Abstract: Catalytic conversion of ketoacids is disclosed, including methods for increasing the molecular weight of ketoacids. An exemlary method includes providing in a reactor a feedstock having at least one ketoacid. The feedstock is then subjected to one or more C—C-coupling reaction(s) in the presence of a catalyst system having a first metal oxide and a second metal oxide.

Abstract: A method has been disclosed of obtaining high purity, colourless monochloroacetic acid encompassing the chlorination of acetic acid with chlorine in the presence of a catalyst, followed by the recovery of the catalyst through vacuum distillation and purification of the obtained liquid raw product by its hydrodehalogenation by hydrogen in the presence of a palladium catalyst and then vacuum distillation.

Abstract: This disclosure relates to amphiphilic compounds containing a cyclobutene or cyclobutane moiety. In some embodiments, the compounds are useful for treating infection by Mycobacterium such as Mycobacterium tuberculosis. Cyclobutene containing compounds are also useful as monomers in the preparation of amphiphilic polymers.

Abstract: A process for carrying out a reaction in a reaction column, said process comprising: providing a first reactant to the reaction column in the liquid phase; contacting said first reactant with an excess of a second reactant such that reaction takes place within the reaction column to form a low boiling product and a high boiling product, at least a portion of said second reactant being provided to the reaction column in the vapour phase; recovering an overhead stream from at, or near, the top of the reaction column, said overhead stream comprising unreacted second reactant and the low boiling product; and recovering a bottoms stream from at, or near, the bottom of the reaction column comprising the high boiling product; wherein at least a portion of the heat required to vaporise the second reactant provided to the reaction column in the vapour phase is provided by heat exchange in a heat exchanger with a hot stream generated within the process other than a hot stream generated within the reaction column.

Abstract: Provided are a production method for compound (II) including reacting compound (I) with a halogenating agent in the presence of at least 0.5 equivalents, relative to compound (I), of a nitrogen atom-containing polar aprotic solvent; a composition containing compound (II), a halogenating agent or the like, and at least 0.5 equivalents, relative to compound (II), of a nitrogen atom-containing polar aprotic solvent; a stabilization method for compound (II); and compound (II).

Abstract: The present invention relates to a process for continuous hydrogenation of a nitro compound to the corresponding amine in a liquid reaction mixture comprising the nitro compound in the presence of a supported catalyst which comprises as the active component at least one element from groups 7 to 12 of the periodic table of the elements, wherein the hydrogenation is performed in the presence of at least one salt selected from the group consisting of the salts of the alkali metals, alkaline earth metals and of the rare earth metals and to a supported catalyst for continuous hydrogenation of a nitro compound to the corresponding amine in a liquid reaction mixture comprising the nitro compound which comprises as the active component at least one element from groups 7 to 12 of the periodic table of the elements and one salt of the alkali metals, alkaline earth metals or of the rare earth metals.

Abstract: Subject-matter of the invention is a process for the preparation of key intermediates in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.

Abstract: The invention relates to a production process for di- and polyamines of the diphenylmethane series by the rearrangement of a condensation product of aniline and a methylene group-supplying agent preferably selected from the group consisting of aqueous formaldehyde solution, gaseous formaldehyde, para-formaldehyde, trioxane and mixtures thereof, wherein said condensation product is reacted in the presence of at least one silica-alumina catalyst, said catalyst having a surface area as determined by the BET method carried out according to ASTM D3663-03 (2015) of from 200 m2/g to 520 m2/g, preferably of from 350 m2/g to 495 m2/g, particularly preferably of from 400 m2/g to 490 m2/g, a molar ratio of silica/alumina on the catalyst surface of A, an overall (bulk) molar ratio of silica/alumina of C, and a quotient B=A/C; said catalyst being characterised in that “low” A values (i.e. equal to or lower than 8.0) are combined with “high” B values (i.e. of from 1.50 to 3.00), and “high” A values (i.e. larger than 8.

Abstract: Provided is a method for purifying 1,5-pentanediamine comprising: providing 1,5-pentanediamine to be purified and treating the 1,5-pentanediamine to be purified by a reduction reaction to obtain purified 1,5-pentanediamine. Meanwhile, further provided is 1,5-pentanediamine prepared by the method. The purification method has a concise process and a simple operation, and is suitable for industrial production, and can significantly improve the quality of 1,5-pentanediamine.

Abstract: The present invention relates to cationic compounds of formula (I) for use as peripheral NMDA receptor antagonists.

Abstract: The present invention provides a method of producing an ethanolamine, with a low production ratio of a dialkanolamine (for example, less than 30% by weight). A process for producing an alkanolamine of the present invention includes reacting an alkylene oxide with ammonia to obtain a reaction product containing a monoalkanolamine, a dialkanolamine, and a trialkanolamine; separating the dialkanolamine from the reaction product; and recycling at least a portion of the dialkanolamine for the reaction of an alkylene oxide with ammonia, wherein in the recycling step, the dialkanolamine is supplied in a molar ratio of the alkylene oxide (moles) to a total amount (moles) of ammonia and the dialkanolamine of 0.08 or more and less than 0.26.

Abstract: A maleamic acid monomer, and a preparation method and a use of the maleamic acid monomer. The structural formula of the monomer is as follows: formula (1), wherein, R is selected from The maleamic acid monomer provided in the present invention may be used as a comonomer to prepare temperature-tolerant and calcium salt-tolerant polymers.

Abstract: The present disclosure relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a —(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the disclosure.

Abstract: The present invention relates to a hydroxamic acid-based contrast agent containing an isotope of fluorine, which comprises a compound having a structure of Formula (III): wherein R1 represents radioactive fluorine-18 (18F) or isotope fluorine-19 (19F), and R2 represents hydroxyamine —(NH)OH. The hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention has the capability of selectively inhibiting histone deacetylase (HDAC) subtypes 8/6/3, and specifically targets to the focus of spinocerebellar ataxia with over-activation of HDAC. By labeling with the radioisotope fluorine-18, a positron emission tomography (PET) image is obtained with the hydroxamic acid-based contrast agent containing radioisotope fluorine-18, whereby spinocerebellar ataxia is effectively detected.

Abstract: The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.

Abstract: The present invention discloses processes for producing methyl ethyl sulfide by contacting dimethyl sulfide and diethyl sulfide in the presence of a suitable catalyst. Methyl ethyl sulfide can be used as an odorant in natural gas. Integrated mercaptan and sulfide manufacturing systems and integrated methods for making mercaptans and sulfides also are disclosed.

Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, R3, m and n are defined herein, which have valuable pharmacological properties, including binding to the GPR40 receptor and modulating its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Abstract: 4,5-Substituted Picolinamide and picolinonitrile compounds of formula (I), where R4 is CONH2 or CN and R1 is an optionally substituted aryl or heteroaryl, are negative allosteric modulators of the metabotropic glutamate receptor 2 (mGlu2). The compounds and pharmaceutical compositions including the compounds may be useful for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject.

Abstract: An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): wherein each of R1, R2, R3, R4, R5, R6 and R7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2):

Abstract: The present invention relates to a process to produce highly purified crystalline 1-(4-chlorophenyl)pyrazol-3-ol (I).

Abstract: Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each selected from the group consisting of a C1-C20 alkyl group, C1-C20 partially fluorinated alkyl group, an aryl group, an aryl group with para CF3 functionality, an aryl group having C1-C20 partially fluorinated alkyl groups or partially fluorinated alkoxy groups, and a C1-C20 partially fluorinated aliphatic group, and a C1-C20 aryl group; and X is an anion. The method comprises cyclization of a halogenated acrylate with a formamidine with Hünig's base in a solvent.

Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.

Abstract: The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.

Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

Abstract: The present invention relates to novel compounds represented by the formula I having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. (I) The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase (HDAC) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases.

Abstract: An integrated process is described for producing 2,5-furandicarboxylic acid and/or a derivative thereof from a six carbon sugar-containing feed, comprising: a) dehydrating a feed comprising a six-carbon sugar unit, in the presence of a bromine source and of a solvent, to generate an oxidation feed comprised of at least one of 5-hydroxymethylfurfural and/or a derivative or derivatives of 5-hydroxymethylfurfural in the solvent, together with at least one bromine containing species; b) contacting the oxidation feed from step (a) with a metal catalyst and with an oxygen source under oxidation conditions to produce an oxidation product mixture comprising 2,5-furandicarboxylic acid (FDCA) and/or a derivative thereof, the solvent, and a residual catalyst; c) purifying and separating the mixture obtained in step (b) to obtain FDCA and/or a derivative thereof and the solvent; and d) recycling at least a portion of the solvent obtained in step (c) to step (a).

Abstract: Prodrugs of galiellactone, and derivatives thereof, are provided by reacting the parent compound, e.g. galiellactone, with a thiol. Such drugs may be administered orally to treat cancer and other proliferative diseases.

Abstract: The present invention provides PI3K protein kinase modulators of Formula (I) wherein R, R1,R2,L1, Cy1 and Cy2 are as disclosed herein, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

Abstract: A medicinal agent for the prevention and/or treatment of diseases caused by EP4 receptor activation. A compound having antagonistic activity against the EP4 receptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EP4 receptor for the prevention and/or treatment of diseases caused by EP4 receptor activation.

Abstract: To provide a method for producing 3-methyl-2-thiophenecarboxylic acid. A method for producing 3-methyl-2-thiophenecarboxylic acid, which comprises reacting 3-methylthiophene with chlorosulfonyl isocyanate, and hydrolyzing the obtained reaction product.

Abstract: Disclosed is a method of preparing an intermediate for an oxazolidinone derivative, which enables 5-bromo-2-(2-methyl-2H-tetrazol-5-yl)pyridine to be produced at high yield and high purity, thus exhibiting high preparation efficiency under optimal processing conditions and making it suitable for industrial mass production.

Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

Abstract: The present invention relates to a crystal form of a potassium-competitive acid blocker, that is, 1-[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrole-3-yl]-N-methyl methylamine fumaric acid salt (which is briefly referred to as a formula I) and a preparation method thereof. An X-ray powder diffraction characteristic peak thereof is shown in FIG. 1. The crystal form that is represented by formula I, provided in the present invention, is stable, reproducible, and is suitable for drug development.

Abstract: Provided is a purifying method for dabigatran etexilate free base, comprising subjecting a dabigatran etexilate free base crude product to water slurrying to obtain a crude product B; then conducting recrystallization on the crude product B with acetone and water to obtain a crude product C; and subsequently, purifying the crude product C with a mixed solvent of tetrahydrofuran and ethyl acetate, filtering and drying to obtain a dabigatran etexilate free base finished product. The purifying method of the present invention can effectively remove various impurities and is suitable for workshop production. Salts and water-soluble organic impurities are removed by purified water slurrying, impurities with a high polarity are removed by purifying with an acetone-water solution, and impurities with a low polarity are removed by purifying with a mixed solvent of tetrahydrofuran and ethyl acetate.

Abstract: Disclosed are amino triazole compounds substituted with a piperidinyl ring that is itself substituted with a heterocyclic ring. These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.

Abstract: Methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. A method described herein, in some embodiments, comprises providing a reaction mixture including a photoredox catalyst, a transition metal catalyst, a coupling partner and a substrate having a carboxyl group. The reaction mixture is irradiated with a radiation source resulting in cross-coupling of the substrate and coupling partner via a mechanism including decarboxylation, wherein the coupling partner is selected from the group consisting of a substituted aromatic compound and a substituted aliphatic compound.

Abstract: Disclosed are a compound for an organic optoelectronic device represented by Chemical Formula 1, a composition for an organic optoelectronic device, an organic optoelectronic device including the same, and a display device. Details of Chemical Formula 1 are the same as defined in the specification.

Abstract: Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: 2-Acylindazole compounds of formula I or formula II are disclosed: These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.

Abstract: The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.

Abstract: A compound has a first structure represented by a formula (1), a second structure represented by a formula (2), a third structure represented by a formula (3), and a fourth structure represented by a formula (4), the first structure, the second structure, the third structure and the fourth structure being mutually independently present in a molecule,

Abstract: This invention relates to HIV-inhibiting compounds consisting of other Formulae I, II or III isatin derivatives, as shown below (Formulae I, II and III), whereby in Formulae I, II and III, R1 is selected from H, CH3 or Cl; R2 is selected from one of the following radicals: zidovudine, amprenavir or an acyclic phosphonate chain, as shown below. This invention also relates to the use and treatment method using the Formulae I, II and III compounds. According to this invention, these compounds are also used for the treatment of infections caused by HBV or co-infection caused by HIV and HBV.

Abstract: An amyloid fibril formation inhibitor comprising a compound represented by the following general formulae (I) to (III): wherein Q is —C(?O)—; X is —C(?O)—, —NH—C(?O)—; Y is —(CH2)m—; Z is —(CH2)n—; R1, R2, and R3 are each independently a hydrogen atom, an alkyl group, a hydroxyalkyl group, an alkylaminoalkyl group; and R4 is an amino group, an alkylamino group or the like; or a pharmaceutically acceptable salt thereof or a solvate thereof.

Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: To an appropriate reactor equipped with mechanical stirrer was charged acetic acid (12 L), tert-butyl 4-(3-(6-(3,5-dimethoxyphenyl)-2-(methylthio)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl)propyl)piperazine-1-carboxylate (2000 g) and triethylamine (639 g, 2.3 eq.). Internal temperature was adjusted to approximately 20° C. and N-chlorosuccinimide (1651 g, 4.5 eq.) was added at 20-30° C. Reaction was stirred for 2 hours. Ethyl acetate (30 L) was added. 5% aqueous NaCl solution (20 L) was added. The organic layer was separated and the aqueous layer was extracted with EtOAc. The combined organic layers were washed with 30% aqueous potassium carbonate solution (14 L). The organic layer was concentrated to ˜12 L and used for next step directly.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: Benzamide and nicotinamide compounds and uses of the compounds. The compounds can be used to treat, for example, cancers such hematopoietic cancers (e.g., leukemia).

Abstract: The present invention provides a novel 2,4,6-substituted pyrimidine derivative, which is a compound represented by formula (I) (in the formula, ring A is a 6-membered heteroaryl group having at least one N atom optionally substituted with R1, R2, and R3; Z is an optionally substituted alkoxy group, an optionally substituted amino group, an optionally substituted heterocycloalkyl group, or an optionally substituted heteroaryl group; and R1, R2, and R3 are each independently selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted alkoxy group, an optionally substituted cycloalkyloxy group, an optionally substituted heterocycloalkyloxy group, an optionally substituted phenoxy group, an optionally substituted amino group, a nitro group, and a hydroxy group) or a pharmaceutically acceptable salt thereof.

Abstract: The disclosure provides brassinosteroid mimetics and method of using such mimetics.