Abstract: Thrombin-inhibiting acylated pyrazole-pyridone compounds of formula (II) are disclosed herein, as well as pharmaceutical compositions, including tablets, that contain acylated pyrazole-pyridone compounds. These compounds are useful for the treatment and prevention of thrombin-related related diseases and disorders. Processes for making tablets containing acylated pyrazole-pyridones are also included.

Abstract: This disclosure is drawn to pyridine derivatives, compositions thereof, and associated methods, useful for inhibition of SARM1 activity and/or for treating or preventing neurological disorders.

Abstract: Anti-tubercular compounds include trisubstituted indolizines having the following structural formula: wherein R1 is selected from the group consisting of 4-OCH3, 4-Cl, 4-Br, 4-F, 2-NO2, 3,5-CF3, CN, CH3, R2 is COOCH3, COOC2H5, and R3 is H and COOCH3.

Abstract: Compound I of the formula (I) and/or pharmaceutically acceptable salt(s) of Compound I comprised in a pharmaceutical composition and methods of using the same to treat cystic fibrosis.

Abstract: Disclosed are crystalline free base ansolvate forms of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the free base Form I, Form II and Material N. Also disclosed are crystalline free base solvates of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1).

Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

Abstract: The present invention presents 2-(acylamino)imidazoles with therapeutic activity, including selective activity against cancer cells, and compositions comprising them. Methods of using and preparing the 2-(acylamino)imidazoles are also presented.

Abstract: The present invention is directed to agricultural compositions containing clothianidin, at least one dispersant selected from the group consisting of sodium alkyl naphthalene sulfonate condensate, alkyl polyglycoside and a mixture thereof, an inorganic compound selected from the group consisting of attapulgite, magnesium aluminum silicate, silicon dioxide and aluminum oxide and glycerol. The present invention is further directed to compositions containing clothianidin, at least one dispersant selected from the group consisting of sodium alkyl naphthalene sulfonate condensate, alkyl polyglycoside and a mixture thereof, an inorganic compound selected from the group consisting of attapulgite, magnesium aluminum silicate, silicon dioxide and aluminum oxide, glycerol and at least one liquid fertilizer.

Abstract: The present invention relates to a method of increasing cell proliferation in a population of pancreatic beta cells and a method of treating a subject for a condition associated with an insufficient level of insulin secretion. Also disclosed is a composition. The composition includes a dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1 A) inhibitor and a transforming growth factor beta (TGFP) superfamily signaling pathway inhibitor.

Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

Abstract: The present invention relates to a feed supplement or a food supplement which comprises a resin acid based composition comprising over 10% (w/w) resin acids for use in in the prevention of intestinal disorders. The invention further relates to a use of the feed supplement or the food supplement and a feed composition or a food composition comprising the feed supplement or the food supplement, respectively.

Abstract: Provided is a CCR2/CCR5 receptor antagonist and the use thereof in the preparation of a drug for treating diseases associated with the CCR2/CCR5. In particular, disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof.

Abstract: Compositions and methods related to the amelioration of pancreatitis through the pharmaceutical manipulation of calcium signaling are disclosed. Such compositions and methods may be used to ameliorate symptoms of acute or chronic pancreatitis or to reduce the chance or severity of pancreatitis in an individual at risk of the condition. In other embodiments, disclosed herein are compositions and methods related to the amelioration of viral diseases through the pharmaceutical manipulation of calcium signaling. In further embodiments, disclosed herein are compositions and methods related to the amelioration of Th17-induced diseases through the pharmaceutical manipulation of calcium signaling.

Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.

Abstract: Compositions and methods related to the amelioration of pancreatitis through the pharmaceutical manipulation of calcium signaling are disclosed. Such compositions and methods may be used to ameliorate symptoms of acute or chronic pancreatitis or to reduce the chance or severity of pancreatitis in an individual at risk of the condition. In other embodiments, disclosed herein are compositions and methods related to the amelioration of viral diseases through the pharmaceutical manipulation of calcium signaling. In further embodiments, disclosed herein are compositions and methods related to the amelioration of Th17-induced diseases through the pharmaceutical manipulation of calcium signaling.

Abstract: The present invention relates to a process for the preparation of apalutamide. In particular, the present invention relates to a process for the preparation of apalutamide and its intermediates. The present invention also relates to pharmaceutical compositions comprising apalutamide.

Abstract: In one aspect, a method of treating a disorder associated with chronic inflammation includes administering to an individual in need thereof a therapeutically effective amount of isomyosmine or a pharmaceutically acceptable salt thereof. In some aspects, the disorder is a cancer, an autoimmune disorder, hypertension, or autism. In other aspects, isomyosmine is administered to treat viral infections or disorders associated with elevated levels of hydrogen peroxide and/or other Reactive Oxygen Species (ROS).

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.

Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.

Abstract: A formulation is provided comprising a) at least one agriculturally active ingredient; b) at least one amide of formula (I) wherein R1 is selected from the group consisting of a non-aromatic hydrocarbyl group having from 1 to 16 carbon atom and benzyl; R2 is selected from the group consisting of a hydrocarbyl group having from 1 to 4 carbon atoms and benzyl; and R3 is selected from the group consisting of hydrogen and a hydrocarbyl group having from 1 to 16 carbon atoms and c) at least one acyl morpholine according to the formula (II), wherein R is H, CH3 or C2H5. A method for treating a plant or seed with such formulation is also provided.

Abstract: A method of treating the skin or hair on a dog containing an effective amount of an ectoparasiticide previously applied to the skin or hair, comprising applying a quantity of a cleansing composition directly to the skin or hair, wherein the treatment does not result in reducing the efficacy of the ectoparasiticide against adult fleas (C. felis) or adult ticks (R. sanguineus) below 90% efficacy for at least a month after application of the ectoparasiticide; wherein the cleansing composition comprises about 1-3% glycerin; about 2-4% silicone copolyol esters, water and is essentially free of surfactant.

Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.

Abstract: In one aspect, a method of treating a disorder associated with chronic inflammation includes administering to an individual in need thereof a therapeutically effective amount of isomyosmine or a pharmaceutically acceptable salt thereof. In some aspects, the disorder is a cancer, an autoimmune disorder, hypertension, or autism. In other aspects, isomyosmine is administered to treat viral infections or disorders associated with elevated levels of hydrogen peroxide and/or other Reactive Oxygen Species (ROS).

Abstract: The present invention comprises compounds of Formula I and their use in the inhibition of cell proliferation in therapeutic treatments. Pharmaceutical compositions comprising at least one compound of Formula I and at least one pharmaceutical excipient are disclosed, as well as methods of using compounds of Formula I and pharmaceutical compositions thereof for treatment of hyper-proliferative diseases and other disorders.

Abstract: In the present invention there is provided an oral pharmaceutical composition, comprising bendamustine or a pharmaceutically acceptable, ester, salt or solvate thereof as an active ingredient, and a pharmaceutically acceptable excipient, which is a pharmaceutically acceptable non-ionic surfactant, selected from the group consisting of polyethoxylated castor oil or derivative thereof and a block copolymer of ethylene oxide and propylene oxide.

Abstract: Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts and/V-oxides thereof, wherein X1, X2, Z1, Z2, the ring system denoted by “a”, R1, A1A, L1B, A1B, L1A, L2, Q, L3, R3, A4A, L4B, A4B, L4A, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein disrupt the eIF4E/eiF4G interaction, and can be used to treat hyperproliferative disorder, a neurological disease or disorder, or autism.

Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.

Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.

Abstract: The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.

Abstract: Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy-induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain).

Abstract: The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices, and to electronic devices containing one or more compounds of the formula (I). The invention furthermore relates to preparation processes for compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I).

Abstract: Graphene, a composition for preparing graphene, and a method of preparing graphene using the composition are disclosed.

Abstract: The present disclosure relates to a method of preventing and/or treating liver disease comprising administering an ASK1 inhibitor in combination with a FXR agonist, to a patient in need thereof.

Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.

Abstract: Methods of treating a subject having or at risk of developing a neurodegenerative disease or condition associated with demyelination, insufficient myelination, or underdevelopment of myelin sheath are described. The methods include administration of a therapeutically effective amount of sobetirome, or a pharmaceutically acceptable salt thereof.

Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 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: Soybean plants comprising event SYHT0H2, methods of detecting and using the same, and soybean plants comprising a heterologous insert at the same site as SYHT0H2.

Abstract: There are provided compounds of formulas III and VIIa: or a salt or protected derivative thereof, wherein Z2 represents a structural fragment of formula V, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity, for example through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Abstract: Disclosed are substituted aromatic N-heterocyclic compounds. The disclosed compounds typically exhibit kinase inhibition activity, for example, and inhibit Mnk1 kinase and/or Mnk2 kinase. The disclosed compounds may be used in pharmaceutical compositions and methods for treating diseases or disorders associated with Mnk1 kinase activity and/or Mnk2 kinase activity, such as cancers, diabetes, autism, and fragile X syndrome.

Abstract: The present invention relates to compounds of formula I wherein R1? is CH3; R1 is methyl, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1? and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tertbutyl, cyclopropyl, hydroxmethyl, or 2-propyl-2-ol; R3 is Cl, F, CF3, methyl, methoxy, isopropyl, cyano or cyclopropyl; R4 is hydrogen, methyl, F or Cl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

Abstract: A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: Z is selected from O, S and N; Y is N X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof.

Abstract: Provided herein are methods for predicting the clinical sensitivity of an inflammatory disease (e.g., ankylosing spondylitis) and a subject's response to treatment with apremilast using the level of a biomarker (e.g., MCP1). Also provided herein are methods for treating an inflammatory disease.

Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoismers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.

Abstract: Phenyl triazole derivative (specifically, 1-[6-[[5-(2-fluorophenyl)-3-methyl-triazol-4-yl]methoxy]-3-pyridyl]imidazole-4-carbonitrile or a pharmaceutically acceptable salt thereof), pharmaceutical compositions containing this compound, and methods of treatment therewith. The compound is in particular considered useful for the treatment of central nervous system diseases and disorders which are responsive to modulation of GABAA receptors containing the ?5 subunit.

Abstract: The present invention relates to methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells. Specifically, the invention relates to methods of using compounds comprising a N-(1H-pyrazol-4-yl)-nicotinamide moiety having a Formula I: and pharmaceutically acceptable salts thereof.

Abstract: Provided is an amorphous solid dispersion including a taxane or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable polymer, and a pharmaceutically acceptable surfactant, which has enhanced solubility. Also provided is a method for preparing the solid dispersion. The present subject matter also provides a tablet having good solubility, bioavailability and stability, which comprises the amorphous solid dispersion, an intragranular excipient, and an extragranular excipient.

Abstract: Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.

Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.

Abstract: The present invention relates to novel anthranilamide derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q, Y and n are each as defined in the description—, to the use thereof as insecticides and acaricides for control of animal pests, and to several processes for preparation thereof.