Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.

Abstract: A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

Abstract: Ebola virus and Marburg virus are filoviruses and are responsible for outbreaks that cause up to 90% fatality, including the recent outbreak in West Africa that has resulted in over 11,000 deaths. The present disclosure generally relates to series novel arylnaphthalene compounds, having a formula (I) or a pharmaceutically acceptable salt thereof, as a vacuolar-ATPase inhibitor that are useful for the treatment for a broad spectrum of viral infections, including those infections caused by filoviruses. Pharmaceutical composition matters and methods of use are within the scope of this invention.

Abstract: Novel pyrrolo[2,3-c]quinoline compounds, a method of synthesizing these compounds, a pharmaceutical composition comprising these compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[2,3-c]quinoline compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Disclosed herein is a method of administering to a patient in need thereof a therapeutically effective amount of an extracellular thiol isomerase inhibitor compound to treat or prevent a disease or condition influenced by the activity of one or more extracellular thiol isomerases (e.g. protein disulfide isomerase, ERp5, ERp57, ERp72 and thioredoxin). The disease or condition includes arterial thrombosis, venous thrombosis, a thrombotic disease, a cancer, an infectious disease, a viral disease, an immune disorder, inflammation, a neurologic disease, and a neurodegenerative disorder.

Abstract: The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I): or pharmaceutically acceptable salts thereof wherein R, R1, R2, R3, R4, R5, R6, R7, and R8, are as defined herein. The disclosure also relates to methods of making and using compounds of Formula (I) or pharmaceutically acceptable salts thereof.

Abstract: Described herein are methods of using compounds of Formula (I) to modulate PKM2 activity in a subject. These compounds are represented by Formula (I): wherein R1, R2, L1, and L2 are as defined herein.

Abstract: The present invention relates to novel substituted dihydrothienopyrimidines with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

Abstract: Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R1a, R1b, R2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.

Abstract: Disclosed is a method for refining 5-fluorouracil, comprising the following steps: dissolving 5-fluorouracil in an organic solvent, preferably DMSO, heating and stirring until dissolved; naturally cooling the filtrate until a crystal is precipitated; filtering, washing a filter cake using a polar solvent, and draining and drying under reduced pressure. By using the new refining method, the content of impurities in 5-fluorouracil may be reduced to less than 0.01%, the product purity is more than 99.98%, and the refining yield is higher than 70%. In addition, the refining method of the present invention has a simple process, convenient operation, low production costs, high product purity, a stable process, and is suitable for industrial production.

Abstract: This invention is directed to synthetic co-crystals of anhydrous guanine and at least one additional material, wherein the co-crystals have a high refraction index and therefore, provide products with pearlescence or whiteness with high coverage. The invention is further directed to a process for the preparation of anhydrous guanine and of the co-crystals.

Abstract: A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

Abstract: A process for the synthesis of melamine from urea, preferably of the high-pressure type, wherein offgas quenching is performed in a quenching vessel wherein in the upper part of the vessel, a rising flow of offgas is contacted in counter-current with liquid ammonia to obtain precipitation of melamine contained in the offgas and melamine-free anhydrous washed offgas; in the lower part of the vessel, the solid melamine is contacted with a liquid solvent to form a solution of melamine or a melamine slurry.

Abstract: The present invention discloses deuterated benzylaminopyrimidinedione derivatives, the use thereof and the pharmaceutical composition containing the same. They may be used for suppressing the activities of myosin. The present invention also relates to the method of preparing this type of compounds and the pharmaceutical composition, and their use in treatment of hypertrophic cardiomyopathy and related heart diseases.

Abstract: The present invention to a process for the preparation of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]-amino]-butanoic acid, compound also known as Elagolix sodium salt, having the formula (I) reported below:

Abstract: A process for the purification of a melamine melt (5) containing melamine and by-products, comprising the steps of: (a1) In quenching of said melamine melt; (a2) decomposition of by-products with alkali, providing an alkaline aqueous solution of melamine (26); (b) stripping of said alkaline aqueous solution of melamine (26); (c) crystallization of melamine with a first alkali-containing solution (6b) and separation of solid melamine (7) from a mother liquor (8); (d) treatment of said mother liquor, providing a waste water stream (11) containing carbonates; (e) decomposition of at least part of the carbonates contained in said waste water stream (11) into carbon dioxide and alkali, providing a second alkali-containing aqueous solution (30); (f) recycle of at least part of said alkali-containing aqueous solution (30) to at least one of said steps (a1), (a2) and (c).

Abstract: The present invention relates to compounds of formula (I): comprising a 5-membered nitrogen-containing heteroaryl ring A, wherein the heteroaryl ring A is substituted with at least one group containing an oxygen atom, and wherein said oxygen atom is attached to the heteroaryl ring A via at least two other atoms. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Abstract: A process for the purification of a melamine melt (5) containing melamine and by-products, comprising the steps of: (a1) In quenching of said melamine melt; (a2) decomposition of by-products with alkali, providing an alkaline aqueous solution of melamine (26); (b) stripping of said alkaline aqueous solution of melamine (26); (c) crystallization of melamine with a first alkali-containing solution (6b) and separation of solid melamine (7) from a mother liquor (8); (d) treatment of said mother liquor, providing a waste water stream (11) containing carbonates; (e) decomposition of at least part of the carbonates contained in said waste water stream (11) into carbon dioxide and alkali, providing a second alkali-containing aqueous solution (30); (f) recycle of at least part of said alkali-containing aqueous solution (30) to at least one of said steps (a1), (a2) and (c).

Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

Abstract: The present invention provides methods of preparing 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one, and 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one monohydrate, as well as new intermediate compounds.