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The dominance of safener can unite with herbicides acquiring the efficient protection of crop and qualifying control of weeds in agricultural fields. In order to solve the crop toxicity problem and exploit the novel potential safener for fenoxaprop-P-ethyl herbicide, a series of trichloromethyl dichlorobenzene triazole derivatives were designed and synthesized by the principle of active subunit combination. A total of 21 novel substituted trichloromethyl dichlorobenzene triazole compounds were synthesized by substituted aminophenol and amino alcohol derivatives as the starting materials, using cyclization and acylation. All the compounds were unambiguously characterized by IR,1H-NMR,13C-NMR, and HRMS. A greenhouse bioassay indicated that most of the title compounds could protect wheat from injury caused by fenoxaprop-P-ethyl at varying degrees, in which compound 5o exhibited excellent safener activity at a concentration of 10 mumol/L and was superior to the commercialized compound fenchlorazole. A structure?activity relationship for the novel compounds was determined, which demonstrated that those compounds containing benzoxazine groups showed better activity than that of oxazole-substituted compounds. Introducing a benzoxazine fragment and electron-donating group to specific positions could improve or maintain the safener activity for wheat against attack by the herbicide fenoxaprop-P-ethyl. A molecular docking model suggested that a potential mechanism between 5o and fenoxaprop-P-ethyl is associated with the detoxication of the herbicide. Results from the present work revealed that compound 5o exhibited good crop safener activities toward wheat and could be a promising candidate structure for further research on wheat protection.

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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

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A single and simple ortho-sulfonyl benzonitrile template was developed to achieve remote C?H olefination of six different classes of N-heterocycles. We demonstrate that, by varying precatalysts and conditions, the same template can be applied to the remote C?H activation of six structurally distinct heterocyclic scaffolds, and the site-selectivity can be predicted based on distance and geometry. Furthermore, this new development shows that template-directed remote C?H activation is possible through macrocyclopalladation processes with smaller ring sizes.

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A single and simple ortho-sulfonyl benzonitrile template was developed to achieve remote C?H olefination of six different classes of N-heterocycles. We demonstrate that, by varying precatalysts and conditions, the same template can be applied to the remote C?H activation of six structurally distinct heterocyclic scaffolds, and the site-selectivity can be predicted based on distance and geometry. Furthermore, this new development shows that template-directed remote C?H activation is possible through macrocyclopalladation processes with smaller ring sizes.

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The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.

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The present invention relates to certain amide derivatives that have the ability to inhibit 11-beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

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A systematic investigation of reductive ring expansion reaction of oximes with diisobutylaluminum hydride (DIBAH) was performed. The reaction regiospecifically provided a variety of unsubstituted bicyclic heterocycles 3a-3g or tricyclic heterocycles 3h, 3j-3l that contained nitrogen attached to an aromatic ring.

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The invention relates to a high efficiency, two-way selective tertiary aromatic amide and organic silicon reagent silicon hydrogenation reduction reaction green new method. Selecting non-metal catalytic system, under mild conditions can be successfully catalytic three-stage aromatic amide with low-cost of the peripheric (PHMS) or triethoxy silane to selective production of secondary or tertiary organic amine compound. The first time the use of organosilicon reagent breakthrough of electronic effect of steric differences and realize three-stage aromatic amide-way selective reduction reaction, is the reduction of amides and derivatives thereof provides a completely new strategy, also the method overcomes the prevailing poor substrate functional group compatibility, high costs of production and the like, industrial production or laboratory preparation amine compounds have provided broad prospects. (by machine translation)

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Compounds of Formula (I) wherein R1, R2 R3, R4, R5, R6, and X are as defiend herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocoricoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

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There are described novel greenish-yellow cationic dyes of the formula STR1 wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy or NO2, R2 is unsubstituted lower alkyl, or lower alkyl which is substituted by: hydroxyl, lower alkoxy, halogen, CN, carboxylic acid amide, carboxylic acid alkyl ester or phenyl, or R2 is alkenyl (C3 -C4), the R3 ‘s independently of one another are each lower alkyl, or both R3 ‘s together form a carbocyclic 5-, 6- or 7-membered ring, R4 is hydrogen, lower alkyl, unsubstituted aryl or substituted aryl, R5, R6 and R7 independently of one another are hydrogen, lower alkyl, lower alkoxy, halogen, NO2, CN or lower alkylsulfonyl, and A is an anion; processes for producing them, and their use for dyeing and printing textile materials, particularly polyacrylonitrile materials.

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