Abstract: The present invention relates to a novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivative as inhibitor of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the compound, to processes for preparing such compound and compositions, and to the use of such compound and compositions for the prevention and treatment of disorders in which PDE2 is involved, such as neurological and psychiatric disorders.

Abstract: Provided are co-assembled nanoparticles including at least one polypeptide including a polyanion; and at least one amphiphilic peptide capable of forming a ?-sheet structure, a derivative or a salt thereof, the amphiphilic peptide including at least 2 pairs of alternating hydrophobic/hydrophilic amino acid residues in which the hydrophilic amino acid residue is positively charged, and methods of preparation of the nanoparticles. Further provided are pharmaceutical compositions including the co-assembled nanoparticles and a pharmaceutically active ingredient, dissolved, entrapped, encapsulated or attached to the co-assembled nanoparticles. Further provided are therapeutic uses of the pharmaceutical compositions.

Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

Abstract: The present invention relates to a Ru—Pd bimetallic catalyst for use in hydrogenation of a compound, and more particularly to a catalyst prepared by loading both ruthenium and palladium on a g-C3N4 support and to a selective hydrogenation process of a pyridine group in a reaction system containing both a pyridine group and a benzene group using the catalyst.

Abstract: The present invention is directed to processes from producing beta-lactone and beta-lactone derivatives using heterogenous catalysts. In preferred embodiments of the present invention, the processes comprise the steps: passing a feed stream comprising an epoxide reagent and a carbon monoxide reagent to a reaction zone; contacting the epoxide reagent and the carbon monoxide reagent with a heterogenous catalyst to produce a beta-lactone product in the reaction zone; and removing the beta-lactone product from the reaction zone. In preferred embodiments, the heterogenous catalyst comprises a solid support containing a cationic Lewis acid functional group and a metal carbonyl compound comprising at least one of anionic metal carbonyl compound or a neutral metal carbonyl compound. In certain preferred embodiments, the epoxide reagent and carbon monoxide reagent have a biobased content.

Abstract: The present invention relates to a composition comprising urolithin A, urolithin B, urolithin C, urolithin D, or a combination thereof, for the stimulation of insulin secretion, and to the use of a compound chosen among urolithin A, urolithin B, urolithin C, urolithin D, or a combination thereof, intended for the stimulation of insulin secretion. The present invention also relates to a composition comprising an effective amount of urolithin B, urolithin C, urolithin D, or a combination thereof, for the treatment or the prevention of diabetes mellitus, and in particular for the treatment or the prevention of type 2 diabetes, and to the use of a compound chosen among urolithin B, urolithin C, urolithin D, and a combination thereof, intended for the treatment or the prevention of diabetes mellitus, and in particular of type 2 diabetes.

Abstract: A method of purifying a cyclic ester, the method including: granulating a crude cyclic ester, an average particle size of resulting granules being 0.05-1.00 mm; adding the granules to 0-4° C. water to yield a mixture, a mass ratio of the water to the granules being (0.5-2):1; stirring the mixture, and performing solid-liquid separation on the mixture; repeating the stirring and solid-liquid separation for 1-4 times, to yield a purified cyclic ester; drying the purified cyclic ester at 0-4° C. and at an absolute pressure of less than or equal to 10 pascal for 4-6 hours, and continually drying the purified cyclic ester at 40-60° C. and at an absolute pressure of less than or equal to 5 pascal for 1-2 hours.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R3, R4 and R5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: A method for treatment of disease by reduction in macrophages-mediated bacterial killing, including administration to patients in need a compound of formula (I): wherein A is N or CH; B is NO, or S; R1 is H, (C1-C4)alkyl group, methyl(C1-C6)cycloalkyl group or (C1-C6)cycloalkyl group; R2 is an aryl, arylmethyl group or methylheteroaryl group as methylpyridine and methylthiophene; R3 is absent when B is O or S, or is H or (C1-C4)alkyl group when B is N; R4 is (C1-C5)alkyl group or (C1-C4)cycloalkyl group, groups bearing a carboxylic acid group, and (C1-C5)alkyl group or (C1-C4)cycloalkyl substituted by hydroxyl group, halogen group or methoxy group, when B is N, R3 and R4 can together form a 5- or 6-membered heterocycle substituted by carboxylic acid group, substituted by a halogen atom, hydroxyl group, methoxy group or hydroxymethyl group, or pharmaceutically acceptable salt. Also provided are new compounds relating to this use.

Abstract: The invention relates to compounds of formula (I) or the salts thereof, said compounds of formula (I) being selected from among the group consisting of homoeriodictyol (1), eriodictyol (2), hesperetin (3) and sterubin (4), for use in the treatment of an ailment which can be alleviated or prevented by influencing the serotonin level and the concentration of free fatty acids in the blood.

Abstract: The invention relates to process for the preparation of gamma valerolactone (GVL) from levulinic acid (LA), said process comprising a) subjecting LA to a hydrogenation reaction comprising hydrogen and a solid catalyst system comprising a metal and a support in the liquid phase, to yield a first reaction mixture comprising GVL, hydroxypentanoic acid (4HPA), and water; b) removing water from said first reaction mixture; and c) subjecting the mixture obtained in step b) to a further reaction under conditions suitable to convert said 4-HPA to GVL, to yield a further reaction mixture. Steps b) and c) can be integrated. Optionally, water can be removed from the further reaction mixture. The process may include recycling the—optionally at least partially dewatered—further reaction mixture back to step (b). This is particularly advantageous when the first reaction mixture is low in, or even free of levulinic acid.

Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Abstract: A fused polycyclic heteroaromatic compound represented by Chemical Formula 1A or 1B that has a compact planar structure in which eight or more rings are fused together.

Abstract: The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.

Abstract: A compound of formula (I?) or (I?) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.

Abstract: Glycosphingolipids (GSLs) compositions and methods for iNKT-independent induction of chemokines are disclosed.

Abstract: A method of stabilizing aqueous solutions of antimicrobial silanol quaternary ammonium compounds (SQACs) from premature polymerization where the stabilizing agent is selected from a list of antimicrobial, naturally occurring, renewable, volatile, liquid phytochemical essential oils that easily form crystal clear microemulsions when water is added to the concentrated SQAC/essential oil mixture. These non-foaming oil-in-water microemulsions have excellent long term storage stability, remain very low in viscosity and do not phase or precipitate for many months. Many essential oils found to be useful in this process are non-toxic food additives having pleasant scents, have low flammability yet are volatile enough to evaporate upon cure down of the SQAC, resulting in a higher concentration of SQAC in the cured, antimicrobial film.

Abstract: The disclosure includes high purity compounds having CCR5 and/or CCR2 antagonism, or a salt thereof, and processes for synthesizing the same.

Abstract: Disclosed is a color material dispersion liquid for a color filter, the dispersion liquid being capable of forming a high-luminance coating film with excellent light resistance; a color resin composition for a color filter, the composition being capable of forming a high-luminance coating film with excellent light resistance; a color material that has, while it can form a high-luminance coating film, excellent light resistance; a high-contrast, high-luminance color filter; a liquid crystal display device including the color filter; and a light-emitting display device including the color filter. The color material dispersion liquid for a color filter, includes: (A) a color material, (B) a dispersant and (C) a solvent, wherein the color material (A) contains a cerium lake color material of an acid dye.

Abstract: Disclosed herein are methods for synthesizing 1,2,5,6-hexanetetrol (HTO), 1,6 hexanediol (HDO) and other reduced polyols from C5 and C6 sugar alcohols or R glycosides. The methods include contacting the sugar alcohol or R-glycoside with a copper catalyst, most desirably a Raney copper catalyst with hydrogen for a time, temperature and pressure sufficient to form reduced polyols having 2 to 3 fewer hydoxy groups than the starting material. When the starting compound is a C6 sugar alcohol such as sorbitol or R-glycoside of a C6 sugar such as methyl glucoside, the predominant product is HTO. The same catalyst can be used to further reduce the HTO to HDO.