Abstract: Provided is a fluoroboron compound which is highly safe and stable and is capable of forming a cyclic ether-fused ring by the intramolecular alkoxymethylation reaction, or a salt thereof. The compound can be synthesized by the intramolecular alkoxymethylation reaction of a fluoroboron compound represented by the formula (I) or a salt thereof in the presence of a metal catalyst. (wherein the moiety represented by the formula represents an aromatic ring; L represents a substituent such as a halogen atom; R represents a substituted or unsubstituted alkylene group having 1 or 2 carbon atoms; and M represents an alkali metal cation or the like, with the proviso that L and —R—OCH2BF3M are respectively located on contiguous carbon atoms on the aromatic ring, or in the case of a fused aromatic ring, on two carbon atoms adjacent to one carbon at the fused position).

Abstract: The invention disclosed relates to cross-linkable composites of boronic acid or a boronic acid derivative such as a boronate, and an organic or organo-metallic moiety having a functionality such as hole transporting, electron transporting and light emitting, to cross-linked composites and to methods for making same. Multi-layer materials and optoelectronic devices including such cross-linked composites are also disclosed.

Abstract: The present invention provides an economically and industrially superior simple process that enables the selective production of an aromatic heterocyclic monoboron compound and aromatic heterocyclic diboron compound at a satisfactory yield and in a desired ratio by reacting an aromatic heterocyclic compound and a boron compound in a single step under mild conditions while changing only the charged ratios of the raw materials. The present invention provides a production process of a heteroaryl mono- or diboron compound comprising an aromatic heterocyclic compound and a boron compound in the form of bis(pinacolate)diboron or pinacolate diborane in the presence of a iridium-containing catalyst and a ligand such as a bipyridyl ligand.

Abstract: The present invention provides compounds of Formula (I): along with compositions containing the same and methods of use thereof in treating oxidative stress.

Abstract: The present invention provides novel compounds which mimic peptides with a C-terminal penultimate proline, such compounds being useful as protease inhibitors, particularly as inhibitors of serine proteases, and more particularly as inhibitors of the NS3 serine protease from hepatitis C. The compounds find utility as antiviral agents directed at hepatitis C. The invention further provides methods of employing such inhibitors, alone or in combination with other therapeutic agents, to treat hepatitis C infection in a subject in need of such treatment.

Abstract: Polyfluorene polymers and copolymers having substantial amounts (10-100%) of fluorenes coupled at the 2 and 5 positions of fluorene are useful as active layers in OLED devices where triplet energies >2.10 eV are required.

Abstract: The invention provides compounds that inhibit a viral protease enzyme of the hepatitis C virus (HCV). The compounds are adapted for treatment of a HCV infection in a patient with the disease. The compounds include analogs of tripeptides and tetrapeptides that resemble the viral protease substrate. The invention also provides pharmaceutical compositions and combinations, methods of preparation of the compounds, and methods of treatment of patients afflicted with HCV using the compounds.

Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.

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: Organic compounds of formula I may be used in optoelectronic devices wherein R1 is, independently at each occurrence, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; R2 is, independently at each occurrence, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; a is, independently at each occurrence, an integer ranging from 0-4; b is, independently at each occurrence, an integer ranging from 0-3; Ar1 is a direct bond or heteroaryl, aryl, or alkyl or cycloalkyl; Ar2 is heteroaryl, aryl, or alkyl or cycloalkyl; c is 0, 1 or 2; and n is an integer ranging from 2-4.

Abstract: The intermediate (4aS-Cis)-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-8-me-thoxy-4-oxo-1,4-dihydro-3-quinoline carboxylic acid-O3,O4)bis(acyloxy-0) borate and a method of preparation. The intermediate is useful in an improved process for the preparation of moxifloxacin hydrochloride from ethyl 1-cyclopropyl 6,7-difluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinolinecarboxylate.

Abstract: The present invention relates to new dialkylborane amine complexes, a process for the synthesis of new dialkylborane amine complexes, solutions comprising new dialkylborane amine complexes and a method of using new dialkylborane amine complexes for organic reactions.

Abstract: There are provided a novel compound which captures a multisite phosphorylated peptide or protein specifically to a phosphorylation site and a method for detecting a multisite phosphorylated peptide or protein using the same. In particular, there are provided a compound which specifically detects an excessively phosphorylated tau protein observed in the brain affected by Alzheimer's disease and a method for diagnosing Alzheimer's disease in vitro or in vivo using the compound.

Abstract: A process is used for the preparation of 1,3,2-oxazaborolidine compounds. This process prepares compounds of formula (I) or (IA): in which: R1 is an alkyl or an aryl; and R2, R3, R4 and R5 are especially a hydrogen atom or an alkyl, wherein the following are reacted in two steps: a) a boric precursor compound with an acetal compound to give a boronate compound; and b) the boronate compound with an amino alcohol compound. This process avoids by-products and exhibits a very good stereospecificity.

Abstract: Processes are described for the synthesis of 3-hydroxymorphinan derivatives by hydrolysis of side products from the O-demethylation of 3-methoxymorphinan derivatives.

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: The invention relates to a method for producing alkyl-substituted aromatic and heteroaromatic compounds by cross-coupling alkyl boronic acids with aryl- or heteroaryl-halogenides or with aryl- or heteroaryl-sulfonates in the presence of a catalyst and of a Brönsted base in a solvent or solvent mixture.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: A process for producing solid triphenylboron-pyridine (TPBP) spherical particles by separately feeding into a vigorously agitated reaction zone (i) a stream of pyridine and a (ii) stream comprising a solution of sodium hydroxide adduct of triphenylboron (TPBA) whereby the total concentration of TPBA in the combined feed streams is in the range of from 1 wt % to 6 wt %, and simultaneously removing a product stream from said reaction zone and recovering the triphenylboron-pyridine (TPBP) particles.

Abstract: The present invention provides methods for preparing complexed diaryl boronic acids from alkyl diarylborinates.

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: In a process for the accelerated reduction of organic substrates, selected from the group consisting of ester, amides, nitriles, acids, ketones, imines or mixtures thereof, the substrates are reacted with an amine borane, sulfide borane or ether borane complex as a borane source in the presence of organic accelerator compounds containing both Lewis acidic and Lewis basic sites in their structure, of which the Lewis acidic site can coordinate with the carbonyl or nitrile or imine group of the substrate and the Lewis basic site can coordinate with the borane.

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: A class of 2,4-; 2,3,4-; 2,4,6-; 2,3,4,5,6-substituted pyridines is provided which include novel compounds. The substitutions are achieved according to methods disclosed herein in which a metallated pyridine is reacted with an electrophile. Suitable electrophiles include CO2, SO2, dialkylcarbonates, ureas, formamides, amides, carboxylic acid esters, mono- and dihaloalkyls, halogens such as chlorine, fluorine, bromine, and iodine, metallic salts, sulfones, sulfonyls, aldehydes, ketones, anhydrides, nitriles, and electrophilic boron compounds including, but not limited to, boron trialkoxides and boron trihalides.

Abstract: Emissive phosphorescent organometallic compounds that produce electroluminescence and organic light emitting devices employing such emissive phosphorescent organometallic compounds are provided. More specifically the present invention is directed to novel primarily non-emitting ligands which produce a blue shift in emitted light when associated with a cyclometallated ligand.

Abstract: Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.

Abstract: Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-?) in a subject in need thereof.

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 boron complexes are blue emissive electroluminescent compounds.

Abstract: Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: Provision of a novel platinum complex which is useful as a material for a light-emitting device of good light emission characteristic and light emission efficiency, and a novel light-emitting material that may be utilized in various fields. A platinum complex represented by the following general formula (1): (in which two rings of ring A, ring B, ring C, and ring D represent nitrogen-containing heterocyclic rings which may have a substituent and the remaining two rings of them represent aryl rings or hetero aryl rings which may have a substituent, the ring A and the ring B, the ring A and the ring C or/and the ring B and the rind D may form condensed rings. Two of X1, X2, X3, and X4 represent nitrogen atoms coordination bonded to a platinum atom and the remaining two of them represent carbon atoms or nitrogen atoms.

Abstract: The present invention provides fused ring heterocycles as kinase modulators, pharmaceutical compositions containing these modulators, and methods of using these modulators to treat diseases mediated by kinase activity.

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: Metal hydride materials react with BZ3 compounds in the presence of ligand to form BH3-L compounds. A compound of the formula HBZ2 is prepared from a compound of the formula BZ3 by reacting a first amount of a compound of the formula HBZ2 with a metal hydride material “MH” and a compound “L” to form a material of the formula BH3-L, and then reacting the BH3-L thus formed with a compound of the formula BZ3 to form HBZ2 in a second amount greater than the first amount of HBZ2. Z is selected from alkoxy, aryloxy, amido, arylamido, doubly substituted alkoxy, doubly substituted aryloxy, doubly substituted amido, doubly substituted arylamido, alkoxy-amido, and aryloxy-arylamido. When Z is bidentate, then HBZ2 has a ring structure. “L” is selected from ethers, aromatic ethers, amines, aromatic amines, heterocyclic nitrogen compounds, sulfides, aromatic sulfides, and heterocyclic sulfur compounds. “L” becomes a ligand in the BH3-L material.

Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.

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.

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 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: A hole transporting or hole conducting material for use in electroluminescent devices is a diamino dianthracene.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: A process for the preparation of the boron difluoride chelate of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolone carboxylic acid via: (a) the reaction of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolone carboxylic acid ethyl ester with, (b) fluoroboric acid in the presence of poly(methylhydrosiloxane) or hexamethyldisiloxane.

Abstract: Monomers having the formula X1—Ar1-[triarylamine]—Ar2-X2 wherein the triarylamine unit comprises at least one nitrogen atom in the backbone of the monomer and at least three substituted or unsubstituted aryl or heteroaryl groups and wherein X1 and X2 are the same or different polymerizable groups and wherein Ar1 and Ar2 are the same or different substituted or unsubstituted aryl or heteroaryl groups. Polymers and copolymers comprising such monomers are also described. The polymers have particular application in organic optoelectronic devices such as organic electroluminescent devices and organic photovoltaic devices.

Abstract: A process for producing solid triphenylboron-pyridine (TPBP) spherical particles by separately feeding into a vigorously agitated reaction zone (i) a stream of pyridine and a (ii) stream comprising a solution of sodium hydroxide adduct of triphenylboron (TPBA) whereby the total concentration of TPBA in the combined feed streams is in the range of from 1 wt % to 6 wt %, and simultaneously removing a product stream from said reaction zone and recovering the triphenylboron-pyridine (TPBP) particles.

Abstract: Disclosed are borate and boronate compounds of the formulae where R1, R2 and R3 are independently hydrogen, straight or branched chain alkyl of 1 to 24 carbon atoms, straight or branched chain alkenyl of 2 to 24 carbon atoms, cycloalkyl of 5 to 12 carbon atoms, aryl of 6 to 10 carbon atoms, aralkyl of 7 to 15 carbon atoms, alkaryl of 7 to 15 carbon atoms; Ar is substituted or unsubstituted aryl of 6 to 10 carbon atoms; and R4 and R5 are independently defined as for R1 and may also be hydroxyphenyl or alkylated hydroxyphenyl, or R4 and R5 together with the —OBO— group form a substituted or unsubstituted 5 or 6 membered ring. The borate and boronate compounds are effective as antiwear, extreme pressure, and friction modifying additives for lubricating oils and fuels.

Abstract: Hydroxynaphthyridinone carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein L, R1a, R1b, R1c, R2a, R2b, R3, R4, and R5 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process.

Abstract: An organic EL device according to the present invention has a layered structure in which a hole injection electrode (anode), a hole injection layer, a hole transport layer, a light emitting layer, a hole blocking layer, an electron injection layer, and an electron injection electrode (cathode) are layered in this order on a substrate. The light emitting layer is composed of a host material and an emitting dopant. A compound for light emitting device which is an organic material is employed for the emitting material. The compound for light emitting device is a metal complex employing a ligand having a substituent containing boron.

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: Salts of a pharmaceutically acceptable divalent metal and an organoboronic acid drug. Examples of such metals are calcium, magnesium and zinc. The organoboronic acid drug may be a boropeptide protease inhibitor. The salts may be formulated in oral dosage form.