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-2019276389-A1 优先权日:2015-12-18 标题:Synthesis of aryl cyclohexane ester derivatives useful as sensates in consumer products 发明人:WOS JOHN AUGUST; YELM KENNETH EDWARD; BUNKE GREGORY MARK; FREDERICK HEATH ALAN; REILLY MICHAEL; HAUGHT JOHN CHRISTIAN; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Personal care compositions, such as oral care and skin care compositions containing a flavor/perfume system comprising one or more coolants. The pleasant cool sensation provided by a coolant is enhanced in terms of quicker onset, greater intensity, impact or longer duration, which improves appeal and acceptability of the compositions to consumers.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include 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.
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.
专利号:WO-9966934-A1 优先权日:1998-06-22 标 题 :CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS 发明人:AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 摘要:Disclosed are compounds which 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.
专利号:US-6774125-B2 优先权日:1998-06-22 标 题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which 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.
参考标题:Racemization Free Longer N-Terminal Peptide Hydroxamate Synthesis On Solid Support Using Ethyl 2-(Tert-Butoxycarbonyloxyimino)-2-Cyanoacetate 作者:Srinivasa Rao Manne,Kishore Thalluri,Rajat Subhra Giri,Ashim Paul,Bhubaneswar Mandal |发布日期:2015.10 摘要:Protocol For The Synthesis Of Peptide Hydroxamic Acids Directly From Carboxylic/amino Acids By Ethyl 2-(Tert-Butoxycarbonyloxyimino)-2-Cyanoacetate In The Presence Of Dipea/dmap At Room Temperature Is Described. The Compatibility Of This Method With Fmoc Based Solid Phase Peptide Synthesis (Spps) Is Also Demonstrated By Synthesizing Three Relatively Large N-Terminal Peptide Hydroxamic Acids On Resin. Also
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