DERIVATIVES OF AMPHOTERICIN B
    4.
    发明公开

    公开(公告)号:EP3929203A1

    公开(公告)日:2021-12-29

    申请号:EP21175661.4

    申请日:2016-04-15

    IPC分类号: C07H17/08 A61P31/04 A61P31/10

    摘要: Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3'-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2'epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.

    MACROCYCLIC POLYMORPHS, COMPOSITIONS COMPRISING SUCH POLYMORPHS, AND METHODS OF USE AND MANUFACTURE THEREOF

    公开(公告)号:EP3412678A1

    公开(公告)日:2018-12-12

    申请号:EP18167730.3

    申请日:2008-01-22

    摘要: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (" C . difficile" ) , Clostridium perfringens ( "C. perfringens" ) , Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.

    DERIVATIVES OF AMPHOTERICIN B
    10.
    发明公开
    DERIVATIVES OF AMPHOTERICIN B 审中-公开
    两性霉素B的衍生物

    公开(公告)号:EP3283171A1

    公开(公告)日:2018-02-21

    申请号:EP16780813.8

    申请日:2016-04-15

    IPC分类号: A61P31/10 A61P31/04 C07H17/08

    CPC分类号: C07H17/08

    摘要: Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3′-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2′epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.