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The present invention provides a novel compound having a superior activity as an ERR-alpha modulator and useful as an agent for the prophylaxis or treatment of ERR-alpha associated diseases. The present invention relates to a compound represented by the formula (1) wherein each symbol is as defined in the specification, or a salt thereof

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2698O – PubChem

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Dianions (2), (5), and (10), can be derived from the corresponding benzofurancarboxylic acids using lithium diisopropylamide, and are useful intermediates for the homologation of the parent acids.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2725O – PubChem

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Salts of compounds according to formula (I) wherein the X is selected from the group consisting of H2SO4, HSO3R’, HSO3Ar, H3PO4, HCl, HBr, CF3CO2H and CCl3CO2H. The preferred salt being the p-toluene sulfonate. These compounds and their pharmaceutical composition are useful as Fabl inhibitors for treating bacterial infections.

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Benzofuran – Wikipedia,
Benzofuran | C8H2702O – PubChem

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Pd-catalyzed decarboxylative Heck coupling of aromatic carboxylic acids with various olefins is developed using O2 as the terminal oxidant. Enhancement of O2 pressure leads to improving reaction turnover in this transformation and allows significantly reducing catalyst loading for efficient conversion of electron-rich benzoic acids. A Pd catalyst supported by a carbene ligand enables using electron-deficient benzoic acids as coupling partners.

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Benzofuran – Wikipedia,
Benzofuran | C8H2740O – PubChem

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Pd-catalyzed aerobic oxidative coupling of various benzoic acids with silyl enol esters proceeds via a combination of decarboxylation with sp3 beta-C-H bond activation to give Heck-type products. Mechanistic studies reveal this coupling involves in situ generation of olefin from aerobic oxidation of silyl enolate, followed by decarboxylative Heck coupling.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2739O – PubChem

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Human 15-lipoxygenase-1 (h-15-LOX-1) is a mammalian lipoxygenase and plays an important role in several inflammatory lung diseases such as asthma, COPD, and chronic bronchitis. Novel potent inhibitors of h-15-LOX-1 are required to explore the role of this enzyme further and to enable drug discovery efforts. In this study, we applied an approach in which we screened a fragment collection that is focused on a diverse substitution pattern of nitrogen-containing heterocycles such as indoles, quinolones, pyrazoles, and others. We denoted this approach substitution-oriented fragment screening (SOS) because it focuses on the identification of novel substitution patterns rather than on novel scaffolds. This approach enabled the identification of hits with good potency and clear structure-activity relationships (SAR) for h-1-5-LOX-1 inhibition. Molecular modeling enabled the rationalization of the observed SAR and supported structure-based design for further optimization to obtain inhibitor 14d that binds with a Ki of 36 nM to the enzyme. In vitro and ex vivo biological evaluations of our best inhibitor demonstrate a significant increase of interleukin-10 (IL-10) gene expression, which indicates its anti-inflammatory properties.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2735O – PubChem

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The copper-catalyzed decarboxylative selenation of aromatic carboxylic acids with diselenide is reported. This transformation tolerated a diverse set of functional groups on the substrates, including pentafluorobenzoic acid and heteroaromatic acids, delivering diaryl and methyl aryl selenides in good to excellent yields. Mechanistic studies indicated that the copper catalyst is essential in the activation of the Se-Se bond and the decarboxylation of aromatic acids. The utility of the products has been demonstrated in the facile synthesis of 10H-phenoselenazine and 11-methyldibenzo-(b,f)-1,4-selenazepine.

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Benzofuran – Wikipedia,
Benzofuran | C8H2783O – PubChem

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The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget’s disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2704O – PubChem

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Metal-catalyzed cycloisomerization reactions of 1,n-enynes have become conceptually and chemically attractive processes in the search for atom economy, which is a key subject of current research. However, metal-catalyzed cycloisomerization between aryl enol ether and silylalkynes has not been developed. The ruthenium hydride complex catalyzed cycloisomerization between aryl enol ether and silylalkynes is reported to give benzofurans having useful functional groups, vinyl and trimethylsilylmethyl, on the 2- and 3-positions, respectively.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2764O – PubChem

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Due to the interesting pharmacological activity observed for CI-988, a potent and selective CCK-B receptor antagonist, we have continued to study the SAR of this antagonist. This particular study examines the importance of the indole moiety for binding affinity. The synthesis and receptor binding affinity for analogs containing functionalized indole derivatives and replacing the indole with various heterocycles are reported.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2718O – PubChem