Abstract: Halogenated S-(perfluoroalkyl)dibenzothiophenium salt represented by the following general formula (I): This compound is a new, reactive, and industrially useful reagent for perfluoroalkylating organic compounds. The reagent can be prepared by a one-pot process or a two-step reaction process from a halogenated biphenyl and easily isolated by a filtration method. In addition, the halogenated biphenyl can be recovered by desulfurization from a halogenated dibenzothiophene obtained as a side-product by the usage of the reagent.

Abstract: Disclosed is a 2-morpholin-4,6-disubstituted pyrimidine derivative as shown in formula (1) below, and a pharmaceutically acceptable salt, solvate, stereoisomer or prodrug thereof, and a pharmaceutical composition thereof and a use thereof, wherein the definition of each group is as shown in the description. The compound has a PI3K kinase inhibition activity, and has a relatively high inhibitive ability and a low cytotoxicity against PIK3CA mutant breast cancer cell strains T47D and MCF-7.

Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.

Abstract: The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.

Abstract: Disclosed herein are positive allosteric modulators of melanocortin receptor and methods of using such modulators.

Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.

Abstract: The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.

Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Abstract: Novel chemokine CXCR1 and CXCR2 receptor antagonist compounds of general formula (I) are described. Also described, are pharmaceutical compositions including the compounds, and use of the compounds and the compositions for the treatment of chemokine-mediated pathologies, more specifically in the field of dermatology.

Abstract: The invention discloses compounds of Formula I, wherein X1, X2, R1, and R2 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

Abstract: Compound of formula (I) wherein: R1 is heteroaryl either unsubstituted or substituted by methyl, ethyl, halo or ?O; and R2 is H, methyl or ethyl; and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: The present invention provides novel compounds of formula (I) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, fibrotic diseases, or cholestatic diseases.

Abstract: A compound represented by general formula (I) and having a quinoline skeleton has a strong Axl inhibitory activity, and therefore the compound can be an agent for treating Axl-related diseases, for example, cancer such as acute myeloid leukemia, chronic myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.

Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.

Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: Compounds having a structure of formula (I), including stereoisomers and pharmaceutically acceptable salts and solvates thereof: wherein R1 is as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (VMAT2) and have utility for treating, for example, hyperkinetic disorders. Also disclosed are compositions containing these compounds in combination with a pharmaceutically acceptable carrier or diluent, as well as methods relating to the use in a subject in need thereof.

Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.

Abstract: The present invention relates to novel antiproliferative 1H-1, 8-naphthyridin-2-ones of the general formula (I) or pharmaceutically acceptable salts thereof: In which the variable groups are as defined herein, and their preparation and use in therapeutic treatment of disorders related to inhibition of tyrosine kinases in warm blooded animals. The compounds can overcome imatinib induced drug resistance.

Abstract: The invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by SUV420H1. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract: The present invention provides novel derivative of ?-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).

Abstract: The invention concerns novel substituted bicyclic pyrazolo pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.

Abstract: The present application discloses an A-type polymorphic substance of yonkenafil hydrochloride and a preparation method, a composition and use thereof. The powder diffraction pattern of the A-type polymorphic substance of yonkenafil hydrochloride comprises diffraction peaks at three or more 2? values selected from: 8.4±0.2°, 11.3±0.2°, 13.9±0.2°, 14.2±0.2°, 14.7±0.2°, 16.8±0.2°, 17.1±0.2°, 19.7±0.2°, 21.0±0.2°, 21.7±0.2°, 22.4±0.2°, 23.3±0.2°, 23.8±0.2°, 26.8±0.2°, 27.5±0.2°, 28.0±0.2°.

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.

Abstract: The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.

Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I-1 or I-A: wherein the variables are as defined herein.

Abstract: The present disclosure provides a compound of Chemical Formula (1) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same: wherein X, Z, R1 and R2 are as defined in the specification. The compound of Chemical Formula (1) or pharmaceutically acceptable salt thereof acts as a positive allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5), thereby being useful in the prevention or treatment of disorder mediated by glutamate dysfunction and mGluR5.

Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidinyl carboxamide compounds described herein include 2-heterocyclyl-4-alkyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof.

Abstract: The invention provides substituted imidazo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,5-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-imidazo[1,5-a]pyrimidine-8-carboxamide compounds and variants thereof.

Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

Abstract: The present invention provides an improved process for preparation of the substantially pure (3aR,7aR)-4?-(benzo[d]isothiazol-3-yl)octahydrospiro[isoindole-2,1?-piperazin]-1?-ium methanesulfonate (referred to as compound-II), which is useful as a key intermediate for the synthesis of lurasidone ((3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione). The process comprises reaction of the compound-III (as described herein) with the compound-IV (as described herein) in the presence of a solvent mixture selected from an alcohol and water; and a base The improved process for the preparation of compound II provides the product with total amount of unreacted compound-IV as impurity in less than 0.06% and the product with HPLC purity as ?99.8%. The process further refers purification of Lurasidone hydrochloride, wherein the product contains the residual acetone <5000 ppm.

Abstract: The invention concerns novel substituted tricyclic pyrazolo pyrimidine compounds of formula (I-a) or (I-b) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use Sin the treatment of respiratory syncytial virus infection.

Abstract: The present invention relates to a method of producing and purifying a high-purity anhydrosugar alcohol in high yield by a simple process and apparatus, the method includes the steps of: allowing a sugar alcohol to react in the presence of an acid catalyst in a reactor, and, at the same time, evaporating a product of the reaction; cooling the evaporated product to remove water and obtain a crude anhydrosugar alcohol; and introducing the crude anhydrosugar alcohol into a melt crystallization process to obtain a high-purity anhydrosugar alcohol.

Abstract: The present invention provides a substituted pyridine compound of the formula I or an agriculturally suitable salt or N-oxide thereof, wherein the variables in the formula I are defined as in the description. Substituted pyridine compounds of formula I are useful as herbicides.

Abstract: The present invention relates to a condensed heterocyclic compound that has an enteropeptidase inhibitory effect and is useful in the treatment or prevention of obesity, diabetes mellitus, or the like, and a medicament containing the same. Specifically, the present invention relates to a compound represented by the following formula (I) or a salt thereof, and a medicament containing the same [in the formula, each symbol is as defined in the specification].

Abstract: The present disclosure relates generally to systems, methods, and compounds for therapeutic use against parasitic infections. More particularly, the disclosure relates to anti-parasitic compounds, and methods for making and for using the anti-parasitic compounds, where the anti-parasitic compounds have the general formula: where X, R1, R2, R3, R4, R5, and R6 are defined more fully below.

Abstract: Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: A novel crystalline form of rifaximin and process for its preparation are described. A pharmaceutical composition comprising crystalline rifaximin is also described.

Abstract: A novel crystalline form is defined by diffraction angle 2?° of X-ray powder diffraction pattern and characteristic peak of differential scanning calorimetry (DSC). The novel crystalline form of Cefamandole Nafate is prepared as follows: adding Cefamandole Nafate in solid state to an organic solvent to form a suspension with a concentration of 0.04˜0.3 g/ml, stirring the suspension at 40˜50° C. for a period of time, and then cooling to 5˜15° C. at certain cooling rate, continuing to stir for a period of time, then suction filtrating the obtained suspension, the resulting filer cake is Cefamandole Nafate as wet product, which is dried to constant weight to provide the novel crystalline form of Cefamandole Nafate as final product.

Abstract: The invention relates to a process for the cost-effective and environmentally responsible preparation of alkyl indium sesquichloride in high yield and with high selectivity and purity. The alkyl indium sesquichloride prepared in accordance with the invention is particularly suitable, also as a result of its high purity and yield, for preparation of indium-containing precursors in accordance with demand, in high yield and with high selectivity and purity. As a result of the high purity, the indium-containing precursors that are preparable are particularly suitable for metal-organic chemical vapor deposition (MOCVD) or metal-organic vapor phase epitaxy (MOVPE). The novel process according to the invention is characterized by the improved execution of the process, in particular by rapid process control. Owing to targeted and extensive use of raw materials that are inexpensive and have a low level of environmental pollution, the process is also suitable for use on an industrial scale.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: Modified silica particles are provided. Aspects of the particles include an outer layer that is composed of organically-modified silica comprising a siloxane-linked hydrophilic group, such as a charged functional group or a polar neutral functional group. The modified silica particles can form the basis of a variety of chromatography support materials. Also provided are methods of preparing the subject particles. Aspects of the methods include contacting silica particles with water, an ionic fluoride and an organosilane reagent comprising a hydrophilic moiety to produce modified silica particles wherein the hydrophilic moiety of the organosilane reagent is incorporated into an outer layer of the silica particles. Chromatography supports and kits including the subject particles and methods of using the same are also provided.

Abstract: The present invention concerns a method for depolymerizing oxygenated polymer materials and the use of said method in the recycling of plastic materials and the preparation of aromatic compounds that can be used as fuel, synthesis intermediates and raw materials in the construction sectors and in the petrochemical, electrical, electronic, textile, aeronautical, pharmaceutical, cosmetics and agrochemical industries. The present invention also concerns the use of aromatic compounds obtained by the method for depolymerizing oxygenated polymer materials according to the invention, in the production of fuels, electronic components, plastic polymers, rubber, drugs, vitamins, cosmetic products, perfumes, food products, synthetic threads and fibres, synthetic leathers, glues, pesticides and fertilizers.

Abstract: The purpose of the present invention is to obtain an organosilicon compound containing an isocyanate group by thiol-ene addition reaction from a corresponding organosilicon compound having a mercapto group and an isocyanate compound having a polymerizable group. Provided is a silane coupling agent which includes a specific linking structure in which a sulfur atom is indispensably contained in a linking chain which connects an isocyanate group to a hydrolyzable silyl group. Compared to silane coupling agents for use in existing technologies, this silane coupling agent has enhanced hydrophobicity and an increased organic-moiety proportion due to the sulfur-containing linking structure.

Abstract: The present disclosure relates to novel platinum compositions having a heterocycle ligand and nanoparticles and methods using such compositions, e.g. for treating cancer.

Abstract: The present invention provides novel metal complexes, methods of making, and methods of using the same.