Abstract: The present invention relates to a method of treating cataplexy in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of certain carbamate compounds.

Abstract: Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.

Abstract: Provided is a method for producing an organic tellurium compound that enables the production of an organic tellurium compound in high yield using metallic tellurium as a source material and produces less amount of side products. A method for producing an organic tellurium compound includes the steps of: (A) reacting metallic tellurium with a compound represented by a general formula (1) below; and (B) reacting a compound obtained by the step (A) with an organic halogen compound, the metallic tellurium having a copper content of less than 100 ppm, M(R1)m ??Formula (1) where R1 represents an alkyl group having 1 to 8 carbon atoms, an aryl group or an aromatic heterocyclic group, M represents an alkali metal or an alkaline earth metal, m represents 1 when M is an alkali metal, and m represents 2 when M is an alkaline earth metal.

Abstract: Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents.

Abstract: Herein are provided novel salts of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylate namely the oxalate salt and the dibenzoyltartrate salt

Abstract: The invention relates to a crystalline form of [(2R,3S,4R,5S)-1-butyl-2-(hydroxymethyl)-piperidine-3,4,5-triol, processes for the preparation thereof, pharmaceutical compositions containing such a crystalline form, and its use as a medicament, especially as glycolipid biosynthesis inhibitor.

Abstract: Disclosed herein are methods and processes of preparing vadadustat and pharmaceutically acceptable salts thereof, and intermediates of formula (I) and their salts useful for the synthesis of vadadustat.

Abstract: The present disclosure provides compounds of Formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. where R1, alk, R2, Z1, Z2, X, R3, R4, B, a, and b are as described herein.

Abstract: This disclosure relates to medicines, and more particularly to a platelet aggregation inhibitor, a pharmaceutical composition containing the same and a preparation and application thereof. The platelet aggregation inhibitor provided herein is a compound of formula (I), or a pharmaceutically-acceptable salt, a tautomer or a pharmaceutically-acceptable solvate thereof. This application also provides an application of the compound of formula (I), or a pharmaceutically-acceptable salt, a tautomer, a pharmaceutically-acceptable solvate or a pharmaceutical composition thereof in the treatment of thrombus.

Abstract: Described herein is crystalline sodium (E)-2-(4-((3-(4-fluorophenyl)-3-(4-(3-morpholinoprop-1-yn-1-yl)phenyl)allyl)oxy)-2-methylphenoxy)acetate, uses of such crystalline material in the preparation of pharmaceutical compositions for the treatment of diseases or conditions that would benefit by administration with a PPAR? agonist compound.

Abstract: A sulfonamide benzamide derivative has the structure shown in Formula II that can be prepared as an anti-HBV (hepatitis B virus) pharmaceutical composition; it is prepared by sulfonation reaction, acylation reaction and sulfonylation reaction; the sulfonamide benzamide derivative has been shown effective activity for anti-HBV by inhibiting HBV DNA replication in vitro.

Abstract: The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and prophylaxis of diseases, in particular hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

Abstract: In some aspects, the present disclosure provides gadolinium based sensors which may be used to image zinc ions in vivo. In some embodiments, the compounds show appropriate reactivity with zinc ions while maintaining high relaxivity to achieve improved background relative to other sensors.

Abstract: 5-substituted difluoropiperidine compounds having a capacity to cross the blood-brain barrier are provided. The compound has the structural formula represented by formula (I): The 5-substituted difluoropiperidine compounds, derivatives and pharmaceutically acceptable salts thereof of the present invention have the ability to cross the blood-brain barrier and are capable of acting as a drug characteristic of a protein kinase inhibitor, in particular for the expression of a protein through a vascular endothelial growth factor receptor 2 or SRC kinase family (FYN) and can be used to treat or prevent disorders associated with abnormal protein kinase activity, such as cancer, cancer with brain metastases, primary brain cancer (glioma), glioblastoma, cancer with meningeal metastases, Alzheimer's disease and central nervous system diseases, and the like.

Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein R2a, R2b, R3, R3a, R4, R6, R7, R8, A, Z, X1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

Abstract: Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof.

Abstract: The present invention relates to novel crystalline polymorphs of 1-[2-[5-[(3-Methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine monobenzenesulfonate, and to methods for their preparation. The invention further relates to pharmaceutical compositions containing one or more forms and optionally one or more suitable pharmaceutical carriers. The invention also relates to methods of using the crystalline polymorphs of the invention in the treatment of disease.

Abstract: Provided is a heterocyclic compound that can have an antagonistic action on an NMDA receptor containing the NR2B subunit, and is expected to be useful as a prophylactic or therapeutic agent for major depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

Abstract: Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Abstract: A process for the preparation of a disubstituted diaryloxybenzoheterodiazole compound having general formula (XII): wherein: Z represents a sulfur atom, an oxygen atom, a selenium atom; or a group NR6 wherein R6 is selected from linear or branched C1-C20 alkyl groups, or from optionally substituted aryl groups; R2 and R3, identical or different, represent a hydrogen atom, provided that R1 does not represent a hydrogen atom; or R1, R2 and R3 are selected from linear or branched C1-C20 alkyl groups optionally containing heteroatoms, optionally substituted cycloalkyl groups, optionally substituted aryl groups, optionally substituted, linear or branched C1-C20 alkoxy groups, optionally substituted phenoxy groups, or a cyano group; or R1 and R2, may optionally be bound together so as to form, together with carbon atoms to which R1 and R2 are bound, a saturated, unsaturated, or aromatic, cyclic or a polycyclic system containing from 3 to 14 carbon atoms, optionally containing one or more heteroatoms selected

Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds and methods of using such compounds to treat respiratory diseases.

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, R4, R5, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGK?) and diacylglycerol kinase zeta (DGK?), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

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

Abstract: Compositions and methods of making and using thereof are provided with a specific antimicrobial activity and efficacy toward Gram-positive and Gram-negative bacteria and low levels of toxicity toward mammalian cells. The compositions include water-soluble molecules characterized by a hydrophobic interior fragment and side groups containing cationic groups. A class of these molecules is provided with variations in the length of the internal conjugated segment and in other molecular features, which impact the efficacy and toxicity. The substituents on the cationic functional group, the structural variations on the solubilizing group, and the length of the conjugated segment are important features affecting the antimicrobial property and the non-toxicity to mammalian cells of the composition.

Abstract: The present invention describes compounds comprising at least one structural element having at least three fused aromatic or heteroaromatic rings (AR) and at least one structural element having an aromatic or heteroaromatic valerolactam (AV), especially for use in electronic devices. The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these.

Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, Darier's disease, scleroderma, cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

Abstract: Compounds having activity as inhibitors of NEK7 are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein, A, X, Y, R1, R2, R3, R4 and R5 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 the NLRP3 inflammasome are also provided.

Abstract: Provided herein are benzimidazole derivatives, for example, or Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

Abstract: Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: A compound of general formula I and pharmaceutical compositions, kits, methods of making, and methods for treating cancer using the same.

Abstract: A compound of Chemical Formula 1, and an organic photoelectric device, an image sensor, and an electronic device including the same are disclosed: In Chemical Formula 1, each substituent is the same as defined in the detailed description.

Abstract: The present invention relates to compounds of formula (I), ab (I), wherein R1 to R3 and L are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

Abstract: A method for producing an alkenyl or alkynyl-containing organosilicon precursor composition, the method comprising the steps of distilling at least once a composition comprising an alkenyl or alkynyl-containing organosilicon compound having the formula RnSiR14?n wherein R is selected a linear or branched C2 to C6 alkenyl group, a linear or branched C2 to C6 alkynyl group; R1 is selected from hydrogen, a linear or branched C1 to C10 alkyl group, and a C3 to C10 cyclic alkyl group; and n is a number selected from 1 to 4, wherein a distilled alkenyl or alkynyl-containing organosilicon precursor composition is produced after distilling; and packaging the distilled alkenyl or alkynyl-containing organosilicon precursor composition in a container, wherein the container permits transmission into the container of no more than 10% of ultraviolet and visible light having a wavelength of between 290 nm to 450 nm.

Abstract: The invention relates to intermediates useful in the preparation of halichondrin compounds, methods for preparing the same and use thereof, such as halichondrins, eribulin, or their analogs. The intermediates, the methods and use thereof are used for the synthesis of the C20-C26 fragment of halichondrin compounds. The raw materials in the synthetic route of the invention are cheap and easily obtained, the sources and the qualities of the raw materials are reliable. The choice of the methods useful in the synthesis of chiral central structures are based on the structural characteristics of the reactants, thus effectively improving the synthesis efficiency, reducing the difficulties and risks of product quality control, and avoiding the use of highly toxic and expensive organotin catalysts to significantly decrease costs and improve environmental friendliness.

Abstract: The present disclosure generally relates to the field of ultrasensitive microbial pathogen detection and identification utilizing genomic sequence recognition.

Abstract: The invention provides extended bisphosphonate-based metal complexes using benzene1,4-bis(bisphosphonic acid) (BBPA), an analog of benzene 1,4-dicarboxylic acid (BDC). Hydrothermal synthesis of BBPA with the bioactive metals Ca2+, Zn2+, and Mg2+ leads to four crystals phases, namely, BBPA-Ca forms I and II, BBPA-Zn form I, and BBPA-Mg form I. Out of the three structures, BBPA-Ca form II presents large channels (8 ?×12 ?), potentiating the use of this framework to load drugs. Cytotoxicity effects of BBPA was elucidated in a human breast cancer MDA-MB-231 and a normal osteoblast hFOB 1.19 cell lines. The half-maximal inhibitory concentration (IC50) for BBPA used to treat both cell lines were >200 ?M at 24, 48, and 72 h of treatment. The BBPA in the range of concentration employed (0-200 ?M) was not cytotoxic against these cell lines.

Abstract: The present invention relates to metal complexes and to electronic devices, in particular organic electroluminescent devices, containing these metal complexes.

Abstract: Provided are an organometallic compound, an organic light-emitting device including the organometallic compound, and a diagnostic composition including the organometallic compound.

Abstract: A method of preparing a self-healing composition is disclosed, the method including following steps. An isocyanate solution, a dihydric alcohol solution, and a metal salt solution are provided. The dihydric alcohol has heterocyclic structures. The isocyanate solution and the dihydric alcohol solution are mixed, causing the isocyanate and the dihydric alcohol polymerize to form a polymer precursor. The polymer precursor includes a hard segment and a soft segment. The hard segment includes urethane groups, the soft segment includes heterocyclic structures. The polymer precursor and the metal salt solution are mixed, causing the heterocyclic structures and metal ions to undergo a chelation reaction to form a coordination complex, thereby forming the self-healing composition. A self-healing composition prepared by the method, and self-healing film using the self-healing composition are also disclosed.

Abstract: Disclosed are aminocoumarin compounds, pharmaceutical compositions containing aminocoumarin compounds, and methods of their use, e.g., in the treatment of a Gram-negative bacterial infection.

Abstract: The present invention pertains to peptides and peptide-containing complexes/nanoparticles that are useful for stabilizing and delivering cargo molecules such as nucleic acids.

Abstract: Cell penetrating peptides that target many cells types including cells of the retina and cornea with high efficiency are provided herein. These peptides can be used to deliver cargo molecules across a plasma membrane, without the need for chemical conjugation. Compositions and viral vectors comprising these cell-penetrating peptides are also provided. Methods of using the peptides, compositions and viruses to deliver various agents to target cells and tissues are also provided.

Abstract: There is described herein, multimers comprising a plurality of compounds covalently linked together, the compounds independently being of formula (I).

Abstract: A method of macrocyclization of peptidomimetics is described which comprises substitution of one or more of the backbone amide C?O bonds with a turn-inducing motif. The method is general with enhancements seen across a range of ring sizes (e.g. tri-, tetra-, penta- and hexapeptides). Specifically, a peptidomimetic macrocycle is described comprising a carbonyl bioisosteric turn-inducing element having the structure: wherein X is a heteroatom; and wherein R1 to R6 are each independently selected from alkyl, aryl, heteroaryl and H.

Abstract: Described herein are novel divalent nucleobases that each bind two nucleic acid strands, matched or mismatched when incorporated into a nucleic acid or nucleic acid analog backbone (a genetic recognition reagent, or genetic recognition reagent). In one embodiment, the genetic recognition reagent is a peptide nucleic acid (PNA) or gamma PNA (?PNA) oligomer. Uses of the divalent nucleobases and monomers and genetic recognition reagents containing the divalent nucleobases also are provided.

Abstract: Engineered, non-naturally occurring antimicrobial NCR13 variant peptides (NVPs), or agriculturally acceptable salts thereof, are described, along with methods of making and using the same. The present disclosure is also related to and describes novel antimicrobial compositions, formulations, and methods of using the same, that are useful for the control of pathogenic microbes.

Abstract: The present disclosure encompasses compositions and methods for targeted cytokine delivery. The compositions disclosed herein comprise a cytokine linked to a ligand and may improve immunotherapy by limiting side effects associated with immunotherapy.