专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-2018297925-A1 优先权日:2015-10-12 标题 :Methods for total synthesis of resolvin e1 发明人:JAGTAP PRAKASH 权利人:SALZMAN LOVELACE INVEST LTD 摘要:Methods for total chemical synthesis of Resolvin E1 (RvE1) include Wittig reaction of two compounds having hydroxyl protecting group in the presence of a strong base, removal of the hydroxyl-protecting groups with a deprotecting reagent to produce a compound having an ester group, and hydrolysis of the ester group to obtain RvE1
专利号:US-6271379-B1 优先权日:2000-03-08 标题:Intermediates useful for the synthesis of huperzine A 发明人:TUECKMANTEL WERNER; KOZIKOWSKI ALAN P 权利人:UNIV GEORGETOWN 摘要:Intermediates useful for the synthesis of huperzine A represented by the structures below, n and methods for their synthesis, wherein: n R 1 is lower alkyl, benzyl, or substituted benzyl; n X is a suitable leaving group; n Y is an electron withdrawing group that can subsequently be converted into an amino group; n one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.
专利号:US-6262251-B1 优先权日:1995-10-19 标题 :Method for solution phase synthesis of oligonucleotides 发明人:PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING 权利人:PROLIGO LLC 摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides. The method lends itself to automation and is ideally suited for large scale manufacture of oligonucleotides with high efficiency.
专利号:US-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-5808019-A 优先权日:1994-12-19 标题 :Intermediate compounds for the synthesis of glycolipids 发明人:HASEGAWA AKIRA; KISO MAKOTO; ISOGAI YUKIHIRO; KITAMURA SEIICHI; UEDA HIROSHI 权利人:TOA BOSHOKU KABUSHIKI KAISHA 摘要:The invention provides important intermediate compounds for the synthesis of acidic glycolipids which are identical with the glycolipid antigens isolated from the acidic glycolipid fractions of peripheral nerve and embryonic central nervous system and preparation methods thereof. By the adoption of the present intermediate compounds, sulfation of 3-hydroxyl group of end glucuronic acid portion of the acidic glycolipid can be quite easily carried out and total synthetic yield be greatly improved.
1: Miura M, Nishino M, Kawaguchi K, Li S, Shimakami T, Tamai T, Nakagawa H, Terashima T, Iida N, Takatori H, Arai K, Sakai Y, Yamashita T, Honda M, Kaneko S, Mizukoshi E, Yamashita T. Programmed cell death-1 is involved with peripheral blood immune cell profiles in patients with hepatitis C virus antiviral therapy. PLoS One. 2024 May 23;19(5):e0299424. doi: 10.1371/journal.pone.0299424. 2: Moon C, Porges E, Roberts A, Bacon J. A combination of nirmatrelvir and ombitasvir boosts inhibition of SARS-CoV-2 replication. Antiviral Res. 2024 May;225:105859. doi: 10.1016/j.antiviral.2024.105859. Epub 2024 Mar 14. 169(3):45. doi: 10.1007/s00705-024-05990-z. 257(Pt 2):128672. doi: 10.1016/j.ijbiomac.2023.128672. Epub 2023 Dec 11. 11:1179531. doi: 10.3389/fpubh.2023.1179531.
合成参考文献
参考文献:10.1007/s40265-014-0232-6 摘要:Bichoupan K, Dieterich DT. Hepatitis C in HIV-infected patients: impact of direct-acting antivirals. Drugs. 2014 Jun;74(9):951–61. doi: 10.1007/s40265-014-0232-6. 参考文献:10.1128/aac.01778-15 摘要:Badri PS, Dutta S, Wang H, Podsadecki TJ, Polepally AR, Khatri A, Zha J, Chiu YL, Awni WM, Menon RM. Drug Interactions with the Direct-Acting Antiviral Combination of Ombitasvir and Paritaprevir-Ritonavir. Antimicrob Agents Chemother. 2016 Jan;60(1):105–14. 参考文献:10.1016/j.jhep.2015.10.005 摘要:Feld JJ, Moreno C, Trinh R, Tam E, Bourgeois S, Horsmans Y, Elkhashab M, Bernstein DE, Younes Z, Reindollar RW, Larsen L, Fu B, Howieson K, Polepally AR, Pangerl A, Shulman NS, Poordad F. Sustained virologic response of 100% in HCV genotype 1b patients with cirrhosis receiving ombitasvir/paritaprevir/r and dasabuvir for 12weeks. J Hepatol. 2016 Feb;64(2):301–7. doi: 10.1016/j.jhep.2015.10.005.