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The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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GPR40 partial agonism is a promising new mechanism for the treatment of type 2 diabetes mellitus with clinical proof of concept. Most of the GPR40 agonists in the literature have a carboxylic acid functional group, which may pose a risk for idiosyncratic drug toxicity. A novel series of GPR40 agonists containing a tetrazole as a carboxylic acid bioisostere was identified. This series of compounds features a benzo[b]thiophene as the center ring, which is prone to oxidation during phase 1 metabolism. Following SAR optimization targeting GPR40 agonist activity and intrinsic clearance in microsomes (human and rat), potent and metabolically stable compounds were selected for in vivo evaluation. The compounds are efficacious at lowering blood glucose in a SD rat oGTT model.

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Benzothiophene – Wikipedia,
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This invention relates to compounds of formula (I) where R1 to R12,–W–V–,–X–Y–, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.

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[Formula 1] the present invention refers to a and luminescent organic compound represented by including organic light emitting diode is provided, using the luminescent organic compound the present invention according to the organic light emitting display element a a material conventional than has high brightness and good cycle property. [Formula 1] (by machine translation)

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A novel traceless protecting strategy is presented for the long-standing challenge of conducting the palladium-catalyzed alpha-arylation of carboxylic aids and secondary amides with aryl halides. Both of the presented coupling processes occur with a variety of carboxylic acids and amides and with a variety of aryl bromides containing a broad range of functional groups, including base-sensitive functionality like acyl, alkoxycarbonyl, nitro, cyano, and even hydroxyl groups. Five commercial drugs were prepared through this method in one step in 81-96% yield. Gram-scale synthesis of medication Naproxen and Flurbiprofen with low palladium loading further highlights the practical value of this method.

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The enzyme aryl/alkenyl malonate decarboxylase (AMDase) catalyses the enantioselective decarboxylative protonation (EDP) of a range of disubstituted malonic acids to give homochiral carboxylic acids that are valuable synthetic intermediates. AMDase exhibits a number of advantages over the non-enzymatic EDP methods developed to date including higher enantioselectivity and more environmentally benign reaction conditions. In this report, AMDase and engineered variants have been used to produce a range of enantioenriched heteroaromatic alpha-hydroxycarboxylic acids, including pharmaceutical precursors, from readily accessible alpha-hydroxymalonates. The enzymatic method described here represents an improvement upon existing synthetic chemistry methods that have been used to produce similar compounds. The relationship between the structural features of these new substrates and the kinetics associated with their enzymatic decarboxylation is explored, which offers further insight into the mechanism of AMDase. Versatile decarboxylase: Aryl malonate decarboxylase (AMDase) and engineered variants have been shown to catalyse the enatioselective decarboxylative protonation of a range of alpha-heteroaryl alpha-hydroxy malonates with excellent yields and enantioselectivity (see scheme).

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.

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Benzothiophene – Wikipedia,
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A palladium-catalyzed reductive and carbonylative cyclization of ortho-iodo-tethered methylenecyclopropanes (MCPs) using N-formylsaccharin as CO source has been developed, affording the desired indanone derivatives in moderate to good yields with high regio- and stereoselectivity and good functional group compatibility.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The synthesis and characterisation is described of six diaryltetrayne derivatives [Ar-(C?C)4-Ar] with Ar=4-NO2-C 6H4- (NO24), 4-NH(Me)C6H 4- (NHMe4), 4-NMe2C6H4- (NMe 24), 4-NH2-(2,6-dimethyl)C6H4- (DMeNH24), 5-indolyl (IN4) and 5-benzothienyl (BTh4). X-ray molecular structures are reported for NO24, NHMe4, DMeNH24, IN4 and BTh4. The stability of the tetraynes has been assessed under ambient laboratory conditions (20 C, daylight and in air): NO24 and BTh4 are stable for at least six months without observable decomposition, whereas NHMe4, NMe24, DMeNH24 and IN4 decompose within a few hours or days. The derivative DMeNH24, with ortho-methyl groups partially shielding the tetrayne backbone, is considerably more stable than the parent compound with Ar=4-NH2C6H4 (NH24). The ability of the stable tetraynes to anchor in Au|molecule|Au junctions is reported. Scanning-tunnelling-microscopy break junction (STM-BJ) and mechanically controllable break junction (MCBJ) techniques are employed to investigate single-molecule conductance characteristics. Lay anchor: Oligoynes with a range of terminal functional groups, for example, benzo[b]thiophene (BTh4; see figure) have been synthesised. The charge transport characteristics of oligoynes in single-molecular junctions anchored between gold electrodes were studied. With careful choice of the anchor group oligoynes are shown to be a viable family of stable molecular wires for molecular-electronics applications.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The invention provides a preparation method of deuterated aromatic compound. The invention firstly halogenated aromatic compounds and alkali metal salt dissolved in deuterated solvent MA together with conventional solvent or deuterated solvent in the mixed solvent, then drip organosilicon reagent is added, in – 40 C to 150 C under stirring reaction, separation and purification after the reaction, to obtain the deuterated aromatic compound; the method does not require transition metal or metal tin reagent participation, can be efficient, economic, green preparation deuterated aromatic compound, in the preparation of the deuterated product deuterium generation rate greater than 95%. The mild conditions, substrate pervasive is good, high yield, the preparation of the deuterated compounds widely employed in pharmaceutical chemistry and organic chemistry field. (by machine translation)

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem