Abstract: Crystals of [8-chloro-3-(4-chlorobenzyl)-4-difluoromethoxy-2-ethylquinolin-5-yloxy]acetic acid L-lysine salt, i.e., a crystal A which has peaks at diffraction angles 2?=6.0°, 10.0°, 10.7°, 12.1°, 18.4°, 19.2° and 20.1° in powder X-ray diffraction spectra and a crystal B which has peaks at diffraction angles 2?=6.0°, 11.7°, 12.4°, 15.2°, 16.4°, 20.3° and 22.6° in powder X-ray diffraction spectra. These crystals are chemically stable and have excellent thermal stability and physical properties, and are therefore suitable as medicinal substances.

Abstract: The present invention relates to methods and compounds for regulating or enhancing ethropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.

Abstract: The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.

Abstract: Crystalline polymorph forms of 3-[2-butyl-1-(2-diethylamino-ethyl)-1H-benzoimidazol-5-yl]-N-hydroxy-acrylamide are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of diseases and conditions are also presented.

Abstract: The present invention relates to new polymorphic forms of Crystalline Rosuvastatin calcium along with novel processes for crystalline as well as amorphous Rosuvastatin calcium.

Abstract: Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).

Abstract: This invention relates to a cyanotriazole compound represented by the formula (1): wherein each symbols are defined in the specification, or a salt thereof. The compound or a salt thereof stimulates the citric acid cycle activity and/or improves hyperglycemia with less side effects, and excellent safety, and therefore, it is useful for treating and/or preventing diseases or disorders on which citric acid cycle activation and/or improvement of hyperglycemia has a prophylactic and/or therapeutic effect, for example, diabetes, impaired glucose tolerance, insulin resistance, diabetic complications, obesity, dyslipidemia, hepatic steatosis, atherosclerosis and/or cardiovascular disease, as well as diseases or disorders that would benefit from stimulating energy expenditure.

Abstract: The present invention relates to a novel azole derivative as an apelin receptor agonist and a method for treating cardiovascular disease, diabetic disease, renal disease, hypertension, and arteriosclerosis, etc., using the same. The present invention provides a compound represented by formula (I) or a pharmacologically acceptable salt thereof wherein X1 represents —NH? or —CH?, X2 represents —CH? or —N?, R1 and R2 each represent a C1 to C6 alkoxy group or the like, R3 represents a heteroaryl group (the heteroaryl group is optionally substituted by a methyl group or the like) or the like, and R4 represents a C1 to C6 alkylthio group or a C2 to C6 alkenyl group (the C1 to C6 alkylthio group and the C2 to C6 alkenyl group are each optionally substituted by one carboxy group or the like) or the like.

Abstract: The present invention relates to an improved process for making hydroxyethyl piperazine compounds especially mono-hydroxyethyl piperazine. The improvement comprises reacting piperazine and an alkylene oxide, preferably ethylene oxide in a reactive distillation column.

Abstract: Copoly(imide oxetane) materials are disclosed that can exhibit a low surface energy while possessing the mechanical, thermal, chemical and optical properties associated with polyimides. The copoly(imide oxetane)s are prepared using a minor amount of fluorinated oxetane-derived oligomer with sufficient fluorine-containing segments of the copoly(imide oxetane)s migrate to the exterior surface of the polymeric material to yield low surface energies. Thus the coatings and articles of manufacture made with the copoly(imide oxetane)s of this invention are characterized as having an anisotropic fluorine composition. The low surface energies can be achieved with very low content of fluorinated oxetane-derived oligomer. The copolymers of this invention can enhance the viability of polyimides for many applications and may be acceptable where homopolyimide materials have been unacceptable.

Abstract: The present disclosure provides processes for preparing (+)-pleuromutilin and synthetic (+)-pleuromutilin produced therefrom. Also provided are intermediates prepared thereby and processes for preparing these intermediates.

Abstract: The present invention provides a compound having the structure: wherein R1 is halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-5 alkyl-aryl, or C1-5 alkyl-NH-aryl; Ar1 is phenyl or thiophene; wherein when Ar1 is phenyl, then R1 is other than —C(?O)—NR5R6, where one of R5 or R6 is phenyl or quinoline and the other of R5 or R6 is hydroxyalkyl, or where one of R5 or R6 is quinoline and the other of R5 or R6 is H; and wherein when Ar1 is phenyl, then R1 is other than —NR5—C(?O)—R6, where one of R5 is H and R6 is quinoline, or a pharmaceutically acceptable salt thereof.

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: Disclosed is a process for the synthesis of efinaconazole (I), starting from 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole and 4-methylenepiperidine, as free base or hydrochloride, in an organic solvent, under anhydrous conditions and in the presence of neutralising agents and reaction-promoting metal species. (1) The process is particularly advantageous because it gives rise to efinaconazole in high yields and purity, and uses little more than the stoichiometric amount of 4-methylenepiperidine, a rather expensive commercially available reagent.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. 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 generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. 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: Described are deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds of structural Formula (I), which are agonists of 5-hydroxytryptamine receptors. Also described are pharmaceutical compositions comprising the deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds, and methods of use thereof.

Abstract: The invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.

Abstract: A crystal form and a salt type of a substituted 2-hydro-pyrazole derivative, preparation method therefor, and use of the crystal form and the salt type in preparation of a medicament for treating cancers such as breast cancer, lung cancer and the like.

Abstract: The current invention relates to a compound of formula (I) which can be used for the treatment of, or against viral influenza infections.

Abstract: The present invention relates to fungicidal N-hetarylcarbonyl-2-(benzocycloalken-1-yl)piperidines or pyrrolidines of formula (I), and their thiocarbonyl derivatives, wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl group that can be substituted by up to four groups R that can be the same or different; T represents 0 or S; n represents 1 or 2; m represents 1, 2 or 3; p represents 1, 2, 3 or 4, L1 and L2 independently represent CZ4Z5, NZ6, 0, S, S(O) or S(0)2; and R and Z1-Z6 are as defined in the claims; their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract: The present disclosure provides a crystalline form F of Pazopanib HCl, which is characterized by an X-ray diffraction (XRD) pattern having peaks at about 11.3, 14.6, 16.9, 19.5, 19.7, 23.5 and 25.9°±0.2° 2?. The present disclosure also provides a preparation process of a crystalline form F of Pazopanib HCl.

Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.

Abstract: The invention provides for novel benzonaphthyridine derivatives and compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the compounds are phosphodiesterase inhibitors. The invention further provides for methods for inhibition of phosphodiesterase comprising contacting phosphodiesterase with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. The invention further provides for methods for treatment of neurodegenerative diseases, increasing memory or long term potentiation with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the phosphodiesterase is PDE5.

Abstract: The present application relates to crystalline solid forms of an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of diseases such as cancer.

Abstract: The present invention concerns novel fused pyrimidinone and triazinone derivatives containing bridged nitrogen, their process of preparation and their use as antifungal or antiparasitic agents.

Abstract: The present invention relates to a crystalline form of a BTK kinase inhibitor and the preparation method thereof. In particular, the present invention relates to a crystal form I of (R)-4-amino-1-(1-(but-2-ynoyl)pyrrolidin-3-yl)-3-(4-(2,6 -difluorophenoxy)phenyl)-1 H-pyrrolo[2,3-d]pyridazin-7(6H)-one (the compound of formula (I)) and the preparation method thereof. The crystal form I of the compound of formula (I) obtained by the present invention has a good crystalline stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, thus making it more suitable for use in clinical treatment.

Abstract: The present invention relates to an improved process for the preparation of Ibrutinib with high purity and high yields. The present process is cost effective and feasible in large scale production also. The present process avoids the mitsunobu reagent conditions also. The present Invention also relates to a process for the preparation of Crystalline form A and Crystalline form C of Ibrutinib.

Abstract: The present application relates to the field of pharmaceutical chemistry. The application specifically relates to a crystal form A and crystal form B of a pyrrolopyrimidine (formula I) for preparing a JAK inhibitor. The application further relates to a method for preparing the crystal form A and crystal form B, a crystalline composition comprising the crystal form A or crystal form B, a pharmaceutical composition comprising the crystal form A, crystal form B, or crystalline composition, and a pharmaceutical application of the pharmaceutical composition, the crystal form A, and the crystal form B. The crystal form A and crystal form B of the application has the advantages of high purity, high crystallinity, and good stability.

Abstract: This invention relates to a process of manufacturing cucurbituril and/or one or more derivatives thereof with low formaldehyde content and to the use of said cucurbituril and/or one or more derivatives thereof, in particular in consumer and industrial products, and in industrial processes.

Abstract: The present disclosure relates to N-demethylation of a compound containing a tertiary N-methylamine, including for example a morphinan alkaloid, in a continuous flow system. In particular, the present disclosure relates to N-demethylation of oxymorphone-3,14-diacetate or 14-hydroxymorphinone-3,14-diacetate using highly active catalytic palladium (0) in a continuous flow system under elevated temperature and pressure condition. The methodology can be utilized towards the synthesis of noroxymorphone via aerobic palladium-catalyzed continuous flow N-demethylation.

Abstract: Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

Abstract: Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated modulate the NMDA receptor.

Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.

Abstract: The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

Abstract: There are provided 5,6-dihydro-4H-dithieno[3,2-b:2?,3?-d]azepine derivatives(as defined in the disclosure) which are useful in the treatment of RSV infection and for the prevention of disease associated with RSV infection.

Abstract: Thallium salens can be synthesized by reacting thallium alkoxide with a salen ligand. As examples of the invention, the dinuclear complexes Tl2-(salo-But) and Tl2-(saloPh-But) were synthesized by the reaction of thallium ethoxide with (H2-salo-But) or (H2-saloPh-But). These thallium salens may have applications as fluorescent tracers (or taggants) for subterranean fluid flows.

Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.

Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.

Abstract: A process can prepare a colourless, methanolic solution of 3-(N-benzyl-2-aminoethyl)aminopropyltrimethoxysilane hydrochloride. The process includes, in step 1 fractionally distilling the vinylbenzyl chloride reactant component with addition of at least one stabilizer, and in step 2, metering and mixing the distillate (vinylbenzyl chloride) from step 1 into an initial charge of N-(2-aminoethyl)-3-aminopropyltrimethoxysilane and methanol in a molar ratio of the N-(2-aminoethyl)-3-aminopropyltrimethoxysilane to vinylbenzyl chloride of 1.0:0.80 to 1.0:1.15 and at a temperature in the range from 40 to 60° C. and leaving them to react further. The colourless, methanolic solution has an APHA colour number of <200 mg Pt—Co/l.

Abstract: The invention relates to a process for preparing isocyanate containing alkoxysilane groups, in which, in the sequence of steps A) to D), A) alkoxysilano(cyclo)alkylamine is reacted with dialkyl carbonate in the presence of a basic catalyst to give alkoxysilano(cyclo)alkylurethane, B) simultaneously or successively, the catalyst is removed and/or deactivated, and low boilers, solids, salt burdens and/or high boilers are removed, C) alkoxysilano(cyclo)alkylurethane obtained after B) is thermally cleaved to release isocyanate containing alkoxysilane groups and by-product, leaving bottoms material, and D) isocyanate containing alkoxysilane groups and by-product are separated from one another and from bottoms material and collected, wherein the basic catalyst is a guanidine base.

Abstract: The present invention provides: a novel organic titanium compound having an effect as an adhesion promoter by itself; a production method of such organic titanium compound; and a room temperature-curable resin composition containing such organic titanium compound both as a curing catalyst and as an adhesion promoter. Provided are an organic titanium compound represented by an average composition formula (I): Ti(OR1)4-a(Y3Si-A-O—CO—CH?C(O)R)a (wherein R1 represents a substituted or unsubstituted monovalent hydrocarbon group having 1 to 12 carbon atoms, R represents a substituted or unsubstituted monovalent hydrocarbon group having 1 to 12 carbon atoms, A represents a divalent hydrocarbon group having 3 to 6 carbon atoms, Y represents a hydrolyzable group, and a represents a number satisfying 0<a<4); a production method of such organic titanium compound; and a room temperature-curable resin composition that contains a room temperature-curable resin.

Abstract: To provide an electrochromic compound, represented by the following general formula where X1, X2, X3, X4, X5, X6, X7 and X8 are each independently a hydrogen atom or a monovalent substituent; R1 and R2 are each independently a monovalent substituent; A? and B? are each independently a monovalent anion; and Y is represented by the following general formula (II) or (III): where X9, X10, X11, X12, X13, X14, X15, X16, X17, and X18 are each independently a hydrogen atom or a monovalent substituent.

Abstract: Catalyst systems and methods for making and using the same are disclosed. In an example, a method of synthesizing a monocyclopentadienyl compound is provided. The method includes melting a dicyclopentadienyl compound including the following structure: As used herein, M is hafnium or zirconium. Each R is independently an H, a hydrocarbyl group, a substituted hydrocarbyl group, a heteroatom group. Each X is a leaving group selected from a halogen or a heteroatom group.

Abstract: The present disclosure relates to novel crystalline forms of a sodium-glucose co-transporter inhibitor drug (Sotagliflozin), processes for preparation and use thereof. The present disclosure also relates to pharmaceutical composition comprises novel crystalline forms of Sotagliflozin and use of novel crystalline forms and pharmaceutical composition of Sotagliflozin for preparing drugs for treating diseases. The crystalline forms provided by the present disclosure have advantages of good stability, relatively low hygroscopicity, suitability for process development and post-treatment, simple processes for preparation, low cost, and has significant value for future drug optimization and development.

Abstract: Polymorphic and amorphous forms of Rebaudioside X and methods for preparing the same are provided herein. Also provided herein are Rebaudioside X complexes and methods for preparing the same. Sweetener compositions and sweetened compositions comprising Rebaudioside X forms and Rebaudioside X complexes are described, as well as and methods of their preparation. Methods of improving the flavor and/or temporal profile of sweetenable compositions, such as beverages, are also provided herein.

Abstract: Truncated triterpene saponin analogues containing a trisaccharide or tetrasaccharide ester are disclosed. Also disclosed are pharmaceutical compositions comprising truncated saponin analogues and synthetic methods of producing the truncated saponin analogues. Another aspect of the present application relates to a method for immunizing a subject, comprising administering to the subject the pharmaceutical composition comprising a minimal saponin analogue and an antigen.

Abstract: Provided herein are analogs of unnatural nucleotides bearing predominantly hydrophobic nucleobase analogs that form unnatural base pairs during DNA polymerase-mediated replication of DNA or RNA polymerase-mediated transcription of RNA. In this manner, the unnatural nucleobases can be introduced in a site-specific way into oligonucleotides (single or double stranded DNA or RNA), where they can provide for site-specific cleavage, or can provide a reactive linker than can undergo functionalization with a cargo-bearing reagent by means of reaction with a primary amino group or by means of click chemistry with an alkyne group of the unnatural nucleobase linker.