Abstract: The present invention provides an organic electroluminescent element and electronic device thereof, wherein the organic electroluminescent element comprises the compound represented by Formula 1 as material for an emission-auxiliary layer, and by comprising the compound represented by Formula 1 in the emission-auxiliary layer, the driving voltage of the organic electroluminescent element can be lowered, and the luminous efficiency and life time of the organic electroluminescent element can be improved.

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 pharmaceutical agents 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: The present invention generally relates to an improved process for the preparation of dapagliflozin of Formula I or its solvates or co-crystals thereof. Dapagliflozin is an inhibitor of sodium dependent glucose transporters and used for treating diabetes. The present invention also encompasses novel intermediates and their use in the preparation of dapagliflozin. An exemplary process according to the present is shown below, wherein X1, R1, R2, P1, P2, P3 and P4 are as described herein.

Abstract: Disclosed are a pharmaceutical composition for treating locally advanced mismatch repair-proficient/microsatellite stable (pMMR/MSS) colorectal cancer (CRC) and use thereof. The pharmaceutical composition of the present disclosure includes mFOLFOX6, bevacizumab, and a PD-1 inhibitor. Experimental results show that, when the pharmaceutical composition is used to treat 18 locally advanced (T4N×MO) MSS CRC cases, major pathological remission (tumor regression exceeds 90%) is achieved in 14 cases and pathological complete remission (no residual tumor cells) is achieved in 10 cases; tumor marker levels are all lowered to normal levels; there is no fatal serious adverse event (SAE); and the pharmaceutical composition has prominent safety and efficacy.

Abstract: An antibiotic compound of formula (I): or a salt or stereoisomer thereof; wherein: R1-R3 and R5-R6 are independently selected from H or a C1-C5 alkyl group or a C1-C5 substituted alkyl group; R4 is a C1-C5 alkyl group or a C1-C5 substituted alkyl group; X1-X2 are independently selected from the group consisting of ?O, H, and OH; Y is an acyclic hydrocarbon chain having 2 to 20 carbon atoms or a substituted acyclic hydrocarbon chain having 2 to 20 carbon atoms; and Z is a neutral or positively charged organic group including a nitrogen or phosphorus atom, the nitrogen or phosphorous atom forming a covalent bond with a carbon atom of Y. Also disclosed are methods of treating a bacterial disease including administering an effective amount of the compound to a subject in need thereof, wherein the bacterial disease is caused by a gram-negative bacteria.

Abstract: The present disclosure relates to compounds and compositions that inhibit the NLRP3 inflammasome, for example, a compound according to formula I wherein R1 is C1-4 alkyl; and R2 is H or C1-4 alkyl, provided that when R2 is H. R1 is not CH3. Also disclosed are methods for treating multiple sclerosis using the compounds and compositions.

Abstract: Provided herein are inhibitors of AKT1, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the AKT1 inhibitory compounds for the treatment of disease.

Abstract: This invention relates to a novel continuous process for making alkyl 7-amino-5-methyl-[1,2,5]-oxadiazolo¬[3,4-b]pyridine-carboxylate, wherein R is C1-3-alkyl. The process of the invention present invention overcomes disadvantages of processes of the prior art by avoiding the highly energetic intermediates, using readily available and inexpensive starting materials and reagents, and avoiding the isolation of intermediates. The process according to the invention is suitable for use on industrial scale.

Abstract: Pharmaceutical compositions comprising filgotinib maleate Form I characterized by an XRPD pattern substantially the same as shown in FIG. 1 and uses thereof are described herein.

Abstract: A 4-(4,5-bis(4-bromophenyl)-2-phenyl-1H-imidazol-1-yl)benzoic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The present disclosure provides compositions that inhibit the SH2-containing inositol 5?phosphatase (SHIP) as well as methods using such composition for use in treating or ameliorating the effects of a medical condition in a subject. For examples, compositions including the general formula as disclosed herein are suitable for use herein.

Abstract: The present invention relates to new pharmaceutical agents, and to their use in the treatment of proliferative diseases, such as cancer (in particular, brain cancer).

Abstract: Compounds, such as compounds having Formula (I): wherein each variable is as described herein, that modulate the conversion of AMP to adenosine by 5?-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5?-nucleotidase, ecto is also provided.

Abstract: Certain 2?-alkyloxy-6?-phenyl[3,4?-bipyridine]-3?-carbonitrile compounds, their synthesis, and their use as an insecticidal agent.

Abstract: The invention relates to compounds of formula (I) with low cytotoxicity for blocking the ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of disorders including, but not limited to, cancers.

Abstract: The present disclosure provides compounds of Formulas (I), (II), and pharmaceutically acceptable salts thereof. The compounds described herein are useful in treating proliferative diseases, for example, cancer (e.g., lung cancer), and infectious diseases (e.g., bacterial infections).

Abstract: The present invention relates to a novel fused ring compound having urea structure that exhibits excellent NAMPT activating effect, and a method using the same for treating/preventing metabolic disorder, cardiovascular and kidney disease, mitochondrial disease, neurodegenerative disease, ocular disease, and muscle wasting disorder. The present invention provides a compound represented by following formula (I) or a pharmacologically acceptable salt: Formula (I) wherein A, B, R, R2 and R3 represent the same meanings as in the claims.

Abstract: A method for producing 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid is disclosed that includes steps of adding hydrazine sulfate with 2-ketoglutaric acid in a container as a solid, adding water to the solid creating a heterogenous mixture of the hydrazine sulfate, 2-ketoglutaric acid and water, blending the heterogenous mixture for at least one hour, and measuring the heterogenous mixture to confirm that it has converted into 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid. Hydrazine sulfate can be added to the 2-ketoglutaric acid in the container at a ratio of greater than 1.1. The compound 6-oxo-1,4,5,6-tetrahydropyridazine-3-carboxylic acid (PCA) has many uses. It has been used for medical applications and as a building block and for medical applications. The compound is also a product of the remediation of hydrazine using 2-ketogluraric acid.

Abstract: Provided is a method for decomposing a flavonoid glycoside, wherein a flavonoid glycoside-containing raw material is hydrothermally treated to decompose a flavonoid glycoside into a flavonoid.