Abstract: Disclosed herein are methods for recovering phosphorus-containing ligand from mixtures comprising organic mononitriles and organic dinitriles, using liquid-liquid extraction. Also disclosed are treatments to enhance extractability of the phosphorus-containing ligand.

Abstract: Substituted vinyl- and alkynylcyanocycloalkanols and vinyl- and alkynylcyanoheterocyclylalkanols of the general formula (I) or salts thereof where [X—Y], Q, R1, R2, A1, A2, V, W, m and n are each as defined in the description, processes for preparation thereof and the use thereof for enhancing stress tolerance in plants with respect to abiotic stress, and/or for increasing plant yield.

Abstract: The present invention relates to novel ortho alkynyl anilines of formula (I) which are useful in synthesis of drug intermediates and natural products and process for preparation of these ortho alkynyl anilines of formula (I) via copper catalyzed Multi Component Reactions (MCR).

Abstract: The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

Abstract: A method for preparing a cationic sulfoxide intermediate having the following formula wherein Ar1 and Ar2 are substituted or unsubstituted aryl groups that are the same or different, includes reacting hydrogen peroxide with (i) a compound having the following formula (2) or sulfonic acid R?SO3H, wherein R? is CH3, CF3, phenyl, toluene, or OH, and (ii) a cationic thioether intermediate having the following formula (4) to obtain the cationic sulfoxide intermediate: wherein R is a substituted or unsubstituted C1-C6 alkyl group; and wherein Ar1 and Ar2 are as defined above and Y is an anion.

Abstract: A method for preparing an aromatic sulfide or a salt thereof is provided. The method for preparing an aromatic sulfide or a salt thereof includes reacting a compound having a structure represented by Formula (I) to a compound having a structure represented by Formula (III) in the presence of a compound having a structure represented by Formula (II) to obtain a compound having a structure represented by Formula (IV) wherein R1 and R2 are independently C1-6 alkyl group, or C5-7 cycloalkyl group; R3 is independently C1-6 alkyl group, C5-7 cycloalkyl group, C1-6 haloalkyl group, or aryl group; R4 is independently H, or C1-6 alkyl group; Y is H, aryl group, or —X—R5; X is —O—, —NH—, —PH—, or —S—, or Y and an adjacent R4 are optionally combined with the carbon atoms to which they are attached, to form an aryl group; and R5 is H, C1-6 alkyl group, C5-7 cycloalkyl group, or aryl group; and Z? is R3SO3?.

Abstract: Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: Provided herein are functionalized pegylated cyanine compounds containing a reactive group suitable for labeling a biomolecule or pharmaceutical compositions and methods of use thereof. In one embodiment, the compounds are based on formula I shown below. In other embodiments, the compounds can be pegylated at one or more of the following locations R1, R4, R6, R9, or L.

Abstract: Provided is a salt including a compound represented by a formula (4) and a compound represented by a formula (5). A method for producing the salt includes reacting a compound represented by a formula (2) with a compound represented by a formula (3) in the presence of a quaternary onium salt and a base to form the compound represented by the formula (4); and mixing the compound represented by the formula (4) with the compound represented by the formula (5). A method for producing a compound represented by a formula (6) includes removing, from the salt including the compounds of formulae (4) and (5), a protecting group P1. In the following formulae, P1 and P2 are both protecting groups.

Abstract: The present invention relates to novel heterocyclic derivatives which are allosteric modulators of cannabinoid receptor 1 (CB1) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with endocannabinoid dysfunction and diseases in which the CB1 subtype of cannabinoid receptor is involved; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.

Abstract: The invention relates to 3-(carboxyethyl)-8-amino-2-oxo-1,3-diazaspiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

Abstract: Problem to be Solved It is intended to provide an industrially preferable fluoroalkylating agent and use thereof. Solution The present invention provides a fluoroalkylating agent represented by the general formula (1) wherein R1 is a C1 to C8 fluoroalkyl group; R2 and R3 are each independently a C1 to C12 alkyl group or the like; Y1 to Y4 are each independently a hydrogen atom, a halogen atom, or the like; and X? is a monovalent anion. A compound of the general formula (3): R4—S—R1 having an introduced C1 to C8 fluoroalkyl group is easily obtained by reacting a compound of the general formula (2): R4—S—Z wherein R4 is a hydrocarbon group or the like; and Z is a leaving group, with the compound of the general formula (1).

Abstract: The present invention relates to benzimidazol-2-amines of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.

Abstract: The present invention relates to benzimidazol-2-amines of general formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.

Abstract: Bifunctional compounds that increase uric acid excretion and reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders or uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are provided. Pharmaceutical compositions comprising the bifunctional compounds are also provided.

Abstract: The present application relates to 1,4-disubstituted 1,2,3-Triazole antifungal agents of the formula (I) wherein, R1 is halogens such as fluorine, chlorine or bromine, CF3, alkyl; R2 is alkyl or hydrogen; R3 is halogen selected from fluorine, chlorine or bromine; and n is 0 or 1. The application further relates to the synthesis of said compounds, to fungicidal compositions containing said compounds and to their use in a method for treating fungal infections.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.

Abstract: The invention relates to benzoic acid amides of general formula (I) as herbicides. In formula (I) X, Z and R represent radicals such as alkyl and cycloalkyl. Q represents a 5-membered heterocycle.

Abstract: The present disclosure provides a deuterium substituted 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine compound with a structure represented by formula (I) or a derivative thereof, a pharmaceutical composition containing the compound or the derivative thereof, and an application of the compound or the derivative thereof in preparing drugs. The compound can reduce oxidative metabolism thereof, increase the drug concentration in blood and the effective bioavailability, so as to lower the dosage and reduce the toxicity and other side effects. The deuterium 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine compound and its derivative thereof provided by the present disclosure can be used to treat related diseases such as affective disorders, depression and anxiety.

Abstract: An aryl compound terminated with at least three glycidyl groups and at least three (meth)allyl groups, having formula (1) wherein R1 is a C3-C20 hydrocarbon, R2 is hydrogen or methyl, and n is 3 or 4 is novel. It is prepared by reacting an aryl compound having at least three (meth)allyl-containing phenol groups with a 2-halomethyloxirane.

Abstract: A catalyst, method of using, and use of a hydrogenation catalyst, preferably palladium on a support, preferably alumina or activated charcoal support. This in the presence of lithium salts, with salts such as the borates being preferred. This provides hydrogenation of precursors to give rise to a stereoselective, such as diastereoselective bias in the product of alkene hydrogenation using the catalyst.

Abstract: The present disclosure provides processes for the production of 2-5-furandicarboxylic acid (FDCA) and intermediates thereof by the chemocatalytic conversion of a furanic oxidation substrate. The present disclosure further provides processes for preparing derivatives of FDCA and FDCA-based polymers. In addition, the present disclosure provides crystalline preparations of FDCA, as well as processes for making the same.

Abstract: Disclosed herein are an apparatus and method for continuously producing a cyclic carbonate. The apparatus includes an adiabatic reactor to be filled with a heterogeneous catalyst for reacting an epoxide with carbon dioxide, a circulation path for returning at least a portion of a fluid mixture in a liquid form flowed out through a reactor outlet into the reactor, a carbon dioxide supply means for continuously supplying carbon dioxide in a liquid form or a supercritical state into the circulation path, and an epoxide supply means for continuously supplying an epoxide in a liquid or solution form into the circulation path.

Abstract: The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrant Stat3 pathway activity; to pharmaceutical compositions containing such compounds.

Abstract: Compounds of formula A-I and B-I, compositions comprising the compounds, methods of making the compounds and methods of their uses are disclosed.

Abstract: Solid forms comprising 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.

Abstract: The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections.

Abstract: Our invention relates to novel enantiomer derivatives of 8-hydroxyquinoline derivatives with general formula (I) and (II) and the synthesis thereof and pharmaceutically acceptable salts and metal complexes thereof, and the medicinal and/or pharmaceutical compositions comprising these compounds. The essence of the subject matter of the invention relates to the fact that prior art discloses the biological effect and characteristics only of the racemic products, the novel enantiomer derivatives according to the invention appear in our application for the first. The subject matter of the invention furthermore relates to a novel, stereoselective synthesis for the preparation of the novel enantiomer derivatives according to the invention. The novel medicinal and/or pharmaceutical compositions comprising these enantiomers are suitable for the treatment of the named diseases, and the enanatiomers are used for manufacture of these compositions.

Abstract: A novel crystalline form is defined by using diffraction angle 2?° of X-ray powder diffraction pattern and characteristic peaks of differential scanning calorimetry (DSC). Pantoprazole Sodium solid is added to an alcohol solvent to form a suspension with a concentration of 0.05˜0.2 g/mL, and then an antioxidant is added to the suspension, completely dissolving the solid at a temperature of 15˜35° C., and a solventing-out agent is dropwise added to the solution under the application of ultrasonic wave, wherein the amount of the solventing-out agent is 3˜10 times (in volume) of the alcohol solvent; followed by cooling the solution down to 0˜5° C., continuing to stir for 1˜3 h, and suction filtrating obtained solid-liquid suspension to provide a novel crystalline form of Pantoprazole Sodium crystal after drying the product to constant weight.

Abstract: The present invention relates to a compound of formula (1) in the form of a base or addition salt with an acid, particularly a pharmaceutically acceptable acid. It further relates to a pharmaceutical composition including the compound and at least one pharmaceutically acceptable excipient, to a process for preparing said compound and to a corresponding intermediate compound.

Abstract: The present invention relates to compounds of Formula I and their prodrugs and pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as TrkA antagonists.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present disclosure generally relates to methods for separating ondansetron and related impurities using CO2-based chromatography.

Abstract: The present invention relates to a Sonogashira-Carbonylation reaction using two types of gas, as well as novel crystals which can control a heat of the said reaction and the process of producing the same. In addition, the present invention relates to a ligand (additive) to prevent the deactivation of a palladium catalyst.

Abstract: An improved process is provided for the preparation of Ledipasvir and its pharmaceutically acceptable salts or solvates thereof, which is useful as an antiviral agent. This disclosure also provides a process for the preparation of key intermediates of Ledipasvir.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, G1, G2, L1, L2, m1, m2, n, X and E are as defined herein and, wherein at least one of R3a, R3b, R4a or R4b is not H. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: The present invention relates to kojic acid-derived mannich base compounds with biological effect, and hydrates, solvates, pharmacologically acceptable salts or geometric isomers thereof. Said compounds have antidermatophytic, antimycobacterial, antityrosinase, anti-aging and antioxidant effect.

Abstract: The invention relates to 3-((hetero-)aryl)-alkyl-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

Abstract: Method for producing carboxylic anhydride, the method includes heating raw material compound represented by the following general formula (1): [in the formula (1), R1 is tetravalent organic group having at least two carbon atoms adjacent to each other, and groups represented by the formulae: —COOR2 and —COOR3 are bonded to one and the other of the two adjacent carbon atoms, respectively, R2 and R3 each represent hydrogen atom or the like, X represents hydrogen atom or the like, and Y represents hydrogen atom or the like] in carboxylic acid having 1 to 5 carbon atoms with catalyst being used, to thereby obtain the carboxylic anhydride, wherein the catalyst is homogeneous acid catalyst having acid dissociation constant (pKa) of ?6.5 or lower and boiling point of 100° C. or higher, the acid dissociation constant (pKa) being determined by quantum chemistry calculation based on density functional method.

Abstract: The invention relates to 8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention relates to a process for the preparation of Azilsartan Medoxomil Potassium. The invention further relates to novel highly crystalline polymorph of Azilsartan Medoxomil Potassium and composition comprising it. The invention provides thermostable highly crystalline polymorph of Azilsartan Medoxomil Potassium and process to produce a composition comprising the novel highly crystalline polymorph of Azilsartan Medoxomil Potassium.

Abstract: The invention relates to a compound comprising the following general formula (1) and said compound for use as a medicament, in particular for use in the treatment psychiatric or neurological disorders and inflammation, in particular neuroinflammation: (formula 1) wherein each of R1, R2 and R3 are selected independently from each other from alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, or heteroaryl.

Abstract: The present invention provides a compound of Formula I (The chemical formula should be inserted here.) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Abstract: The specification relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where Q, R, R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent GLS1 mediated disease, including cancer. The specification further relates to crystalline forms of compounds of Formula (I) and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating GLS1 kinase mediated disease, including cancer, using such compounds and salts.

Abstract: [Problem] To provide a compound which is useful as an active ingredient for a pharmaceutical composition for preventing or treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. [Means for Solution] The present inventors have found that a thiazole derivative substituted with pyrazinylcarbonylamino at the 2-position is an excellent muscarinic M3 receptor-positive allosteric modulator and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, thereby completing the present invention. 2-Acylaminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, for example voiding dysfunction such as underactive bladder.

Abstract: It is intended to provide: a compound useful as an amyloid oxidation catalyst which is applicable in vivo and is applicable not only to A? peptides but to other amyloids; and a prophylactic or therapeutic drug for an amyloid-related disease, comprising the same. The present invention provides a benzothiazole compound represented by the following formula (1) wherein X represents a halogen atom; R1 represents an optionally substituted hydrocarbon group; R2 represents a hydrogen atom or an optionally substituted hydrocarbon group; R3 and R4 are the same or different and each represent a hydrogen atom, an optionally substituted hydrocarbon group, an alkoxy group, a halogen atom, an amino group, a nitro group, or a cyano group; R2 and R4 optionally together form an alkylene group; and R5 represents an anion.

Abstract: The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

Abstract: Provided herein are small molecule agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions. The present invention is based on the seminal discovery of a series of potent small molecule agonists of the apelin receptor, which are useful for the treatment of diseases including heart failure, chronic kidney disease, hypertension, and metabolic disorders such as insulin resistance/diabetes and obesity. The compounds disclosed herein are highly specific for the apelin receptor versus the angiotensin II receptor (ATI).