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专利信息

专利号:US-9242925-B2
优先权日:2011-08-29
标题:Versatile and stereospecific synthesis of γ,δ-unsaturated amino acids by Wittig reaction
发明人：JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE
权利人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE; CENTRE NAT RECH SCIENT; UNIV BOURGOGNE
摘要:The γ,δ-unsaturated α-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). n n n n n n n n n n n n Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.

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-5783577-A
优先权日:1995-09-15
标题 :Synthesis of quinazolinone libraries and derivatives thereof
发明人：HOUGHTEN RICHARD A; OSTRESH JOHN M
权利人:TREGA BIOSCIENCES INC
摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.

专利号:WO-9710221-A1
优先权日:1995-09-15
标 题:Synthesis of quinazolinone libraries
发明人：HOUGHTEN RICHARD A; OSTRESH JOHN M
权利人:TORREY PINES INST
摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.

专利号:US-6664282-B2
优先权日:1999-09-17
标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds
发明人：ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A
权利人:TORREY PINES INST
摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.

专利号:WO-9967219-A1
优先权日:1998-06-22
标 题:Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
发明人：AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING
权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING
摘要:Compounds of formula (I), wherein W is a cyclic group of the type (2); (3); Y is represented by the formula (II); these compounds inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.