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The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimers disease as well as measureing clinical efficacy of Alzheimers disease therapeutic agents.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The present invention relates to intermediates and processes for preparing benzothiophenes of the following formula: wherein Y is chloro, bromo, iodo or -SO2R9; and, R9is C1-C4alkyl, trifluoromethyl, trichloromethyl, phenyl, p-tolyl, p-anisyl, or mono- or di(halo or nitro)phenyl.

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The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction. Recommanded Product: Methyl 3-aminobenzo[b]thiophene-2-carboxylate, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S

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 time. This transformation proceeds via an “extrude-and-sew” strategy with an unprecedented radical reactivity of 3-aminoindazoles.

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Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. Recommanded Product: 17402-83-4, C8H7NS. A document type is Patent, introducing its new discovery., Recommanded Product: 17402-83-4

Provided are a pyrimidinyl amino compound having protein kinase inhibitor activity, and a pharmaceutical composition containing said compound; also provided are a use and application of said compound. What is provided is selected from a group consisting of the compound represented by formula (I), a stereoisomer thereof, a tautomer thereof, a pharmacologically acceptable salt thereof, a solvate thereof, and a prodrug thereof. The described compound has good inhibitory activity against the JAK family of kinases and the SYK family of kinases, and therefore may serve as a JAK inhibitor and SYK inhibitor, and is effective in use for the prevention or treatment of diseases related to the JAK and SYK families of kinases.

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Reference:
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Background Pyridoquinazolinecarboxamides have been reported as RNA polymerase I inhibitors and represent a novel class of potential antitumor agents. BMH-21, was reported to intercalate with GC-rich rDNA, resulting in nucleolar stress as a primary mechanism of cytotoxicity. Methods The interaction of BMH-21 and analogues with DNA G-quadruplex structures was studied by NMR and molecular modelling. The cellular response was investigated in a panel of human tumor cell lines and protein expression was examined by Western Blot analysis. Results and conclusions We explored the ability of BMH-21 and its analogue 2 to bind to G-quadruplex present in the c-MYC promoter, by NMR and molecular modelling studies. We provide evidence that both compounds are not typical DNA intercalators but are effective binders of the tested G-quadruplex. The interaction with c-MYC G-quadruplex was reflected in down-regulation of c-Myc expression in human tumor cells. The inhibitory effect was almost complete in lymphoma cells SUDHL4 characterized by overexpression of c-Myc protein. This downregulation reflected an early and persistent modulation of cMyc mRNA. Given the relevance of c-MYC in regulation of ribosome biogenesis, it is conceivable that the inhibition of c-MYC contributes to the perturbation of nuclear functions and RNA polymerase I activity. Similar experiments with CX-5461, another RNA polymerase I transcription inhibitor, indicate the same behaviour in G-quadruplex stabilization. General significance Our results support the hypothesis that BMH-21 and analogue compounds share the same mechanism, i.e. G-quadruplex binding as a primary event of a cascade leading to inhibition of RNA polymerase I and apoptosis.

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New Advances in Chemical Research in 2021. Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, new energy materials, preparation and modification of special coatings. 4923-87-9. Introducing a new discovery about 4923-87-9, Name is 5-Bromobenzothiophene

The functionalization of thiophenes is a fundamental and important reaction. Herein, we disclose iridium-catalyzed one-pot annulation reactions of (benzo)thiophenes with (hetero)aromatic or alpha,beta-unsaturated carboxylic acids, which afford thiophene-fused coumarin-type frameworks. Dearomatization reactions of 2-substituted thiophenes with alpha,beta-unsaturated carboxylic acids deliver various thiophene-containing spirocyclic products. The occurrence of two interconnected reactions provides direct evidence for a Heck-type pathway. The mechanistic scenario described herein is distinctly different from the SEAr and concerted metalation?protodemetalation (CMD) pathways encountered in the well-described oxidative C?H/C?H cross-coupling reactions of thiophenes with other heteroarenes.

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Disclosed are compositions comprising (a) a GPR40 agonist and (b) an SGLT2 inhibitor, and methods for treating of disorders that are affected by the modulation of the GPR40 receptor and SGLT2 transporter. Such GPR40 compounds are represented by Formula (I) as follows: wherein ring W, R1, R2, R3, R5, R6, A, and Z, are defined herein.

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New Advances in Chemical Research, May 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and transition states. Quality Control of 4-Chlorobenzo[b]thiophene, C8H5ClS. A document type is Patent, introducing its new discovery., Quality Control of 4-Chlorobenzo[b]thiophene

The invention provides a piripiprazole derivative and a preparation method, wherein the chemical structural formula of the epiprazole derivative is expressed by a chemical structural formula. The epiprazole derivative is composed of epiconazole, (HCHO). m N – hydroxymethyl according to the first basic catalyst is prepared; and then N – hydroxymethyl-piripiprazole and an alkylformylchloride compound are reacted under second basic catalyst to prepare. The half-life of the epiprazole derivative is prolonged, the drug delivery frequency can be reduced; and the epiprazole derivative prepared by the preparation method is low in impurity, and low in cost. (by machine translation)

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Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.

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New Advances in Chemical Research in 2021. Catalysts allow a reaction to proceed that has a lower activation energy than the uncatalyzed reaction. In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. Application In Synthesis of 5-Bromobenzothiophene. Introducing a new discovery about 4923-87-9, Name is 5-Bromobenzothiophene

The present invention relates to a novel indole-based compound having excellent hole injection and transport capabilities, light-emission, and other properties, and to an organic electroluminescent device the luminous efficiency, driving voltage, service life, and other characteristics of which are improved due to containing the compound in one or more organic material layers.

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Reference:
Benzothiophene – Wikipedia,
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