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    • 5. 发明申请
    • PLEUROMUTILIN DERIVATIVES FOR USE IN THE TREATMENT OF DISEASES MEDIATED BY MICROBES
    • 用于治疗由MICROBES介导的疾病的胰岛素衍生物
    • US20130274329A1
    • 2013-10-17
    • US13821446
    • 2011-08-11
    • Rosemarie RiedlKlaus ThirringWerner Heilmayer
    • Rosemarie RiedlKlaus ThirringWerner Heilmayer
    • C07C323/52
    • C07C323/52A61K31/235A61K45/06C07C2601/04C07C2601/08C07C2601/18C07C2602/42C07C2602/44C07C2603/99
    • Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.
    • 选自N-取代或N-烷基化或N-酰化的14-O- [(氨基(C 0-4)烷基 - 羟基 - 环烷基 - 或双环烷基硫烷基) - 乙酰基] - 木霉素的化合物是14-O- [ (氨基(C0-4)烷基 - 羟基 - 环丁基硫烷基) - 乙酰基] - 木兰林,14-O - [(氨基(C0-4)烷基 - 羟基 - 环戊基硫烷基) - 乙酰基] - 木霉素,14-O - [ (C0-4)烷基 - 羟基 - 环庚基硫烷基) - 乙酰基] - 木兰林,14-O - [(氨基(C0-4)烷基 - 羟基 - 环辛基硫烷基) - 乙酰基] - 木兰林,或14-O - [(氨基 C0-4)烷基 - 羟基 - 双环烷基硫烷基) - 乙酰基] - 木素,任选呈盐和/或溶剂化物形式,包含这些化合物的药物组合物及其作为药物的用途,例如 用于治疗微生物感染和治疗痤疮,任选地与其它药物活性剂组合。