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231 条记录 (耗时 0.021 秒)

    2'-N-Substituted fortimicin B and derivatives
    113.
    发明授权
    2'-N-Substituted fortimicin B and derivatives 失效
    2-N取代的fortimicin B及其衍生物

    公开(公告)号：US4214076A

    公开(公告)日：1980-07-22

    申请号：US863013

    申请日：1977-12-21

    申请人： James B. McAlpine

    发明人： James B. McAlpine

    IPC分类号： C07H15/224 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/224

    摘要： 2'-N-substituted fortimicin B and fortimicin B derivatives represented by the formula ##STR1## wherein: R is selected from the group consisting of .beta.-naphthoyl, .gamma.-naphthoyl, .gamma.-naphthyl, (.gamma.-amino-.gamma.-hydroxybutyryl) or 1-(2-amino-4-hydroxybutyl) and R.sub.1 is N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, an amino acid residue, 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.

    摘要翻译： 2'-N-取代的fortimicin B和由下式表示的fortimicin B衍生物：其中：R选自β-萘甲酰基，γ-萘甲酰基，γ-萘基，（γ-氨基-γ-羟基丁酰基） 或1-（2-氨基-4-羟基丁基），R 1为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，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， ，氨基羟基低级烷基，N-低级烷基氨基羟基低级烷基，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。 该化合物可用作抗生素。

    3-De-O-methyl-2-N-acyl and alkyl fortimicins A and B
    115.
    发明授权
    3-De-O-methyl-2-N-acyl and alkyl fortimicins A and B 失效
    3-脱-O-甲基-2-N-酰基和烷基fortimicins A和B

    公开(公告)号：US4187297A

    公开(公告)日：1980-02-05

    申请号：US863014

    申请日：1977-12-21

    申请人： Jerry R. Martin ,  John S. Tadanier ,  Paulette Collum

    发明人： Jerry R. Martin ,  John S. Tadanier ,  Paulette Collum

    IPC分类号： A01N43/14 ,  C07H15/224 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/224

    摘要： 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.

    摘要翻译： 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。

    Antibiotic aminoglycosides, processes of preparation and pharmaceutical compositions
    116.
    发明授权
    Antibiotic aminoglycosides, processes of preparation and pharmaceutical compositions 失效
    抗生素氨基糖苷类，制备方法和药物组合物

    公开(公告)号：US4064339A

    公开(公告)日：1977-12-20

    申请号：US557310

    申请日：1975-03-11

    申请人： Daniel Coussediere ,  Jean-Claude Gasc

    发明人： Daniel Coussediere ,  Jean-Claude Gasc

    IPC分类号： C07H5/06 ,  B01J23/00 ,  C07B61/00 ,  C07H15/224 ,  C07H15/234 ,  C07H15/236 ,  C07H15/22 ,  A61K31/71

    CPC分类号： C07H15/224 ,  C07H15/234

    摘要： There are disclosed pharmaceutically-active aminoglycosides comprising 4-O-(2',6'-diamino 2',6'-didesoxy .alpha.,D-glucopyrannosyl) 6-O-(3"-amino 3",4",6"-tridesoxy .alpha., D-xylohexopyrannosyl) 2-desoxy streptamine of the formula: ##STR1## and the addition salts thereof with mineral acids or organic acids. Also disclosed are methods for preparation of the novel products as well as certain novel intermediate products. There are also disclosed pharmaceutical compositions in which the novel products are the active agents as well as methods for use of compositions as antibiotic agents.

    摘要翻译： 公开了包含4-O-（2'，6'-二氨基2'，6'-二脱氧-α，D-吡喃葡萄糖基）6-O-（3“ - 氨基3”，4“'的药学活性氨基糖苷类 ，6“ - 三酰氧基α，D-木糖六吡喃葡糖基）2-脱氧链霉胺，及其与无机酸或有机酸的加成盐。 还公开了制备新产品以及某些新型中间产物的方法。 还公开了其中新产品是活性剂的药物组合物以及用作组合物作为抗生素剂的方法。

    Aminoglycoside antibiotics
    118.
    发明授权
    Aminoglycoside antibiotics 失效
    氨基糖苷类抗生素

    公开(公告)号：US4006133A

    公开(公告)日：1977-02-01

    申请号：US515814

    申请日：1974-10-18

    申请人： Eiji Ohki ,  Hiromichi Saeki ,  Shinichi Sugawara

    发明人： Eiji Ohki ,  Hiromichi Saeki ,  Shinichi Sugawara

    IPC分类号： B01J23/00 ,  B01J25/00 ,  C07B61/00 ,  C07H15/224 ,  C07H15/23 ,  C07G11/00

    CPC分类号： C07H15/224 ,  C07H15/23

    摘要： New derivatives of the antibiotic butirosin A having the formula: ##STR1## in which R is a radical of formula (II): ##STR2## and pharmaceutically acceptable acid addition salts thereof. The butirosin A derivatives of formula (I) can be prepared by reduction of a 5"-azido compound having the formula (III): ##STR3## in which R' is the same groups R or a group which, on reduction, gives a group of formula (II).The butirosin A derivatives of general formula (I) and pharmaceutically acceptable acid addition salts thereof are active against a broad spectrum of Gram-positive and Gram-negative bacteria, including some butirosin-resistant strains.

    摘要翻译： 具有下式的抗生素丁酸钠A的新衍生物：其中R是式（II）的基团：其中R 1是（II）基团及其药学上可接受的酸加成盐。

    1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl]
    119.
    发明授权
    1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] 失效
    1-N - （（S） - ' - 羟基-γ-氨基乙酰胺）UMEZAWA; 哈马

    公开(公告)号：US4001208A

    公开(公告)日：1977-01-04

    申请号：US402085

    申请日：1973-10-01

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Kenji Maeda ,  Osamu Tsuchiya ,  Shinichi Kondo ,  Shunzo Fukatsu

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Kenji Maeda ,  Osamu Tsuchiya ,  Shinichi Kondo ,  Shunzo Fukatsu

    IPC分类号： C07H15/224 ,  C07H15/23 ,  C07H15/236

    CPC分类号： C07H15/224 ,  C07H15/23 ,  C07H15/234 ,  Y02P20/55

    摘要： A new and useful 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl]derivative of an aminoglycosidic antiobiotic, including its deoxy derivative, such as kanamycin B, 3'-deoxyneamine, 3',4'-dideoxyneamine, 3',4'-dideoxyribostamycin or 3', 4'-dideoxykanamycin B is now synthetized from the parent substance, aminoglycosidic antibiotic. The new 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivative shows a wider and/or higher antibacterial activity than the parent substance and is useful in the treatment of infections by gram-negative and gram-positive bacteria, including drug-resistant strains thereof. The preparation of this new derivative may be made by 1-N-acylating the parent aminoglycosidic antibiotic with (S)-.alpha.-hydroxy-.omega.-aminocarboxylic acid with the amino group being protected, and chromatographically separating the acylated products to isolate the desired 1-N-acyl derivative, followed by the removal of the amino-protecting group.