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8 条记录 (耗时 0.016 秒)

    Pradimicin derivatives
    5.
    发明公开
    Pradimicin derivatives 失效
    普拉定霉素衍。

    公开(公告)号：EP0428132A1

    公开(公告)日：1991-05-22

    申请号：EP90121709.1

    申请日：1990-11-13

    申请人： Bristol-Myers Squibb Company

    发明人： Kamachi, Hajime ,  Iimura, Seiji ,  Okuyama, Satsuki ,  Aburaki, Shimpei ,  Naito, Takayuki ,  Ueda, Yasutsugu ,  Crast, Leonard B., Jr. ,  Mikkilineni, Amarendra B.

    IPC分类号： C07H15/244 ,  A61K31/71

    CPC分类号： C07H15/244

    摘要： The present invention provides pradimicin analogs of formula (II) which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.
    wherein R¹ is selected from the group consisting of H, methyl, and hydroxymethyl, and when R¹ is methyl or hydroxymethyl, the resulting amino acid has the D -configuration;
    R² is H or β-D-xylosyl;
    R³ is H or methyl; and
    R⁴ is selected from the group consisting of (C₂₋₅)alkenyl; (C₂₋₅)alkynyl; substituted (C₁₋₅)alkyl; substituted (C₂₋₅)alkenyl; wherein the substituent for both the alkyl and alkenyl is a group selected from the group consisting of, carboxy, (C₁₋₅)alkoxycarbonyl, carbamyl, (C₁₋₅)alkylcarbamyl, di(C₁₋₅)alkylcarbamyl, and sulfonyl; (C₁₋₅)alkanoyl substituted with a group selected from the group consisting of amino, (C₁₋₅)alkylamino, and di(C₁₋₅)alkylamino; L-glutamyl; formyl; benzyl; and p-tolylsulfonylcarbamyl; or
    a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供了相对于母体化合物表现出改善的水溶性的式（II）的普拉迪霉素类似物。 这些新型药剂可用于治疗真菌感染。 其中R 1选自H，甲基和羟甲基，当R 1为甲基或羟甲基时，得到的氨基酸具有D-构型; R 2是H或β-D-木糖基; R 3是H或甲基; 和R 4选自（C 2-5）烯基; （C 2-5）炔基; 取代的（C 1-5）烷基; 取代的（C2-5）烯基; 其中烷基和链烯基的取代基是选自羧基，（C 1-5）烷氧基羰基，氨基甲酰基，（C 1-5）烷基氨基甲酰基，二（C 1-5）烷基氨基甲酰基和磺酰基的基团。 被选自氨基，（C 1-5）烷基氨基和二（C 1-5）烷基氨基的基团取代的（C 1-5）烷酰基; L-谷氨酰; 甲酰基; 苄基; 和对甲苯磺酰基氨基甲酰基; 或其药学上可接受的盐。

    Cephalosporin derivatives
    8.
    发明公开
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：EP0727426A2

    公开(公告)日：1996-08-21

    申请号：EP96400295.0

    申请日：1996-02-13

    申请人： BRISTOL-MYERS SQUIBB COMPANY

    发明人： Kim, Choung U. ,  Misco, Peter F. ,  Wichtowski, John A. ,  Ueda, Yasutsugu ,  Hudyma, Thomas W. ,  Matiskella, John D. ,  D'Andrea, Stanley W. ,  Hoeft, Shelley E. ,  Miller, Raymond F. ,  Mansuri, Muzammil M. ,  Bronson, Joanne J.

    IPC分类号： C07D501/36 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： Novel cephem derivatives represented by the general formula

    in which the Acyl substituent is a group of the formula

    wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R 1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R 2 and R 3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).

    摘要翻译： 由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团其中Ar是亲脂性的任选取代的苯基，萘基，吡啶基或苯并噻唑基; R1选自某些任选取代的脂族，芳族，芳基脂族或糖部分，R2和R3各自独立地为氢，烷基或氨基烷基羰基氨基为革兰氏阳性抗菌剂，特别用于治疗由耐甲氧西林金黄色葡萄球菌引起的感染性疾病 MRSA）。