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    • 3. 发明申请
    • Solid- and solution-phase synthesis of heparin and other glycosaminoglycans
    • 固相和溶液相合成肝素和其他糖胺聚糖
    • US20030013862A1
    • 2003-01-16
    • US10054724
    • 2002-01-22
    • Peter H. SeebergerHernan OrgueiraPeter Schell
    • C07H013/02C07H005/04
    • C07H3/06C07H3/04C08B37/0075
    • Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specific sequences involved in receptor binding holds great promise for the development of molecular tools which will allow modulation of processes underlying viral entry, angiogenesis, kidney diseases and diseases of the central nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.
    • 描述了一种模块化的,一般的合成策略,用于制备溶液和固体支持肝素,肝素样糖胺聚糖,糖胺聚糖和它们各自的非天然类似物。 此外,模块化策略为制备组合文库和定义的糖胺聚糖寡糖的平行文库提供了基础。 所定义的糖胺聚糖结构可用于高通量筛选实验以鉴定调节宿主识别和信号转导过程的碳水化合物序列。 涉及受体结合的具体序列的确定对于分子工具的开发具有很大的希望,这将允许调节病毒进入,血管生成,肾脏疾病和中枢神经系统疾病的过程。 值得注意的是,本发明能够以与肽和寡核苷酸当前组装的大致相同的方式自动合成糖胺聚糖。
    • 6. 发明申请
    • Trans-acidolysis process for the preparation of carbohydrate fatty-acid esters
    • 用于制备碳水化合物脂肪酸酯的反式酸解过程
    • US20020120133A1
    • 2002-08-29
    • US10050402
    • 2002-01-15
    • Olobo Jonathan Obaje
    • C07H013/02
    • C07H13/04Y02P20/582
    • The present invention relates to a low temperature, solvent-free trans-acidolysis process for preparing surface-active carbohydrate fatty-acid esters comprising the steps of: (e) reacting acylated carbohydrate with free fatty acid in the presence of acid catalyst, under reduced pressure, and without adding any solvent; (f) decolorizing and separating the reaction mixture obtained in step (a) into unreacted fatty acid layer and a carbohydrate fatty-ester layer; (g) precipitating out the unreacted acylated carbohydrate; (h) librating the hydroxyl groups by partial hydrolysis in the presence of an acid catalyst; (i) removing the unreacted free fatty acids and unreacted carbohydrate esters of low molecular-weight carboxylic acids during purification, and recycling the removed unreacted free fatty acids and carbohydrate esters to the starting reactant mixture.
    • 本发明涉及一种用于制备表面活性碳水化合物脂肪酸酯的低温无溶剂的反式酸解方法,包括以下步骤:(e)在酸催化剂存在下,将酰化碳水化合物与游离脂肪酸反应, 压力,不加任何溶剂; (f)将步骤(a)中获得的反应混合物脱色并分离成未反应的脂肪酸层和碳水化合物脂肪酸酯层; (g)沉淀未反应的酰化碳水化合物; (h)在酸催化剂存在下,通过部分水解来回收羟基; (i)在纯化期间除去低分子量羧酸的未反应游离脂肪酸和未反应的碳水化合物酯,并将除去的未反应的游离脂肪酸和碳水化合物酯循环到起始反应物混合物中。