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18 条记录 (耗时 0.021 秒)

    1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, methods for their use as antibacterial agents, and compositions useful therefor
    2.
    发明授权
    1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, methods for their use as antibacterial agents, and compositions useful therefor 失效
    1-N-烷基-4,6-二 - （氨基糖基）-1,3-二氨基二醇，其制备方法，用作抗菌剂的方法及其用途

    公开(公告)号：US4002742A

    公开(公告)日：1977-01-11

    申请号：US492998

    申请日：1974-07-30

    申请人： John J. Wright ,  Peter J. L. Daniels ,  Alan K. Mallams ,  Tattanahalli L. Nagabhushan

    发明人： John J. Wright ,  Peter J. L. Daniels ,  Alan K. Mallams ,  Tattanahalli L. Nagabhushan

    IPC分类号： C07H15/236 ,  A61K31/70

    CPC分类号： C07H15/236

    摘要： 1-N-Alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols, valuable as antibacterial agents, are prepared by treating an acid addition salt of a 4,6-di-(aminoglycosyl)-1,3-diamonocyclitol antibacterial agent in an inert solvent, preferably a protic solvent containing water, with one equivalent of a hydride donor reducing agent and with at least one equivalent of an aldehyde.The 1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols are also prepared by treating the corresponding 1-N-acyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitol with an amide-reducing hydride reagent in an inert organic solvent.Other methods of preparing 1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols include carrying out the foregoing processes with partially N-protected intermediates. Another useful process involves preparing a Schiff base of the 1-amino function of a partially N-protected 4,6-di-(aminoglycosyl)-1,3-diaminocyclitol followed by reduction of said Schiff base and removal of the N-protecting groups.Pharmaceutical compositions comprising 1-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols are described as well as the method of using said compositions to elicit an antibacterial response in a warm blooded animal having a susceptible bacterial infection.

    摘要翻译： 通过将4,6-二（氨基糖基）-1,3-二氨基二（氨基糖基）-1,3-二氨基环己烷酸的酸加成盐处理，制备作为抗菌剂有价值的1-N-烷基-4,6-二（氨基糖基） - 二氨基环醇醇抗菌剂在惰性溶剂中，优选含有水的质子溶剂，与一当量的氢化物供体还原剂和至少一当量的醛。

    1-N-alkyl-aminoglycoside-XK-88 derivatives and methods for their manufacture
    3.
    发明授权
    1-N-alkyl-aminoglycoside-XK-88 derivatives and methods for their manufacture 失效
    1-N-烷基 - 氨基糖苷-XK-88衍生物及其制备方法

    公开(公告)号：US4002608A

    公开(公告)日：1977-01-11

    申请号：US628638

    申请日：1975-11-04

    申请人： John J. Wright ,  Peter J. L. Daniels ,  Alan K. Mallams ,  Tattanahalli L. Nagabhushan

    发明人： John J. Wright ,  Peter J. L. Daniels ,  Alan K. Mallams ,  Tattanahalli L. Nagabhushan

    IPC分类号： C07H15/236 ,  C07H15/22

    CPC分类号： C07H15/234

    摘要： 1-N-Alkyl-Aminoglycoside-XK-88 derivatives, valuable as antibacterial agents, are prepared by the reaction of an acid addition salt of the corresponding 1-N-unsubstituted-Aminoglycoside-XK-88 antibacterial derivative or of a 2"-N-alkanoyl-Aminoglycoside-XK-88-5 derivative in an inert solvent, preferably a protic solvent containing water, with one equivalent of a hydride-donor reducing agent and with at least one equivalent of an aldehyde.The 2"-N-alkanoyl-Aminoglycoside-XK-88-5 intermediates are prepared by the reaction of a partially neutralized acid addition salt of Aminoglycoside-XK-88-5 with an acylating agent, and isolating the 2"-N-alkanoyl-Aminoglycoside-XK-88-5.

    摘要翻译： 通过使相应的1-N-未取代的氨基糖苷-XK-88抗菌衍生物的酸加成盐或2“的N-取代的氨基糖苷-XK-88衍生物作为抗菌剂有价值的1-N-烷基 - 氨基糖苷-XK-88衍生物， -N-烷酰基 - 氨基糖苷-XK-88-5衍生物在惰性溶剂中，优选含有水的质子溶剂与一当量的氢化物供体还原剂和至少一当量的醛反应。

    1-N-aminohydroxyacyl derivatives of gentamicin B
    4.
    发明授权
    1-N-aminohydroxyacyl derivatives of gentamicin B 失效
    庆大霉素B的1-N-氨基羟基酰基衍生物

    公开(公告)号：US4283528A

    公开(公告)日：1981-08-11

    申请号：US32808

    申请日：1979-04-24

    申请人： Peter J. L. Daniels ,  Tattanahalli L. Nagabhushan

    发明人： Peter J. L. Daniels ,  Tattanahalli L. Nagabhushan

    IPC分类号： C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/236

    摘要： 1-N-(R-.beta.-amino-.alpha.-hydroxypropionyl) gentamicin B, 1-N-(R-.gamma.-amino-.alpha.-hydroxybutyryl) gentamicin B, 1-N-(R-.delta.-amino-.alpha.-hydroxyvaleryl) gentamicin B and the corresponding diastereoisomers derived from the respective S-aminohydroxy acids and the acid addition salts thereof exhibit substantial antibacterial activity, especially against strains of bacteria which are resistant to gentamicin B and acid addition salts thereof.

    摘要翻译： 1-N-（R-β-氨基-α-羟基丙酰基）庆大霉素B，1-N-（R-γ-氨基-α-羟基丁酰基）庆大霉素B，1-N-（R-α-氨基-α-羟基戊酰基 ）庆大霉素B和衍生自相应的S-氨基羟酸及其酸加成盐的相应的非对映异构体表现出显着的抗菌活性，特别是抗庆大霉素B及其酸加成盐的细菌菌株。

    2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, method for their use as antibacterial agents, and compositions useful therefor
    5.
    发明授权
    2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, method for their use as antibacterial agents, and compositions useful therefor 失效
    2'-脱氧-2'-脱氨基-4,6-二-O-（氨基糖基）-1,3-二氨基环糊精，其制备方法，其用作抗菌剂的方法和可用于其的组合物

    公开(公告)号：US4212859A

    公开(公告)日：1980-07-15

    申请号：US912603

    申请日：1978-06-05

    申请人： Peter J. L. Daniels ,  Stuart McCombie ,  Tattanahalli L. Nagabhushan

    发明人： Peter J. L. Daniels ,  Stuart McCombie ,  Tattanahalli L. Nagabhushan

    IPC分类号： C07H15/234 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： 2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols having a 6'-amino function exhibit antibacterial activity and are prepared by reaction of the corresponding N-protected (except the 2'-amino)-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol with hydrogen peroxide in the presence of tungstate ion, followed by cleavage of the thereby formed 2'-oximino derivative, thence reduction of the resulting 2'-oxo derivative and removal of the N-protecting groups.Preferred compounds are 1-N-(.omega.-amino-.alpha.-hydroxyalkanoyl)-2'-hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols which exhibit antibacterial activity against bacteria resistant to the parent aminoglycoside.

    摘要翻译： 具有6'-氨基功能的2'-羟基-2'-脱氨基-4,6-二-O-（氨基糖基）-1,3-二氨基二醇具有抗菌活性，并通过相应的N-保护（除 2'-氨基）-4,6-二-O-（氨基糖基）-1,3-二氨基环糊精与过氧化氢在钨酸根离子存在下，然后裂解由此形成的2'-肟基衍生物，从而减少 得到的2'-氧代衍生物和N-保护基团的除去。 优选的化合物是对细菌具有抗菌活性的1-N-（ω-氨基-α-羟基烷酰基）-2'-羟基-2'-脱氨基-4,6-二-O-（氨基糖基）-1,3-二氨基二醇 对母体氨基糖苷类具有抗性。

    5-Epi-amino and 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines 1-N-alkyl-5-epi-amino and 1-N-alkyl-5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines
    9.
    发明授权
    5-Epi-amino and 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines 1-N-alkyl-5-epi-amino and 1-N-alkyl-5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines 失效
    5-EPI-氨基和5-EPI-AZIDO-4,6-DI-O-（氨基甲酰基）-2,5-二羧基甲苯胺1-N-烷基-5-丙烯酰胺和1-N-烷基-5-EPI -AZIDO-4,6-DI-O-（氨基甲酰基）-2,5-二脱氧酪氨酸

    公开(公告)号：US4000262A

    公开(公告)日：1976-12-28

    申请号：US611290

    申请日：1975-09-08

    申请人： Peter J. L. Daniels

    发明人： Peter J. L. Daniels

    IPC分类号： C07H15/234 ,  C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234 ,  C07H15/22 ,  C07H15/236

    摘要： 5-Epi-azido- and 5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines and 1-N-alkyl derivatives thereof, valuable as antibacterial agents, are prepared from the corresponding 5-O-hydrocarbonsulfonyl (or substituted hydrocarbonsulfonyl)-4,6-di-O-(aminoglycosyl)-2-deoxystreptamine wherein all other hydroxyl functions and all amino functions are protected, by the reaction thereof with an alkali metal azide in an organic solvent followed by the reaction of the resulting 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamine with base to remove the protecting groups, or with hydrogen in the presence of a catalyst or with an alkali metal in liquid ammonia, and thence cleavage of any remaining hydroxyl and amino protecting groups in the thereby formed 5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamine or 1-N-alkyl derivative thereof.In addition to the foregoing, methods are described whereby the 1-N-alkyl-5-epi-azido and 1-N-alkyl-5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines are prepared from the corresponding 1-N-unsubstituted-5-epi-azido and 1-N-unsubstituted-5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines.Pharmaceutical compositions comprising 5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines, 1-N-alkyl-5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines, 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines and 1-N-alkyl-5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines elicit an antibacterial response in a warm blooded animal having a susceptible bacterial infection.

    Method of isolating gentamicin C.sub.2a
    10.
    发明授权
    Method of isolating gentamicin C.sub.2a 失效
    分离庆大霉素C（HD 2a

    公开(公告)号：US3984395A

    公开(公告)日：1976-10-05

    申请号：US498495

    申请日：1974-08-19

    申请人： Peter J. L. Daniels ,  Joseph A. Marquez

    发明人： Peter J. L. Daniels ,  Joseph A. Marquez

    IPC分类号： C07H15/236 ,  C07H15/22

    CPC分类号： C07H15/236 ,  Y10S435/863 ,  Y10S435/865

    摘要： Fermentation of Micromono spora purpurea NRRL 2953 under controlled aerobic conditions produces a plurality of antibiotic substances including gentamicin C.sub.2a which has been heretofore unknown and unrecognized. A method of isolating said antibiotic is described as are the chemical and biological properties of the same.

    摘要翻译： 在受控的有氧条件下发酵微生物紫草NRRL 2953产生了许多抗生素物质，包括迄今为止未知和未被认识的庆大霉素C2a。 描述了分离所述抗生素的方法是其化学和生物学特性。