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-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-2005164912-A1 优先权日:2003-12-31 标 题:Methods for recovering cleaved peptide from a support after solid phase synthesis 发明人:BIGELOW ROGER D; CAIN ROBERT O 摘要:Methods for the solid phase synthesis of peptides and peptide intermediates, in particular methods involving recovering peptides from resin supports at excellent yield. In this invention, an alternating at least partially repeating cycle of shrinking and swelling treatments are used. Each shrinking or swelling part of a cycle may involve one or more washes. The process provides excellent recovery of peptide in a very efficient manner in terms of the number of individual washes and the total volume of wash reagents used.
专利号:US-5990273-A 优先权日:1993-06-29 标 题:Synthesis of cyclic peptides 发明人:ANDERSSON LARS HENRIK HARALD; SKOLDBACK JAN-AKE 权利人:FERRING BV 摘要:A process for preparing and purifying cyclic peptides having disulfide moieties in a two step processing operation including reverse phase chromatography which simplifies synthesis and reduces production costs, yet produces high, quality yield. The improved process is particularly useful for the preparation of vasopressin and oxytocin and their respective derivatives and analogs.
专利号:US-2008300418-A1 优先权日:2004-11-08 标 题:Synthesis of Cardiolipin Analogues and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
1: Belletti A, Musu M, Silvetti S, Saleh O, Pasin L, Monaco F, Hajjar LA, Fominskiy E, Finco G, Zangrillo A, Landoni G. Non-Adrenergic Vasopressors in Patients with or at Risk for Vasodilatory Shock. A Systematic Review and Meta-Analysis of Randomized Trials. PLoS One. 2015 Nov 11;10(11):e0142605. doi: 10.1371/journal.pone.0142605. eCollection 2015. Review. 2: Cavallin M, Fasolato S, Marenco S, Piano S, Tonon M, Angeli P. The Treatment of Hepatorenal Syndrome. Dig Dis. 2015;33(4):548-54. doi: 10.1159/000375346. Epub 2015 Jul 6. Review. doi: 10.1371/journal.pone.0107466. eCollection 2014. 4: Celis P, Rada G. Noradrenaline or terlipressin for hepatorenal syndrome? Medwave. 2015 Aug 27;15 Suppl
合成参考文献
参考文献:10.1042/bst0080105 摘要:Jones GR, Baum R, Merkel R, Schwarz M. Disturbance to energy production in vivo caused by hormones and sympathomimetics in the S180 sarcoma, with consequent drug-induced necrosis [proceedings]. Biochem Soc Trans. 1980 Feb;8(1):105. doi: 10.1042/bst0080105. 参考文献:10.1016/0024-3205(80)90165-4 摘要:Berntson GG, Berson BS. Antinociceptive effects of intraventricular or systemic administration of vasopressin in the rat. Life Sci. 1980 Feb 11;26(6):455–9. doi: 10.1016/0024-3205(80)90165-4. 摘要:Sirakov M. [Application of Remestip for genital hemorrhages in pubescent youth]. Akush Ginekol (Sofiia). 2000;40 Suppl 3():17–8. 参考文献:10.1007/s002100100439 摘要:Ramírez MC, Martínez-Cuesta MA, D'Ocon P, Noguera MA, García-Zaragoza E, Bosch J, Melin P, Esplugues JV. Comparative effects of the novel vasotocin analogue F-180 vs. vasopressin and terlipressin on systemic and splanchnic isolated vessels from portal hypertensive rats. Naunyn Schmiedebergs Arch Pharmacol. 2001 Sep;364(3):199–204. doi: 10.1007/s002100100439. 摘要:Primo J, Molés JR, Fernández J, Llorca P, Hinojosa J. [Terlipressin in the treatment of portal hypertension]. Gastroenterol Hepatol. 1999 May;22(5):258–60.