89671-31-8 = 86933-74-6 反应条件:1.1 Catalysts: Subtilisin Solvents: Dimethylformamide,Tert-Butyl Methyl Ether; 16 H,37 °C1.2 Reagents: Trifluoroacetic Acid,Triisopropylsilane,Water; 60 Min,Rt 标题:Enzymatic Fragment Condensation Of Side Chain-Protected Peptides Using Subtilisin A In Anhydrous Organic Solvents: A General Strategy For Industrial Peptide Synthesis 作者:Nuijens,Timo; Et Al 参考文献:Advanced Synthesis & Catalysis 日期:2013 卷标:355(2-3) 页码:287-293]
86933-74-6 = 86933-74-6 反应条件:1.1 Reagents: Trifluoroacetic Acid,Triisopropylsilane Solvents: Water; 2 H,Rt 标题:N-Terminus Fitc Labeling Of Peptides On Solid Support: The Truth Behind The Spacer 作者:Jullian,Magali; Et Al 参考文献:Tetrahedron Letters 日期:2009 卷标:50(3) 页码:260-263]
99029-63-7 + 101536-48-5 = 86933-74-6 反应条件:1.1 Reagents: Trifluoroacetic Acid1.2 Reagents: Triethylamine Solvents: Dimethylformamide2.1 Reagents: Dimethyl Sulfide,Thioanisole,M-Cresol,Trifluoromethanesulfonic Acid Solvents: Trifluoroacetic Acid 标题:Studies On Peptides. Cxxviii. Application Of New Heterobifunctional Crosslinking Reagents For The Preparation Of Neurokinin (A And B)-Bsa (Bovine Serum Albumin) Conjugates 作者:Fujii,Nobutaka; Et Al 参考文献:International Journal Of Peptide & Protein Research 日期:1985 卷标:26(2) 页码:121-9]
101536-49-6 = 86933-74-6 反应条件:1.1 Reagents: Dimethyl Sulfide,Thioanisole,M-Cresol,Trifluoromethanesulfonic Acid Solvents: Trifluoroacetic Acid 标题:Studies On Peptides. Cxxviii. Application Of New Heterobifunctional Crosslinking Reagents For The Preparation Of Neurokinin (A And B)-Bsa (Bovine Serum Albumin) Conjugates 作者:Fujii,Nobutaka; Et Al 参考文献:International Journal Of Peptide & Protein Research 日期:1985 卷标:26(2) 页码:121-9]
86933-74-6 + 97185-84-7 = 86933-74-6 反应条件:1.1 Reagents: Triethylamine,S-[3-Oxo-3-(2-Thioxo-3-Thiazolidinyl)Propyl] Ethanethioate Solvents: Dimethylformamide,Water1.2 Reagents: Triethylamine,Hydroxyamine Hydrochloride Solvents: Water1.3 Reagents: Triethylamine,Hydroxyamine Hydrochloride Solvents: Water1.4 Reagents: Hydrochloric Acid Solvents: Dimethylformamide,Water1.5 Reagents: 4-Methylmorpholine Solvents: Dimethylformamide,Water 标题:Studies On Peptides. Cxxviii. Application Of New Heterobifunctional Crosslinking Reagents For The Preparation Of Neurokinin (A And B)-Bsa (Bovine Serum Albumin) Conjugates 作者:Fujii,Nobutaka; Et Al 参考文献:International Journal Of Peptide & Protein Research 日期:1985 卷标:26(2) 页码:121-9
专利号:US-9475814-B2 优先权日:2011-10-03 标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof 发明人:HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC 权利人:EUROSCREEN SA 摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
专利号:WO-9108220-A1 优先权日:1989-12-01 标 题:A method for the stepwise, controlled synthesis of chemical species, particularly peptides, coupled products obtained by the method and the use of these coupled products, e.g. as vaccines 发明人:HOUEN GUNNAR; HOLM ARNE 权利人:HOUEN GUNNAR; HOLM ARNE 摘要:Chemical species, particularly peptides, are synthesized by a stepwise, controlled process, in which a proteinaceous substance such as a protein is used as the synthesis substrate. The products obtained by the process can be used e.g. as vaccines against various diseases and as matrix materials or carrier molecules.
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-6600970-B2 优先权日:2000-09-06 标 题:Method of establishing synthesis paths 发明人:BLEY KLEMENS 权利人:MERCK PATENT GMBH 摘要:A method of establishing a synthesis path in a multiplicity of potentially interlinakable reactions, and a computer program to prepare a synthesis path.
专利号:US-2022401561-A1 优先权日:2019-09-30 标题 :Protein-macromolecule conjugates and methods of use thereof 发明人:SONG YUNTAO; LI HUI; ZHOU HAIPING; LIAO CHUAN 权利人:BEIJING XUANYI PHARMASCIENCES CO LTD 摘要:The present disclosure provides protein-macromolecule conjugates, releasable linkers, and macromolecules, as defined herein. The disclosed conjugates provide unique properties that ae based at least upon the properties of linker and number of linker-Macromolecule moieties. Also provided herein are a method of synthesis and use of conjugates in treating diseases and disorders.
专利号:US-6420110-B1 优先权日:1998-10-19 标 题 :Methods and reagents for isolating biologically active peptides 发明人:GYURIS JENO; MORRIS AARON J 权利人:GPC BIOTECH INC 摘要:One aspect of the present invention is the synthesis of a binary method that combines variegated peptide display libraries, e.g., in a “display modeâ€?, with soluble secreted peptide libraries, e.g., in a “secretion modeâ€?, to yield a method for the efficient isolation of peptides having a desired biological activity.
1: Jankowska E, Błaszak M, Kowalik-Jankowska T. Copper(II) complexes of neurokinin A with point mutation (S5A) and products of copper-catalyzed oxidation; role of serine residue in peptides containing neurokinin A sequence. J Inorg Biochem. 2013 Apr;121:1-9. doi: 10.1016/j.jinorgbio.2012.11.010. Epub 2012 Dec 7. doi: 10.1016/j.jinorgbio.2010.03.016. Epub 2010 Apr 11. doi: 10.1016/j.fertnstert.2016.07.007. Epub 2016 Jul 25. doi: 10.1002/eji.201141845. Epub 2011 Dec 27. Plasma, hypothalamus, anterior and posterior pituitary. J Neurosci Res. 1996 Sep 1;45(5):598-609. doi: 10.1262/jrd.2014-109. Epub 2014 Oct 27. 10: Sun J, Usune S, Zhao Y, Migita K, Katsuragi T. Multidrug resistance protein transporter and Ins(1,4,5)P₃-sensitive Ca²+-signaling involved in adenosine triphosphate export via Gq protein-coupled NK₂-receptor stimulation with neurokinin A. J Pharmacol Sci. 2010;114(1):92-8. Epub 2010 Aug 21. Epub 2007 May 24. 14: Goso C, Astolfi M, Parlani M, Manzini S. [3H][beta-Ala8]neurokinin A-(4-10): a novel, selective radioligand for the tachykinin NK2 receptor. Eur J Pharmacol. 1995 Dec 27;294(1):239-45. doi: 10.1016/j.npep.2012.07.005. Epub 2012 Aug 29. doi: 10.1258/acb.2010.010024.
合成参考文献
参考文献:10.1016/0162-3109(96)00038-0 摘要:Srivastava VP, Goodfellow VS, Zuzack JS, Jones S, Francis M, Beckey VE, Whalley ET. Hybrid peptides having mixed substance P (NK1), neurokinin A (NK2) and bradykinin (BK2) antagonist properties. Immunopharmacology. 1996 Jun;33(1-3):194–7. doi: 10.1016/0162-3109(96)00038-0. 参考文献:10.1016/s0022-3565(25)20983-1|10.1163/2211730x96x00225 摘要:Mussap CJ, Stamatakos C, Burcher E. Radioligand binding, autoradiographic and functional studies demonstrate tachykinin NK-2 receptors in dog urinary bladder. The Journal of Pharmacology and Experimental Therapeutics. 1996 Oct;279(1):423–34. doi: 10.1016/s0022-3565(25)20983-1. 参考文献:10.1111/j.1472-8206.1996.tb00584.x 摘要:Floch A, Thiry C, Cavero I. Pharmacological evidence that NK-2 tachykinin receptors mediate hypotension in the guinea pig but not in the rat. Fundam Clin Pharmacol. 1996;10(4):337–43. doi: 10.1111/j.1472-8206.1996.tb00584.x. 参考文献:10.1111/j.1472-8206.1996.tb00588.x 摘要:Naline E, Cui YY, Michel A, Bonnet PA, Bakdach H, Advenier C. Effects of SCA40 on human bronchi and on guinea pig main bronchi in vitro. Comparison with cromakalim. Fundam Clin Pharmacol. 1996;10(4):368–78. doi: 10.1111/j.1472-8206.1996.tb00588.x. 参考文献:10.1002/(sici)1097-4547(19960901)45:5<598::aid-jnr9>3.0.co;2-7 摘要:Duval P, Lenoir V, Moussaoui S, Garret C, Kerdelhué B. Substance P and neurokinin A variations throughout the rat estrous cycle; comparison with ovariectomized and male rats: I. Plasma, hypothalamus, anterior and posterior pituitary. J Neurosci Res. 1996 Sep 01;45(5):598–609. doi: 10.1002/(sici)1097-4547(19960901)45:5<598::aid-jnr9>3.0.co;2-7.