Arrays with cleavable linkers
    93.
    发明申请

    公开(公告)号:US20070213297A1

    公开(公告)日:2007-09-13

    申请号:US11645188

    申请日:2006-12-22

    申请人: Chi-Huey Wong

    发明人: Chi-Huey Wong

    IPC分类号: A61K31/716 C40B40/12

    摘要: The invention provides arrays of molecules where the molecules (e.g., glycans) are attached to the arrays by cleavable linkers. The invention also provides methods for using these arrays, methods for identifying the structural elements of molecules bound to these arrays by using the cleavable linkers, especially the structural elements that are important for binding to test samples. The invention further provides methods for evaluating whether test samples and test molecules can bind to distinct glycans on the arrays and useful glycans identified using the methods and arrays provided herein.

    Synthesis of synthons for the manufacture of bioactive compounds
    94.
    发明申请
    Synthesis of synthons for the manufacture of bioactive compounds 审中-公开
    用于生产生物活性化合物的合成子的合成

    公开(公告)号:US20070015260A1

    公开(公告)日:2007-01-18

    申请号:US11481653

    申请日:2006-07-05

    IPC分类号: C08B37/00 C12P19/02 C12N9/24

    摘要: The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.

    摘要翻译: 本发明基于以下发现:2-脱氧核糖-5-磷酸醛缩酶(DERA,EC 4.1.2.4)及其变体可用于催化多种供体和受体醛之间的顺序不对称醛醇反应。 反应产物通常含有至少两个新的立体中心并且可以以对映体纯的形式制备。 因此,DERA催化的不对称醛醇化学可以被利用来产生用于合成各种生物活性分子的合成物。

    Mannosyl transfer with regeneration of GDP-mannose

    公开(公告)号:US07018824B2

    公开(公告)日:2006-03-28

    申请号:US11145810

    申请日:2005-06-06

    申请人: Chi-Huey Wong

    发明人: Chi-Huey Wong

    IPC分类号: C12N9/10 C12N15/54 C12N15/70

    摘要: A one-pot glycosylation reaction is disclosed in which a mannosyl (Man) group is enzymatically transferred to an acceptor molecule. The starting glycoside is a mannosyl 1-phosphate that is enzymatically converted to its GDP derivative via UTP and a pyrophorylase. The formed GDP derivative is used in the enzyme-catalyzed glycosyl transfer. That enzyme-catalyzed glycosyl transfer to an acceptor releases GDP that is enzymatically converted to GTP for further conversion of mannosyl 1-phosphate into its GDP derivative. Also disclosed are a recombinant α1,2-mannosyltransferase that is enzymatically active, is dispersible in an aqueous reaction medium, and free of the transmembrane portion of the native enzyme, as well as DNA encoding that transferase, an expression vector containing exogenous DNA that encodes that enzyme and E. coli cells containing that vector.

    HIV protease inhibitors
    96.
    发明授权
    HIV protease inhibitors 失效
    HIV蛋白酶抑制剂

    公开(公告)号:US06900238B1

    公开(公告)日:2005-05-31

    申请号:US09077712

    申请日:1996-12-09

    摘要: Combinatorial libraries of HIV and FIV protease inhibitors are characterized by α-keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or substituted tyrosines. The libraries are synthesized via a one step coupling reaction. Highly efficacious drug candidates are identified by screening the libraries for binding and inhibitory activity against both HIV and FIV protease. Drug candidates displaying clinically useful activity against both HIV and FIV protease are identified as being potentially resistive against a loss of inhibitory activity due to development of resistant strains of HIV.

    摘要翻译: 艾滋病病毒和FIV蛋白酶抑制剂的组合文库的特征在于α-酮酰胺或羟乙胺核心结构,其侧面为取代的吡咯烷酮,哌啶或氮杂环庚烷,另一侧为苯丙氨酸,酪氨酸或取代的酪氨酸。 文库通过一步偶联反应合成。 通过筛选文库对HIV和FIV蛋白酶的结合和抑制活性来鉴定高效药物候选物。 鉴于HIV和FIV蛋白酶对临床有用的活性的候选药物被鉴定为可能阻止由于HIV的抗性株的发展而导致的抑制活性丧失。

    Medicaments comprising sialic acid derivatives as active ingredients
    98.
    发明授权
    Medicaments comprising sialic acid derivatives as active ingredients 失效
    包含唾液酸衍生物作为活性成分的药物

    公开(公告)号:US06664235B1

    公开(公告)日:2003-12-16

    申请号:US09640776

    申请日:2000-08-18

    IPC分类号: A61K317028

    CPC分类号: A61K31/7012

    摘要: 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.

    摘要翻译: 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。

    Polymer compounds comprising glycosphingosine
    100.
    发明授权
    Polymer compounds comprising glycosphingosine 失效
    含有鞘氨醇的高分子化合物

    公开(公告)号:US06358919B1

    公开(公告)日:2002-03-19

    申请号:US09109870

    申请日:1998-07-06

    IPC分类号: A61K3816

    CPC分类号: A61K47/645

    摘要: A polymer compound or a salt thereof which comprises a biodegradable polymer such as polyglutamic acid acetylated at N-terminal thereof containing a glycosphingolipid such as lysoganglioside GM3, and which exerts antiviral activity against variety of viruses and is useful as an active ingredient of a medicament.

    摘要翻译: 一种高分子化合物或其盐,其包含生物降解性聚合物,例如在其N末端乙酰化的聚谷氨酸,其含有鞘糖脂如溶血性神经节苷脂GM3,并且针对各种病毒发挥抗病毒活性,并且可用作药物的活性成分。