Abstract: Recent advancements in LNA oligonucleotides include the use of amine linkers to link an LNA antisense oligonucleotide to a conjugate group. For example please see WO2014/I18267. The present invention originates from the identification of a problem when de-protecting LNA oligonucleotides which comprise an aliphatic amine group and DMF protected LNA G nucleoside, which results in the production of a +28 Da impurity. This problem is solved by using acyl protection groups on the exocyclic nitrogen of the LNA-G residue, rather than the standard DMF protection group.

Abstract: Biomarkers are provided that are predictive of a subject's responsiveness to a therapy comprising a JAK inhibitor. The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having, suspected of having, or at risk of developing Graft-Versus-Host Disease.

Abstract: The present specification relates to a compound containing nitrogen, and a color conversion film, a backlight unit, and a display device, including the same.

Abstract: The present disclosure provides a process for preparing Bortezomib, intermediates, and crystalline forms thereof.

Abstract: An amino-containing organosilicon compound having formula (1) is used for surface treatment of an inorganic filler for thereby rendering the filler more compatible with and adhesive to a polymer material. In formula (1), R1 is alkyl, alkenyl, aryl or aralkyl, R2 is alkenyl, aryl or aralkyl, R3 and R4 each are a monovalent hydrocarbon group, and n is 0, 1 or 2.

Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Abstract: A composition consisting essentially of 90-99 parts by weight of a nitrogen-containing organoxysilane compound and 1-10 parts by weight of an isomer affords an appropriate cure behavior and is useful as paint additive, adhesive, silane coupling agent, textile treating agent, and surface treating agent.

Abstract: The present disclosure relates to an organic electroluminescent compound of Formula 1 (variables Y1, Y2 and R1 to R4 defined herein), and an organic electroluminescent device comprising the same. The organic electroluminescent compound according to the present disclosure can be used for the manufacture of an organic electroluminescent device showing improvement in luminous efficiency, especially in current efficiency.

Abstract: Novel branched oligoarylsilanes of general formula (I) A method of preparation of branched oligoarylsilanes is that a compound of general formula (III) Y-Qk-SiArn—R)3??(III), where Y stands for a residue of boronic acid or its ester or Br or I, reacts under Suzuki conditions with a reagent of general formula (IV) A-Xm-A??(IV), where A stands for: Br or I, provided that Y stands for a residue of boronic acid or its ester; or a residue of boronic acid or its ester, provided that Y stands for Br or I. A technical result is preparation of novel compounds, featured by a high luminescence efficiency, efficient intramolecular energy transfer from some molecular fragments to others, and an increased thermal stability.

Abstract: A reaction method comprising combining a carbonyl-substituted arylboronic acid or ester and an ?-effect amine in aqueous solution at a temperature between about ?5 C to 55 C, and a pH between 2 and 8 to produce an adduct. A process is also provided comprising: contacting a composition having a boron atom bonded to a sp2 hybridized carbon, the boron having at least one labile substituent, conjugated with a cis-carbonyl, with an ?-effect amine, in an aqueous medium for a time sufficient to form an adduct, which may proceed to further products.

Abstract: A process for producing bortezomib N-(pyrazin-2-yl)carbonyl-L-phenylalanine-L-leucine boronic acid) comprising the step of deprotecting the compound of formula XII: to yield bortezomib.

Abstract: Silyl-protected nitrogen-containing cyclic compounds having formula (1) are provided wherein R1, R2 and R3 each are a monovalent hydrocarbon group, R4 and R5 each are a divalent hydrocarbon group, R6, R7 and R8 each are H or a monovalent hydrocarbon group. A is —C(O)OR9 or —C?N, R9 is a monovalent hydrocarbon group, and a is 0 or 1. The compounds are added to polyurethane, polyester or polycarbonate resins to form one part type curable compositions for imparting stiffness, mechanical strength and transparency thereto.

Abstract: The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB and characterized by having water content ranging between 3.5-6.0% w/w; X-ray powder diffraction pattern comprising characteristic 2?° peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6±0.20 2?°, wherein peaks at 9.8 and 11.39±0.20 2?° are un-split and 100% intensity peak is present at 5.6±0.20 2?°, DSC isotherm comprising the endothermic peaks ranging between 45 to 60° C. (Peak-1) and 175 to 185° C. (Peak-2) and IR absorption characteristic peaks approximately at 3387 cm?1, 3304 cm?1, 2953 cm?1, 2927 cm?1, 2868 cm?1, 1627 cm?1, 1455 cm?1, 1400 cm?1, 1201 cm?1, 1150 cm?1, 1020 cm?1, 747 cm?1 and 702 cm?1 and Raman absorption spectra having characteristic peaks approximately at 3066 cm?1, 1583 cm?1, 1528 cm?1, 1281 cm?1, 1213 cm?1, 1035 cm?1, 1022 cm?1 and 1004 cm?1.

Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.

Abstract: The present invention relates to electroluminescent compounds of formula 1 where A and/or B represent fluorene, carbazole, dibenzo[b,d]thiophene or dibenzo[b,d]furan derivatives and L1, X1, Ar1, Ar2, R5, R6 and R7 are as defined herein, and organic electroluminescent devices comprising the same. The compounds according to the present invention have an advantage in manufacturing an organic electroluminescent device which has a high luminous efficiency and a long operational lifetime.

Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compounds, nucleic acids synthesis inhibitory active compounds, mitosis and cell

Abstract: A method for producing a modified conjugated diene polymer usable as a raw material of a crosslinked polymer which is used for use in tires and the like of automobiles and can enhance low fuel consumption performance of automobiles and the like is provided. A method for producing a modified conjugated diene polymer comprising a polymerization step in which a monomer including a conjugated diene compound or a monomer including a conjugated diene compound and an aromatic vinyl compound is polymerized in the presence of at least one compound selected from the group consisting of the following formulae (1) and (2) and an alkali metal compound or an alkaline earth metal compound to obtain a modified conjugated diene polymer. (In the formulae, A1 is a hydrocarbylsilyl group in which three H's (hydrogen atoms) in a “—SiH3” structure are each substituted by a hydrocarbyl group, and R1 and R2 are hydrocarbylene groups.

Abstract: There is disclosed is a method of treating a pulmonary disease using a pyrimidinecarboxamide compound, and a pharmaceutical composition suitable for inhalation comprising the pyrimidinecarboxamide compound.

Abstract: Classes of liquid aminosilanes have been found which allow for the production of silicon carbo-nitride films of the general formula SixCyNz. These aminosilanes, in contrast, to some of the precursors employed heretofore, are liquid at room temperature and pressure allowing for convenient handling. In addition, the invention relates to a process for producing such films. The classes of compounds are generally represented by the formulas: and mixtures thereof, wherein R and R1 in the formulas represent aliphatic groups typically having from 2 to about 10 carbon atoms, e.g., alkyl, cycloalkyl with R and R1 in formula A also being combinable into a cyclic group, and R2 representing a single bond, (CH2)n, a ring, or SiH2.

Abstract: Provided are a compound represented by the following Chemical Formula 1 for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode. The structure of Chemical Formula 1 is described in the specification. The compound for the organic photoelectric device provides an organic light emitting diode having excellent life-span characteristics due to excellent electrochemical and thermal stability and high luminous efficiency at a low driving voltage.

Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.

Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.

Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.

Abstract: This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.

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

Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes a diversity element which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the diversity element. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to said diversity element, and is capable of forming a reversible covalent bond or non-covalent interaction with a binding partner of the linker element. The monomers can be covalently or non-covalently linked together to form a therapeutic multimer or a precursor thereof. Also disclosed is a method of screening for therapeutic multimer precursors which bind to a target molecule associated with a condition and a method of screening for linker elements capable of binding to one another.

Abstract: The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.

Abstract: Provided herein, inter alia, are compositions and methods of synthesis and detection of tetrazines and diazonorcaradienes.

Abstract: Disclosed herein are mono-functional silylating compounds that may exhibit enhanced silylating capabilities. Also disclosed are method of synthesizing and using these compounds. Finally methods to determine effective silylation are also disclosed.

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 heterocyclic compound and an organic light-emitting device including the heterocyclic compound, the heterocyclic compound being represented by Formula 1 below:

Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract: There is disclosed a pyrimidinecarboxamide compound useful as a pharmaceutical agent, synthetic processes, and pharmaceutical compositions which include the pyrimidinecarboxamide compound. More specifically, there is disclosed a CXCR1/2 inhibitor useful for treating a variety of inflammatory and neoplastic disorders.

Abstract: The present invention provides compounds useful for detection of hydrogen peroxide and methods of using same.

Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.

Abstract: An arylalkyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group, a dioxolane group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; Y is CH or a nitrogen atom; q is an integer of 1 to 3; m is an integer of 0 to 5; and n is 0 or 1 or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.

Abstract: Use of a precursor of an n-dopant for doping an organic semiconductive material, as a blocking layer, as a charge injection layer, as an electrode material, as a storage material or as a semiconductor material itself in electronic or optoelectronic components, the precursor being selected from the following formulae 1-3c:

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

Abstract: The present invention relates to boron compounds for use in electronic devices, especially organic electroluminescent devices, and to a process for preparing these compounds and to electronic devices, especially organic electroluminescent devices, comprising these compounds.

Abstract: This invention relates to hydrolysable silanes useful in the modification of elastomers, and as coupling agents for diene elastomer compositions containing a filler. In particular the invention relates to novel hydrolysable silanes containing a piperazine ring and an ether or thioether linkage.

Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The present invention provides compounds of Formula (I) as inhibitors of LMP7 for the treatment of autoimmune and inflammatory diseases.

Abstract: Silyl-protected nitrogen-containing cyclic compounds having formula (1) are provided wherein R1, R2 and R3 each are a monovalent hydrocarbon group, R4 and R5 each are a divalent hydrocarbon group, R6, R7 and R8 each are H or a monovalent hydrocarbon group. A is —C(O)OR9 or —C?N, R9 is a monovalent hydrocarbon group, and a is 0 or 1. The compounds are added to polyurethane, polyester or polycarbonate resins to form one part type curable compositions for imparting stiffness, mechanical strength and transparency thereto.

Abstract: The invention pertains to a near-infrared fluorescent dye that is cell permeable and can be attached to selected proteins in living cells. The dye has the general formula or its corresponding spirolactone wherein Y is chosen from the group consisting of Si, Ge and Sn; R0 is —COO? or COOH; R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are substituents, including hydrogen, independently from each other. The dye (i) absorbs and emits light at wavelengths above 600 nm; (ii) possesses high photostability; (iii) has high extinction coefficients and high quantum yields; (iv) can be derivatized with different molecules; and (v) is membrane-permeable and shows minimal background binding to biomolecules and biomolecular structures.

Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.