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    • 74. 发明申请
    • NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    • 新型半合成糖苷作为抗菌剂
    • US20120252741A1
    • 2012-10-04
    • US13440692
    • 2012-04-05
    • Daniel ChuTao YeBing Wang
    • Daniel ChuTao YeBing Wang
    • A61K38/14A61P31/04C07K1/06C07K9/00
    • C07K9/006
    • Provided herein are semi-synthetic glycopeptides having antibacterial activity. The semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide 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 with certain acyl groups; conversion of the amide group in amino acid-3 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 to certain substituted amides. Also provided herein are pharmaceutical compositions comprising the semi-synthetic glycopeptides, and methods of use of the semi-synthetic glycopeptides for the treatment and/or prophylaxis of diseases, especially bacterial infections.
    • 本文提供具有抗菌活性的半合成糖肽。 本文所述的半合成糖肽通过在酸性介质中水解母体糖肽的氨基酸-4的二糖部分而使糖肽进行化学修饰来制备,得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 用某些酰基酰化氨基酸4氨基取代的糖部分上的氨基取代基; 氨基酸-3中的酰胺基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上氨基甲基化与含有磺酰胺或酰基磺酰胺基团的取代基; 并将大环上的酸部分转化为某些取代的酰胺。 本文还提供了包含半合成糖肽的药物组合物,以及使用半合成糖肽来治疗和/或预防疾病,特别是细菌感染的方法。
    • 80. 发明申请
    • Masking to prevent overexposure and light spillage in microarray scanning
    • 掩蔽以防止微阵列扫描过度暴露和轻度溢出
    • US20070132831A1
    • 2007-06-14
    • US11302695
    • 2005-12-13
    • Daniel Chu
    • Daniel Chu
    • B41J15/14
    • G01N21/253G01N2201/0446G01N2201/1042
    • Scanning of a microarray is performed through a mask that exposes a plurality, but not all, of the sites of the microarray, and either the mask is movable relative to the microarray or the microarray is movable relative to the mask, or both. The mask is useful as a means of restricting the illumination of sites on the microarray to those that can be illuminated while the scan head is traveling at a steady, target velocity, blocking the passage of light between the scan head and the microarray at those points in the scan head trajectory where the scan head is either accelerating or decelerating. The mask is also useful for reducing background noise in the microarray image by preventing light spillage to sites adjacent to those being scanned.
    • 微阵列的扫描通过暴露微阵列的多个但不是全部的掩模进行,并且掩模相对于微阵列是可移动的,或者微阵列相对于掩模或两者都是可移动的。 该掩模可用作将扫描头以稳定的目标速度行进的情况下将微阵列上的部位的照明限制在可照亮的位置的手段,阻止在那些点处扫描头和微阵列之间的光通过 在扫描头轨迹中扫描头正在加速或减速。 该掩模也可用于通过防止光泄漏到与扫描的那些相邻的位置来减少微阵列图像中的背景噪声。