Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a 6,5-heterocyclic structure (e.g., compounds having a imidazopyridine, imidazopyrimidine, imidazopyrazine, imidazopyridazine, imidazotriazine, benzoimidazole, benzotriazole, benzoisoxazole, purine, indazole, triazolotriazine, triazolopyridazine, triazolopyrimidine, triazolopyrazine, triazolotetrazine, triazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolopyridazine, pyrazolotriazine, pyrazolopyridine, isoxazolopyrazine, isoxazolopyrimidine, isoxazolopyrdiazine, isoxazolotriazine, or isoxalopyridine structure) which function as inhibitors of DYRK1A, DYRK1B, and Clk-1, and their use as therapeutics for the treatment of Alzheimer's disease, Down syndrome, diabetes, glioblastoma, autoimmune diseases, cancer (e.g., glioblastoma, prostate cancer), inflammatory disorders (e.g., airway inflammation), and other diseases.

Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.

Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

Abstract: The present disclosure relates to polymorphic forms of the compound methyl (3R,6S)-6-amino-sulfonylamino-1-(thiazol-2-yl)-3-(2,3,4-trifluorophenyl)-3,5,6,7-tetrahydropyrrolo[1,2-c]pyrimidin-4-formate (compound 1). The present disclosure further relates to a pharmaceutical composition and pharmaceutical use and a preparation method of the polymorphic forms of compound 1.

Abstract: The present disclosure provides: a compound capable of providing high light-emitting efficiency, low driving voltage, and improved lifetime of a device; an organic electronic element using the same; and an electronic device therefor.

Abstract: The present application provides heteroaryl amide compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.

Abstract: 10-oxo-6,1-dihydrobenzo[e]pyrido[1,2-c][1,3]oxazine-9-carboxylic acid derivatives of formula (I) as hepatitis B surface antigen inhibitors or pharmaceutically acceptable salts thereof, and uses of a compound of formula (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions thereof in preparation of medicaments for treatment of viral hepatitis B.

Abstract: The present invention is directed to compositions, methods and kits for treatment of cancer, e.g. hepatocellular carcinoma (HCC). In some embodiments, the present invention discloses the use of a small-molecule compounds of Formula (I)-(V) to inhibit tubulin methylation or to modulate chromatin or cytoskeleton modification in a cell.

Abstract: The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

Abstract: The present disclosure relates to amine-substituted heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., cancer) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

Abstract: An object of the present invention is to provide a method for producing 1,2,4,5-cyclohexanetetracarboxylic dianhydride, which is capable of stably achieving a high dehydration rate. The method for producing 1,2,4,5-cyclohexanetetracarboxylic dianhydride of the present invention is a method for producing 1,2,4,5-cyclohexanetetracarboxylic dianhydride by subjecting 1,2,4,5-cyclohexanetetracarboxylic acid to a dehydration reaction in a slurry state in the presence of a dehydrating agent, wherein the 1,2,4,5-cyclohexanetetracarboxylic acid is fed in a divided or continuous manner to the dehydrating agent.

Abstract: The present disclosure relates to novel sesquiterpenoid compounds as SHP2 and/or POLE3 inhibitors for potential treatment for cancers, and to methods of making and using the sesquiterpenoid compounds. The present invention therefore provides a method of using the disclosed compounds as chemosensitizations agent to a DNA damaging drugs for cancers.

Abstract: The present disclosure provides compounds of Formula (I) and Formula (II). The compounds described herein may be useful in treating proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV and formula V and the methods for the treatment of xerostomia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral mucosal inflammatory, dry mouth or oral dry mouth mediated infectious diseases.

Abstract: The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have great potential as new leads for developing drugs to be used for treating diseases.

Abstract: Antibacterial agents against D,D- and L,D-transpeptidases are disclosed. Pharmaceutical compositions and methods of using the same also are disclosed.

Abstract: The present invention relates to novel compounds of formula (I) as GPR119 agonist, composition compositions containing such compounds and method of preparation thereof.

Abstract: Provided are novel crystalline forms of a spiro-compound which acts as a muscarinic acetylcholine receptor agonist. In particular, isolated crystalline polymorphs of (S)-2-ethyl-8-methyl-1-thia-4,8-diazaspiro[4.5]decane-3-one are described which have favorable properties in pharmaceutical manufacture. Also provided are methods to prepare said crystalline polymorphs, and to convert them into each other as well as methods for preparing medicaments containing the same which are suitable for use in the treatment of diseases and disorders that respond to modulation of the muscarinic acetylcholine receptor.

Abstract: Disclosed are a dihydroartemisinin dimer derivative, a pharmaceutical composition, and an application thereof. The derivative is an artemisinin dimer used for drugs treating or preventing malaria caused by plasmodium, drugs treating autoimmune diseases such as lupus erythematosus, and anti-tumour drugs, which is a pharmaceutical composition prepared from the dihydroartemisinin dimer derivative and a pharmaceutically acceptable carrier.

Abstract: The present application provides tricyclic heteroaryl compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.

Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat inflammatory bowel diseases, and processes and intermediates useful for preparing such compounds.

Abstract: Nitrogen-containing cyclic compounds for color conversion film, and a color conversion film, a backlight unit and a display apparatus including the compound(s).

Abstract: The invention relates to powdery, highly reactive alkali and alkaline earth hydride compounds, and to mixtures with elements of the third main group of the periodic table of elements (PTE) and to the preparation thereof by reacting alkali or alkaline earth metals in the presence of finely dispersed metals or compounds of the third main group of the PTE, wherein the latter have one or more hydride ligands or said hydride ligands are converted in situ, under the prevailing reaction conditions, i.e., in the presence of hydrogen gas or another H source, into hydride species, and to the use thereof for the preparation of complex hydrides and organometallic compounds.

Abstract: Compounds and method of preparation of Si—X and Ge—X compounds (X=N, P, As and Sb) via dehydrogenative coupling between the corresponding unsubstituted silanes and amines (including ammonia) or phosphines catalyzed by metallic catalysts is described. This new approach is based on the catalytic dehydrogenative coupling of a Si—H and a X—H moiety to form a Si—X containing compound and hydrogen gas (X=N, P, As and Sb). The process can be catalyzed by transition metal heterogenous catalysts such as Ru(O) on carbon, Pd(O) on MgO) as well as transition metal organometallic complexes that act as homogeneous catalysts. The —Si—X products produced by dehydrogenative coupling are inherently halogen free. Said compounds can be useful for the deposition of thin films by chemical vapor deposition or atomic layer deposition of Si—containing films.

Abstract: The present invention provides a compound that thickens or gels a fluid organic substance to a desired viscosity, or uniformly stabilizes a composition containing a fluid organic substance. The compound of the present invention is a compound represented by Formula (1) below: wherein, R1 represents a monovalent aliphatic hydrocarbon group having 4 or more carbons; R2 represents a divalent aliphatic hydrocarbon group having from 1 to 12 carbons; R3 represents a monovalent aliphatic hydrocarbon group having from 1 to 12 carbons; m represents an integer from 0 to 10; and n represents an integer from 1 to 4; in a case where n is 1 or 2, (4?n) R1s may be the same or different; and in a case where n is from 2 to 4, n R2s, n R3s, and n m's each may be the same or different.

Abstract: The present invention provides a composition comprising nanoparticles of prodrugs of certain pharmaceutically active agents, wherein the nanoparticles of prodrugs are dispersed within a carrier material. The present invention further provides processes for the making of the same.

Abstract: Functionalized F-POSS compounds comprising synthetic blends of at least two feedstocks that produce a distribution of fluorinated polyhedral oligomeric silsesquioxane molecule structures and/or functional groups.

Abstract: A method of preparing a solid-supported phospholipid bilayer is provided. The method includes a) a first step of providing a solution comprising a bicellar mixture of a long-chain phospholipid and a short-chain phospholipid; b) at least one second step of decreasing the temperature of the solution to below 0° C., increasing the temperature to above room temperature and causing the solution to be blended; and c) a third step of depositing the solution obtained after the second step on a surface of a support, wherein the concentration of the long-chain phospholipid in the solution is at most 0.1 mg/mL, for obtaining a solid-supported phospholipid bilayer. A solid-supported phospholipid layer obtained by the method as defined above is also provided.

Abstract: The present disclosure is drawn to an amine synergist including a tertiary benzylamine with a substituted benzene ring attached to a tertiary amine. The tertiary amine can be modified with multiple water soluble groups.

Abstract: There is a need for a new antibiotic having a novel mechanism of action, which exhibits strong antibacterial activity not only against sensitive bacteria, but also against resistant bacteria thereof, and at the same time possess excellent solubility and safety profile amenable to human use. As a result of intensive research, the present inventors have found that N-phosphonoxymethyl prodrugs of hydroxyalkyl thiadiazole derivatives represented by general formula (I), a regioisomer, a stereoisomer, or a pharmaceutically acceptable salt thereof possess excellent solubility and safety profile for use in human for the treatment of bacterial infectious diseases.

Abstract: Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomersynthesis while maintaining overall yield and purity of a synthesized oligomer.

Abstract: The invention comprises novel chiral metal complex compounds of the formula wherein M, PR2, R3 and R4 are outlined in the description, its stereoisomers, in the form as a neutral complex or a complex cation with a suitable counter ion. The chiral metal complex compounds can be used in asymmetric reactions, particularly in asymmetric reductions of ketones, imines or oximes.

Abstract: The invention relates to a method for treating lignin, wherein the method comprises the following steps: a) dissolving lignin into an aqueous composition, which contains a compound selected from the class of phenols, while keeping the temperature of the composition at 0-16° C.; and b) allowing the composition to react while keeping the temperature of the composition at 60-100° C. and the pH of the composition at a pH valise of 6-14. The invention relates further to a method for producing a binder composition and to different applications thereof.

Abstract: Allulose crystals are efficiently produced from an allulose syrup using seed crystals.

Abstract: The invention described herein relates to processes for preparing ketolide antibacterial agents. In particular, the invention relates to intermediates and processes for preparing ketolides that include a 1,2,3-triazole substituted side chain.

Abstract: This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to compounds, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.

Abstract: What is described is a trinucleotide cap analog comprising m7G(5?)p3-N1pN2 for increased efficiency of in vitro transcription of m7G(5?)p3-RNA, wherein m7G is N7-methylguanosine or analog, (5?)p3 is a 5?,5?-triphosphate bridge, and N1 or N2 or both ribonucleotide analogs linked to each other by a phosphate, p, and wherein the trinucleotide cap analog increases the efficiency of in vitro transcription.

Abstract: Provided herein are analogs of unnatural nucleotides bearing predominantly hydrophobic nucleobase analogs that form unnatural base pairs during DNA polymerase-mediated replication of DNA or RNA polymerase-mediated transcription of RNA. In this manner, the unnatural nucleobases can be introduced in a site-specific way into oligonucleotides (single or double stranded DNA or RNA), where they can provide for site-specific cleavage, or can provide a reactive linker than can undergo functionalization with a cargo-bearing reagent by means of reaction with a primary amino group or by means of click chemistry with an alkyne group of the unnatural nucleobase linker.

Abstract: Cyclic dinucleotides are described, which in contrast to their natural congeners carry lipophilic nucleobases and have higher membrane permeability and increased biological activity.

Abstract: The present invention refers to a new process for the synthesis of (9?,10?)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below.

Abstract: Disclosed herein is a method of producing collagen particles. Each of the collagen particle is characterized in having a particle size of about 10-250 ?m, in which the integrity of collagen fibers therein is relatively intact.

Abstract: The present invention relates to compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof for the use in the treatment or prevention of infections and resulting diseases caused by Pseudomonas aeruginosa.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R8?, R9, R9?, X1, X2, X3, X4, X5, X6, X7, X8, X9 and X10 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baurnannii.

Abstract: Provided herein is a novel epitope that can be used as a tag in methods for rapid and effective characterization, purification, and subcellular localization of polypeptides of interest, which comprise the tag. The tag is specifically recognized by an epitope specific antibody, which can be used to detect, capture, quantify, and/or purify polypeptides of interest that are tagged with the epitope. Also provided is novel epitope specific antibody.

Abstract: IL-2R? ligands and IL-2R?c ligands and compounds comprising the ligands are disclosed. The ligands and compounds such as heterodimers and fusion proteins comprising the IL-2R? ligands and/or the IL-2R?c ligands can be IL-2 receptor agonists.

Abstract: The present invention relates to an antimicrobial peptide having an improved antibacterial effect through glutamic acid substitution and, more specifically, to a use of the antimicrobial peptide as an active ingredient in an antibacterial pharmaceutical composition, a food additive, a feed additive, an antiseptic composition, and an antibacterial quasi-drug composition. Not only does the antimicrobial peptide of the present invention exhibit significant antibacterial activity against gram-negative bacteria, but it also exhibits a significant synergistic effect when combinedly treated with antibiotics which have strong antibacterial activity only against gram-positive bacteria and has no or low antibacterial activity against gram-negative bacteria, thereby exhibiting excellent antibacterial effects on gram-positive bacteria, E. coli and Acinetobacter bacteria among gram-negative bacteria, and antibiotic-resistant strains thereof.

Abstract: IL-2R? ligands and IL-2R?c ligands and compounds comprising the ligands are disclosed. The ligands and compounds such as heterodimers and fusion proteins comprising the IL-2R? ligands and/or the IL-2R?c ligands can be IL-2 receptor agonists.

Abstract: The present invention provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel diseases.

Abstract: The invention provides processes of preparing a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-249 described herein.