6'-Modified fortimicin compounds
    6.
    发明授权
    6'-Modified fortimicin compounds 失效
    6'-改性的fortimicin化合物

    公开(公告)号:US4431799A

    公开(公告)日:1984-02-14

    申请号:US79129

    申请日:1979-09-26

    CPC分类号: C07H15/224

    摘要: Described is a method for the preparation of 6'-modified fortimicin compounds including 6'-epi fortimicin by converting 1,2-di-N-protected fortimicin B into 4,6'-di-N-substituted alkoxycarbonyl-1,2'-di-N-protected fortimicin B which is further converted to 1,2'-di-substituted fortimicin B-4,5-carbamate, a compound whose substitution pattern is particularly suited to modification at the 6'-amino group and novel compounds thereof.

    摘要翻译: 描述了通过将1,2-二-N-保护的fortimicin B转化成4,6'-二-N-取代的烷氧基羰基-1,2'的6'-改性的fortimicin化合物,包括6'-epi fortimicin的方法, -di-N-保护的fortimicin B,其进一步转化为1,2'-二取代的fortimicin B-4,5-氨基甲酸酯,其取代模式特别适于在6'-氨基改性的化合物和新化合物 其中。

    3-Amino-3-demethoxyfortimicins, pharmaceutical compositions thereof and
method of use
    7.
    发明授权
    3-Amino-3-demethoxyfortimicins, pharmaceutical compositions thereof and method of use 失效
    3-氨基-3-脱甲氧基有益霉素,其药物组合物和使用方法

    公开(公告)号:US4427662A

    公开(公告)日:1984-01-24

    申请号:US366798

    申请日:1982-04-09

    CPC分类号: C07H15/224

    摘要: Disclosed herein are fortimicin derivatives represented by the formula: ##STR1## wherein R is hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, loweracyl, aminoloweracyl, diaminoloweracyl, hydroxyloweracyl, N-loweralkylaminoloweracyl, N,N-diloweralkylaminoloweracyl, or aminohydroxyloweracyl, and the pharmaceutically acceptable salts thereof. Also disclosed are intermediates useful in the preparation of these compounds and compositions of these compounds together with a pharmaceutically acceptable carrier and/or diluent.

    摘要翻译: 本文公开的是由下式表示的强力衍生物衍生物:其中R是氢,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,N,N-二烷基氨基羟基低级烷基, 氨基酰基酰基,二氨基低级酰酰基,羟基低级酰基,N-低级烷基氨基低聚酰西酰,N,N-二 - 低级烷基氨基低聚酰基或氨基羟基酰基,及其药学上可接受的盐。 还公开了可用于制备这些化合物和这些化合物的组合物以及药学上可接受的载体和/或稀释剂的中间体。

    2-Epi-fortimicin A and derivatives
    8.
    发明授权
    2-Epi-fortimicin A and derivatives 失效
    2-Epi-fortimicin A及其衍生物

    公开(公告)号:US4331804A

    公开(公告)日:1982-05-25

    申请号:US079130

    申请日:1979-09-26

    CPC分类号: C07H15/224

    摘要: What is described is 2-epi-fortimicin A, 2-epi-fortimicin B or a 2-epi-fortimicin B derivative represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen or hydroxy; R.sub.3 is methyl or hydrogen; and R.sub.4 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoalkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, acyl of the formula ##STR2## wherein R.sub.5 is loweralkyl, aminoacyl, diaminoacyl, hydroxyacyl, N-loweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue other than those defined above and the pharmaceutically acceptable salts thereof useful in the treatment of infections.

    摘要翻译: 描述的是2-epi-fortimicin A,2-epi-fortimicin B或由下式表示的2-epi-fortimicin B衍生物:其中R 1是氢或低级烷基; R2是氢或羟基; R3是甲基或氢; 并且R 4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,N,N-二烷基氨基羟基低级烷基,式 是低级烷基,氨基酰基,二氨基酰基,羟基酰基,N-低级烷基氨基酰基,N,N-二低级烷基氨基酰基,羟基取代的氨基酰基或除上述定义之外的氨基酸残基及其可用于治疗感染的药学上可接受的盐。

    4
    9.
    发明授权
    4"-O-sulfonyl erythromycin-9-O-oxime derivatives 失效
    4 {41-磺酰基红霉素-9-O-肟衍生物

    公开(公告)号:US4063014A

    公开(公告)日:1977-12-13

    申请号:US586127

    申请日:1975-06-12

    IPC分类号: C07H17/08 A61K31/70

    CPC分类号: C07H17/08

    摘要: A 4"-O-sulfonyl erythromycin derivative of the following structural formula: ##STR1## where R is selected from the group consisting of oxygen, oxime, and substituted oxime, R.sub.1 is hydrogen or hydroxy and R.sub.2 is selected from the group consisting of phthalimide, substituted amides, benzamides, substituted benzamides, sulfonamides, substituted sulfonamides, amines, substituted amines, phenylurea, substituted phenylurea, phenylthiourea, substituted phenylthiourea, thiophenol and substituted thiophenol, phenoxides and substituted phenoxides and R.sub.3 is hydrogen or methyl. The present sulfonyl derivatives of erythromycin A, B and C are useful as antibiotics.

    摘要翻译: 一种具有下列结构式的4'-“O-磺酰基红霉素衍生物:其中R选自氧,肟和取代的肟,R 1是氢或羟基,R 2选自 邻苯二甲酰亚胺,取代的酰胺,苯甲酰胺,取代的苯甲酰胺,磺酰胺,取代的磺酰胺,胺,取代的胺,苯基脲,取代的苯基脲,苯基硫脲,取代的苯基硫脲,苯硫酚和取代的苯硫酚,苯氧基和取代的苯氧基,R3是氢或甲基。 本发明的红霉素A,B和C的磺酰基衍生物可用作抗生素。