Abstract: The present invention relates to a novel anthracene derivative and an organic electronic device using the same. The anthracene derivative can act as a hole injecting, hole transporting, electron injecting and transporting, or light emitting material in an organic light emitting device and an organic electronic device. In particular, the anthracene derivative can act as a light emitting host. The organic electronic device according to the present invention has excellent characteristics in views of efficiency, the driving voltage, and the stability.

Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.

Abstract: Novel pyridinium salts functionalized with boronic acid and methods of making them are disclosed. When combined with a fluorescent dye, the compounds are useful in the detection of polyhydroxyl-substituted organic molecules.

Abstract: Novel thienylpyridylcarboxamides of the formula (I) The present application is also directed to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.

Abstract: The reaction of halo-boron compounds (B—X compounds, compounds having one or more boron-halogen bonds) with silanes provides boranes (B—H compounds, compounds having one or more B—H bonds) and halosilanes. Inorganic hydrides, such as surface-bound silane hydrides (Si—H) react with B—X compounds to form B—H compounds and surface-bound halosilanes. The surface bound halosilanes are converted back to surface-bound silanes electrochemically. Halo-boron compounds react with stannanes (tin compounds having a Sn—H bond) to form boranes and halostannanes (tin compounds having a Sn—X bond). The halostannanes are converted back to stannanes electrochemically or by the thermolysis of Sn-formate compounds. When the halo-boron compound is BCl3, the B—H compound is B2H6, and where the reducing potential is provided electrochemically or by the thermolysis of formate.

Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.

Abstract: Ionic compounds comprising: (a) a cationic radical of a charge transporting compound which has one or more reactive groups; and (b) a counter anion. The reactive functional groups on the cation allow the ionic compound to cross-link with a host charge transport compound. Such ionic compounds may have various properties, such as thermodynamic stability, hole injection/transport capabilities, electrochemical durability, and/or solubility in organic solvents that allows them to be useful in organic electronic devices. Also provided are electronic devices made using the ionic compounds of the present invention, and methods of making an electronic device.

Abstract: The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent. The invention provides a method for producing a compound represented by formula (2): (wherein n is an integer of 2 to 5; R1 represents a (substituted) alkyl group or a (substituted) aryl group; and R2 represents a (substituted) alkoxycarbonyl group, a (substituted) aralkyloxycarbonyl group, a (substituted) aliphatic acyl group, or a (substituted) aromatic acyl group), which includes treating a compound represented by formula (1): (wherein n, R1, and R2 are the same as defined above; and R3 represents a hydrogen atom, a (substituted) alkyl group, or a (substituted) aralkyl group) under a hydrogen gas atmosphere in the presence of a metallic catalyst.

Abstract: The invention features a class of 2-nitroimidazole compounds with a secondary basic nitrogen atom and a linker bearing one or more therapeutic agents, cytotoxic agents, detectable labels, or chelating groups. In particular, the invention provides 2-nitroimidazole compounds containing a cluster of boron atoms for use in boron neutron capture therapy (BNCT). The 2-nitroimidazole compounds can be used to treat hypoxic conditions, including, e.g., cancer, inflammation, and ischemia. The weakly basic 2-nitroimidazole compounds target to hypoxic tissue and provide increased tissue concentration overall.

Abstract: Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form.

Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.

Abstract: Compounds of formula (I): wherein R, R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

Abstract: The present invention provides novel boron compounds which are useful, depending on their characteristics, as light-emitting materials, electron-transport materials, electron-injection materials, hole-blocking materials, or organic semiconductor materials, and which have new molecular structures quite different from those of the heretofore known boron compounds; their production processes; and functional electronic devices using the same. The novel boron compounds are, for example, those of the following formula (1): These boron compounds can be produced by, for example, reacting boron compounds of the following formula (4): with compounds of the following formula (5): in the presence of a catalyst containing at least one metal element selected from the group consisting of palladium, platinum, and nickel. These boron compounds are used for the functional electronic devices.

Abstract: The present invention relates to pentarylenetetracarboximides of the formula (I) or (Ia) or mixtures thereof to processes for preparation thereof, and to the precursors and use thereof.

Abstract: The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.

Abstract: The object of the present invention is to provide a photobase generator capable of efficiently generating amines (tertiary amines and amidine) high in catalytic activity by sensing light with a wavelength of from 350 to 500 nm (especially, from 400 to 500 nm). The present invention is a photobase generator characterized in being represented by general formula (1) or (2). Y+ is a quaternary ammonio group of general formula (3) to (5), and X? is a counter anion selected from among a borate anion, a phenolate anion, and a carboxylate anion.

Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.

Abstract: Aromatic heterocycles incorporating boron and nitrogen atoms, in particular, 1,2-azaborine compounds having the formula and their use as synthetic intermediates.

Abstract: Rylenetetracarboximides of the general formula I in which the variables are defined as follows: R are identical or different radicals: hydrogen; alkyl, cycloalkyl, aryl or hetaryl, each substituted if desired; R? are identical or different radicals: hydrogen; aryloxy, arylthio, hetaryloxy or hetarylthio, each substituted if desired; n is 1 or 2, and also a process for preparing the rylenetetracarboximides I and their use for coloring high molecular weight organic and inorganic materials, for preparing aqueous polymer dispersions which absorb in the near infrared region of the electromagnetic spectrum, for producing markings and inscriptions which absorb infrared light and are invisible to the human eye, as infrared absorbers for heat management, as IR laser beam-absorbing materials in fusion treatment of plastics parts, and also as active components in photovoltaics.

Abstract: The present invention relates to novel compounds, particularly derivatives of boroarginine, boroornithine and borolysine that selectively modulate, regulate, and/or inhibit enteropeptidase. The invention also relates to compositions, particularly pharmaceutical compositions, as well as methods to treat excess weight, obesity and diseases associated with an abnormal fat metabolism.

Abstract: Quaternary nitrogen heterocyclic boronic acid-containing compounds are described, which are sensitive to glucose and fructose, as well as a variety of other physiologically important analytes, such as aqueous chloride and iodide, and a method of using the compounds. Also disclosed is a contact lens doped with the quaternary nitrogen heterocyclic boronic acid-containing compound, and a method of using the doped contact lens to measure the concentration of analyte in tears under physiological conditions.

Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.

Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.

Abstract: The invention relates to a class of glucose-responsive, polyviologen boronic acid quenchers that may be used in combination with fluophores to achieve real-time measurement of glucose levels in vivo.

Abstract: The invention relates to novel metal complexes. Said compounds can be used as functional material in a series of different applications which in the broadest sense can be attributed to the electronics industry. The inventive compounds are described by the formula (1) and by compounds (1) to (52).

Abstract: The invention relates to novel metal complexes. Said compounds can be used as functional materials in a series of different types of applications that can be attributed in the broadest sense to the electronics industry The inventive compounds are defined by formula (1).

Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.

Abstract: Substituted aryl-boron compounds comprising at least one 18F atom, as illustrated by the formula (I), where at least one of Y1 or Y2 is 18F and A1 is a substituted aromatic ring, with G1-5 being, independently, C or N, and where the substitutents of the aromatic ring or polycyclic moiety (other than boron) comprise at least one electron-withdrawing group (EWG), providing that sigma total (?total) for all substituents on the aromatic ring or polycyclic moiety except B is about 0.06 or more when said at least one EWG is positioned ortho to B, or about 0.2 or more when no EWG is positioned ortho to B. The compounds include neutral (N=1) and ionic borate (N=2) embodiments. The compounds are useful as positron emission tomography (PET) imaging agents.

Abstract: According to this invention, it is possible to provide an organic electroluminescence element material comprising a metal complex having a specific ligand, and an organic electroluminescence element which exhibits high emission efficiency as well as long emission life, employing the organic electroluminescence element material, and to provide an illumination device and a display device. The electroluminescence element material is characterized by containing a metal complex having a ligand represented by following Formula (1).

Abstract: The disclosure relates to compounds of formula (I): wherein A, Z, Z?, L, R2 and R3 are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.

Abstract: This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation.

Abstract: There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

Abstract: The present invention is directed to arginase inhibitor compounds of formula IA or formula IB: or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.

Abstract: The present invention provides a light emitting device material which enables a light emitting device having high efficiency and excellent chromatic purity and durability using a light emitting device material containing a pyrene compound represented by formula (1), wherein any one of R1 to R10 is a group represented by formula (2), or 1 to 4 substituents is/are group(s) represented by formula (3), and a light emitting device using the same.

Abstract: A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph.

Abstract: A method for stabilizing triphenylboron-pyridine (TPBP) in a solvent-based anti-fouling coating, such as a marine anti-fouling coating, by adding to the coating about 0.04 to about 0.40% wt., based on the total amount of the triphenylboron-pyridine, of 2,2,6,6-tetramethylpiperidinyl-1-oxy-radical (“TEMPO”). Also disclosed is a solvent-based anti-fouling coating, such as a marine anti-fouling coating, composition containing TPBP and TEMPO.

Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.

Abstract: Quaternary nitrogen heterocyclic boronic acid-containing compounds are described, which are sensitive to glucose and fructose, as well as a variety of other physiologically important analytes, such as aqueous chloride and iodide, and a method of using the compounds. Also disclosed is a contact lens doped with the quaternary nitrogen heterocyclic boronic acid-containing compound, and a method of using the doped contact lens to measure the concentration of analyte in tears under physiological conditions.

Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.

Abstract: Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH2)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.

Abstract: One aspect of the present invention relates to “boronium” ions that are stable, hydrophobic, room-temperature ionic liquids. In certain embodiments, ionic liquids of the instant invention are represented by the formula [XnBY4?n]+(n?1)(n?1)Z?1, wherein X refers to a Lewis base, Y refers to a substituent covalently bonded to boron, Z?1 is a charge diffuse anion, and x is 2, 3 or 4. In certain embodiments, the ionic liquids of the instant invention are of the general type [X2BY2]+1Tf2N?1, wherein each X is independently a tertiary amine, a N-alkylimidazole or a pyridine; and each B—X bond is a B—N bond.

Abstract: An organoborane complex is disclosed. The complex includes a blocking agent comprising a bifunctional Lewis base. The blocking agents include an amine group and a second functional group that has a lower Lewis basicity than the first functional group. The blocking is based on amino alkyl pyridines.

Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

Abstract: A bisboron compound represented by the general formula (I): wherein B represents a boron atom, Y represents an oxygen or sulfur atom, R1 and R2 independently represent a monocyclic aromatic group, a polycyclic aromatic group, or a heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur atoms, R3 represents a hydrogen atom; —(CH2)m—NR4R5; —CO—(CH2)m—NR4R5; —COCH(NH2)R6; —CHR7R8; —CH2CH(NH2)—R9; quinolyl substituted with C1-C4 alkyl group; or C1-C4 alkyl substituted with pyridyl, piperidino or pyrrolidinyl group, and X represents a monocyclic aromatic group, a polycyclic aromatic group or a heterocyclic group, which may be the same as or different from R1 and R2, or a bifunctional group having a monocyclic aromatic group, polycyclic aromatic group or heterocyclic group bonded to each side of a group selected from the group consisting of a single bond, O, CH2, S, SO2, CH2OCH2, OCH2, OCH2CH2OCH2, OCH2OCH2CH2 and CH2OCH2CH2, or a salt thereof, and a composition for contr

Abstract: [Problem] To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. [Means for Solving Problems] The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R1 represents alkyl, alkenyl, etc.; R2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m+ represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: A process for improving the recovery of solid triphenylboron-pyridine compound (TPBP), while retaining desirable particle characteristics comprises the addition of an acid to neutralize at least a portion of the alkali contained in the aqueous mother liquor. By adjusting the pH of the product slurry to between about 8.5 and about 12, it is possible to increase product recovery by more than 10%, while maintaining desirable particle characteristics.