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    • 1. 发明公开
    • BETA-HAIRPIN PEPTIDOMIMETICS
    • BETA-HAIRPIN多肽
    • EP3201218A1
    • 2017-08-09
    • EP15778875.3
    • 2015-09-29
    • Polyphor AG
    • OBRECHT, DanielLUTHER, AnatolBERNARDINI, FrancescaDENIAU, GildasLEDERER, Alexander
    • C07K7/64
    • C07K7/64A61K38/00Y02A50/473
    • Beta-hairpin peptidomimetics of the general formula (I), cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2], and pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
    • 通式(I)的β-发夹肽模拟物,环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2]及其药学上可接受的盐与 P1至P12,T1和T2是说明书和权利要求书中定义的元素,对例如,具有Gramegative抗微生物活性 抑制生长或杀死微生物如肺炎克雷伯氏菌和/或鲍曼不动杆菌和/或大肠杆菌。 它们可以用作治疗或预防感染的药物,或用作食品,化妆品,药​​物或其他含营养物质的消毒剂。 这些肽模拟物可以通过基于混合固相和液相合成策略的方法制造。