Abstract: Disclosed herein a convenient process for preparation of insecticidal anthranilamide compounds and intermediate thereof.

Abstract: Small molecules acting through the ligand binding domain of nuclear receptor TLX (NR2E1) are disclosed, as well as the use thereof for promoting neurogenesis and treating disorders associated with nuclear receptor TLX, including neurological disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula II as described herein, and pharmaceutically acceptable salts or isomers thereof.

Abstract: Provided herein are inhibitors of MET receptor tyrosine kinase, pharmaceutical compositions comprising said inhibitory compounds, and methods for using said MET kinase inhibitory compounds for the treatment of disease.

Abstract: The present invention relates to novel pyridazin-3-yl phenol compounds of formula (I): wherein R1, R2, R3, R4 and R5 are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

Abstract: The present invention relates to specific salts of (1S,5R)-(1?,5?,6?)-N-[1,1-dimethyl-2-[(3-methyl-2-pyridyl)oxy]ethyl]-3-azabicyclo[3.1.0]hexane-6-carboxamide, to pharmaceutical compositions comprising said salts, to methods of using said salts to treat physiological disorders, and to intermediates useful in the synthesis of the salts.

Abstract: The invention provides compounds having Formula (I): or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.

Abstract: A novel aryl ether substituted heterocyclic compound has GLP1R agonist activity. A GLP1R agonist is represented by formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, isotope substituent or isomer thereof.

Abstract: Provided herein are compounds of formula (A): or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, Ry, and Rz are as defined herein. Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (A), or a pharmaceutically acceptable salt thereof, as well as methods of using a compound of formula (A), or a pharmaceutically acceptable salt thereof, to treat various diseases and conditions mediated by nicotinamide phosphoribosyltransferase (NAMPT).

Abstract: Provided herein are compounds and compositions thereof that reduce WEE1 kinase protein levels. In some embodiments, the compounds and compositions are provided for treatment WEE1 associated diseases such as cancer.

Abstract: Provided are a compound of formula (I), a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a eutectic thereof, or a pharmaceutical composition comprising same, and use thereof as a ketohexokinase inhibitor in the preparation of drugs for treating related diseases. Each group in formula (I) is as defined in the description.

Abstract: This disclosure relates generally to inhibitors of MHC-I downmodulation, and methods of treating or preventing an HIV infection by administering the inhibitors to a patient in need of treatment thereof.

Abstract: Described herein are compounds and methods of treating a disease or disorder, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, ischemic stroke, and prion disease, comprising administering a therapeutically effective amount of a cromolyn ester.

Abstract: The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.

Abstract: The present invention provides compounds of formula (I) and/or salts thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA ?5 positive allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA ?5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

Abstract: The present invention relates to imidazo[1,2-a]pyridine and [1,2,4]triazolo[1, 5-a]pyridine derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, nonalcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).

Abstract: Disclosed herein are compounds that selectively bind an expanded transcribed repeat r(G4C2)exp, prevent sequestration of RNA-binding proteins, and inhibit translation of repeat associated non-ATG (RAN) translation responsible for generation of toxic dipeptide repeats underlying diseases such as amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). The compounds and their pharmaceutical compositions are useful in treating a disease or condition characterized by an expanded G4C2 repeat RNA (r(G4C2)exp), such as ALS and FTD.

Abstract: Compounds useful as linker-payload compounds are disclosed. The compounds have the following Structure (I): as a stereoisomer, enantiomer or tautomer thereof or a mixture thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X1, X2, X3, X4, X5, R4a, and R4b are as defined herein. Additional compounds, conjugates, methods of preparation, pharmaceutical compositions, and methods of treatment related to conjugates of compounds of Structure (I) and a targeting moiety, or binding fragment thereof, are also provided.

Abstract: The application relates to a compound of Formula (I): which modulates the activity of TRIM33, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which TRIM33 plays a role.

Abstract: The present invention relates to compositions and methods for the treatment of BAF-related disorders, such as cancers and viral infections.

Abstract: The present invention relates to new pyrrolopyridine compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK1 and JAK3 kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis.

Abstract: The present invention relates to polymorphs of the hydrochloride salt of 5-{2-[({8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridine-6-yl}carbonyl)-amino]ethoxy}-5-oxopentanoic acid (linaprazan glurate), more specifically Form 1 and Form 2 of the HCl salt of linaprazan glurate. The invention also relates to a process for the preparation of such polymorphs, to pharmaceutical compositions comprising such polymorphs, and to the use of these polymorphs in the treatment or prevention of gastrointestinal inflammatory diseases or gastric acid related diseases, in particular erosive gastroesophageal reflux disease (eGERD).

Abstract: The present invention relates to a heterocyclic compound, represented by chemical formula 1, exhibiting a diacylglycerol kinase inhibitor activity, a pharmaceutical composition comprising same as an active ingredient, and a use thereof.

Abstract: Provided herein are compounds of Formula (I): and forms thereof, including compositions thereof and uses therewith for treating spinal muscular atrophy.

Abstract: The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

Abstract: The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging.

Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonizes or partially agonizes) NLRP3 that are useful, e.g., for treating a condition, disease or disorder in which an increase in NLRP3 signaling may correct a deficiency in innate immune activity (e.g., a condition, disease or disorder associated with an insufficient immune response) that contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.

Abstract: The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.

Abstract: Disclosed are prodrugs of myeloperoxidase (MPO) inhibitors, methods of treating MPO related disorders, e.g., multiple system atrophy, amyotrophic lateral sclerosis, and Huntington's disease, and methods of neuroprotection, which include administering to a patient in need thereof the prodrugs, pharmaceutical compositions including the prodrugs, and kits including the pharmaceutical compositions and instructions for use.

Abstract: The invention provides novel methods for preparing indolinobenzodiazepine monomer compounds and their synthetic precursors.

Abstract: Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.

Abstract: This invention relates to compounds of formula (I) and salts, solvates, tautomers, N-oxides, stereoisomers, polymorphs and/or prodrugs thereof. Also disclosed is the use of the compounds of formula (I) to modulate the activity of oxytocin at the oxytocin receptor.

Abstract: The present invention relates to novel compounds that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

Abstract: The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R7, and R8 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compound, and methods of using the Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.

Abstract: The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): wherein R is as described herein.

Abstract: The present invention relates to: a novel method for preparing a heterocyclic derivative compound of chemical formula I below; a novel intermediate compound used in the preparation method; a composition for treatment or prevention of hyperuricacidemia, gout, nephritis, chronic renal insufficiency, nephrolith, uremia, urolithiasis, or a uric acid-related disease, the composition containing the compound of chemical formula I at a dose of more than 2 mg and equal to or less than 10 mg and being orally administered once a day; and a hydrochloride 1.5 hydrate of the novel compound of chemical formula I.

Abstract: The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

Abstract: Described herein are PHD inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of anemia.

Abstract: The present disclosure provides KRAS inhibitors. Methods of treating cancers using the compounds are also provided.

Abstract: An yttrium compound, a method of manufacturing an integrated circuit device, and a raw material for forming an yttrium-containing film, the yttrium compound being represented by the following General formula (1):

Abstract: A novel organic compound that is highly convenient, useful, or reliable is to be provided. The organic compound is represented by General Formula (G0). In General Formula (G0), X and Y each independently represent an oxygen atom or a sulfur atom. Ar1 to Ar4 each independently represent an aromatic ring or a nitrogen-containing heteroaromatic ring, the aromatic ring contains 6 to 10 carbon atoms, and the nitrogen-containing heteroaromatic ring is composed only of one or more six-membered rings and contains 4 to 9 carbon atoms. R, R11, R21, R21, R22, R31, R32, R41, and R42 each independently represent hydrogen, a straight-chain alkyl group having 1 to 6 carbon atoms, a branched alkyl group having 3 to 7 carbon atoms, a substituted or unsubstituted aryl group having 6 to 13 carbon atoms, substituted or unsubstituted diarylamine having 6 to 13 carbon atoms, or substituted or unsubstituted heteroarylamine having 3 to 18 carbon atoms.

Abstract: Disclosed are compounds, compositions, and methods useful for boron neutron capture therapy.

Abstract: Provided are a novel boron-containing compound and an electrolyte solution additive for a secondary battery including the same. The electrolyte solution for a secondary battery provided in one embodiment includes the novel boron-containing compound, thereby suppressing the decomposition of an electrolyte solution to improve the capacity and the life characteristics of a battery.

Abstract: The present disclosure provides an organic compound, a mixture, a composition, and an organic electronic device.

Abstract: The present invention relates to a heteroaryl derivative compound and a use thereof. Since the heteroaryl derivative of the present invention exhibits excellent inhibitory activity against EGFR, the heteroaryl derivative can be usefully used as a therapeutic agent for EGFR-associated diseases.

Abstract: An organometallic compound represented by Formula 1: M1(L1)n1(L2)n2??Formula 1 wherein M1 is a transition metal, L1 is a ligand represented by Formula 1A, L2 is a ligand represented by Formula 1B, and n1 and n2 are each independently 1 or 2, wherein X1 to X4 are each independently C or N, Y1 is O, S, Se, C(R5)(R6), N(R7), or Si(R8)(R9), ring CY2 and ring CY4 are each independently a C5-C30 carbocyclic group or a C1-C30 heterocyclic group, ring CY3 is a 6-membered heterocyclic group, a 6-membered heterocyclic group condensed with a C5-C30 carbocyclic group, or a 6-membered heterocyclic group condensed with a C1-C30 heterocyclic group, Z1 comprises at least one deuterium, and the other variables are as provided herein.

Abstract: The disclosure provides a process for preparing bis(monoalkyl-substituted cyclopentadiene) tungsten hydride compounds, for example bis(isopropylcyclo-pentadienyl) tungsten dihydride, via the corresponding magnesium compound and tungsten hexachloride, followed by treatment with a hydride reagent. Also provided is a process for preparing bis(monoalkyl-substituted cyclopentadiene) metal halide compounds. This latter aspect is achieved by reaction of the corresponding magnesium compound with a metal halide. Exemplary metals in this process include hafnium, zirconium, titanium, tantalum, niobium, tungsten, and molybdenum.

Abstract: Disclosed in the present disclosure is a purification method for sucralose-6-ethyl ester, and the method comprises: a secondary water boiling step: taking a sucralose-6-ethyl ester mother liquor, which has been subjected to boiling with water and a negative pressure treatment, adding a predetermined proportion of water to the sucralose-6-ethyl ester mother liquor, fully stirring and heating for boiling with water, and after stirring and boiling with water for a predetermined time, carrying out solid-liquid separation to obtain a secondary water-boiled mother liquor in which sucralose-6-ethyl ester is dissolved; a phase separating extraction step: leaving the secondary water-boiled mother liquor to stand for phase separation, taking the separated upper phase, extracting with an alkane extractant at a predetermined temperature, and removing residual white oil in the upper phase; a recrystallizing purification step: evaporating a lower-layer effluent obtained from extraction, so as to obtain a solid, and purifyi

Abstract: Provided are a flavone derivative represented by formula I and a pharmaceutically acceptable salt, hydrate or solvate thereof. (I) In formula I, R1 is selected from the group consisting of H, C1-4 alkyl, amino and C1-4 acyl; R2 is isopentenyl or 2-hydroxy-isopentyl; R3 is selected from the group consisting of H, methyl and deuterated methyl; R4 is selected from the group consisting of C1-4 alkyl, amino, C1-4 acyl, and (II), wherein R5 represents a monosaccharide residue or an oligosaccharide residue; L is selected from the group consisting of a polypeptide, C1-C20 linear alkyl or a derivative thereof, a derivative of C1-C20 linear or branched acyl, C1-C20 glycol or a derivative thereof, and (III), wherein Y is (IV), a is an integer from 0-100, b is an integer from 1-100, c is an integer from 1-10, d is an integer from 0-100, and e is an integer from 0-100. The flavone derivative according to the present invention exhibits an potent and broad-spectrum anti-cancer activity.

Abstract: A modified nucleoside or nucleotide, the 3?-OH of the modified nucleoside or nucleotide being reversibly blocked; meanwhile, the present invention also relates to a kit comprising the nucleoside or nucleotide, and a sequencing method based on the nucleoside or nucleotide.