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61. 发明授权

US06900238B1 HIV protease inhibitors 失效
标题翻译： 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
申请人： Chi-Huey Wong , Deborah H. Slee , Karen Laslo
发明人： Chi-Huey Wong , Deborah H. Slee , Karen Laslo
IPC分类号： G01N33/15 , A61K31/00 , A61K31/40 , A61K45/00 , A61P31/00 , A61P31/18 , C07B61/00 , C07D207/08 , C07D207/16 , C12N9/99 , C12Q1/02 , C12Q1/37 , A01N43/36 , C07D207/00 , C07F9/02
CPC分类号： C12Q1/37 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/60 , C12Q1/18 , C40B40/04 , G01N2333/16
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。

62. 发明授权

US06774140B1 Iminocyclitol inhibitors of hexoaminidase and glycosidase 失效
标题翻译：己糖胺苷酶和糖苷酶的咪嗪环醇抑制剂
公开(公告)号：US06774140B1
公开(公告)日：2004-08-10
申请号：US09980869
申请日：2002-02-12
申请人： Chi-Huey Wong , Jungie Liu
发明人： Chi-Huey Wong , Jungie Liu
IPC分类号： A61K3140
CPC分类号： C07D207/12 , A61K31/40 , A61K31/4025 , A61K31/445
摘要： Designed iminocylitols that have potent inhibition activity with respect to hexominidases and glycosides are disclosed.
摘要翻译：公开了相对于己糖苷酶和糖苷具有有效抑制活性的设计的亚氨基二醇。

63. 发明授权

US06664235B1 Medicaments comprising sialic acid derivatives as active ingredients 失效
标题翻译：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
申请人： Osamu Kanie , Chi-Huey Wong , Yasuo Suzuki
发明人： Osamu Kanie , Chi-Huey Wong , Yasuo Suzuki
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。

64. 发明授权

US06462193B1 Hydroxyazepanes as inhibitors of glycosidase and HIV protease 失效
标题翻译：羟基氮芥作为糖苷酶和HIV蛋白酶的抑制剂
公开(公告)号：US06462193B1
公开(公告)日：2002-10-08
申请号：US09367919
申请日：1999-08-23
申请人： Chi-Huey Wong , Francisco Moris-Varas
发明人： Chi-Huey Wong , Francisco Moris-Varas
IPC分类号： C07D22308
CPC分类号： G11C11/22 , C07D233/08 , H01L27/11502 , H01L27/11585 , H01L27/1159
摘要： Hydroxyazepanes display inhibitory activity with respect to glycosidase, with Ki values from-moderate to low micromolar range. Benzyl and 3,6-dibenzyl derivatives of hydroxyazepanes display inhibitory activity with respect to HIV protease. These compounds are synthesized either by chemoenzymatic or chemical methodologies.
摘要翻译：羟基氮芥对糖苷酶显示抑制活性，Ki值从中到低微摩尔范围。羟基氮杂环庚烷的苄基和3,6-二苄基衍生物对HIV蛋白酶表现出抑制活性。这些化合物通过化疗或化学方法合成。

65. 发明授权

US06358919B1 Polymer compounds comprising glycosphingosine 失效
标题翻译：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
申请人： Osamu Kanie , Chi-Huey Wong , Hiroshi Kamitakahara
发明人： Osamu Kanie , Chi-Huey Wong , Hiroshi Kamitakahara
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。

66. 发明授权

US06319695B1 Production of fucosylated carbohydrates by enzymatic fucosylation synthesis of sugar nucleotides; and in situ regeneration of GDP-fucose 失效
标题翻译：通过糖核苷酸的酶解岩藻糖基化合成生产岩藻糖基化碳水化合物; 和GDP-岩藻糖的原位再生
公开(公告)号：US06319695B1
公开(公告)日：2001-11-20
申请号：US07961076
申请日：1992-10-14
申请人： Chi-Huey Wong , Yoshitaka Ichikawa , Gwo-Jenn Shen , Kun-Chin Liu
发明人： Chi-Huey Wong , Yoshitaka Ichikawa , Gwo-Jenn Shen , Kun-Chin Liu
IPC分类号： C12P1918
CPC分类号： C07H5/02 , C07H3/06 , C07H11/04 , C07H13/04 , C07H13/08 , C07H15/18 , C07H19/20 , C12P19/18 , C12P19/26
摘要： This invention contemplates improved methods of enzymatic production of carbohydrates especially fucosylated carbohydrates. Improved syntheses of glycosyl 1- or 2-phosphates using both chemical and enzymatic means are also contemplated. The phosphorylated glycosides are then used to produce sugar nucleotides that are in turn used as donor sugars for glycosylation of acceptor carbohydrates. Especially preferred herein is the use of a disclosed method for fucosylation.
摘要翻译：本发明考虑了碳水化合物，特别是岩藻糖基化碳水化合物的酶促生产的改进方法。还考虑了使用化学和酶学方法改进的1或2-磷酸糖基酯的合成。然后将磷酸化糖苷用于产生糖核苷酸，其又被用作供体糖用于受体碳水化合物的糖基化。本文特别优选使用所公开的岩藻糖基化方法。

67. 发明授权

US06255088B1 Enzymatic sulfation of biomolecules 失效
标题翻译：生物分子的酶硫酸化
公开(公告)号：US06255088B1
公开(公告)日：2001-07-03
申请号：US09393013
申请日：1999-09-10
申请人： Chi-Huey Wong , Michael D. Burkart
发明人： Chi-Huey Wong , Michael D. Burkart
IPC分类号： C12P1100
CPC分类号： C12N9/13
摘要： 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.
摘要翻译：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。

68. 发明授权

US6111084A Fuopeptide mimetics 失效
标题翻译：富肽模拟物
公开(公告)号：US6111084A
公开(公告)日：2000-08-29
申请号：US88411
申请日：1998-06-01
申请人： Chi-Huey Wong , Thomas F. J. Lampe
发明人： Chi-Huey Wong , Thomas F. J. Lampe
IPC分类号： C07H5/04 , A61K31/35 , A61K31/351 , A61K31/70 , A61K31/7008 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61K38/00 , A61P7/02 , A61P9/00 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/08 , C07D309/10 , C07H7/02 , C07H15/04 , C07H15/22 , C07K9/00
CPC分类号： C07H15/22 , C07H15/04 , C07H7/02 , C07K9/001 , A61K38/00
摘要： Bioactive fucopeptides and libraries of fucopeptides having advanced activities against P-selectin as sialyl Lewis X mimetics with IC.sub.50 values in the low mM range are synthesized by solid phase synthesis using para-acyloxymethylenzlidene acetal (p-AMBA) as an anchoring group. A rapid parallel synthesis is employed which proceeds with a bi-directional functionalization of glycosylated amino acid derivatives.
摘要翻译：通过使用对酰氧基甲基亚苄基缩醛（p-AMBA）作为锚定基团的固相合成，合成具有针对P-选择蛋白的先进活性的唾液酸肽作为唾液酸基路易斯X模拟物的生物活性uc肽和文库。使用快速并行合成，其进行糖基化氨基酸衍生物的双向官能化。

69. 发明授权

US5766887A Synthesis of 9-0-acetyl N-acetylneuraminic acid oligosaccharides 失效
标题翻译： 9-0-乙酰基N-乙酰神经氨酸寡糖的合成
公开(公告)号：US5766887A
公开(公告)日：1998-06-16
申请号：US703093
申请日：1996-08-26
申请人： Chi-Huey Wong , Shuichi Takayama
发明人： Chi-Huey Wong , Shuichi Takayama
IPC分类号： C07H15/10 , C12P19/26 , C12P19/44 , C12N9/24
CPC分类号： C07H15/10 , C12P19/26
摘要： Regioselective acetylation of the 9-hydroxyl group on N-acetylneuraminic acid is achieved enzymatically for producing oligosaccharides which contain a terminal N-acetylneuraminic acid moiety. This method provides access to O-acylated disialogangliosides as well as other N-acetyl-neuraminic acid oligosaccharides. These compounds are biologically and medicinally important and are difficult to obtain from nature or by chemical acylations. The methodology affords simple reaction conditions and minimal purification steps. In addition, the process affords good yields and the enzymes and reagents employed are commercially available with high stability and low costs.
摘要翻译：在N-乙酰神经氨酸的N-羟基上的区域选择性乙酰化被酶促用于制备含有末端N-乙酰神经氨酸部分的寡糖。该方法提供了获得O-酰化二唾液酸神经节苷脂以及其它N-乙酰神经氨酸寡糖。这些化合物在生物学和医学上是重要的，并且难以从自然或通过化学酰化获得。该方法提供简单的反应条件和最小的纯化步骤。此外，该方法提供良好的产率，所用的酶和试剂可以高稳定性和低成本商业获得。

70. 发明授权

US5759825A Method for synthesizing 2-ketoaldonic acids 失效
公开(公告)号：US5759825A
公开(公告)日：1998-06-02
申请号：US475777
申请日：1995-06-07
申请人： Chi-Huey Wong
发明人： Chi-Huey Wong
IPC分类号： C07H1/08 , C07H7/027 , C07H7/033 , C12N9/88 , C12P7/58 , C12P9/00 , C12P19/02 , C12P7/40 , C07H1/00
CPC分类号： C12N9/88 , C07H1/08 , C07H7/027 , C07H7/033 , C12P19/02 , C12P7/58 , C12P9/00
摘要： 2-Ketoaldonic acid is synthesized by aldolase condensation reaction involving pyruvate and an aldose acceptor in the presence of excess pyruvate. After the reaction is substantially complete, the excess pyruvate is removed from the reaction mixture by treatment with pyruvate decarboxylase.

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