- Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase
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Influenza viruses (Flu) are responsible for seasonal epidemics causing high rates of morbidity, which can dramatically increase during severe pandemic outbreaks. Antiviral drugs are an indispensable weapon to treat infected people and reduce the impact on
- Massari, Serena,Bertagnin, Chiara,Pismataro, Maria Chiara,Donnadio, Anna,Nannetti, Giulio,Felicetti, Tommaso,Di Bona, Stefano,Nizi, Maria Giulia,Tensi, Leonardo,Manfroni, Giuseppe,Loza, Maria Isabel,Sabatini, Stefano,Cecchetti, Violetta,Brea, Jose,Goracci, Laura,Loregian, Arianna,Tabarrini, Oriana
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- Synthesis method of iridium-containing complex
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The invention discloses a synthesis method of an iridium-containing complex. The synthesis method is characterized in that a compound Ir (La) (Lb) 2 is prepared through one-step reaction of a substance shown in the specification and La in the presence of one or more solvents or in the absence of solvents. The synthesis method is suitable for an iridium-containing complex containing two same bidentate C-N ligands and one bidentate 1, 3-diketone, 1, 3-dithione or 1, 3-diimine ligand. Compared with the traditional synthesis method, the synthesis method has higher synthesis efficiency, can be carried out under milder reaction conditions, and can realize the synthesis of some complexes which cannot be realized by the traditional method. The iridium-containing complex prepared by the synthesis method is easier to be used in production and manufacturing of organic electroluminescent devices.
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Paragraph 0141-0144
(2020/08/02)
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- Cu-Catalyzed Denitrogenative Transannulation of 3-Aminoindazoles to Assemble 1-Aminoisoquinolines and 3-Aminobenzothiophenes
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We disclose a novel Cu-catalyzed denitrogenative transannulation of 3-aminoindazoles to afford diverse functionalized 3-aminobenzothiophenes and 1-aminoisoquinolines, in which denitrogenative transannulation of 3-aminoindazoles is reported for the first t
- Zhou, Yao,Wang, Ya,Lou, Yixian,Song, Qiuling
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p. 8869 - 8873
(2019/09/12)
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- From cycloheptathiophene-3-carboxamide to oxazinone-based derivatives as allosteric HIV-1 ribonuclease H inhibitors
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The paper focussed on a step-by-step structural modification of a cycloheptathiophene-3-carboxamide derivative recently identified by us as reverse transcriptase (RT)-associated ribonuclease H (RNase H) inhibitor. In particular, its conversion to a 2-aryl-cycloheptathienoozaxinone derivative and the successive thorough exploration of both 2-aromatic and cycloheptathieno moieties led to identify oxazinone-based compounds as new anti-RNase H chemotypes. The presence of the catechol moiety at the C-2 position of the scaffold emerged as critical to achieve potent anti-RNase H activity, which also encompassed anti-RNA dependent DNA polymerase (RDDP) activity for the tricyclic derivatives. Benzothienooxazinone derivative 22 resulted the most potent dual inhibitor exhibiting IC50s of 0.53 and 2.90 μM against the RNase H and RDDP functions. Mutagenesis and docking studies suggested that compound 22 binds two allosteric pockets within the RT, one located between the RNase H active site and the primer grip region and the other close to the DNA polymerase catalytic centre.
- Massari, Serena,Corona, Angela,Distinto, Simona,Desantis, Jenny,Caredda, Alessia,Sabatini, Stefano,Manfroni, Giuseppe,Felicetti, Tommaso,Cecchetti, Violetta,Pannecouque, Christophe,Maccioni, Elias,Tramontano, Enzo,Tabarrini, Oriana
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- COMPOUND FOR ORGANIC OPTOELECTRIC DEVICE, ORGANIC OPTOELECTRIC DEVICE AND DISPLAY DEVICE
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The present invention relates to a compound for an organic photoelectronic device, the organic photoelectronic device comprising the same, and a display device comprising the organic photoelectronic device, wherein the compound for an organic photoelectronic device is represented by chemical formula 1. In the chemical formula 1, A1, A2, X, R1 to R5, L1 to L3 are the same as defined in the specification.
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Paragraph 0124-0126; 0130; 0131
(2017/01/26)
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- Bicarbazole containing compounds for OLED
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The present disclosure generally relates to novel compounds containing carbazole and triazine with different number of phenyl units attached to its core. In particular, the disclosure relates to compositions and/or devices comprising these compounds as ho
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Paragraph 0072-0073
(2015/02/02)
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- Organic electroluminescent materials and devices
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The present disclosure provides novel compounds based on azadibenzothiophenes, azadibenzofurans and azadibenzoselenophenes with at least two nitrogen atoms in the aza rings. The compounds can be used in green, red, yellow and white emitting devices as electron-transporting hosts.
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Paragraph 0070
(2015/09/23)
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- DONOR-ACCEPTOR COMPOUNDS WITH NITROGEN CONTAINING HETEROPOLYAROMATICS AS THE ELECTRON ACCEPTOR
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Disclosed is a light emitting substance that is used as an emitter in an organic light emitting diode. The light emitting substance includes a donor-acceptor compound having a high triplet energy heteropoly aromatic system. In other words, the donor-acceptor compound includes dibenzofuran, dibenzothiophene, and dibenzoselenophene that are electron acceptors and have multiple nitrogen atoms in one ring. The compound is represented by Chemical Formula 1 below.COPYRIGHT KIPO 2015
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Paragraph 0186; 0187
(2016/10/10)
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- New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: Synthesis, spectroscopic studies, and biological activity
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New benzothieno[3,2-d]-1,2,3-triazines, together with precursors triazenylbenzo[b]thiophenes, were designed, synthesized and screened as anticancer agents. The structural features of these compounds prompted us to investigate their DNA binding capability
- Lauria, Antonino,Alfio, Alessia,Bonsignore, Riccardo,Gentile, Carla,Martorana, Annamaria,Gennaro, Giuseppe,Barone, Giampaolo,Terenzi, Alessio,Almerico, Anna Maria
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supporting information
p. 3291 - 3297
(2014/07/22)
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- Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b] thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents
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Two new series of inhibitors of tubulin polymerization based on the 2-(alkoxycarbonyl)-3-(3′,4′,5′-trimethoxyanilino)benzo[b] thiophene and thieno[2,3-b]pyridine molecular skeletons were synthesized and evaluated for antiproliferative activity on a panel
- Romagnoli, Romeo,Baraldi, Pier Giovanni,Kimatrai Salvador, Maria,Preti, Delia,Aghazadeh Tabrizi, Mojgan,Bassetto, Marcella,Brancale, Andrea,Hamel, Ernest,Castagliuolo, Ignazio,Bortolozzi, Roberta,Basso, Giuseppe,Viola, Giampietro
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supporting information
p. 2606 - 2618
(2013/05/09)
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- PYRIDO [3',2' :4,5] THIENO [3, 2-D] PYRIMIDIN- 4 - YLAMINE DERIVATIVES AND THEIR THERAPEUTICAL USE
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The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain fused triaryl amine compounds of the following formula (for convenience, collectively referred to herein as "FTA compounds"), which, inter alia, inhibit LIM kinase (LIMK) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit LIMK activity, and in the treatment of diseases and conditions that are mediated by LIMK, that are ameliorated by the inhibition of LIMK activity, etc., including proliferative conditions such as cancer (e.g., breast cancer, prostate cancer, melanoma, glioma, etc.), as well as vasodilation (including, e.g., hypertension, angina, cerebral vasospasm, and ischemia following subarachnoid hemorrhage), neurodegenerative disorders, atherosclerosis, fibrosis, and inflammatory diseases (including, e.g., Crohn's disease and chronic obstructive pulmonary disease (COPD)), and glaucoma (also known as ocular hypertension).
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Page/Page column 85
(2012/10/18)
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- New efficient synthesis of 2-substituted benzothieno[3,2-d]pyrimidin-4(3H)- ones via a tandem aza-Wittig reaction
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1-Aryl-3-[2-(ethoxycarbonyl)benzothien-3-yl]carbodiimides 4, obtained from aza-Wittig reactions of iminophosphorane 3 with aryl isocyanates, reacted with secondary amines, phenols, or alkanols in the presence of a catalytic amount of potassium carbonate o
- Xu, Sheng-Zhen,Hu, Yang-Gen,Ding, Ming-Wu
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p. 4180 - 4186
(2008/03/13)
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- A preparative route to fused 4-hydroxy-3-phenylindeno(benzothieno)pyridin-2-ones
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Syntheses of fused 4-hydroxy-3-phenylindeno(benzothieno)-pyridin-2-one derivatives (1a,b) are described.
- Genevois-Borella, Arielle,Vuilhorgne, Marc,Mignani, Serge
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p. 317 - 322
(2007/10/03)
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- Synthesis of [1]Benzothieno[3,2-d]pyrimidines Substituted with Electron Donating Substituents on the Benzene Ring
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Various 2-fluorobenzonitriles were converted to the corresponding 3-amino[1]benzothiophenecarboxylic acid esters, which in turn were annulated with formamidine or various equivalents to produce the desired tricyclic benzothienopyrimidines. Various methoxy and nitro/amino substituants were placed on the phenyl ring, requiring several different strategies to prepare the desired benzothiophenes. Several different pyrimidone annulations were also required. The use of an electron rich 2-bromobenzonitrile in a four-step one-pot low temperature lithiation sequence to produce highly electron-rich amino[1]benzothiophenecarboxylate esters is also described. The synthesis of 7-amino-8-fluoro[1]benzothieno[3,2-d]pyrimid-4(3H)-one was relatively straightforward, but synthesis of the corresponding 7-amino-8-protio analogue proved to be very difficult, and required several approaches before a successful one was found.
- Bridges, Alexander J.,Zhou, Hairong
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p. 1163 - 1172
(2007/10/03)
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