Abstract: The present invention provides a method for preparing a solid acrylamide alkyl sulfonate. Said method comprises: reacting 2-acrylamido-2-methylpropanesulfonic acid and analogs thereof with an alkaline substance in a solvent. The 2-acrylamido-2-methylpropanesulfonic acid and the analogs thereof and the alkaline substance are significant excess with respect to the solvent, so that the amount of the resulting acrylamido alkyl sulfonate exceeds the solubility under the reaction condition. The acrylamido alkyl sulfonate can be continuously generated and directly massively precipitated, and the precipitated solid product, i.e. the product, is collected. The method of the present invention can greatly improve production efficiency of products, save time, reduce cost, and easy to operate by leaving out the re-crystallization step and the like in the prior art.

Abstract: A process for producing dimethyl sulfoxide, wherein said process comprises the following steps: (1) contacting hydrogen sulfide with methanol to produce a mixture containing dimethyl sulfide, and separating dimethyl sulfide from the mixture; and (2) in the presence or absence of a solvent, contacting dimethyl sulfide obtained in step (1) with at least one oxidant and a catalyst to produce a mixture containing dimethyl sulfoxide, said catalyst comprises at least one Ti—Si molecular sieve.

Abstract: The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.

Abstract: Provided herein are new processes for the preparation of aminosulfone intermediates for the synthesis of 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, which is useful for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. Further provided herein are processes for the commercial production of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine.

Abstract: In a process for oxidizing a feed comprising cyclohexylbenzene, the feed is contacted with oxygen and an oxidation catalyst in a plurality of reaction zones connected in series, the contacting being conducted under conditions being effective to oxidize part of the cyclohexylbenzene in the feed to cyclohexylbenzene hydroperoxide in each reaction zone. At least one of the plurality of reaction zones has a reaction condition that is different from another of the plurality of reaction zones. The different reaction conditions may include one or more of (a) a progressively decreasing temperature and (b) a progressively increasing oxidation catalyst concentration as the feed flows from one reaction zone to subsequent reaction zones in the series.

Abstract: Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.

Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.

Abstract: Lactams of formulae (I) and (II) and their use in the treatment of microbial infections and microbial contamination of surfaces, particularly infections and surface contaminations characterized by biofilm formation. Compounds of formula (I) and (II) substituted with acrylate or methacrylate groups and their attachment to surfaces or polymers to inhibit microbial contamination are also provided.

Abstract: The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention relates to the use of compounds of general formula wherein R1 is phenyl or pyridinyl, which are optionally substituted by halogen, cyano or lower alkyl substituted by halogen, or is dihydro-pyran-4-yl; R2 is hydrogen or lower alkyl; R3 is —(CHR)n-phenyl, optionally substituted by lower alkoxy or S(O)2-lower alkyl, or is heterocycloalkyl, optionally substituted by ?O and lower alkyl, or is —(CH2)n-five or six membered heteroaryl, optionally substituted by lower alkyl, or is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, —NR—S(O)2-lower alkyl, —(CH2)n-cycloalkyl or —(CH2)n—S(O)2-lower alkyl; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl ring, selected from the group consisting of 1,1-dioxo-thiomorpholinyl, morpholinyl, or pyrrolidinyl, optionally substituted by hydroxyl; R is hydrogen or lower alkyl; n is 0, 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture

Abstract: The present invention relates to a method for preparing (?)-huperzine A. The method involves: allowing a mixture of (±)-huperzine A obtained from chemical synthesis and a chiral acid to form (±)-huperzine A chiral acid salt under suitable conditions; recrystallizing the chiral acid salt from an organic solvent and basifying with an alkali to obtain optically pure (?)-huperzine A. The method is convenient to operate and suitable for industrial production. The chemical purity and optical purity of (?)-huperzine A obtained by the method are each greater than 99.5%, satisfying the requirement for raw pharmaceutical purity in the pharmaceutical industry.

Abstract: A compound having a V2 receptor agonistic activity is provided. Providing a pharmaceutical composition which contains, as an active ingredient, a compound represented by general formula (I) described below: [R1 is formula described below: (A is a lower alkylene group which may be substituted with lower alkyl group; R6 is a hydrogen atom; R7 is a hydroxyl group, an aromatic heterocyclic group which may be substituted with lower alkyl group, carbamoyl group); R2 is a hydrogen atom or lower alkyl group; R3 is lower alkyl group which may be substituted with 1-3 fluorine atoms, or halogen atom; R4 is a five-membered aromatic monocyclic heterocyclic group, five-membered non-aromatic monocyclic heterocyclic group, (provided each heterocyclic groups contain at least one nitrogen atom and may be substituted with a lower alkyl group); and R5 is a lower alkyl group, halogen atom], or pharmacologically acceptable salt thereof.

Abstract: Method of lightening the color of mixtures comprising imidazolium salts or imidazoles, wherein the mixtures are treated with an oxidant.

Abstract: Provided herein are compositions of matter and pharmaceutical compositions thereof, for use in inhibiting the growth of various microbial pathogens, including bacteria, fungi, protozoa, and viral pathogens. Also provided herein are methods of treating microbial diseases/infections and cancer with the compositions. The compositions are additionally useful in wood preservation and food preservation by inhibition of microbial growth.

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.

Abstract: Provided is a 5,6-diaryl-2-pyrazyl triflate, its synthetic method, and a method for synthesizing an organometallic complex having a triarylpyrazine ligand from the 5,6-diaryl-2-pyrazyl triflate. The triflate is readily obtained from the corresponding 5,6-diarylpyrazin-2-ol, and the palladium-catalyzed coupling of the 5,6-diaryl-2-pyrazyl triflate with an arylboronic acid derivative leads to a high yield of a triarylpyrazine derivative having high purity. The use of the triarylpyrazine derivative in the reaction with a metal compound such as a metal chloride results in an ortho-metallated organometallic complex with high purity. The high purity of the organometallic complex contributes to the extremely high durability of a light-emitting element.

Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.

Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.

Abstract: Disclosed is a 2-substituted-2H-1,2,3-triazole derivative, a compound as represented by formula I or II. Also disclosed is a preparation method of the compound as represented by formula I or II, in particular to a preparation method of 2-substituted-4-bromo-5-chloro-1H-1,2,3-triazole, 2-substituted-4-bromo-5-iodo-1H-1,2,3-triazole, and 2-substituted-5-chloro-1H-1,2,3-triazole-4-carboxylic acid. The preparation methods of the present invention are simple and feasible, and has high yield of the obtained compounds.

Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of Linezolid, in high yield and purity, using novel intermediates. In one aspect, provided herein are efficient, industrially advantageous and environmentally friendly processes for the preparation of linezolid, in high yield and with high purity, using novel intermediates. The processes disclosed herein avoid the tedious and cumbersome procedures of the prior processes, thereby resolving the problems associated with the processes described in the prior art, which is more convenient to operate at lab scale and in commercial scale operations.

Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.

Abstract: Base compounds including 1,3-oxazinan-6-one derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde, and their application as corrosion inhibitors with multifunctional properties serving as inhibitory/dispersant of asphaltene in production processes, transportation, refining and storage of crude oil and derivatives. The corrosion inhibitor with inhibitory/dispersant of asphaltenes properties comprises an active substance base of 1,3-oxaninan-6-ones and hydrocarbon solvents such as benzene, toluene, mixed xylenes, o-xylene, m-xylene and p-xylene, diesel, kerosene, jet fuel, alcohols, aliphatic branched and unbranched alcohols containing from 3 to 10 carbon atoms, such as isopropanol, butanol and pentanol, and mixtures of hydrocarbon solvents with aliphatic branched or unbranched liquid fuels. In addition, a process for obtaining 1,3-oxazinan-6-ones derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde is described.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-3 integrin antagonists to target cells expressing alpha-V-beta-3.

Abstract: A polymerizable compound has a practical low melting point, excellent solubility in a general-purpose solvent, and can produce an optical film at low cost, exhibits low reflected luminance, and achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article. A carbonyl compound is useful as a raw material for producing the polymerizable compound. (In the formula (I), Y1 to Y8 represent —C(?O)—O—, G1 and G2 represent a C1-20 divalent linear aliphatic group, Z1 and Z2 represent a C2-10 alkenyl group that is unsubstituted, or substituted with a halogen atom, Ax represents a C2-30 organic group with at least one aromatic ring, Ay represents a hydrogen atom or C1-20 alkyl group, A1 represents a trivalent aromatic group, A2 and A3 represent a C3-30 divalent alicyclic hydrocarbon group, A4 and A5 represent a C6-30 divalent aromatic group or the like, and Q1 represents a hydrogen atom.

Abstract: Compositions useful as plastic additives may be prepared from renewable resources such as vegetable oils by functionalizing an unsaturated fatty acid ester with epoxy, acyloxy, and optionally alkoxy groups.

Abstract: The present invention relates to a new anhydrous crystalline form of Cabazitaxel of formula (I), designated as form H. A further object of the present invention is a processes for the preparation of the above mentioned form H by recrystallization of Cabazitaxel from a mixture of decanoyl- and octanoyl triglycerides or from glycerol trioctanoate. Form H of Cabazitaxel is useful for the preparation of Cabazitaxel, Cabazitaxel salts, and polymorphic forms thereof. It is also particularly useful as a medicament, especially for the treatment of cancers.

Abstract: Industrial scale conversions of 5-hydroxymethylfurfural to commodity chemicals such as 1,2,6-hexanetriol and 1,6-hexanediol by chemocatalytic conversions using hydrogen and a heterogeneous reduction catalyst are provided. The reactions are suitable for use in continuous flow reactors. Methods of carrying out the conversions are provided, as are product and catalyst compositions.

Abstract: PROBLEM TO BE SOLVED A burdock fruit extract containing arctigenin at high content and its production method are provided, and both of which are used for treatment of pancreatic cancer. SOLUTION The burdock fruit extract containing arctigenin at high content by enzymatically converted arctiin into arctigenin with beta-glucosidase, which is an enzyme occurring endogenously in a burdock fruit, and adding ethanol, extracting, concentrating and then freeze-drying or spray drying.

Abstract: The present disclosure provides methods for purifying a 5-(halomethyl)furfural composition, including 5-(chloromethyl)furfural, at operating conditions that decrease or minimize the decomposition or degradation of 5-(chloromethyl)furfural during the process. The methods may employ certain solvents, operating conditions, and/or techniques (e.g., gas stripping). The gaseous 5-(halomethyl)furfural produced from the process can be condensed or deposited to yield 5-(halomethyl)furfural in liquid or solid form. The solid 5-(halomethyl)furfural may be amorphous or crystalline.

Abstract: A process is provided for carrying out an oxidation on a sprayable feed including a furanic substrate to be oxidized and a catalytically effective combination of cobalt, manganese, and bromide components for catalyzing the oxidation of the furanic substrate, which process comprises spraying the feed into a reactor vessel as a mist, supplying an oxidant, reacting the furanic substrate and the oxidant, and managing the exothermic temperature rise due to the reaction through a selection and control of the operating pressure within the reactor vessel. A crude dehydration product from the dehydration of fructose, glucose or both, including 5-hydroxymethylfurfural, can be directly oxidized by the process to produce 2,5-furandicarboxylic acid in surprisingly increased yields.

Abstract: An organic compound that emits blue light with high color purity and has a long lifetime is provided as a novel substance. The organic compound is a fluorescent organic compound having a structure in which benzonaphthofuranylamine is bonded to the 1-position and the 6-position of a pyrene skeleton.

Abstract: This invention relates to novel (±)1-(Dimethylamino)ethyl substituted 6H-benzo[c]chromen-6-one compounds which are useful as pharmaceutical compositions.

Abstract: Embodiments of the present disclosure provide for a method of making an alkylene carbonate, catalysts, methods of converting CO2 to an alkylene carbonate, and the like.

Abstract: Provided is a method for continuously producing a cyclic carbonate, by which generation of a glycol in a reaction for synthesizing a cyclic carbonate is suppressed, and a cyclic carbonate having a high purity can be efficiently obtained even by simple purification. A method for continuously producing a cyclic carbonate, including filling a catalyst in a fixed-bed tube reactor, and continuously feeding carbon dioxide and an epoxide to the fixed-bed tube reactor to thereby bringing the carbon dioxide and the epoxide into contact with the catalyst, while continuously withdrawing the reaction liquid in the fixed-bed tube reactor, wherein the method includes a pre-treatment step in which a pre-treatment liquid containing a cyclic carbonate is brought into contact with the catalyst before feeding the carbon dioxide and the epoxide to the fixed-bed tube reactor, and the generated glycol is removed out of the system.

Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.

Abstract: Provided are quinazolinone compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

Abstract: The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.

Abstract: The present invention is directed to 2-pyridyloxy-4-methyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-methyl compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) wherein R1, R2, R3, R4, R5, R6, R7, L1 and Q1 have the meaning defined in the claims and the description. The present invention also relates to a process for the preparation of the compound of formula (I). The present invention also relates to the use of a compound of formula (I) as an in situ precursor of a triazolinedione reagent for the functionalization of enes, dienes, aryl and heteroaryl systems via the ene reactions, Diels-Alder reactions, and electrophilic aromatic substitution reactions of said reagent.

Abstract: A heteroarylamine compound includes protein kinase inhibition activity, a pharmaceutically acceptable salt thereof and a pharmaceutical composition for preventing and treating a disease caused by abnormal cell growth, which contains the compound as an active ingredient.

Abstract: Compounds of Formulae I? and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.

Abstract: The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract: The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R1, R2, R3, R3?, R4, R5, R6, X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.

Abstract: The present invention provides a method of treating breast cancer that is nonresponsive to treatment with trastuzumab, comprising administering to a subject in need of such treatment a therapeutically effective amount of compound N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.

Abstract: The invention relates to novel bilaterally-substituted tricyclic compounds and pharmaceutical compositions containing them, for use as medicaments. Due to their ability to interact with an internal RNA loop and to mimic a protein ?-helix these compounds are effective in the treatment and/or prevention of HIV-1 (Human Immunodeficiency Virus-1) infection and other diseases such as those caused by other RNA viruses and by gram-positive and gram-negative bacteria, or infectious or chronic diseases responsive to inhibition of DNA transcription, or infectious or chronic diseases where these compounds can be used to modulate the function of RNA internal loops, or infectious or chronic diseases where these compounds can be used as agonists or inhibitors of ?-helical proteins in interaction with other biomolecules.

Abstract: The present invention provides small molecule compounds that can form covalent adducts with specific sequences of RNA, such as the hairpin loop r(CUG)exp sequence which is a cause of myotonic dystrophy type 1 (DM1), or the r(CGG)exp sequence which is a cause of fragile X-associated tremor/ataxia syndrome (FXTAS); to methods of making the small molecule compounds; and to methods of using the small molecular compounds in the treatment of DM1 or of FXTAS in patients afflicted therewith. The invention further provides a method for identifying an RNA target of a small molecule drug in vivo, using a small molecule drug conjugated to an RNA-reactive crosslinker group and a reporter group, contacting a cell or nucleic acid extract with the small molecule drug conjugate, then separating RNA targets crosslinked to the small molecule drug conjugate by interaction of the affinity group with a complementary affinity group.