Abstract: The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

Abstract: An organic amine salt compounds of general formula An?[Bm+]p (I) is disclosed, wherein An? is a CO2-donating anion with a valence of ?n, wherein n=1, 2 or 3; each Bm+ comprises: ammonium ion, hydrazinium ion and/or organic amine B cation; wherein m = 1 ? - ? 10 ; 0 < p ? n m ; and wherein An? is one or more selected from a group consisting of following anions: (a) carbamate orcarbazate; (b) carbonate; (c) formate; (d) bicarbonate; (e) organic monocarbonate; (f) organic poly-carbamate; (g) orthoformate; or (h) organic poly-carbonate. The compound of general formula (I) has at least one of hydroxyalkyl group linked to N atom, i.e., has alkanolamine residue. They can be used as polyurethane foaming agent, and most of them can be used as polystyrene foaming agent or polyvinyl choride foaming agent.

Abstract: A compound represented by general formula (I) (in the formula, all symbols are as described in the description) or a salt thereof has a potent nerve-protecting and/or -repairing activity, and therefore can be used as a therapeutic agent for neuropathy (e.g., chronic inflammatory demyelinating polyneuropathy, Guillain-Barre syndrome, periarteritis nodosa, allergic vasculitis, diabetic peripheral neuropathy, entrapment neuropathy, peripheral neuropathy associated with the administration of a chemotherapeutic drug, or peripheral neuropathy associated with Charcot-Marie-Tooth disease).

Abstract: Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.

Abstract: The present invention provides novel fused bicyclic alkylene linked imidodicarbonimidic diamides. In particular, described herein are N-[2-(indol-3-yl)alkylene]-linked imidodicarbonimidic diamides and N-[2-(pyrrolopyridin-3-yl)alkylene]-linked imidodicarbonimidic diamides (compound of formula (I) or formula (II)), and uses therefor. The compounds of the present invention are believed to be organic cation transporter selective compounds, useful for the treatment of diseases and conditions caused by reduced activity of 5? adenosine monophosphate-activated protein kinase (AMPK).

Abstract: The present disclosure relates to a preparation method of methyl (E)-1-acetyl-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate from methyl 2-oxoindoline-6-carboxylate using high reaction temperatures and a reaction solvent enabling azeotropic removal of acetic acid during the reaction.

Abstract: Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or in treating cancer, are provided herein. The compounds are collectively represented by Formulae Ia or Ib: wherein A, B, D, E, G and R1-R5 are as defined in the specification, with one or more of D, E and G, preferably E, is hydroxy.

Abstract: The present invention also relates to process for the preparation of N-(4-(6,7-dimethoxy quinolin-4-yloxy)phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (S)-malate compound of formula-1a and its polymorphs thereof, represented by the following structural:

Abstract: The present disclosure provides processes for the preparation of a compound of formula: which exhibits 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. The disclosure also provides compounds that are synthetic intermediates.

Abstract: Provided herein are optionally substituted benzoimidazol-1,2-yl amides, pharmaceutical compositions comprising a therapeutically effective amount of such compounds and a pharmaceutically acceptable excipient, and methods of treating Kv7 associated diseases, such as, epilepsy, amyotrophic lateral sclerosis, various types of pain, hyperexcitability, a dyskinesia, dystonia, mania and tinnitus with such compounds and pharmaceutical compositions.

Abstract: The present invention relates to compounds of formula M in which RM has the meaning indicated in claim 1, to liquid crystal mixture comprising the same, to the use of these liquid-crystal media, in particular in components for high-frequency technology, and to components of this type which contain media according to the invention, and to the production and use of these components. The components according to the invention are suitable, in particular, as phase shifters in the microwave and millimetre wave region, for microwave and millimetre wave array antennae and very particularly for so-called tunable “reflectarrays”.

Abstract: Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Abstract: Disclosed herein is a two-piece sensor assembly that includes an attachment collar configured to attach to a body surface of a patient and comprising at least one opening, and a skin sensor configured to seat into the at least one opening in the attachment collar. The skin sensor includes at least one radiation source configured to irradiate the body surface with at least one interrogation light, and at least one detector configured to detect at least one response light incident from the direction of the body surface.

Abstract: The present invention relates to novel lipophilic macrocyclic ligands, the complexes thereof, in particular radioactive complexes, and the uses of same in medical imaging and/or in therapy, in particular in interventional radiology.

Abstract: To provide a method that can efficiently produce 2,5-bis(aminomethyl)tetrahydrofuran. The method for producing 2,5-bis(aminomethyl)tetrahydrofuran, the method including subjecting 2,5-bis(aminomethyl)furan to a reaction with hydrogen source by using a hydrogenation catalyst to obtain 2,5-bis(aminomethyl)tetrahydrofuran.

Abstract: The invention relates to a process for synthesizing 5-hydroxymethylfurfural from a fructose-containing feedstock in the presence of at least one aprotic polar solvent and at least one dehydration catalyst, in which process the maximum instantaneous fructose concentration 5.0 wt %.

Abstract: A method for manufacturing an insecticidal compound and insecticidal compositions comprising the insecticidal compound and methods of use are presented herein. The manufacturing method presented herein allows for a high purity grade of thiocyclam hydrochloride to be synthesized. The insecticidal compositions comprising the thiocyclam hydrochloride can be used for prevention of crop destruction by insects. The use of thiocyclam hydrochloride in insecticidal compositions as described herein can achieve greater efficacy than previously known insecticides, by eliminating the insect pests more reliably and efficiently.

Abstract: The invention relates to an aromatic compound, pharmaceutical composition comprising the same, and a method for preparing the compound and an intermediate thereof. The invention also relates to use of the compound for the manufacture of a medicament for the prevention or treatment of a PPAR-related disease.

Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.

Abstract: A squarylium compound has high transmittance in a visible wavelength spectrum of light and is configured to selectively absorb light in an infrared/near infrared wavelength spectrum of light.

Abstract: The invention relates to a compound according to general formula (I), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament.

Abstract: The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Abstract: The present invention relates to a fluorene derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the same as an effective ingredient for preventing or treating HCV-related disease. A fluorene derivative according to the present invention is identified to exhibit an antiviral performance against not only HCV, but also highly against HCV mutants, particularly double mutants and thus can be used in a pharmaceutical composition for prevention or treatment of HCV-caused liver disease, such as acute hepatitis C, chronic hepatitis C, liver cirrhosis, hepatocellular cancer, etc., particularly, liver disease caused by mutants of HCV. The derivative can be useful in a pharmaceutical composition for prevention or treatment of HCV-related liver disease by which the problem of resistant mutation against conventional therapeutic agents is solved.

Abstract: The present invention relates to a novel amine-based compound represented by Chemical Formula 1 and an organic light emitting device including the same. The compound provides improved efficiency, low driving voltage, and improved lifetime characteristic of the organic light emitting device.

Abstract: The present invention relates to compounds which are of use in the field of agriculture as herbicides. The compounds in question are of formula II and comprise a spirofused tricycle core: wherein R4 and R5 together with the carbon atom to which they are attached form a cyclic group.

Abstract: The present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.

Abstract: Compounds having the general structure A-L-B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.

Abstract: The present invention provides compounds of Formula (Ia) or (Ib):Formula (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Abstract: Methods of detecting a non-explosive analyte can include exposing a sensor compound to a non-explosive analyte and displaying a change in the sensor compound upon exposure of the sensor compound to the non-explosive analyte. A variety of sensor compounds for detecting a target analyte, including both explosive and non-explosive analytes, is also described. Sensor devices for detecting a target analyte can include a substrate and a sensor compound positioned on the substrate in a plurality of detection zones.

Abstract: Provided is a crystal of a novel pyrido[3, 4-d]pyrimidine derivative having excellent CDK 4/6 inhibitory activity. A crystal of a compound represented by formula (I). In the formula, R1 represents a hydrogen atom or a C1-3 alkyl group; R2 represents a hydrogen atom or an oxo group; L represents a single bond or a C1-3 alkylene group; and X represents CH or N.

Abstract: Compounds of formula (I), wherein A, R, W, Q, n, and m have the meaning according to the claims, can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R5, A and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: Compounds of the formula Ia or of the formula Ib in which X, Y, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.

Abstract: Compounds having the chemical formula 1, a method for producing the compounds of chemical formula 1, a pharmaceutical composition comprising same, and use thereof as a GPR120 agonist for prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.

Abstract: Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may allow for selective detection of Hsp90 in a sample.

Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. For example, such compounds include those having the structure: or pharmaceutically acceptable salts thereof. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel, including Dravet syndrome or epilepsy, using such compounds are also provided herein.

Abstract: 2-primary amino-4-secondary amino-quinoline derivatives, their manufacture, pharmaceutical compositions comprising them and their use as medicaments are disclosed. The compounds are useful as a medicament in treating and/or decreasing the severity and/or progression and/or preventing fibrosis and/or related diseases, or for use as a medicament in treating, decreasing the severity and/or progression of and/or preventing autophagy and/or related diseases, for inhibiting autophagy flux, and for inhibiting cathepsins B (CTSB), L (CTSL) and/or D (CTSD) and/or related diseases.

Abstract: A dihydropyrimidine compound and use as a medicament, especially application as a medicament used for treating and preventing hepatitis B, specifically, is a compound having Formula (I) or (Ia), or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein the variables of the formulas are as defined in the specification; and also includes the use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicament, especially use as a medicament for treating and preventing hepatitis B.

Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

Abstract: Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.

Abstract: This invention provides an unexpectedly stable, highly crystalline form of the di-HCl salt of for advantageous therapeutic pharmaceutical efficacy and dosage form stability.

Abstract: Provided is a method for producing a diol represented by Formula (1), the method including using water as a solvent to carry out a cyclodehydration reaction of a 1,4-cyclohexanedione derivative represented by Formula (2) with a triol represented by Formula (3) to produce a diol represented by Formula (1). In Formula (1), R1 and R2 each independently denote a hydrocarbon group, and R3 each independently denotes a hydrogen atom, a heteroatom-containing group, a halogen atom-containing group, a linear alkyl group having from 1 to 6 carbon atoms, a branched alkyl group having from 3 to 6 carbon atoms, or a group including an aryl group and having from 6 to 12 carbon atoms.

Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: A salt serving as an Akt inhibitor and a crystal thereof, specifically related to a salt of the compound of formula (I) and a crystal thereof.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The present invention provides a process for preparing a compound of the formula (II): wherein R2 is unsubstituted alkyl, characterized by reacting a compound of the formula (I): wherein R1 is hydrogen or a protecting group other than unsubstituted alkyl, with a compound of the formula: R2—OH, wherein R2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.

Abstract: The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.

Abstract: Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

Abstract: Selective reduction methods for halogenated carbosilanes and carbodisilanes are disclosed. More particularly, high yields of the desired carbosilanes and carbodisilanes are obtained by reduction of their halogenated counterparts using a reducing agent and tetrabutylphosphonium chloride (TBPC) as a catalyst.