Abstract: The present invention relates to a preparation method of 4-isopropylamino-1-butanol, in which using cheap and readily available tetrahydrofuran and acetic acid solution of hydrogen bromide as starting materials to prepare a novel intermediate of 4-isopropylamino-1-acetoxyl butane and further obtain the target product. The present invention has advantages of convenient process operations, mild reaction conditions, economical and environment-friendly benefits, and suitability for industrial production to obtain the product with high purity and high yield.

Abstract: There is provided a method for producing, at a high yield, a composition containing 3-chloro-4-methoxybenzylamine hydrochloride (CMBA-HCl) in which the purity of CMBA-HCl is high. This method comprises a chlorination step involving a chlorination reaction that generates CMBA-HCl from 4-methoxybenzylamine hydrochloride using hydrogen peroxide and hydrochloric acid. There is also provided a CMBA-HCl-containing composition which is produced by the aforementioned production method and in which the purity of CMBA-HCl is high.

Abstract: Provided is a synthesis process for a chiral cyclopropyl ethynyl tertiary alcohol compound, where a chiral amino alcohol or a chiral amino diol is reacted in the presence of an alkaline reagent and a salt to obtain an optically active propynyl alcohol compound. In particular, the process includes (1) reacting cyclopropyl acetylene with a chiral inducing agent, a chiral auxiliary reagent and zinc halide in an organic solvent in the presence of an alkaline reagent and a sulfonate or a sulphinate to obtain a first reaction mixture; (2) reacting the resultant first reaction mixture with 5-chloro-2-aminotrifluorobenzophenone to form (S)-2-amino-5-chloro-?-cyclopropyl acetylene-?-trifluoromethylbenzyl alcohol. The process avoids an organic zinc reagent and a Grignard reagent, and has the advantages of safe production, an environmentally friendly route, low production costs, a high resultant product yield, a high chiral ee value and is suitable for industrial production.

Abstract: A hitherto unknown crystalline form of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence.

Abstract: The present invention concerns new forms of crystalline minocycline base. In particular, two new crystalline polymorphic forms, designated Form IV and Form V of minocycline base are provided. These are characterized by XRD, FTIR and TGA. Processes for preparing the new polymorphic forms and their use in pharmaceutical compositions are also provided. Form IV and form V are prepared by dissolving and/or suspending minocycline base in an organic solvent followed by crystallization.

Abstract: The invention relates to compounds of the formula and to a process for making same and to the use of the products in the solid phase peptide synthesis. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.

Abstract: The present invention provides an isothiocyanate compound and its application. The compound is an aryl-substituted isothiocyanate compound that has a structure of the general formula I. The isothiocyanate compound of the present invention has very good solubility in water, far better inhibitory activity for XPO1 protein than other non-aryl substituted congeneric compounds, little side effects, and good biological safety and bioavailability, and is quite suitable for clinical application. Therefore, the isothiocyanate compound would have tremendous potential market space and economic benefits.

Abstract: The present invention provides a method of making carboxylic acids from levulinic acid, such as succinic acid and 3-hydroxypropanoic acid, by reacting levulinic acid with an oxidant such as hydrogen peroxide under acidic or basic conditions.

Abstract: The present invention is directed to a process for preparing a compound of formula I-11 through multiple-step reactions:

Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.

Abstract: Disclosed herein is a compound represented by formula (1): A-L-B, wherein: A is a group represented by formula (1-A); B is a group represented by formula (1-B); L is a single bond, a substituted or unsubstituted arylene group having 6 to 50 ring carbon atoms, or a substituted or unsubstituted heteroarylene group having 5 to 50 ring atoms; and L is bonded to one of R1 to R4 of formula (1-A) and R11 to R14 of formula (1-B); in which the groups Q1, Q2, L1, L2, R1-R4, R11-R14, Ra-Rd and Re-Rh defined herein. Also disclosed herein are materials and devices containing the compound represented by formula (1).

Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

Abstract: The invention is directed to compounds of general formula (I), and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

Abstract: Disclosed are novel polymorphic solvated and desolvated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

Abstract: The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous forms.

Abstract: Disclosed are novel compounds of specific chemical structures having inhibitory activity on c-Myc/Max/DNA complex formation or pharmaceutically acceptable salts thereof.

Abstract: Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2?(°) as measured by X-ray powder diffractmetry.

Abstract: Bicyclic compounds for decreasing the expression of bacterial virulence factors thereby preventing, mitigating, or treating bacterial infection are provided.

Abstract: The present invention belongs to the field of fungicides, and relates to an amide compound and the preparation method and use thereof. The amide compound is as shown in general formula I: Each substituent in Formula I is defined in the description. The compound of general formula I of the present invention has an outstanding fungicidal activity, and can be used for controlling fungal diseases.

Abstract: An aliphatic-chain saturated hydrocarbon including an aliphatic hydrocarbon chain which is saturated and has an ion pair at each end of the aliphatic hydrocarbon chain.

Abstract: A method for producing a compound (4), which comprises allowing a compound (1) to react with hydrogen gas in an inert solvent, in the presence of a specific chiral ligand and a ruthenium catalyst, or in the presence of an asymmetric transition metal complex catalyst previously generated from the chiral ligand and the ruthenium catalyst.

Abstract: The invention relates to an improved process for preparing [(S)-1-(4-phenyl-1-H-imidazol-2-yl)-ethyl]-amine. The process involves formation of the novel intermediate crystalline compound [(S)-1-(4-phenyl-1-H-imidazol-2-yl)-ethyl]-carbamic acid tert-butyl ester oxalate.

Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R12, R13, R14, A1, A2, A3, n and m are as described herein.

Abstract: A new class of antibiotics effective against methicillin-resistant Staphylococcus aureus (MRSA) is disclosed. Compounds of this class can impair cell-wall biosynthesis by binding to both the allosteric and the catalytic domains of penicillin-binding protein (PBP) 2a. This class of antibiotics holds promise in reversing obsolescence of staphylococcal PBPs as important targets for antibiotics. Embodiments of the invention thus provide novel antibacterial compounds that target penicillin-binding proteins and/or other important cellular targets. Methods for inhibiting the growth and/or replication of bacteria using the compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, including drug-resistant strains of Staphylococcus aureus.

Abstract: The present invention relates to preparation methods of a prostacyclin receptor agonist of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide and its intermediates. These methods are simple and convenient to operate, environment-friendly and suitable for industrial production to obtain the product with good yield and high purity.

Abstract: Provided is a preparation method for 1-substituted-1H-1, 2, 3-triazole-4-carboxylic acid. 1-Substituted-4, 5-dibromo-1H-1,2,3-triazole is added to an isopropylmagnesium chloride to obtain 1-substituted-4-bromo-1H-1,2,3-triazole by a reaction; then an isopropylmagnesium chloride-lithium chloride composite is added directly to obtain a mixture of 1-substituted-1H-1,2,3-triazole-4-carboxylic acid and 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylic acid; secondly, to the mixture, a base and iodomethane are added to obtain 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylic acid methyl ester by a reaction; the aqueous layer is adjusted with hydrochloric acid to pH=1-5, extracted with an organic solvent and dried; then 1-substituted-1H-1,2,3-triazole-4-carboxylic acid is obtained by concentration and crystallization. The method is suitable for industrialized production and has a greater application value.

Abstract: Anticorrosion compounds and compositions can be used in methods for preventing metal corrosion. More specifically, the method comprises contacting an anticorrosion composition to an aqueous system in contact with a metal. The anticorrosion composition comprises substituted and/or hydrogenated benzotriazoles and tolyltriazoles.

Abstract: Disclosed are triazine compounds of formula (I): wherein X, R, A and B are as defined in the description as photostabilising agents against UV-visible radiation.

Abstract: The present invention relates to a process for preparing substituted phenylisoxazoline derivatives.

Abstract: The present invention relates to novel tricyclic compounds which can bind to FXR and act as modulators of the FXR, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the uses of the compounds for the treatment of diseases and/or conditions mediated by FXR. The invention further provides a pharmaceutical composition containing the compound disclosed herein and a method of treatment of diseases and/or conditions mediated by FXR comprising administering the compound or the pharmaceutical composition.

Abstract: This invention pertains generally to compounds of Formula I as described herein and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention provides methods and compositions comprising these compounds for treating infections caused by Gram-negative bacteria.

Abstract: The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.

Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation

Abstract: Disclosed herein a process for the isolation of intermediate of Vortioxetine in a solid state form and an improved, commercially viable and industrially advantageous process for the preparation of vortioxetine or a pharmaceutically acceptable salt thereof, in high yield and purity.

Abstract: Disclosed is a method for preparing a formamide compound, the method uses carbon dioxide, hydrogen and an amine compound as raw materials and a transition metal complex as a catalyst, and the reaction is carried out in an organic solvent or in the absence of a solvent to form a formamide compound. The method of the present invention is an effective method of chemical utilization of carbon dioxide, which has the advantages of high reaction efficiency, a good selectivity, mild conditions, economic and environmental protection, being simple and convenient to operate and the like, and has a good popularization and application prospect.

Abstract: Epoxidation of an olefin is carried out by continuously reacting the olefin with hydrogen peroxide in the presence of a homogeneous epoxidation catalyst in a reaction mixture comprising an aqueous liquid phase and an organic liquid phase, using a loop reactor with mixing of the liquid phases. The loop reactor comprises a measuring section in which the liquid phases are temporarily separated, at least one pH electrode is arranged in the measuring section in contact with the separated aqueous phase, a pH of the separated aqueous phase is determined with the pH electrode and the pH is maintained in a predetermined range by adding acid or base to the loop reactor.

Abstract: Epoxidation of an olefin is carried out by continuously reacting the olefin with hydrogen peroxide in the presence of a water soluble epoxidation catalyst, comprising a manganese complex, in a reaction mixture comprising an aqueous liquid phase and an organic liquid phase using a loop reactor with mixing of the liquid phases, and during the reaction the concentration of hydrogen peroxide in the aqueous liquid phase is maintained at less than 1.0% by weight.

Abstract: In the method for the epoxidation of an olefin, the olefin is continuously reacted with hydrogen peroxide in a mixed reactor in the presence of a water soluble epoxidation catalyst, comprising a manganese complex, the reaction is carried out in a reaction mixture comprising an aqueous liquid phase and an organic liquid phase with mixing of the liquid phases, reaction mixture is continuously withdrawn from the mixed reactor and separated into a separated aqueous phase and a separated organic phase, and part of the separated aqueous phase is continuously recycled into the mixed reactor, with the combined hold-up time of aqueous phase in withdrawing, separating phases and recycling aqueous phase being kept at less than 15 minutes.

Abstract: A method efficiently and safely manufactures, on an industrial scale, a compound having an N,N-bis(2-hydroxy-3-chloropropyl)amino group. (1) an amine compound or a solution thereof, (2) epichlorohydrin or a solution thereof, and (3) an acidic compound or a solution thereof are continuously supplied to a flow reactor and reacted at a reaction temperature of 40 to 130° C. and a liquid space velocity of 0.2 to 10 h?1 so that a compound having an N,N-bis(2-hydroxy-3-chloropropyl)amino group is manufactured. The obtained compound having an N,N-bis(2-hydroxy-3-chloropropyl)amino group is dehydrochlorinated by reaction with an alkali so that a polyfunctional glycidylamine type epoxy compound is manufactured.

Abstract: The integrated processes herein provide improved carbon efficiency for processes based on coal or biomass gasification or steam methane reforming. Provided are also ethylene oxide carbonylation products such as beta-propiolactone and succinic anhydride having a bio-based content between 0% and 100%, and methods for producing and analyzing the same.

Abstract: Provided are processes for monitoring and maintaining continuous carbonylation of epoxides or lactones. Processes include measuring parameters affecting the rate of the carbonylation reaction and adding supplemental replacement catalyst replacement components to maintain a constant rate of carbonylation.

Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth.

Abstract: Compounds of Formula (I), including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Abstract: Methods for treating a tumor, such as a benign or malignant tumor, are disclosed herein. The methods include administering a therapeutically effective amount of a small molecule that selectively binds to and stabilizes G-quadruplex DNA in the promoter of the c-MYC gene to the subject. The methods are also of use to decrease the size and/or number of metastases. Compounds for use in the disclosed methods are also provided.

Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth.

Abstract: 4,6-difluorodibenzofuran derivatives of the formula I the preparation thereof, the use thereof as components in liquid-crystalline media and electro-optical display elements which contain the liquid-crystalline media.

Abstract: The present invention relates to the composition and methods of use of Stat3 pathway inhibitors or cancer stem cell inhibitors in combination treatment of cancer.

Abstract: The present invention relates to the use of a novel class of cancer stem cell pathway (CSCP) inhibitors; to methods of using such compounds to treat refractory, recurrent, or metastatic cancers; to methods of selective killing cancer cells by using such compounds with specific administration regimen; to methods of targeting cancer stem cells by inhibiting Stat3 pathway; to methods of using novel compounds in the treatment of conditions or disorders in a mammal related to aberrant Stat3 pathway activity; and to processes for preparing such compounds and intermediates thereof, and to the pharmaceutical compositions of relevant compounds, and to the specific methods of administration of these compounds.