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-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:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related 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: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 权利人: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 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:US-4520193-A 优先权日:1980-11-20 标题 :Cephalosporin derivatives 发明人:BERGER CHRISTIAN; FARGE DANIEL; MOUTONNIER CLAUDE; WOLFF GERARD 权利人:RHONE POULENC IND 摘要:The invention provides new cephalosporin derivatives of the general formula, ##STR1## which are in the form of a bicyclooct-2-ene or bicyclooct-3-ene, in which formula R 1 is a radical of the general formula ##STR2## [in which R 5 is hydrogen, alkyl, vinyl, cyanomethyl, protected carboxyalkyl or a protective radical and R 6 is a protective radical] or an amino-protecting radical, R 2 is an acid-protecting radical and R° represents various organic radicals, or alternatively R 1 is an amino-protecting radical or various acyl radicals, R 2 is a protective radical and R° represents various organic radicals, and R 3 and R 4 are alkyl radicals optionally substituted by alkoxy or dialkylamino, or phenyl radicals, or --NR 3 R 4 forms a heterocyclic ring. These products are intermediates for the synthesis of cephalosporins having antibacterial activity.
专利号:US-3994883-A 优先权日:1972-12-27 标 题 :Penicillin and cephalosporin intermediates 发明人:BORREVANG POUL; GUDDAL ERLING; PETERSEN HENNING BORGE; FAARUP PETER; NIELSEN JORGEN ILUM 权利人:NOVO INDUSTRI AS 摘要:Novel penicillin and cephalosporin intermediates for the synthesis of 6-APA or 7-aminocephem compounds involving formation of a 6 or 7 phosphite amido compound and the conversion of such compound to a desired 6-APA or 7-aminocephem compound.
专利号:US-2004106598-A1 优先权日:1998-06-22 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
参考标题:Studies On Cardiotonic Agents. Iv. Synthesis Of Novel 1-(6,7-Dimethoxy-4-Quinazolinyl)Piperidine Derivatives Carrying Substituted Hydantoin And 2-Thiohydantoin Rings. 作者:Yuji Nomoto,Haruki Takai,Tadashi Hirata,Masayuki Teranishi,Tetsuji Ohno,Kazuhiro Kubo 摘要:7-Dimethoxy-4-Quinazolinyl)Piperidines Carrying Substituted Hydantoin And 2-Thiohydantoin Rings Was Synthesized And Examined For Cardiotonic Activity In Anesthetized Dogs. Introduction Of Isopropyl And Sec-Butyl Group At The 5-Position Of The Hydantoin And Thiohydantoin Rings Led To Potent Inotropic Activity. Effects Of Insertion Of An Alkyl Chain Between The Piperidine And The Hydantoin Rings Were
合成参考文献
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