专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2010022767-A1 优先权日:2008-07-25 标题 :Development of a synthesis of syringolin a and b and derivatives thereof 发明人:KAISER MARKUS; CLERC JEROME 权利人:MAX PLANCK GESELLSCHAFT 摘要:The synthesis of syringolin A and B and derivatives thereof as well as to pharmaceutical compositions containing the syringolin A or B or derivatives thereof and the use of syringolin A and B and derivatives thereof for prophylaxis and treatment of cancer.
专利号:US-8044173-B2 优先权日:2005-09-13 标 题 :Asymmetric synthesis of peptides 发明人:HARWOOD LAURENCE M; YAN RAN 权利人:UNIV READING 摘要:A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR 8 , where R 8 is C 1-6 alkyl, C 6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemisation, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.
专利号:US-8399612-B2 优先权日:2005-09-13 标 题 :Asymmetric synthesis of peptides 发明人:HARWOOD LAURENCE M; YAN RAN 权利人:HARWOOD LAURENCE M; YAN RAN; UNIV READING 摘要:A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR 8 , where R 8 is C 1-6 alkyl, C 6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemization, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerization.
专利号:US-6495693-B2 优先权日:1996-11-22 标题:N-(aryl/heteroaryl) amino acid derivatives, 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; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; PORTER WARREN J; THORSETT EUGENE D; WU JING 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-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 beta-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-6248866-B1 优先权日:1997-10-31 标 题:Hypusine reagent for peptide synthesis 发明人:BERGERON JR RAYMOND J 权利人:UNIV FLORIDA 摘要:A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as an improved method for synthesizing the same, the derivative having the formula:wherein: Q1 and Q2 may be the same or different and are amino protective groups; Q3 is an amino protective group which is orthogonal to Q1 and Q2; and Z is a hydroxy protective group.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1007/bf00811333 摘要:Krois D, Lehner H. Chiral discrimination in biliverdin (S)-amino acids, II: Structural variations of the amino acid functional groups. Monatshefte für Chemie - Chemical Monthly. 1986 Oct 01;117(10):1205–17. doi: 10.1007/bf00811333.