专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-3957760-A 优先权日:1970-12-16 标 题:Amino acid derivatives 发明人:BODANSZKY MIKLOS 权利人:SQUIBB & SONS INC 摘要:New lactone intermediates useful in the synthesis of peptides are prepared by reacting an α-amino acid with an active carbonyl compound which forms a Schiff's base. The latter is treated with a condensing agent so that cyclization occurs and a lactone is formed from which a peptide may be produced by reaction with an amino acid ester and removal of the protecting groups.
专利号:US-2007243581-A1 优先权日:2004-04-21 标题:Process for Producing Dipeptides 发明人:HASHIMOTO SHIN-ICHI; TABATA KAZUHIKO; NOGUCHI AYAKO; ADACHI YUGO 权利人:HASHIMOTO SHIN-ICHI; TABATA KAZUHIKO; NOGUCHI AYAKO; ADACHI YUGO 摘要:The present invention provides: a protein having dipeptide-synthesizing activity or a protein for dipeptide synthesis; DNA encoding the protein having dipeptide-synthesizing activity or the protein for dipeptide synthesis; a recombinant DNA comprising the DNA; a transformant carrying the recombinant DNA; a process for producing the protein having dipeptide-synthesizing activity; an enzymatic process for producing a dipeptide using the protein having dipeptide-synthesizing activity or the protein for dipeptide synthesis; and a process for producing a dipeptide using, as an enzyme source, a culture of a microorganism or a transformant having the ability to produce the protein having dipeptide-synthesizing activity or the protein for dipeptide synthesis, or the like.
专利号:US-7439350-B2 优先权日:1993-09-17 标题 :Nucleotide analogs 发明人:BISCHOFBERGER NORBERT W; JONES ROBERT J; ARIMILLI MURTY N; LIN KUEI-YING; LOUIE MICHAEL S; MCGEE LAWRENCE R; PRISBE ERNEST J; LEE WILLIAM A; CUNDY KENNETH C 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.
参考文献:10.1023/a:1010492713247 摘要:Nikitin VP, Kozyrev SA, Shevelkin AV. NMDA Glutamate Receptor Antagonists Selectively Affect the Synaptic Mechanisms of Nociceptive Sensitization in Snails. Neuroscience and Behavioral Physiology. 2001 Jul;31(4):421–7. doi: 10.1023/a:1010492713247. 摘要:P. L. Kirk and C. L. A. Schmidt. J. Biol. Chem. 81, 237 (1929).