- Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
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Taking advantage of microwave-assisted synthesis, efficient and expedite procedures for preparation of a library of fusaric acid and 39 analogues are reported. The fusaric acid analogues were tested in cell-based screening assays for inhibition of the las and rhl quorum sensing system in Pseudomonas aeruginosa and the lux quorum sensing system in Vibrio fischeri. Eight of the 40 compounds in the library including fusaric acid inhibited lux quorum sensing and one compound inhibited activity of the las quorum sensing system. To our delight, none of the compounds showed growth inhibitory effects in the tested concentration ranges.
- Tung, Truong Thanh,Jakobsen, Tim Holm,Dao, Trong Tuan,Fuglsang, Anja Thoe,Givskov, Michael,Christensen, S?ren Br?gger,Nielsen, John
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p. 1011 - 1020
(2016/12/30)
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- PHOTOELECTRIC CONVERSION ELEMENT, DYE-SENSITIZED SOLAR CELL, AND METAL COMPLEX DYE USED IN SAME
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A photoelectric conversion element has a conductive support, a photoreceptor layer containing an electrolyte, a charge carrier layer containing an electrolyte and a counter electrode, and the photoreceptor layer has semiconductor particles on which a metal complex dye represented by Formula (I) is carried. M1(LA)(LD)(Z1).CI??Formula (I) M1 represents a metal atom; Z1 represents a monodentate ligand; LA represents a tridentate ligand represented by Formula (AL-1); LD represents a bidentate ligand represented by Formula (DL-1); and CI represents a counterion necessary for neutralizing the charge.
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Paragraph 0567-570; 0574-0576
(2016/10/24)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. Living organisms have developed tightly regulated processes that specifica
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Page/Page column 46; 47
(2014/04/03)
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- TRIAZOLE DERIVATIVES AS WNT SIGNALING PATHWAY INHIBITORS
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The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear β-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.
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Page/Page column 58
(2012/06/30)
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- FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF
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The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
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Page/Page column 115
(2012/07/14)
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- Facile synthesis and platinum complexes of 4′,5,5′′- trisubstituted-2,2′:6′,2′′-terpyridines
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The synthesis of trisubstituted 4′,5,5′′ terpyridines is described. The strategy begins with synthesis of 2-acetyl-5-bromopyridine (3) from 2,5-dibromopyridine, substitution of the bromine in 3 using a variety of metal-catalyzed reactions and then formation of the terpyridine using the Krohnke reaction. The complexes have been prepared by reaction of [Pt(PhCN) 2Cl2] with the appropriate silver salt followed by addition of the terpyridyl ligand. The crystal structure of two complexes have been determined via X-ray diffraction and the MLCT (metal-to-ligand charge-transfer) emissions determined by UV/Vis spectroscopy. The Royal Society of Chemistry 2011.
- Huo, Jianqiang,Arulsamy, Navamoney,Hoberg, John O.
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scheme or table
p. 7534 - 7540
(2011/10/12)
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- UREA INHIBITORS OF MAP KINASES
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Urea containing compounds that inhibit MAP kinases, pharmaceutical compositions including such compounds and methods for using these compounds to treat inflammatory diseases and cancer are described herein.
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Page/Page column 25
(2010/03/04)
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- Highly efficient borylation Suzuki coupling process for 4-bromo-2-ketothiazoles: Straightforward access to micrococcinate and saramycetate esters
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Image Presented The first palladium-catalyzed borylation of 4-bromo-2-ketothiazoles followed by a Suzuki cross-coupling reaction with haloheteroaromatics using Buchwald's Cy-JohnPhos and XPhos ligands is reported. The methodology has allowed the fast preparation of highly valuable 4-pyridinyl- and 4-thiazolyl-2-ketothiazoles as common subunits of thiopeptide antibiotics. As direct applications, novel concise syntheses of a sulfomycinamate thio-analogue as well as micrococcinate and saramycetate esters are described.
- Martin, Thibaut,Laguerre, Claire,Hoarau, Christophe,Marsais, Francis
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supporting information; experimental part
p. 3690 - 3693
(2011/02/28)
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- SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS
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Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
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Page/Page column 153
(2009/03/07)
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- SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS
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Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
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Page/Page column 155
(2009/03/07)
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- Benzodioxepine derivatives
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This invention relates to compounds of the formula wherein B, X, Y, Z, R1 and R2 are as defined in the description, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by ACCβ inhibitors.
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Page/Page column 8; 12-13
(2010/02/11)
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- BENZO [b][1,4] DIOXEPINE DERIVATIVES
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This invention relates to compounds of the formula (I), wherein B, X, Y, Z, R1 and R2 are as defined in the description, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by ACCβ inhibitors.
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Page/Page column 26
(2010/02/11)
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- Regiospecific carboalkoxylation of 2,5-dibromopyridine
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Carboalkoxylation of 2,5-dibromopyridine with carbon monoxide and an alcohol in the presence of palladium acetate and 1,1'-bis(diphenylphosphino)ferrocene (dppf) occurs regiospecifically to afford esters of 5-bromo-pyridine-2-carboxylic acid in good yield.
- Chambers,Marfat
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p. 515 - 520
(2007/10/03)
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- SYNTHESIS AND DEUTERATION OF SOME HALOGENOQUINOLIZINIUM BROMIDES
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Syntheses and 1H-nmr spectra are reported for the hitherto unknown 1-bromo-, 3-bromo-, 4-bromo-, 2-chloro-, 4-chloro-, 1,2-dibromo-, 3,4-dibromo- and 2,7-dibromoquinolizinium bromide.These compounds, quinolizinium bromide, 1-hydroxy-, 2-hydroxy-, 3-hydroxy-, 2-piperidino- and 2-diethylaminoquinolizinium bromide and 2- and 4-quinolizone were deuterated by heating with D2O (Table I).
- Sanders, Georgine M.,Dijk, Marinus van,Plas, Henk C. van der
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p. 213 - 223
(2007/10/02)
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