6'N-Alkyl- and 6',6'-di-N-alkyl derivatives of fortimicins A and B
    72.
    发明授权
    6'N-Alkyl- and 6',6'-di-N-alkyl derivatives of fortimicins A and B 失效
    fortimicins A和B的6'N-烷基和6',6'-二-N-烷基衍生物

    公开(公告)号:US4205070A

    公开(公告)日:1980-05-27

    申请号:US863018

    申请日:1977-12-21

    CPC分类号: C07H15/224

    摘要: Novel fortimicin antibiotics represented by the formula ##STR1## wherein R.sub.1 is loweralkyl, R.sub.2 is hydrogen or loweralkyl and R.sub.3 is selected from the group consisting of hydrogen, acyl, hydroxyacyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an aminoacid residue, loweralkyl, hydroxyloweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl; and the pharmaceutically acceptable salts thereof, intermediates useful in their preparation, compositions employing the compounds and methods of using the compounds.

    摘要翻译: 由式表示的新颖的具霉素抗生素,其中R1是低级烷基,R2是氢或低级烷基,R3选自氢,酰基,羟基酰基,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 氨基酰基或氨基酸残基,低级烷基,羟基低级烷基,氨基低级烷基,N-单低级烷基氨基低级烷基,N,N-二低级烷基氨基低级烷基或羟基取代的氨基低级烷基; 及其药学上可接受的盐,可用于其制备的中间体,使用该化合物的组合物和使用该化合物的方法。

    2-Deoxyfortimicin A, 4-N-alkyl and 4-N-acyl-2-deoxyfortimicin B
derivatives
    73.
    发明授权
    2-Deoxyfortimicin A, 4-N-alkyl and 4-N-acyl-2-deoxyfortimicin B derivatives 失效
    2-脱氧有机霉素A,4-N-烷基和4-N-酰基-2-脱氧有机霉素B衍生物

    公开(公告)号:US4192867A

    公开(公告)日:1980-03-11

    申请号:US863006

    申请日:1977-12-21

    CPC分类号: C07H15/224

    摘要: 2-Deoxyfortimicin A, 2-deoxy-4-N-alkyl fortimicins and 2-deoxy-4-N-acyl fortimicins represented by the formula ##STR1## wherein R is selected from the group consisting of acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, hydroxyacyl, loweralkyl, aminoloweralkyl, N-monoloweralkylaminoloweralkyl, hydroxyloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl, and the pharmaceutically acceptable salts thereof; intermediates therefor; and pharmaceutical compositions containing the compounds of this invention.

    摘要翻译: 2-脱氧有益霉素A,2-脱氧-4-N-烷基苦味蛋白和由式“IMAGE”表示的2-脱氧-4-N-酰基酪氨酸,其中R选自酰基,氨基酰基,N-单低级烷基氨基酰基, N,N-二烷基氨基酰基,羟基取代的酰基酰基,氨基酸残基,羟基酰基,低级烷基,氨基低级烷基,N-单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或羟基取代的氨基低级烷基。 中间体 和含有本发明化合物的药物组合物。

    4-N-Acylfortimicin B derivatives and the chemical conversion of
fortimicin B to fortimicin A
    74.
    发明授权
    4-N-Acylfortimicin B derivatives and the chemical conversion of fortimicin B to fortimicin A 失效
    4-N-酰基苦霉素B衍生物和fortimicin B对fortimicin A的化学转化

    公开(公告)号:US4188319A

    公开(公告)日:1980-02-12

    申请号:US3053

    申请日:1979-01-12

    CPC分类号: C07H15/224

    摘要: This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R.sup.1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof.The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.

    摘要翻译: 本发明提供了结构为“IMAGE”的4-N-酰基苦味霉素B衍生物,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或下式的取代的酰基酰基,其中R1是 衍生自氨基酸或短肽的酰基及其药学上可接受的盐。 该化合物可用作制备4-N-烷基或取代的烷基富霉菌素B衍生物的中间体。 除了作为中间体的作用外,本发明的一些化合物也可用作抗微生物剂。

    2-N-acyl and alkyl 6-epi-fortimicin B and derivatives
    75.
    发明授权
    2-N-acyl and alkyl 6-epi-fortimicin B and derivatives 失效
    2-N-酰基和6-epi-fortimicin烷基酯及其衍生物

    公开(公告)号:US4187296A

    公开(公告)日:1980-02-05

    申请号:US863007

    申请日:1977-12-21

    CPC分类号: C07H15/224

    摘要: 2'-N-Acyl and alkyl-6'-epi-fortimicin B and fortimicin B derivatives represented by the formula ##STR1## wherein: R is acyl, hydroxyacyl, aminoacyl, N-monoloweralkylamino, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, 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; R.sub.2 is loweralkyl; and R.sub.3 is hydrogen or loweralkyl; and the pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds; and methods of making and using the compounds. The compounds are antibiotics.

    摘要翻译: 2'-N-酰基和烷基-6'-表 - 糊精蛋白B和由式表示的fortimicin B衍生物,其中:R是酰基,羟基酰基,氨基酰基,N-单低级烷基氨基,N,N-二低级烷基氨基酰基,羟基取代 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,N-二低级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, N,N-二烷基氨基羟基低级烷基或氢; R2是低级烷基; 并且R 3是氢或低级烷基; 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。 这些化合物是抗生素。