35212-85-2Relevant academic research and scientific papers
EIF4E INHIBITORS AND USES THEREOF
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Paragraph 00506; 00548, (2021/09/11)
The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
One-pot approach to construct benzo[4,5]thieno[3,2-b]indoles, pyrido[3′,2’:4,5]thieno[3,2-b]indoles and pyrazino[2′,3’:4,5]thieno[3,2-b]indoles based on the Fischer indole synthesis
Irgashev, Roman A.,Steparuk, Alexander S.,Rusinov, Gennady L.
supporting information, (2020/11/06)
During this study, series of benzo[4,5]thieno[3,2-b]indoles, pyrido[3′,2’:4,5]thieno[3,2-b]indoles and pyrazino[2′,3’:4,5]thieno[3,2-b]indoles were efficiently synthesized from benzo- and pyrido- or pyrazino-fused 3-aminothiophene-2-carboxylates, respectively, using one-pot two-step strategy based on the Fischer indolization reaction. The essence of this synthetic approach is acid-promoted reaction of the 3-aminothiophene intermediates, in situ generated from the corresponding ring-fused 3-aminothiophene-2-carboxylates, with arylhydrazines to give arylhydrazones of thiophen-3(2H)-ones, followed by their indolization to afford thieno[3,2-b]indole-cored molecules.
Red phosphorescent compound and organic light-emitting device using same
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Page/Page column 27, (2019/05/08)
The invention relates to a red phosphorescent compound and an organic light-emitting tube device using the same, in particular to a soluble phosphorescent compound with excellent color purity, high brightness and high light-emitting efficiency, and an organic light emitting diode (OLED) device using the same. The structural formula of the phosphorescent compound is shown as (I) (please see the specifications for the formula); in the structural formula (I), Z is independently selected from the following structure (please see the specifications for the formula (I)), wherein Ar is independently selected from one of C6-C30 aryl and C2-C30 heteroaryl, the C6-C30 aryl is selected from one of phenyl, naphthyl, xenyl, terphenyl and phenanthryl, and the C2-C30 heteroaryl is selected from one of pyridyl, bipyridyl, quinolyl, isoquinolyl, phenanthroline and triazinyl. According to the phosphorescent compound, the chemical formula shown as the formula (I) is used as a light-emitting layer of the OLED device, and the phosphorescent compound has the excellent color purity, excellent brightness, and the prolonged durability effect.
Cu-Catalyzed Denitrogenative Transannulation of 3-Aminoindazoles to Assemble 1-Aminoisoquinolines and 3-Aminobenzothiophenes
Zhou, Yao,Wang, Ya,Lou, Yixian,Song, Qiuling
, p. 8869 - 8873 (2019/09/12)
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
2-Amino-4-aryl thiazole: A promising scaffold identified as a potent 5-LOX inhibitor
Sinha, Shweta,Sravanthi,Yuvaraj,Manju,Doble, Mukesh
, p. 19271 - 19279 (2016/03/01)
Human 5-lipoxygenase (5-LOX) is an important enzyme in the biosynthesis of leukotrienes and is a target for asthma and allergy treatment. Zileuton is the only drug currently marketed that targets this enzyme (IC50 ~ 1 μM). So, the development of novel lead compounds is highly desirable. A series of 2-aryl indole, thiazolopyrazole acid, oxadiazolobenzothiophene, 1,4-disubstituted-1,2,3-triazole, 2-amino-4-aryl thiazole and 4,4′-(1,4-phenylene)bis(1,3-thiazole) derivatives when tested against this enzyme resulted in the identification of a potent compound (1d), p-fluoro substituted 2-amino-4-aryl thiazole, with an IC50 of ~10 μM. Another lead compound identified is (4a), a thiazolopyrazole acid derivative (IC50 ~ 40 μM). All the compounds exhibit poor DPPH radical scavenging activity which suggests that their action occurs not due to the disruption of the redox cycle of iron present in the enzyme (unlike zileuton) but through competitive inhibition, since the Vmax remains constant but the Km increases with an increase in inhibitor concentration. Molecular docking of 1d and 4a to the active site of 5-LOX also supports the experimental data, and suggests that their possible mechanism of action is through competitive inhibition. The current study identifies a promising lead molecule which could be improved further to match the activity of the commercial drug.
3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS
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Paragraph 0614-0615, (2016/08/29)
The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
An Aryne-Based Route to Substituted Benzoisothiazoles
Chen, Yiding,Willis, Michael C.
supporting information, p. 4786 - 4789 (2015/10/12)
The combination of arynes, generated using fluoride from the corresponding 2-(trimethylsilyl)aryl triflates, and 3-hydroxy-4-aminothiadiazoles leads to the selective formation of 3-amino-substituted benzo[d]isothiazoles. Variation of the substitution pattern of the aryne precursor, and of the thiadiazole, is possible, with the target heterocycles being obtained in good to excellent yields. In all cases, use of 3-hydroxy-4-aminothiadiazoles leads to incorporation of the amino-substituent in the product heterocycle.
METHOD FOR PROMOTING PLANT GROWTH
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Paragraph 0388, (2015/11/16)
The present invention provides a method for promoting plant growth, which comprises treating a plant with at least one compound selected from a group consisting of a compound represented by the following Formula (1): and an agriculturally acceptable salt thereof, provided that a method for promoting plant growth which comprises treating plants with a compound corresponding to any one of the following (1) to (5) and an agriculturally acceptable salt thereof is excluded: (1) 4-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (2) 5-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (3) 6-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (4) 7-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, and (5) Benzo[b]thiophene-2-carboxylic acid.
Microwave-assisted synthesis of 3-aminobenzo[b]thiophene scaffolds for the preparation of kinase inhibitors
Bagley, Mark C.,Dwyer, Jessica E.,Molina, Maria D. Beltran,Rand, Alexander W.,Rand, Hayley L.,Tomkinson, Nicholas C. O.
, p. 6814 - 6824 (2015/06/25)
Microwave irradiation of 2-halobenzonitriles and methyl thioglycolate in the presence of triethylamine in DMSO at 130°C provides rapid access to 3-aminobenzo[b]thiophenes in 58-96% yield. This transformation has been applied in the synthesis of the thieno
CONDENSED CYCLIC COMPOUND, AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME
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Paragraph 1168, (2016/10/08)
Disclosed are a condensed ring compound and an organic light emitting device comprising the condensed ring compound. The organic light emitting device comprises: a first electrode; a second electrode facing the first electrode; and an organic layer interposed between the first electrode and the second electrode, wherein the organic layer comprises the condensed ring compound.COPYRIGHT KIPO 2015
