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11. 发明申请

WO9910359A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO9910359A2
公开(公告)日：1999-03-04
申请号：PCT/EP9805390
申请日：1998-08-25
申请人： NOVARTIS AG , SCRIPPS RESEARCH INST
发明人： WONG CHI-HUEY , LIN CHUN-CHENG , WOLTERING THOMAS J , WEITZ-SCHMIDT GABRIELE
IPC分类号： C07H1/00 , C07H
CPC分类号： C07H1/00
摘要： Liposomic sLe mimetics of formula MIMETIC-LINKER-LIPID and cross-linked liposomic sLe mimetics of formula (I).
摘要翻译：式（I）的脂质体sLe xM模拟物和式（I）的交联脂质体sLe x模拟物。

12. 发明申请

WO9414954A3 KDO ALDOLASE AND CONDENSATION REACTIONS EMPLOYED THEREWITH 审中-公开
标题翻译： KDO ALDOLASE和冷凝反应
公开(公告)号：WO9414954A3
公开(公告)日：1994-09-29
申请号：PCT/US9312367
申请日：1993-12-17
申请人： SCRIPPS RESEARCH INST , WONG CHI HUEY , SUGAI TAKESHI , SHEN GWO JENN
发明人： WONG CHI-HUEY , SUGAI TAKESHI , SHEN GWO-JENN
IPC分类号： C07H7/027 , C12N9/88 , C12P7/58 , C12P9/00 , C12P19/02 , C07H7/02 , C12N1/20
CPC分类号： C12P19/02 , C07H7/027 , C12N9/88 , C12P7/58 , C12P9/00 , Y10S435/822
摘要： Aureobacterium barkerei strain KDO-37-2 (ATCC 49977) KDO aldolase (EC 4.1.2.23) isolated therefrom are disclosed. The DKDO aldolase is further disclosed to have a broad substrate specificity with respect to its reverse reaction, i.e. the condensation of aldoses with pyruvate to form a wide range of 2-keto-3-deoxy-onic acids, including 2-keto-3-deoxy-nonulosonic acid, 2-keto-3-deoxy-octulosonic acid, 2-keto-3-deoxy-heptulosonic acid, and 2-keto-3-deoxy-hexulosonic acid. In particular, 3-deoxy-D-manno-2-octulosonic acid (D-KDO), a vital component of lipopolysaccharides found in the bacterial outer membrane may be synthesized from D-arabinose and pyruvate in 67 % yield. Additionally, protected forms of the KDO aldolase products, e.g. hexaacetyl 2-keto-3-deoxy-nonulosonic acid and pentaacetyl 2-keto-3-deoxy-octulosonic acid, may be decarboxylated to form the corresponding 2-deoxy-aldoses, e.g. 2-deoxy-octulose and 2-deoxy-heptulose respectively.
摘要翻译：公开了从其分离的巴氏杆菌菌株KDO-37-2（ATCC 49977）和KDO醛缩酶（EC 4.1.2.23）。进一步公开KDO醛缩酶相对于其逆反应具有广泛的底物特异性，即醛糖与丙酮酸的缩合形成宽范围的2-酮-3-脱氧酸，包括2-酮-3- 脱氧 - 非酮酸，2-酮-3-脱氧 - 八环酮酸，2-酮-3-脱氧 - 庚酮酸和2-酮-3-脱氧 - 己酸。特别地，在D-细菌外膜中发现的脂多糖的重要组分3-脱氧-D-壬烯-2-辛酮酸（D-KDO）可由D-阿拉伯糖和丙酮酸合成，产率67％。另外，保护形式的KDO醛缩酶产物，例如，六乙酰基2-酮-3-脱氧 - 非酮缩酮酸和五乙酰基2-酮-3-脱氧 - 八环酮酸可以脱羧以形成相应的2-脱氧醛糖，例如。 2-脱氧 - 八酮糖和2-脱氧 - 七氟醚。

13. 发明申请

WO9221655A3 2-METHYL-5-HYDROXYMETHYL- AND 2,5-DIMETHYL-3,4-DIHYDROXYPYRROLIDINES 审中-公开
标题翻译： 2-甲基-5-羟基甲基 - 和2,5-二甲基-3,4-二羟基吡咯烷
公开(公告)号：WO9221655A3
公开(公告)日：1993-01-07
申请号：PCT/US9204408
申请日：1992-05-26
申请人： SCRIPPS RESEARCH INST
发明人： WONG CHI-HUEY , LIU KUN-CHIN
IPC分类号： C07D207/12 , C07D207/46 , C07H7/02 , C07H11/00 , C07D207/44 , A61K31/40 , C07D207/08
CPC分类号： C07D207/46 , C07D207/12 , C07H7/02 , C07H11/00
摘要： 2-Methyl-5-hydroxymethyl- and 2,5-dimethyl-3,4-dihydroxypyrrolidines, their processes of preparation and use are disclosed. 5-Azido-5-deoxy-hexulose-1-phosphate compounds and processes of making the same are also disclosed.

14. 发明专利

CA2553866A1 TREATMENT OF DEGENERATIVE CARTILAGE CONDITIONS IN A MAMMAL WITH GLYCOSI DASE INHIBITORS 未知
公开(公告)号：CA2553866A1
公开(公告)日：2005-08-11
申请号：CA2553866
申请日：2005-01-20
申请人： OPTIMER PHARMACEUTICALS INC
发明人： WONG CHI-HUEY , SHUE YOUE-KONG , OKUMU FRANKLIN W , ICHIKAWA YOSHITAKA , LOTZ MARTIN , ORIDA NORMAN K
IPC分类号： A61K31/55 , A61K9/00 , A61K31/40 , A61K31/435 , A61K31/70 , A61K45/06
摘要： This invention relates to treating, preventing, and lessening the severity o f conditions selected from the group consisting of osteoarthritis, rheumatoid arthritis, synovitis, subchondral bone edema, and cartilage degradation with administration of glycosidase inhibitors.

15. 发明公开

EP1299109A4 BIFUNCTIONAL ANTIBIOTICS 有权
标题翻译：双功能抗生素
公开(公告)号：EP1299109A4
公开(公告)日：2005-06-08
申请号：EP01927464
申请日：2001-04-27
申请人： SCRIPPS RESEARCH INST
发明人： WONG CHI-HUEY , SUCHECK STEVEN
IPC分类号： A61K31/70 , A61K31/704 , C07H15/224 , C07H15/232 , C07H15/234
CPC分类号： C07H15/234 , A61K31/70 , A61K31/704 , A61K47/552 , C07H15/224 , C07H15/232
摘要： Bifunctional antibiotics that target both bacterial RNA and resistance-causing enzymes are disclosed. The A-site of bacterial 16S rRNA serves as the target site for most aminoglycoside antibiotics. Resistance to this class of antibiotics is frequently developed by microbial enzymatic acetylation, phosphorylation or ribosylation of aminoglycosides, modifications that weaken their interactions with the target RNA. Using surface plasmon resonance (SPR), the binding affinity and stoichiometry of various amino-glycosides have been investigated and it was found that neamine, the key pharmacophore of the deoxystreptamine class of amino-glycosides, binds to the A-site in a two to one stoichiometry with a K d of 10 muM for each binding site. A library of neamine dimers was prepared and their affinities to 16S rRNA A-site were determined by SPR, with K d =40 nM for the best dimer (an ~10 3 -fold increase in affinity). Antibiotic activities of the dimers were determined for several bacterial strains by the Kirby-Bauer method. The most active dimer, based on antibiotic activity, also showed the highest inhibition of in vitro translation (IC 50 =0.055 muM). The latter assay was developed in order to correlate the relationship between SPR-based affinity and translation inhibition. By these combined methods, transport limitations for the semisynthetic aminoglycosides as well as non-ribosomally based antibiotic activity could be determined. Further analysis of these dimers as substrates for aminoglycoside modifying-enzymes identified a neamine dimer that was a potent inhibitor (K is =0.1 muM) of the APH(2'') activity of the bifunctional enzyme AAC(6'')-APH(2''), the primary enzyme responsible for high level gentamicin C resistance in several bacterial strains.

16. 发明公开

EP0832275A4 METHOD FOR SYNTHESIZING 2-KETOALDONIC ACIDS 失效
标题翻译： VERFAHREN ZUR SYNTHESE VON 2-KEOTALDONSÄUREN
公开(公告)号：EP0832275A4
公开(公告)日：1998-11-18
申请号：EP96917264
申请日：1996-06-07
申请人： SCRIPPS RESEARCH INST
发明人： WONG CHI-HUEY
IPC分类号： C07H1/08 , C07H7/027 , C07H7/033 , C12N9/88 , C12P7/58 , C12P9/00 , C12P19/02 , C12P7/44 , C12P7/50 , C12P7/60
CPC分类号： C12N9/88 , C07H1/08 , C07H7/027 , C07H7/033 , C12P7/58 , C12P9/00 , C12P19/02
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.
摘要翻译： 2-酮基醛糖酸是通过涉及丙酮酸和醛糖受体的醛缩酶缩合反应在过量丙酮酸存在下合成的。反应基本完成后，通过用丙酮酸脱羧酶处理将过量的丙酮酸从反应混合物中除去。

17. 发明公开

EP1833489A4 GLYCOLIPIDS AND ANALOGUES THEREOF AS ANTIGENS FOR NK T CELLS 审中-公开
标题翻译：糖脂和类似物作为抗原FOR NK T细胞检测
公开(公告)号：EP1833489A4
公开(公告)日：2011-08-03
申请号：EP05857215
申请日：2005-12-27
申请人： UNIV ROCKEFELLER , SCRIPPS RESEARCH INST
发明人： WONG CHI-HUEY , WU DOUG , FUJIO MASAKAZU , TSUJI MORIYA , HO DAVID
IPC分类号： A61K31/70 , C07H15/00
CPC分类号： C07H15/06 , C07H15/00 , C07H15/18 , C07H15/26

18. 发明公开

EP1996609A4 METHOD OF PREPARING GLYCOPEPTIDES 有权
标题翻译：用于生产糖
公开(公告)号：EP1996609A4
公开(公告)日：2010-09-08
申请号：EP07753745
申请日：2007-03-22
申请人： SCRIPPS RESEARCH INST
发明人： WONG CHI-HUEY , BRIK ASHRAF , YANG YU-YING , FICHT SIMON , PAYNE RICHARD
IPC分类号： A61K38/15 , C07C29/00 , C07K11/02 , C12N5/02
CPC分类号： C07K9/00 , C07K9/001

19. 发明公开

EP0873519A4 HIV PROTEASE INHIBITORS 失效
标题翻译： HIV蛋白酶抑制剂
公开(公告)号：EP0873519A4
公开(公告)日：2005-04-27
申请号：EP96943657
申请日：1996-12-09
申请人： SCRIPPS RESEARCH INST
发明人： WONG CHI-HUEY , SLEE DEBORAH H , LASLO KAREN
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 , G01N33/53
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.

20. 发明公开

EP1039886A4 HIV/FIV PROTEASE INHIBITORS HAVING A SMALL P3 RESIDUE 审中-公开
标题翻译：稍微休息P3感染HIV / FIV蛋白酶抑制剂
公开(公告)号：EP1039886A4
公开(公告)日：2001-05-16
申请号：EP98963800
申请日：1998-12-08
申请人： SCRIPPS RESEARCH INST
发明人： LEE TAEKYU , WONG CHI-HUEY , ELDER JOHN H
IPC分类号： A61K38/00 , C07D207/16 , C07D213/40 , C07D217/26 , C07D277/24 , C07D277/28 , C07D401/12 , C07K5/06 , C07K5/062 , C07K5/065 , A61K31/045 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/38 , A61K31/405 , A61K31/47 , A61K38/05 , C07C205/02 , C07C211/09 , C07C215/18 , C07D217/16
CPC分类号： C07D213/40 , A61K38/00 , C07D207/16 , C07D217/26 , C07D277/28 , C07D401/12 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06078
摘要： With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective against HIV and its drug-resistant mutants, as well as FIV. Modification of existing HIV protease inhibitors by reducing the size of the P3 residue has the same effect. This finding provides a new strategy for the development of HIV protease inhibitors effective against the wild type and drug-resistant mutants and further supports that FIV protease is a useful model for drug-resistant HIV proteases, which often are developed through reduction in size of the binding region for the P3 group or the combined P3 and P1 groups.

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