专利号:US-10730904-B2 优先权日:2012-11-14 标 题:Method for liquid-phase synthesis of nucleic acid 发明人:NONOGAWA MITSURU; NAGATA TOSHIAKI; SAITO HIDEKI; YASUMA TSUNEO 权利人:TAKEDA PHARMACEUTICALS CO 摘要:In this method, an oligonucleotide represented by formula (II) [wherein Y 1 , Q, Base, r and r′ are each as defined in claim 1 ] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 and n are each as defined in claim 1 ]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
专利号:US-10799441-B2 优先权日:2011-06-06 标题:Skin treatments containing pyrroloquinoline quinone (PQQ) esters and methods of preparation and use thereof 发明人:LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C 权利人:LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C; PCR TECH HOLDINGS LC 摘要:The present invention relates to cosmetic or dermatological compositions containing PQQ or its esters, methods of treating or promoting skin changes by topical application of these compositions, and methods of synthesis of PQQ esters. The PQQ ester-containing compositions of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the PQQ esters of the present invention have an antioxidant effect that is useful in treating a skin change.
专利号:US-2009326223-A1 优先权日:2006-07-18 标题 :Synthesis of 2-amino-substituted 4-oxo-4h-chromen-8.yl-trifluoro-methanesulfonic acid esters 发明人:GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS 权利人:GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS 摘要:A method of synthesising a compound of formula (I): wherein R N1 and R N2 are independently selected from hydrogen, an optionally substituted C 1-7 alkyl group, C 3-20 heterocyclyl group, or C 5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; from a compound of formula (III): comprising the steps of: (a) removing the allyl group from the compound of formula (III) with appropriate reaction conditions to yield a compound of formula (II): and (b) reacting the compound of formula (II) with a triflating agent to yield a compound of formula (I).
专利号:US-2015315229-A1 优先权日:2012-11-14 标 题 :Method for liquid-phase synthesis of nucleic acid
专利号:US-10214555-B2 优先权日:2012-11-14 标题 :Method for liquid-phase synthesis of nucleic acid
专利号:US-2019135852-A1 优先权日:2012-11-14 标题 :Method for liquid-phase synthesis of nucleic acid
参考标题:Synthesis Of 2,3-Dihydrobenzo[b][1,4]Dioxine-5-Carboxamide And 3-Oxo-3,4-Dihydrobenzo[b][1,4]Oxazine-8-Carboxamide Derivatives As Parp1 Inhibitors 作者:Xuwei Shao,Steven Pak,Uday Kiran Velagapudi,Shruthi Gobbooru,Sai Shilpa Kommaraju,Woon-Kai Low,Gopal Subramaniam,Sanjai Kumar Pathak,Tanaji T. Talele |发布日期:2020.9 摘要:Using Recombinant Parp1 Enzyme Assay That Resulted In The Acquisition Of Three Parp1 Inhibitors: 3 (Ic50 = 12 μm), 4 (Ic50 = 5.8 μm), And 10 (Ic50 = 0.88 μm). Compound 4 (2,3-Dihydro-1,4-Benzodioxine-5-Carboxamide) Was Selected As A Lead And It Was Subjected To Further Chemical Modifications, Involving Analogue Synthesis And Scaffold Hopping. These Efforts Led To The Identification Of (Z)-2-(4-Hydroxy
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摘要:J. Sunkel and H. Staude, Ber. Bunsenges. Physik. Chem. 72, 567 (1968).