Abstract: A positron emission tomography (PET) radiotracer for imaging lactate uptake, wherein the tracer is [18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof. Also, a process for the radiosynthesis of [18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof. Further, the use of [18F]-3-fluoro-2-hydroxypropionic acid, or a pharmaceutical acceptable salt and/or solvate thereof, for imaging lactate uptake in living cells, especially in humans.

Abstract: A process for preparing glycerol carbonate methacrylate, wherein glycidyl methacrylate is reacted with carbon dioxide in the presence of a catalyst and a solvent, wherein the catalyst is potassium iodide, the solvent is acetonitrile, one or more monoalcohols, or any desired mixture of acetonitrile and one or more monoalcohols, and the reaction of glycidyl methacrylate with carbon dioxide is carried out at a pressure from 0.5 to 5 bar.

Abstract: The present disclosure relates to a method for preparing tolimidone on large scale with maintaining high purity and uniform particle size distribution, and more specifically, a method suitable for preparing tolimidone on industrially large scale by using tetrabutyl ammonium bromide catalyst and recrystallization in ethanol, which can prepare highly pure tolimidone in a time shorter than prior arts while maintaining water content and particle size distribution constantly.

Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. The present invention has been made in view of such circumstances, and an object of the present invention is to develop and provide a novel agricultural and horticultural insecticide. The present invention provides a benzimidazole compound represented by the general formula (1): {wherein R1 represents a hydrogen atom or a cyano group, R2 and R3 each represent a hydrogen atom, R4 represents a hydrogen atom or a haloalkoxy group, R5 represents a haloalkoxy group, a haloalkylthio group, a haloalkylsulfinyl group, or a haloalkylsulfonyl group, and m represents 0 or 2}, or a salt thereof; an agricultural and horticultural insecticide comprising the compound or the salt as an active ingredient; and a method for using the insecticide.

Abstract: Provided are a nobiletin composition having excellent solubility in water and a method for simply producing the same. A method for producing a solid dispersion containing nobiletin, the method involving a step of dissolving nobiletin or a nobiletin-containing substance and a water-soluble hesperidin derivative selected from the group consisting of glucosyl hesperidin and methyl hesperidin in an ethanol aqueous solution having an ethanol concentration of from 20 to 90 vol % and a step of drying the solution.

Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1. The invention further relates to the use of DUB inhibitors in the treatment of cancer.

Abstract: Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds.

Abstract: The present invention relates to a novel process for preparing and isolating 3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide (Isotianil), which can be used as an active compound with microbicidal properties, wherein the amount of waste materials—e.g. solvents and diluents—is significantly reduced and the process meets the requirements of industrial scale production, in particular that it provides the product in high yield, high purity, i.e. minimum amount of by-products and impurities, and can be carried out with tolerable corrosivity in industrial scale metal, in particular stainless steel, vessels or Cr—Ni—Mo alloy pressure filters or centrifuges.

Abstract: The present disclosure relates to modified nucleoside reverse transcriptase inhibitors (NRTIs), such as and compositions thereof, as well as methods useful for treating retinal damage and/or retinal degradation/retinal degeneration, for inhibiting inflammasome activation by Alu RNA associated with a cell, for reducing ATP-induced permeability of a cell, for reducing an amount of mitochondrial reactive oxygen species in a cell, and for reducing an amount of mitochondrial reactive oxygen species in a cell.

Abstract: The present invention relates to compounds of formula (I): wherein the variables have the meaning defined in the Specification. The compounds according to the present invention are useful for therapy and/or prophylaxis in a mammal, and in particular to spiro bicyclic compounds, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes.

Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to salts of (Z)-5-((Z)-3-chloro-4-((R)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one.

Abstract: The present disclosure relates to a crystal form of a key intermediate of a bruton tyrosine kinase (BTK) inhibitor and a method for preparing the crystal form, and belongs to the technical field of medicine. The crystal form is a crystal form II of (R)-1-(1-(tert-butyloxyl)pyrrolidine-3-yl)-3-cyano-4-(4-(2,6-difluorophenoxyl)phenyl)-1H-pyrrole-2-ethyl formate. The obtained crystal form II of (R)-1-(1-(tert-butyloxyl)pyrrolidine-3-yl)-3-cyano-4-(4-(2,6-difluorophenoxyl)phenyl)-1H-pyrrole-2-ethyl formate has good chemical stability and crystal form stability and is convenient for storage and transportation. Meanwhile, the intermediate can be highly purified and a sample with a purity of 99.7% is obtained. The crystal form is important for quality control of a BTK inhibitor (R)-4-amino-1-(1-(butyl-2-alkynyl)pyrrolidine-3-yl)-3-(4-(2,6-difluorophenoxyl)phen yl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one, has a simple preparation process and is suitable for industrial production.

Abstract: The invention discloses a method for preparation of 1,4-sorbitan by dehydration of D-sorbitol, wherein one equivalent of water is removed and a cyclization occurs, followed by a treatment with ethanol and isopropanol.

Abstract: The present disclosure provides compounds and nanostructures having one or more quaternary ammonium salts, compositions including the compounds and nanostructures, and methods useful for treating conditions using the compounds, nanostructures, and compositions. In at least one aspect, a compound is represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein: Q is fluoro, chloro, bromo, or iodo; each of s, b, and n is independently an integer from about 10 to about 100; and each of v, j, p, z, q, x and m is independently an integer from 1 to about 20.

Abstract: Disclosed are 4-pyridinylmethyl-morpholines of formula A and pharmaceutically acceptable salts thereof, wherein R1 and R2 are defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.

Abstract: The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: Disclosed are a diaryl carbonate containing a compound of the following formula (I) in an amount of less than 1,000 ppm by mass, and a method for producing the same: wherein Rl represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an aryl group, or an aryloxy group. Disclosed methods include reacting urea with an alkyl alcohol to provide a dialkyl carbonate; reacting the dialkyl carbonate with an aryl alcohol to provide an alkylaryl carbonate; subjecting the alkylaryl carbonate to disproportionation to yield a mixture comprising a diaryl carbonate; and purifying the mixture.

Abstract: The present invention covers bicyclic pyrazole compounds of general formula (I): in which G, A, R1, R2, R3, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

Abstract: Disclosed is a crystalline form of sepiapterin, a method of preparing the crystalline form, pharmaceutical compositions containing the crystalline form, and a method for treating patients with a disease associated with low intracellular BH4 levels or with dysfunction of various BH4 dependent metabolic pathways, which involves administering to the patient an effective amount of the crystalline form.

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein R1, R2, Ra, G, X, Y, Z, and n are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.