Abstract: The present invention relates to a method for preparing high-purity 1,3-cyclohexanedimethanol capable of achieving a high conversion rate by allowing most of the reactant to participate in the reaction, and of increasing reaction efficiency and economic efficiency by further simplifying the reaction process, while minimizing by-products within a shorter period of time. Specifically, the method for preparing 1,3-cyclohexanedimethanol includes reducing 1,3-cyclohexanedicarboxylic acid in the presence of a metal catalyst, which is fixed to a silica support and includes a ruthenium (Ru) compound, a tin (Sn) compound and a platinum (Pt) compound in a weight ratio of 1:0.8 to 1.2:1.2 to 2.4.

Abstract: Provided herein are methods of CO2 reduction to methanol or CO using a Cu2O catalyst.

Abstract: A device for manufacturing an organic substance, including: a synthesis gas generation unit for generating a synthesis gas; an impurity concentration reducing unit including an adsorbent which is capable of adsorbing impurities contained in the synthesis gas, and produces a purified gas by contact of the adsorbent with the synthesis gas; an organic substance synthesis unit for producing an organic substance-containing solution from the purified gas as a raw material; an extraction unit for extracting the organic substance by heating the organic substance-containing solution; a heating unit for preparing heated gas to be fed to the adsorbent; and a heat supplying unit which supplies the extraction unit with heat of the heated gas fed from the heating unit to the adsorbent.

Abstract: The invention provides a process for the production of a high purity first diol, selected from the group consisting of C2 to C7 diols from a product stream comprising two or more C2 to C7 diols, said process comprising the steps of: (i) subjecting the product stream to distillation in a first distillation column to provide a bottoms stream comprising high boiling by-products and a top stream comprising a mixture comprising the two or more C2 to C7 diols; (ii) providing said mixture comprising the two or more C2 to C7 diols as a feed to a second distillation column; (iii) providing a feed comprising an extractant to the second distillation column above the mixture comprising the two or more C2 to C7 diols; (iv) operating the second distillation column at a temperature in the range of from 50 to 250° C. and a pressure in the range of from 0.

Abstract: The present invention addresses the problem of providing a method for efficiently producing uniform microparticles of curcumin and/or ?-oryzanol at a higher yield. The target microparticles are produced by dissolving a starting material in a solvent to give a starting material solution and then subjecting the starting material solution to crystallization by a poor solvent method to thereby deposit the starting material. To prepare the starting material solution, curcumin and/or ?-oryzanol are used as the starting material(s) and ethanol is used as the solvent. The starting material(s) and the solvent are stirred in a pressurized state at a temperature of 78.3-130° C. inclusive to give the starting material solution. Then, the starting material solution thus obtained is subjected to crystallization by the poor solvent method and thus the target microparticles are produced.

Abstract: Provided herein are compounds, compositions and method of using thereof to treat or prevent malaria.

Abstract: Provided are purification methods, comprising: (a) providing an organic solvent and a phenolic peroxide formation inhibitor, wherein the organic solvent has a first boiling point at standard atmospheric pressure (bp1) and the phenolic peroxide formation inhibitor has a second boiling point at standard atmospheric pressure (bp2) that satisfy the following inequality (I): bp2?(1.10)(bp1) ??(I); and (b) heating the organic solvent and the phenolic peroxide formation inhibitor to a temperature causing the organic solvent and phenolic peroxide formation inhibitor to vaporize, and (ii) condensing the vaporized organic solvent and peroxide formation inhibitor to provide a purified mixture of the organic solvent and peroxide formation inhibitor. The methods find particular use in the purification of solvents that are useful in process chemicals for the manufacture of semiconductor devices.

Abstract: This invention relates to a process for the purification of dicarboxylic acids obtained from the hydrolysis of carboxylic acid triglycerides having more than one acid functional group. The process comprises in particular the separation of at least some of the glycerine from the hydrolysis product in an aqueous phase, evaporating and/or distilling the resultant organic phase and recovering at least some of the evaporated and/or distilled dicarboxylic acids through at least one crystallisation operation.

Abstract: Methods of preparing substituted bicyclo[0.1.1.1]pentane compounds of Formula (I) comprise reacting a compound of Formula (A) with a compound of Formula (B) in the presence of a first transition metal catalyst selected from a palladium catalyst and a nickel catalyst, where the variables R1, R2, X1 and X2 are as described herein.

Abstract: A method for preparing dialkyl carbonate is provided. The preparation method includes the following steps. An alcohol compound, carbon dioxide and a catalyst are mixed to form a mixing solution. Organic acid is added to the mixing solution to carry out a synthesis reaction of dialkyl carbonate. The alcohol compound includes methanol, ethanol, propanol or butanol. The catalyst includes cerium oxide, zirconium oxide, titanium oxide, lanthanum oxide or a combination thereof. The organic acid includes formic acid, acetic acid, propionic acid, butyric acid, valeric acid or a combination thereof.

Abstract: The invention relates to a polyglycerol partial ester obtainable by esterification of a polyglycerol with a carboxylic acid mixture comprising at least one polyhydroxycarboxylic acid of a hydroxycarboxylic acid having 8 to 32 carbon atoms, at least one short-chain dicarboxylic acid having 2 to 16, preferably 6 to 14, particularly preferably 8 to 12, carbon atoms, at least one long-chain dicarboxylic acid having 24 to 44, preferably 30 to 40, particularly preferably 34 to 38, carbon atoms, and at least one fatty acid selected from linear, unsaturated and branched, saturated fatty acids having 14 to 24 carbon atoms, to a method for preparing polyglycerol partial esters, and to the use of corresponding polyglycerol partial esters as W/O emulsifier.

Abstract: The present invention relates to amantadine nitrate compounds having neural protective effect, and preparation method and medical use thereof. The compounds have the structure of the general formula (II). The compounds have multifunctional mechanisms, including inhibiting NMDA receptors, releasing NO, inhibiting calcium influxes, and having protective effects on cells particularly neurocytes. The compounds can be used in the preparation of medicaments having a cellular protective effect, for prevention or treatment of the diseases related to such as NMDA receptors and elevation of calcium anions in cells, including the diseases related to neurodegeneration such as Alzheimer's disease, Parkinson's disease, cerebral paralysis and glaucoma, and the diseases related to cardio-cerebral-vascular system such as Parkinson's syndrome combined with cerebral arteriosclerosis, as well as respiratory tract infections caused by influenza virus.

Abstract: N-hydroxyalkylated polyamines, methods of making N-hydroxyalkylated polyamines, and drilling fluids containing N-hydroxyalkylated polyamines are provided, in which the N-hydroxyalkylated polyamine includes Formula (I): where R1 and R2 are independently a —C or —CH group; R3 is an aliphatic hydrocarbyl; R4 and R5 are independently acyclic hydrocarbyls, or R1, R2, R4, and R5 are covalently connected to form a cyclic hydrocarbyl; and R6, R7, R8, and R9 are independently acyclic hydrocarbyls or acyclic heterohydrocarbyls.

Abstract: In one aspect, the present disclosure provides diaryl compounds of the formula presented herein. The application also provides compositions and methods of treatment thereof. In some embodiments, these compounds are used in the treatment of bacterial infections or in the treatment of cancer.

Abstract: The present invention relates to a process for preparing 3-(2-hydroxybenzoyloxy)-4-(trimethylammonio)butyrobetaine hydrochloride of formula (I), wherein the process comprises reacting 3-hydroxy-4-(trimethylammonio)butyrobetaine or a salt thereof with a 2-alkoxybenzoyl chloride of formula (III), and where R is selected from benzyl and branched C3-C6 alkyl groups. The present invention further relates to compounds of formula (II) and salts thereof, where R is selected from benzyl and branched C3-C6 alkyl groups, and to a process for preparing same.

Abstract: Provided are new crystalline forms A, B, C, D and E of sacubitril sodium salt and a method for preparation thereof, pharmaceutical compositions thereof, and application thereof in preparing drugs for enkephalinase-related diseases.

Abstract: The invention relates to a process for preparing liquid, storage-stable isocyanate mixtures having carbodiimide (CD) and/or uretonimine (UI) groups or prepolymers derived therefrom, wherein (i) in a first step, a starting isocyanate which is an organic isocyanate or a mixture of two or more organic isocyanates is partly carbodiimidized with a catalyst K of the formula cyclo-C4H6P(O)R, where the substituent R is a saturated or unsaturated, optionally substituted, especially halogen-substituted, organic radical, and then (ii) in a second step, the carbodiimidization reaction is stopped at a temperature of ?80° C. by adding a stopper, the stopper used being an organic silane S of the general formula HnSiX4-n, where n is a natural number in the range from 1 to 3, where X is a saturated or unsaturated, optionally substituted, especially halogen-substituted, organic radical.

Abstract: A process for preparing polyaryl ethers in which a polycondensation of the monomer building blocks is carried out using microwave irradiation leads to thermoplastic molding compositions having improved color properties.

Abstract: The present invention discloses an amino mercaptan compound, preparation method thereof and use thereof in radiation protection. The compound has the structure of formula I, wherein A1 is selected from: —C(O)NR8—, —S(O)2—NR8—, —S(O)NR8—, and —R7—NR8—; A2 is selected from: carbonyl, sulfonyl, sulfinyl, substituted or unsubstituted C1-6 alkyl; R1, R2, R5, and R6 may be the same or different and are selected from: hydrogen, substituted or unsubstituted C1-C5 alkyl or heteroalkyl; n is an integer from 0 to 20,000; R3 and R4 are independently selected from: hydrogen, X, substituted or unsubstituted C1-6 alkyl; X is selected from: F, Cl, Br and I; R7 is selected from: substituted or unsubstituted C1-C6 alkyl; and R8 is selected from: hydrogen, substituted or unsubstituted C1-C6 alkyl.

Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

Abstract: A nobel therapeutic agent for diabetes which can suppress occurrence of side effects such as persistent hypoglycemia is provided. The active ingredient is a derivative of 1,1-diphenylsemicarbazide or 1,1-diphenylthiosemicarbazide. In particular, the active ingredient is a derivative of 1,1-diphenyl-4-cyclohexyl-semicarbazide or 1,1-diphenyl-4-cyclohexyl-thiosemicarbazide exhibiting hypoglycemic action when orally administered.

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: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.

Abstract: The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: A compound represented by formula (1) is described: The compound has an excellent efficacy for controlling plant diseases, and is thus useful as an active ingredient for an agent for controlling plant diseases.

Abstract: Provided herein are pyridinethiones, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative, inflammatory, neurodegenerative, or immune-mediated disease (e.g., multiple sclerosis).

Abstract: The present invention relates to a compound having the structure of formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where X, Y, Z, R, R1, R2, R3, R4, R5, and R6 are as described herein. The present invention also relates to compositions containing the compound having the structure of formula (I), and a method of treating cancer in a subject.

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, U, V, Z, W1, W2, W3, and R1-R6 are described herein.

Abstract: The present invention relates to a method for synthesizing a compound of 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid, wherein including the steps of: (A) the diethyl ester compounds represented by the following Formula IV are reacted under the action of amine, alkali and carbonyl reagents to produce the acrylic diester compound represented by the following Formula I, wherein (B) the above compound represented by the Formula I is reacted with a fluoride reagent, a Lewis acid and a methyl hydrazine to form a pyrazole ring-containing diester compound represented by the Formula II, (C) the heterocyclic-containing diester compound represented by the Formula II is reacted with a base to give 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid represented by the Formula III.

Abstract: An electrically conducting organic oligomer made from the steps of preparing an acidic aqueous solution with a monomer; preparing the acidic aqueous solution by mixing a solution of about 1.6 wt % HCl in DI water with a monomer; forming about a 0.3 M solution preparing a second aqueous solution with a sodium persulfate oxidant; mixing the acidic aqueous solution with the second aqueous solution; and allowing a reaction to proceed at about 40° C.

Abstract: The present invention relates to processes for the preparation of eluxadoline and its intermediates.

Abstract: Small molecule inhibitors (SMIs) of the Prolactin receptor, pharmaceutical compositions of the SMIs, and methods for treating patients suffering from disorders characterized increased expression or excitation of the Prolactin receptor, including breast cancer, prostate cancer and nociceptive pain disorders such as migraine headache, by administering pharmaceutical compositions of SMIs are provided.

Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating autism spectrum disorder, which includes piperazine-1-carboxamidine or a pharmaceutically acceptable salt thereof as an active ingredient. In particular, the piperazine-1-carboxamidine of the present invention exhibits, in valproic acid-induced autism rat models, an effect of improving the degrees of social interaction and social preference, reducing repetitive or restricted behaviors, hyperactivity, and impulsive behaviors, and also enhancing electroshock-induced seizure threshold susceptibility, and thus the piperazine-1-carboxamidine of the present invention may be used as an active ingredient of a pharmaceutical composition for preventing or treating direct causative symptoms, such as hyperactivity, lack of sociability, and epileptic convulsions of autism spectrum disorder.

Abstract: The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost.

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases cases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: Compounds of formula (I) and salts thereof: wherein R1, R2, R3, a, X1, X2, X3, X4, and X5 are as defined hereinbefore. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain containing proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.

Abstract: Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and for the treatment of castration-resistant prostate cancer.

Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Abstract: One embodiment provides a compound of Formula I that activates autophagy, a pharmaceutical composition and use thereof:

Abstract: The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of delta opioid receptor, biased and/or unbiased, and/or methods for treating pain, migraines, headaches, depression, Parkinsons Disease, anxiety, and/or overactive bladder, and other disorders and conditions described herein or any combination thereof.

Abstract: The present disclosure provides compounds that may be useful for inhibiting Wnt pathway comprising compounds of the formula: (Ia) or (Ib) wherein the variables are as defined herein. In some aspects, the compounds may be used to inhibit the Wnt pathway and used to treat cancer, myocardial infarction, osteopetrosis, or used in the maturation of a precursor cell to a mature cell. Also provided herein in are pharmaceutical compositions of the compounds described herein.

Abstract: Described herein are crystalline forms of pharmaceutically acceptable salts of the lysyl oxidase-like 2 (LOXL2) inhibitor (3-(4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yloxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl)methanone. Also described are methods of making the LOXL2 inhibitor, pharmaceutical compositions and medicaments comprising the LOXL2 inhibitor, and methods of using the LOXL2 inhibitor in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.

Abstract: Disclosed herein, in various embodiments, are compounds having dual activity as PARP1 and CDK inhibitors, and pharmaceutical compositions comprising the same. In some embodiments, the present disclosure provides for methods of treating diseases or conditions in a subject in need thereof, comprising administering one or more compounds disclosed herein. In some embodiment, the disease is cancer, including breast cancer.

Abstract: Disclosed herein, in various embodiments, are compounds having dual activity as PARP1 and CDK inhibitors, and pharmaceutical compositions comprising the same. In some embodiments, the present disclosure provides for methods of treating diseases or conditions in a subject in need thereof, comprising administering one or more compounds disclosed herein. In some embodiment, the disease is cancer, including breast cancer.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are biased agonists, or ?-Arrestin agonists of the angiotensin II receptor, which may be used as medicaments.

Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.

Abstract: This invention is directed to novel carbocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention.