专利号:US-6818633-B2 优先权日:2001-06-29 标题:Antiviral compounds and methods for synthesis and therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
专利号:US-7115592-B2 优先权日:2003-06-16 标题:Phosphonate substituted pyrimidine compounds and methods for therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN; HOCKOVA DANA 权利人:BIOCHEMISTRY OF THE ACADEMY OF 摘要:Novel compounds are provided having formula (I) n nwheren n R 1 , R 2 , R 3 , R 4 , Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
专利号:US-5585275-A 优先权日:1992-09-02 标 题 :Pilot apparatus for peptide synthesis and screening 发明人:HUDSON DEREK; JOHNSON CHARLES R; GIEBEL LUTZ 权利人:ARRIS PHARM CORP 摘要:Method and apparatus for simple and rapid preparation of reusable, addressable surface-immobilized arrays of biomolecules (libraries) used for screening for interaction with any biologically significant target. A special plate having on or in its surface a plurality of discreet functionalized substrate areas, typically in arrays of 10x10 to 400x400, is provided for chemical synthesis or bonding thereon of desired families of biomolecules (e.g. peptides, DNA, RNA, oligosaccharides). In the case of peptides, such as hexapeptides, the resulting permanently hexapeptide-loaded plate is a reusable Addressable Synthetic Peptide Combinatorial Library (ASPCL), in which 1 to 3 (typically two) of the positions in the sequence are uniquely identified by the address location. The preferred plate embodiment employs an HPMP wink of porous polyolefin removably received in holes in the plate. A unique multi-slot block assembly is used to prepare the ASPCLs. The wink carrier plate is also employed with a vacuum block system to assist in washing, deprotection, and probing. In library applications, for example determining peptides which bind to functional proteins (enzymes, receptors, antibodies), the substrate-bound peptides are assembled with several positions consisting of uniformly distributed equimolar mixtures of residues, and 2 separated or sequential positions uniquely identified by their spatial location on the substrate array, the 'address'. Following identification of the known residues giving the greatest affinity for the arrayed positions in the sequence, optimal binding for the complete peptide sequence is determined by an iterative process replacing formerly mixed positions with known AAs at unique addresses.
专利号:US-5886179-A 优先权日:1993-09-17 标 题 :Nucleotide analogs 发明人:ARIMILLI MURTY N; BISCHOFBERGER NORBERT W; JONES ROBERT J; LEE WILLIAM A; PRISBE ERNEST J 权利人:GILEAD SCIENCES INC 摘要:Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
专利号:US-5656745-A 优先权日:1993-09-17 标题:Nucleotide analogs 发明人:BISCHOFBERGER NORBERT; JONES ROBERT J; ARIMILLI MURTY; LIN KUEI-YING; LOUIE MICHAEL; MCGEE LAWRENCE R; PRISBE ERNEST J 权利人:GILEAD SCIENCES INC 摘要:Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
参考标题:Microbial Deracemization Of α-Substituted Carboxylic Acids: Substrate Specificity And Mechanistic Investigation 作者:Dai-Ichiro Kato,Satoshi Mitsuda,Hiromichi Ohta |发布日期:2003.9.1 摘要:A New Enzymatic Method For The Preparation Of Optically Active Alpha-Substituted Carboxylic Acids Is Reported. This Technique Is Called Deracemization Reaction, Which Provides Us With A Route To Obtain The Enantiomerically Pure Compounds, Theoretically In 100% Yield Starting From The Racemic Mixture. This Means That The Synthesis Of A Racemate Is Almost Equal To The Synthesis Of The Optically Active
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