NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    73.
    发明申请
    NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
    新型半合成糖肽作为抗菌剂

    公开(公告)号:WO2010048340A3

    公开(公告)日:2010-07-29

    申请号:PCT/US2009061555

    申请日:2009-10-21

    CPC classification number: C07K9/006

    Abstract: Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of the a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; conversion of the amide group in amino acid-3 on these scaffolds to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid -7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Abstract translation: 描述了具有抗菌活性的半合成糖肽,具体而言,通过化学修饰糖肽(化合物A,化合物B,化合物H或化合物C)或通过水解二糖制备的单糖来制备本文所述的半合成糖肽 亲本糖肽的氨基酸-4的部分在酸性介质中反应以产生氨基酸-4单糖; 将单糖转化为氨基糖衍生物; 用某些酰基将这些支架上的氨基酸-4氨基取代的糖部分上的氨基取代基酰化; 在这些支架上的氨基酸-3中的酰胺基团转化为各种酰基酰胺,酰基磺酰胺,酰基磺酰脲衍生物; 通过曼尼希反应在氨基酸-7上用含有磺酰胺或酰基磺酰胺基团的取代基氨基甲基化; 并将这些支架的大环上的酸部分转化成某些取代的酰胺。 还提供了用于合成所述化合物的方法,含有所述化合物的药物组合物,以及所述化合物用于治疗和/或预防疾病,特别是细菌感染的方法。

    VIDEO DISPLAY DEVICE
    79.
    发明申请
    VIDEO DISPLAY DEVICE 审中-公开
    视频显示设备

    公开(公告)号:WO2005060250A1

    公开(公告)日:2005-06-30

    申请号:PCT/IB2004/052669

    申请日:2004-12-06

    CPC classification number: H04N5/45 H04N21/4316

    Abstract: A video display device comprising a display to display a primary image, originating from a first input signal, and a picture-in-picture (PIP) overlaying the primary image and originating from a second input signal. The display characteristics of the PIP are changed in response to information, preferably a file extension, relating to the type of the first input signal in order to obscure as little as possible of the important parts of the primary image. In case the primary image contains much visual information the PIP is chosen small, positioned in the periphery of the display and/or transparent. In case the primary image contains little visual information the PIP is chosen large, centered and/or non-transparent. Useful for Integrated Digital TV cum Broadband TV (IDTV-BBTV) devices, where the primary image is a broadband image and the PIP is a TV image.

    Abstract translation: 一种视频显示装置,包括显示器,用于显示源自第一输入信号的主图像和覆盖主图像并源自第二输入信号的画中画(PIP)。 PIP的显示特性响应于与第一输入信号的类型相关的信息,优选地是文件扩展名来改变,以便尽可能少地遮蔽主图像的重要部分。 在主图像包含大量视觉信息的情况下,PIP被选择为小的,定位在显示器的外围和/或透明的位置。 如果主图像包含很少的视觉信息,则PIP被选择为大的,居中的和/或不透明的。 适用于集成数字电视暨宽带电视(IDTV-BBTV)设备,其主要图像是宽带图像,PIP是电视图像。

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