antibiotics.
    • 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,羟基取代的氨基酰基,羟基酰基,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-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,N-二烷基氨基羟基低级烷基。 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,氢; 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。 这些化合物是抗生素。
    • 8. 发明授权
    • 2-Deoxy-2'-N-acyl and alkyl fortimicins A and B
    • 2-脱氧-2'-N-酰基和烷基苦味素A和B
    • US4176178A
    • 1979-11-27
    • US863011
    • 1977-12-21
    • Jerry R. MartinJohn S. TadanierPaulette Collum
    • Jerry R. MartinJohn S. TadanierPaulette Collum
    • C07H15/224A61K31/71C07H15/22
    • C07H15/224
    • 2-Deoxy-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 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, hydroxyacyl, an amino acid residue, loweralkylaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, hydrogen; and the pharmaceutically acceptable salts therefor, pharmaceutical compositions containing the compounds and methods of making and using the compounds. The compounds of this invention are useful as antibiotics.
    • 2-脱氧-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- 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-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或N, 并且R 1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-低级烷基氨基低级烷基,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 ,N-二烷基氨基羟基低级烷基,氢; 及其药学上可接受的盐,含有该化合物的药物组合物和制备和使用该化合物的方法。 本发明的化合物可用作抗生素。