- Triketone compound containing quinoxaline structure, and preparation method and application thereof
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The invention belongs to the technical field of medicine synthesis, and particularly relates to a triketone compound containing a quinoxaline structure, and a preparation method and an application thereof. The quinoxaline-containing triketone compound has a structure represented by general formula (I). The preparation method is mainly characterized in that a compound with a structure represented by formula (II) is contacted in the presence of an alkali and a solvent, and R1, R2, R3 and R4 in the formulas are respectively defined in the description. The quinoxaline-containing triketone compoundhas high herbicidal activity, and especially has an excellent effect of preventing and controlling broadleaf weeds and/or gramineous weeds, and the prevention and control effect is even better than that of some commercial herbicides sold in the market.
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- Palladium-Catalyzed Decarbonylative Difluoromethylation of Acid Chlorides at Room Temperature
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Methods for the direct synthesis of difluoromethylated arenes are sparse, despite the importance of the difluoromethyl group in medical, agro-, and materials chemistry. A palladium-catalyzed decarbonylative cross-coupling reaction of acid chlorides with a difluoromethyl zinc reagent is achieved to access difluoromethylated compounds. The transformation proceeds at room temperature and shows broad functional group tolerance, thus providing a general and efficient method for decarbonylative difluoromethylation of a wide range of aromatic carboxylic acids.
- Pan, Fei,Boursalian, Gregory B.,Ritter, Tobias
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supporting information
p. 16871 - 16876
(2018/11/23)
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- Substituted Pyrazalones
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The invention is related to compounds of formula (I) as antagonists of the TGFβ family type I receptors, Alk5 and/or AIk 4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such a
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Page/Page column 30
(2010/04/23)
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- Synthesis and biological evaluation of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors
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A series of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles (15a-l) have been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 4-[5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-ylmethyl]b enzenesulfonamide (15b) and 4-[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-ylmethyl]be nzenesulfonamide (15c) showed more than 90% inhibition at 0.5 μM in a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct, but inhibited p38α MAP kinase activity only 11 and 8% at a concentration of 10 μM, respectively.
- Kim, Dae-Kee,Jung, Sun Hee,Lee, Ho Soon,Dewang, Purushottam M.
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body text
p. 568 - 576
(2009/09/27)
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- Novel Quinoxaline Derivatives and Their Medical Use
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This invention relates to novel quinoxaline derivatives having medical utility, to use of the quinoxaline derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the quinoxaline derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to positive modulation of AMPA receptor mediated synaptic responses.
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Page/Page column 6
(2009/12/05)
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- PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES
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The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
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Page/Page column 99-101
(2008/06/13)
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- SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
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The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes
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Page/Page column 40
(2008/06/13)
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- QUINOXALINES AS B RAF INHIBITORS
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The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
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Page/Page column 52
(2010/11/08)
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- Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
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Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.
- Scapecchi, Serena,Martini, Elisabetta,Manetti, Dina,Ghelardini, Carla,Martelli, Cecilia,Dei, Silvia,Galeotti, Nicoletta,Guandalini, Luca,Romanelli, Maria Novella,Teodori, Elisabetta
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- AZOLIDINONE-VINYL FUSED-BENZENE DERIVATIVES
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The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1 , R2 and n are as described in the description.
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- Triarylimidazole derivatives as cytokine inhibitors
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Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are various substituent groups; and one of X1 and X2 is N or CR″, and the other is NR″ or CHR″ wherein R″
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- Amide derivatives useful as inhibitors of the production of cytokines
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The invention concerns amide derivatives of formula (I) wherein R3is (1-6C)alkyl or halogeno; Q1is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2is a substituent such as hydroxy and halogeno; q is 0-4; and Q2includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
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