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    • 5. 发明授权
    • Nylon-3 co-polymers and synthetic lung surfactant compositions containing same
    • 尼龙-3共聚物和含有它们的合成肺表面活性剂组合物
    • US09044392B2
    • 2015-06-02
    • US13634576
    • 2011-03-17
    • Samuel H. GellmanShannon S. StahlBrendan P. MoweryAnnelise BarronMichelle Dohm
    • Samuel H. GellmanShannon S. StahlBrendan P. MoweryAnnelise BarronMichelle Dohm
    • C08G69/22A61K31/785A61P11/00C08G69/48A61K9/00A61K47/32C08L77/02
    • A61K31/785A61K9/0082A61K47/32C08G69/22C08L77/02
    • Non-natural oligomers have recently shown promise as functional analogues of lung surfactant proteins Band C (SP-B and SP-C), two helical and amphiphilic proteins that are clitical for normal respiration. The generation of non-natural mimics of SP-B and SP-C has previously been restlicted to step-by-step, sequence-specific synthesis, which results in discrete oligomers that are intended to manifest specific structural attributes. Presented herein an alternative approach to SP-R mimicry that is based on sequence-random copolymers containing cationic and lipophilic subunits. These materials, members of the nylon-3 family, arc prepared by ling-opening polymelization of 13-lactams. The best of the nylon-3 polymers display promising in vitro surfactant activities in a mixed lipid film. Pulsating bubble surfactometry data indicate that films containing the most surface-active polymers attain adsorptive and dynamic-cycling properties that surpass those of discrete peptides intended to mimic SP-B.
    • 近来,非天然低聚物已经表现出作为肺表面活性蛋白质C(SP-B和SP-C)的功能类似物的前景,两种螺旋和两亲性蛋白质对于正常呼吸是关键的。 SP-B和SP-C的非天然模拟物的产生以前已经被逐步地排列为序列特异性合成,其导致旨在表现特定结构特征的离散低聚物。 本文提出了基于含有阳离子和亲脂亚单元的序列无规共聚物的SP-R模拟的替代方法。 这些材料是尼龙-3族的成员,通过开启13-内酰胺的多聚化来制备。 最好的尼龙-3聚合物在混合脂质膜中显示出有希望的体外表面活性剂活性。 脉冲气泡表面测量数据表明,含有最多表面活性聚合物的膜具有超过旨在模拟SP-B的离散肽的吸附和动态循环性能。