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    • 63. 发明授权
    • Medicaments comprising sialic acid derivatives as active ingredients
    • 包含唾液酸衍生物作为活性成分的药物
    • US06664235B1
    • 2003-12-16
    • US09640776
    • 2000-08-18
    • Osamu KanieChi-Huey WongYasuo Suzuki
    • Osamu KanieChi-Huey WongYasuo Suzuki
    • A61K317028
    • A61K31/7012
    • A medicament for treatment of a viral infection which comprises as an active ingredient a compound represented by the following formula (I) or its Pharmaceutically acceptable salt, or a hydrate thereof or a solvate thereof. wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 represents an optionally substituted phenyl group, a C1-20 alkyl group, a C1-20 alkenyl group, or—(CH2)k—[NH—(CH2)m—NH]n—Y or —(CH2)k—[NH—(CH2CH2O)m-1—CH2CH2NH]n—Y in which Y represents phosphatidylethanolamine residue or polyglutamic acid residue, k and m independently represent an integer of from 2 to 10, n represents 0 or 1, provided that when n represents 1, Y represents phosphatidylethyl group; R3 represents hydrogen atom or an optionally substituted hydroxyl group; R4 represents hydrogen atom, a halogen atom, azide group, an optionally substituted amino group, or an optionally substituted hydroxyl group; and R5, R6, R7 and R8 independently represent an optionally substituted hydroxyl group.
    • 一种用于治疗病毒感染的药物,其包含作为活性成分的由下式(I)表示的化合物或其药学上可接受的盐或其水合物或其溶剂合物。其中R 1表示氢原子或C1 -6烷基; R 2表示任选取代的苯基,C 1-20烷基,C 1-20链烯基或 - (CH 2)k - [NH-(CH 2)m -NH] n Y或 - (CH 2) [NH-(CH2CH2O)m-1-CH2CH2NH] nY其中Y表示磷脂酰乙醇胺残基或聚谷氨酸残基,k和m独立地表示2至10的整数,n表示0或1,条件是当n表示1时, Y表示磷脂酰乙基; R 3表示氢原子或任选取代的羟基; R 4表示氢原子,卤素原子,叠氮基,任选取代的氨基或任选取代的羟基; R 5,R 6,R 7和R 8独立地表示任选取代的羟基。
    • 67. 发明授权
    • Enzymatic sulfation of biomolecules
    • 生物分子的酶硫酸化
    • US06255088B1
    • 2001-07-03
    • US09393013
    • 1999-09-10
    • Chi-Huey WongMichael D. Burkart
    • Chi-Huey WongMichael D. Burkart
    • C12P1100
    • C12N9/13
    • Enzymatic sulfations of biomolecules catalyzed by 3′-phosphoadenosine-5′-phosphosulfate (PAPS) dependent sulfotransferases are enhanced by coupling the sulfation reaction an enzymatic regeneration of PAPS. The PAPS is enzymatically regenerated from its hydrolysis product 3′,5′-diphosphate (PAP) using recombinant aryl sulfotransferase as the catalyst and aryl sulfate as the substrate. Biomolecules capable of enhanced sulfation by this method include carbohydrates, oligosaccharides, peptides, proteins, flavonoids, and steroids. When enzymatic sulfation and substrate regeneration steps are coupled, the desulfated aryl group produced in the regeneration step has a spectroscopic signature that can be employed for monitoring the progress of the sulfation of the biomolecule.
    • 通过将硫酸化反应与PAPS的酶促再生耦合,增强了由3'-磷酸腺苷-5'-磷酸硫酸酯(PAPS)依赖的磺基转移酶催化的生物分子的酶促硫酸化。 使用重组芳基磺基转移酶作为催化剂和芳基硫酸盐作为底物,将PAPS从其水解产物3',5'-二磷酸(PAP)酶促再生。 能够通过该方法增强硫酸化的生物分子包括碳水化合物,寡糖,肽,蛋白质,类黄酮和类固醇。 当酶促硫酸化和底物再生步骤偶联时,在再生步骤中产生的脱硫芳基具有可用于监测生物分子的硫酸化进程的光谱特征。