Abstract: The present invention relates, in part, to an improved process for oxidation of alcohols containing oxidatively sensitive functional groups, using inexpensive reagents under mild reaction conditions to provide high yields of carbonyl products such as aldehydes or ketones. In certain embodiments, an aldehyde product is obtained by contacting an oxidatively sensitive alcohol, such as an alkenol, with an oxidant and a TEMPO catalyst under conditions sufficient to convert the alkenol to the aldehyde.

Abstract: The present invention provides a particulate composition wherein an oil component containing reduced coenzyme Q10 is polydispersed forming a domain in a matrix containing a water-soluble excipient, which simultaneously shows high oxidative stability and high oral absorbability, a production method thereof, and a stabilizing method thereof. It also provides a food, food with nutrient function claims, food for specified health uses, dietary supplement, nutritional product, animal drug, drink, feed, pet food, cosmetic, pharmaceutical product, therapeutic drug, prophylactic drug and the like, which contain the composition.

Abstract: Embodiments relate to methods of metal oxide nanocrystals preparation. In embodiments, a metal-organic precursor may be economically synthesized by reacting a metal with an organic acid. The organic acid may include an aliphatic chain longer than three carbon atoms. The metal may be In, Sn, Al, Ga, Zn, Cd, Sb, Bi, Ge, Mn, Ti, Nb, V, Cr, Mo, Fe, Y, Mg, Co, as well as mixtures thereof. Further processing of the metal-organic precursor (e.g. by pyrolysis, hydrolysis, or alcoholysis) produces metal oxide nanocrystals of desired characteristics. An metal-organic precursor of indium tin oxide (ITO) may be synthesized by reacting indium metal and tin metal with an organic acid having an aliphatic chain longer than three carbon atoms (e.g. stearic acid) at a temperature above 200° C. Further processing of the resulting metal-organic precursor yields ITO nanocrystals of regular shape, uniform size, and average diameter ranging of between about 1-500 nm.

Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: The current invention pertains to a process for producing a terephthalate ester comprising: providing reclaimed carpet material comprising a polyester component; and reacting the polyester component with an alcohol having from 6 to 20 carbon atoms and under conditions effective to produce a terephthalate ester; wherein 15-40% of the mass of the terephthalate ester is derived from the polyester present in the reclaimed carpet material.

Abstract: The invention relates to a method for preparing di- or tricarboxylic esters by alkoxycarbonylation of dienes having conjugated double bonds. The method includes the steps of initially charging a diene having two conjugated double bonds, adding a phosphine ligand according to formula (I) and a catalyst precursor, adding an alcohol, feeding in CO, and heating the reaction mixture with conversion of the diene to a di- or tricarboxylic ester.

Abstract: The invention relates to a process for preparing primary amines, which comprises hydrogenating at least one nitrile in an apparatus (V1) in the presence of an unsupported cobalt catalyst to obtain at least one primary amine, with recurrent or continuous addition of at least one compound (I) to the apparatus (V1), said compound (I) comprising at least one component selected from alkali metal, alkaline earth metal and rare earth metal.

Abstract: An asymmetric diamine suitable for preparing a soluble polyimide and a method for preparing the same, including a compound represented by the following formula (1): wherein R1, R2, R3 and R4 are, independently of each other, a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an alkoxy group having 1 to 3 carbon atoms, and A and B are, independently of each other, a nitro group or an amino group. Further, a method for preparing the compound represented by the aforesaid formula (1).

Abstract: The present invention relates to substantially pure metabolites of irara-clomiphene. The invention is also directed to pharmaceutical compositions comprising these metabolites and their use in treating disorders including secondary hypogonadism, type 2 diabetes, elevated cholesterol, elevated triglycerides, wasting, lipodystrophy, female and male infertility, benign prostate hypertrophy, prostate cancer, breast cancer, ovarian cancer and endometrial cancer.

Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Abstract: There are provided pyrrolysine analogs of the formulae (X), (I), (II), (V), (VI), (VII) and (VIII), in which the a, b, d, X, Y, Z, FG, R, R1, R2 and R3 are as defined in the claims, which are useful in bioconjugation processes and mutant proteins containing them.

Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.

Abstract: The invention discloses compounds of Formula (I) wherein R1, R2, R2A, R3, R3A, R4, R4A, and R5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

Abstract: 4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a 3,3-dialkoxyprop-1-yne and a substituted methylene amine by a series of steps.

Abstract: The present invention relates to a new type of eutectic crystal of lorcaserin hydrochloride and benzoic acid, when compared with the prior art, the eutectic crystal has the improved properties of good stability, low solubility, and being suitable for the application of controlled-release preparation; the present invention also relates to a method for preparing the eutectic crystal, a pharmaceutical composition thereof and the use thereof in the manufacture of drugs for treating and/or preventing diseases associated with 5HT2C.

Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract: To provide a hydrogen barrier agent capable of imparting hydrogen barrier performance to various materials; a hydrogen barrier film forming composition including the hydrogen barrier agent; a hydrogen barrier film including the hydrogen barrier agent; a method for producing a hydrogen barrier film, which uses the hydrogen barrier film forming composition; and an electronic element provided with the hydrogen barrier film. A compound having a specific structure including an imidazolyl group is used as the hydrogen barrier agent. Furthermore, the hydrogen barrier film forming composition is prepared by blending the above-mentioned hydrogen barrier agent into the base material component. In addition, the hydrogen barrier film is formed using the hydrogen barrier film forming composition.

Abstract: The present invention relates to colchicine-binding site compounds having anti-cancer activity, compositions comprising the same, and their use for treating various forms of cancer.

Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract: Provided is a preparation method for revaprazan hydrochloride, the method comprising: (1) the preparation of 4-hydroxyl-2-(4-fluoroaniline)-5,6-dimethylpyrimidine; (2) the preparation of 4-chloro-2-(4-fluoroaniline)-5,6-dimethylpyrimidine; (3) the preparation of revaprazan hydrochloride. The method has advantages such as simple operations, high product purity, good yield and suitability for industrial production.

Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,

Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I), (II), (IIa), (III), (IV), (V), or (VI)) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.

Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.

Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

Abstract: The present application relates to 1,4-disubstituted 1,2,3-Triazole antifungal agents of the formula (I) wherein, R1 is halogens such as fluorine, chlorine or bromine, CF3, alkyl; R2 is alkyl or hydrogen; R3 is halogen selected from fluorine, chlorine or bromine; and n is 0 or 1. The application further relates to the synthesis of said compounds, to fungicidal compositions containing said compounds and to their use in a method for treating fungal infections.

Abstract: Disclosed is a process for the integrated production of urea and melamine. A urea production zone produces a urea synthesis stream comprising urea, water and ammonium carbamate. This stream is subjected to processing, preferably involving stripping, so as to separate an aqueous urea stream from residual dissociated carbamate vapor comprising ammonia, carbon dioxide, and water. The urea is fed to a melamine synthesis zone and subjected to melamine forming conditions so as to form melamine and off-gas comprising carbon dioxide and ammonia. The dissociated carbamate vapor and the melamine off-gas are subjected to combined condensation so as to form a dilute melamine off-gas condensate.

Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.

Abstract: The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel heteroaryl butanoic acid derivatives, methods of using said compounds in the treatment of various diseases and disorders, and processes for preparing the said novel compounds.

Abstract: The present invention is directed to process for preparation of ?-form crystal of Mirabegron, (R)-2-(2-aminothiazol-4-yl)-N-(4-(2-((2-hydroxy-2-phenylethyl) amino) ethyl) phenyl) acetamide of formula (1).

Abstract: The present invention relates to aryl sulfoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulfide and aryl sulfoxide derivatives have the general structure (I) in which the respective radicals are as defined in the description.

Abstract: The present invention relates to a method for prevention of premature polymerization during the preparation, purification, transportation and storage of a polymerizable compound with at least one conjugated unsaturated group in the presence of an azine dye-based compound as inhibitor. Further the present invention relates to methods of preparing such inhibitors as well as to the inhibitors itself, as well as to methods of improving solubility and stability of dissolved inhibitors.

Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Abstract: The present invention relates to a process for the preparation of the compounds II from the respective oxo compounds. Furthermore, he invention relates to a process for the preparation of triazole compounds from oxiranes II.

Abstract: A bioderived based plasticizer is produced by reacting a bioderived diol (and/or a bioderived alcohol) and a bioderived carboxylic acid in the presence of N,N?-dicyclohexylcarbodiimide (DCC), wherein the bioderived carboxylic acid includes a hydrolyzed oil. The bioderived carboxylic acid (e.g., linoleic acid, ?-linolenic acid, oleic acid, and mixtures thereof) may be produced by hydrolyzing a triglyceride, such as canola oil, linseed oil, soybean oil, and mixtures thereof. In one embodiment of the present invention, a bioderived based plasticizer is produced by reacting 2,5-bis-(hydroxymethyl)furan and ?-linolenic acid in the presence of DCC. In some embodiments of the present invention, the bioderived based plasticizer is blended into one or more polymers.

Abstract: A surfactant component comprising a compound of formula (I): (I) wherein R1 is a C5 to C39 alkyl or alkenyl group and R2 is a group of formula (a) wherein one of W, X, Y and Z is a covalent bond and the remaining groups are independently selected from H, M, SO3M and a further group of formula R1CO provided at least one of W, X, Y and Z is SO3M; and each M is independently a hydrogen ion, an ammonium ion or a metal ion.

Abstract: Provided is an enzyme-specific fluorescent compound capable of being retained in cells, which can emit fluorescence specifically in a target cell, particularly a cell capable of expressing a reporter enzyme such as ?-galactosidase, and can covalently bind to a protein in the cell to exhibit an excellent property of being retained in the cell. The fluorescent compound comprises a compound represented by formula (I?) or a salt thereof. In formula (I?), A, X, Y and R1 to R9 are as described in claim 1.

Abstract: The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of a specific type and of at least one Bransted acid or in the presence a specific chiral compound having a Bransted acid functional group in the molecule.

Abstract: Provided herein is a pharmaceutical composition comprising an isoflavonoid derivative and a cyclodextrin. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions. In specific instances, provided herein are intravenous compositions and therapies.

Abstract: The disclosure relates to special orthoformic acid esters of formula (I), as defined herein, which can be used as thermally labile and acid-labile fragrance storage substances. The disclosure further relates to detergents and cleaning agents, cosmetic agents and air freshening products containing such orthoformic acid esters, as well as to a method for lastingly fragrancing surfaces.

Abstract: Disclosed herein are compounds according to Formulas 1-12, compositions comprising these compounds, and methods of lowering intraocular pressure (IOP) or causing hair growth, and methods of using the same.

Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Abstract: The present invention relates to aryl sulphide and aryl sulphoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulphide and aryl sulphoxide derivatives have the general structure (I) in which the respective radicals are as defined in the description.

Abstract: A process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]-benzodiazepin-4-yl]propionic acid methyl ester benzenesulfonate by oxidation of 3-[(S)-7-bromo-2-(2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]d-iazepin-3-yl]propionic acid methyl ester in the presence of an oxidation catalyst is provided.

Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to piperidene compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.

Abstract: Disclosed are 2,2?-bipyridyl compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.

Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.

Abstract: The present invention discloses pharmaceutically acceptable acid salts of pyridine-substituted 2-aminopyridine derivatives as protein kinase inhibitors, preparation methods, pharmaceutical compositions thereof, and use thereof for the treatment of diseases associated with protein kinase.

Abstract: Crystalline Forms R5, R5a, R5b and R6 of nilotinib hydrochloride and processes for their preparation.