Abstract: The present application and its embodiments teach stable compositions of fosaprepitant or a pharmaceutically acceptable salt thereof with such compositions lacking polysorbate 80 and containing dual functional excipients of hydrolysis inhibition and solubility enhancement. Further described are methods of preparation of such compositions. Among other advantages of contemplated compositions, fosaprepitant hydrolysis degradation is kept low and the compositions maintain physically and chemically stable for prolonged period.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: Phenyl isocyanates are removed from a solvent stream obtained from an MDI and/or PMDI manufacturing process by reaction in the presence of a carbodiimidization catalyst to form the corresponding N,N-diphenylcarbodiimides. The N,N-diphenylcarbodiimides can be recycled into the MDI and/or PMDI manufacturing process where they can react with MDI and/or PMDI to form uretonimines. The uretonimines have at most minimal effect on the properties and usefulness of the MDI and/or PMDI product and so can be left in the MDI and/or PMDI product.

Abstract: Provided is a method of preparing an N-acetyl dipeptide and an N-acetyl amino acid, the method including producing the N-acetyl dipeptide and the N-acetyl amino acid by reaction of an amino acid with acetic anhydride or acetyl chloride.

Abstract: Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH2 and Boc-D-Arg-DMT. The crystalline forms may be used in the synthesis of elamipretide.

Abstract: The present invention relates to a process for preparing the 2-bromoglutaric acid diester of formula (I) below: comprising the formation of the 2-hydroxyglutaric acid diester of formula (II) by reaction of butyrolactone acid of formula (BA) with the alcohol of formula ROH, in the presence of an acid such as sulfuric acid; and bromination of the 2-hydroxyglutaric acid diester of formula (II), by sparging with gaseous hydrobromic acid. The present invention also relates to a 2-bromoglutaric acid diester of formula (I), having a degree of purity determined by HPLC analysis of greater than or equal to 90%.

Abstract: The present invention relates to method of modulating TIGIT signaling pathway and PD-1 signaling pathway. The invention also encompasses the use of the compound of formula (I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof for the treatment of diseases or disorders mediated by both TIGIT signaling pathway and PD-1 signaling pathway.

Abstract: Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Abstract: Efficient methods of producing L-threonic acid from L-xylonic acid are disclosed.

Abstract: A method for preparing a partially fluorinated ester comprising acyl and alkoxy groups wherein the acyl group comprises a branched or linear fluorine containing C3-C8 group with one of the structures: (Formulae (I), (II)) wherein X and Y are independently selected from: —H, —CH3, —F, —Cl, —CH2F, —CF3—OCF3, —OCH2CF3, OCH2CF2CHF2 and —CH2CF3 (wherein both X and Y cannot be H) comprising reacting an unsaturated halocarbon: (Formula (III)) wherein A and B are independently selected from the group comprising —H, —CH3, —F, —Cl, —CH2F, —CF3, —OCF3, —OCH2CF3, OCH2CF2CHF2 and —CH2CF3 (wherein both A and B cannot be H) with carbon monoxide and an alcohol, in the presence of a catalyst methods.

Abstract: Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.

Abstract: This disclosure relates to a method of reducing a fat deposit comprising injecting an alcohol-containing pharmaceutical composition into the fat deposit. The method may be effective in improving the appearance of or reducing the weight or volume of the fat deposit.

Abstract: The present disclosure relates to the combination of IN10018 and an epidermal growth factor receptor tyrosine kinase inhibitor for the treatment of tumors.

Abstract: In the embodiments, an aqueous hydrochloric acid solution instead of hydrogen chloride gas and solid triphosgene instead of phosgene gas may be used in the process of preparing a diisocyanate from a diamine through a diamine hydrochloride. In addition, the embodiments provide processes for preparing a diisocyanate composition and an optical lens, which are excellent in yield and quality with mitigated environmental problems by controlling the size of the diamine hydrochloride composition, the b* value according to the CIE color coordinate of the diamine hydrochloride composition, or the content of water in the diamine hydrochloride composition within a specific range.

Abstract: Provided herein are cannabinoid-containing complex mixtures suitable for use as active pharmaceutical ingredients. The complex mixtures comprise at least a first major cannabinoid, at least a first minor cannabinoid, and optionally at least a first selected terpene. Also provided are methods of making the complex mixtures; pharmaceutical compositions comprising the complex mixture, and methods of using the pharmaceutical compositions for the treatment of neurodegenerative diseases, including Alzheimer's disease, Parkinson's disease, Lewy Body Dementia, or Huntington's disease.

Abstract: A hybrid vertical plug flow reactor is comprised of a bottom inlet and a top outlet having vertical tubular member disposed there between, wherein the bottom inlet has separate gas reactant inlet and separate liquid reactant inlet whereby the gas reactant is mixed with the liquid reactant and the outlet has an extraction port, the extraction port extending sufficiently to withdraw the liquid product from the reactor and maintain a gaseous head space within the tubular member of the reactor. The hybrid vertical bubble plug flow reactor is useful to react a gas reactant and liquid reactant that are reacted at a molar ratio of gas reactant/liquid reactant that is in excess of a stoichiometric requirement of gas reactant so that the gas reactant forms bubbles and the reactants react in the presence of a catalyst to form a reaction product.

Abstract: The present disclosure encompasses crystalline polymorphs of Rigosertib Sodium, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: This invention concerns a process for the production of vinyl esters of carboxylic acids with 3 to 20 carbon atoms, via vinylation in the presence of palladium (Pd) catalyst in combination with copper (Cu) as co-catalyst stabilized by organic salts in the presence of ethylene and air or oxygen.

Abstract: The present disclosure provides a preparation method of resveratrol nervonic acid ester, comprising the following steps of: step 1: weighing resveratrol, a nervonic acid and thiocarbonyldiimidazole according to a molar ratio of 1:1:0.8 to 1:7:11.2 in a reactor; step 2: adding a certain amount of solvent into the reactor to completely dissolve the reactants; and step 3: stirring for reaction at room temperature for 30 min to 180 min. The preparation method is safe, efficient and clean, and enables synthesis of the resveratrol nervonic acid ester with high conversion rate, high purity and high yield.

Abstract: There is provided a compound having a structure represented by the following Formula (1), in Formula (1), R1 and R2 each independently represent a phenyl group having a substituent or an unsubstituted phenyl group, R3 and R4 each independently represent a C2-C12 alkyl group having a substituent or an unsubstituted C2-C12 alkyl group, a cyano group, a trifluoromethyl group, or a halogen atom, R5 and R6 each independently represent a hydrogen atom or an alkyl group, R7 represents a phenyl group having a substituent, an unsubstituted phenyl group, or a heteroaromatic group having a specific structure, and X? represents an anion, and in a case where at least one anionic substituent is included in a molecule, X? may not be present.