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Sumitomo Chemical Company, Limited

Novel penicillins of the formula SPC1 Wherein EQU1 represents a substituted or unsubstituted benzene or nitrogen atom-containing heteroaromatic ring which may be substituted, EQU2 represents a pyridine, pyrazine or pyridazine ring, X represents an oxygen or sulfur atom, Y represents a hydrogen atom or a loer alkoxycarbonyl or lower alkanoyl group, and R1, R2 and R3 are each a hydrogen or halogen atom or a nitro, lower alkylamino, di(lower)alkylamino, aine, lower alkoxycarbonylamino, lower alkanoylamino, amino(lower)alkyl, lower alkyl, lower alkoxy, hydroxyl, sulfamoyl, trifluoromethyl, lower alkylthio or lower alkylsulfonyl group, excluding the cases where all of R1, R2 and R3 are hydrogen atoms and where R1 is a hydroxyl group and R2 and R3 are each a hydrogen or halogen atom, and their nontoxic, pharmaceutically acceptable salts, which can be prepared by reacting a carboxylic acid of the formula: EQU3 wherein EQU4 X and Y are each as defined above or its reactive derivative with a compound of the formula: SPC2 Wherein R1, R2 and R3 are each as defined above or its reactive derivative, and are ueful as antimicrobial agents against gram-positive and gram-negative bacteria including Pseudomonas.

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Shenzhen University; Yang Chuluo; Zhou Xue

The invention discloses a kind of fluorescent material, preparation method and application, wherein the fluorescent material of the molecular structure of the general formula as follows: R1 – R6 are each independently selected from H atom, deuterium atoms, to the electronic group or pulling in the electronic group a; and R1 – R6 at least one electron-donating groups, at least one of the is dragging the electronic group. The present invention provides fluorescent material, with twisted of – A D (Donor) (Acceptor) structure, at the same time with a heat-activated delay fluorescent and aggregation induced characteristic, not only can realize 100% internal quantum efficiency, but also can reduce the aggregation caused by the luminescence quenching process. These material is used as the doping and-layer films of the organic electroluminescent device in the light-emitting layer of the light-emitting object, its efficiency can be comparable with the phosphorescence, and avoid the problems of the prior phosphorescent material usually to use heavy metal is the iridium, platinum and the problem of expensive heavy metal, the cost is reduced. (by machine translation)

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Human cathepsin B has many house-keeping functions, such as protein turnover in lysosomes. However, dysregulation of its activity is associated with numerous diseases, including cancers. We present here the structure-based design and synthesis of new cathepsin B inhibitors using the cocrystal structure of 5-nitro-8-hydroxyquinoline in the cathepsin B active site. A focused library of over 50 compounds was prepared by modifying positions 5, 7, and 8 of the parent compound nitroxoline. The kinetic parameters and modes of inhibition were characterized, and the selectivities of the most promising inhibitors were determined. The best performing inhibitor 17 was effective in cell-based in vitro models of tumor invasion, where it significantly abrogated invasion of MCF-10A neoT cells. These data show that we have successfully explored the structure-activity relationships of nitroxoline derivatives to provide new inhibitors that could eventually lead to compounds with clinical usefulness against the deleterious effects of cathepsin B in cancer progression.

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A series of group III metal chelates have been synthesized and characterized for the versatile application of organic light-emitting diodes (OLEDs). These metal chelates are based on 4-hydroxy-1,5naphthyridine derivates as chelating ligands, and they are the blue version analogues of well-known green fluorophore AIq3 (tris(8-hydroxyquinolinato)aluminum). These chelating ligands and their metal chelates were easily prepared with an improved synthetic method, and they were facially purified by a sublimation process, which enables the materials to be readily available in bulk quantity and facilitates their usage in OLEDs. Unlike most currently known blue analogues of AIq3 or other deep blue materials, metal chelates of 4-hydroxy-1,5-naphthyridine exhibit very deep blue fluorescence, wide band gap energy, high charge carrier mobility, and superior thermal stability. Using a vacuum-thermal-deposition process in the fabrication of OLEDs, we have successfully demonstrated that the application of these unusal hydroxynaphthyridine metal chelates can be very versatile and effective. First, we have solved or alleviated the problem of exciplex formation that took place between the hole-transporting layer and hydroxynaphthyridine metal chelates, of which OLED application has been prohibited to date. Second, these deep blue materials can play various roles in OLED application. They can be a highly efficient nondopant deep blue emitter: maximum external quantum efficiency etaext of 4.2%; Commision Internationale de L’Eclairage x, y coordinates, CIExy = 0.15, 0.07, Compared with AIq3, Bebq 2 (beryllium bis(benzoquinolin-IO-olate)), or TPBI (2,2 ,2 -(1,3,5-phenylene)tris(1-phenyl-1 H-benzimidazole), they are a good electron-transporting material: low HOMO energy level of 6.4 – 6.5 eV and not so high LUMO energy level of 3.0-3.3 eV. They can be ambipolar and possess a high electron mobility of 10-4cm2/V s atan electric field of 6.4 ¡Á 105 V/cm. They are a qualified wide band gap host material for efficient blue perylene (CIExy = 0.14, 0.17 and maximum etaext 3.8%) or deep blue 9,10-diphenylanthracene (CIE x,y= 0.15, 0.06 and maximum etaext2.8%). For solid state lighting application, they are desirable as a host material for yellow dopant (rubrene) in achieving high efficiency (etaext 4.3% and etap 8.7 Im/w at an electroluminance of 100 cd/m2 or etaext 3.9% and etap 5.1 Im/w at an electroluminance of 1000 cd/m2) white electroluminescence (CIEx,y= 0.30, 0.35).

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 5423-54-1, and how the biochemistry of the body works.COA of Formula: C8H6N2O

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 5423-54-1, name is 1,5-Naphthyridin-4-ol, introducing its new discovery. COA of Formula: C8H6N2O

Antiphotobleaching is a critical challenge in the field of luminescent lanthanide complexes (LLCs) as well as in many disciplines concerning organic luminescent processes. In this work, a type of structurally rigid organic ligand, 4-hydroxy-1,5-naphthyridine (ND), is developed, which can not only efficiently sensitize the europium emission but also demonstrate unique photostability. A series of ND derivatives with different substituent groups are synthesized and their singlet and triplet excited state energy levels are systematically investigated. Photophysical characterizations of the corresponding europium complexes reveal that the sensitization efficiencies (etasens) are close to 100% and the total photoluminescence quantum yields can reach up to 84%. Most importantly, these structurally rigid luminescent europium complexes exhibit outstanding photostability and thermostability. Unlike the widely used beta-diketone complexes that are easily photodegraded, ND-based chelates show no obvious degradation during the UV aging test (10 W m-2 340 nm Ultraviolet A irradiation) within 200 h. Such superior UV resistance is even better than that of the famous compound tris(8-hydroxyquinolate)aluminum (Alq3). Possible reasons are discussed and a general rule for designing photostable LLCs is proposed. Such a chromophore is very promising for introducing luminescent materials with good photostability in potential application in many disciplines.

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THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE; YIN, Hang Hubert; ZHANG, Shuting; HU, Zhenyi

Toll-like receptor 8 (TLR8)-specific inhibitors and methods of using the same in individuals having an autoimmune disease or an inflammatory disorder.

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3M INNOVATIVE PROPERTIES COMPANY

This invention provides methanesulfonate and ethanesulfonate salts of 1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine, pharmaceutical compositions containing the salts, methods of making, and methods of use.

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ASTRAZENECA AB; ASTRAZENECA UK LIMITED

The invention concerns naphthyridine derivatives of Formula (Ia) or (Ib) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, G1, G2, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders or disease states associated with angiogenesis and/or vascular permeability.

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The proteasome plays a crucial role in degradation of normal proteins that happen to be constitutively or inducibly unstable, and in this capacity it plays a regulatory role. Additionally, it degrades abnormal/damaged/mutant/misfolded proteins, which serves a quality-control function. Inhibitors of the proteasome have been validated in the treatment of multiple myeloma, with several FDA-approved therapeutics. Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. A fragment-based drug discovery (FBDD) approach was utilized to identify fragments with activity against Rpn11. Screening of a library of metal-binding pharmacophores (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value ?2.5 muM) displayed strong inhibition of Rpn11. Further synthetic elaboration of 8TQ yielded a small molecule compound (35, IC50 value ?400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation of tumor cells in culture.

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4-Hydoxy-1,5-naphthyridines (HNt) are derivatives of 8-hydroxyquinolines, yet possess a wider HOMO and LUMO band gap than the latter. The cyclometalated complex of platinum(II) with Nt exists in a square planner geometry, and has a high tendency to aggregate in condensedmedia. Such a phenomenon was verified by examining its photo-luminescence spectra in different concentrations. In a dilute solution, it exhibits a yellow phosphorescence centered at 530?555 nm, yet red-shifted to ?660 nm in a concentrated solution or in the solid state. This series of compounds can be used as emitting dyes in light-emitting diodes (LED). The LED devices with a configuration ITO/NPB/dye (6%) in CBP/BCP/AlQ3 or TPBI/LiF/Al displayed a yellow to red color, where NPB, CBP, BCP, AlQ3 and TPBI denote 4,4?-bis[N-(1-naphthyl), Nphenylamino] biphenyl, 4,4?-bis(carbazol-9-yl)biphenyl, 2,9-dimethyl-4,7-diphenyl-1,10-phenanthroline, tris(8-hydoxyquinolinato) aluminium, and 2,2?,2?-(1,3,5-benzenetriyl)tris(1-phenyl-1H- benzimidazole), respectively. The maximal light intensity exceeds 2.6 ¡Á 104 cd/m2 with an external quantum efficiency up to 5.8%.

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