Abstract: The present disclosure is concerned with N-(5-chloro-4-((4-chlorophenyl)(cyano)methyl)-2-methylphenyl)benzamide compounds that are capable of inhibiting SPAK kinase function, methods of treating hypoxic brain injuries due to, for example, ischemic stroke. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Propargyl-functionalized macrocyclic compounds can include non-aggregating compounds having at least one phthalocyanine (Pc), azaphthalocyanine (AzaPc), or naphthalocyanine (Nc) unit. The compounds can be metal-free or metal-complexed. The metal-complexed compounds can include zinc (II), for example. The compounds can include multiple propargyl moieties at different sites, e.g., peripheral or non-peripheral sites, as described herein. Exemplary compounds include an azaphthalocyanine complex (AzaPc1) and phthalocyanine complexes (Pc2-Pc5). The compounds may provide efficient solubility in aqueous and/or organic solvents, optimal physicochemical properties, improved photo-sensitizability, significant tumor specificity, and electron transfer tunability. The compounds can provide suitable non-aggregated molecular scaffolds for construction of numerous macrocycle derivatives via different organic transformation methodologies, e.g., Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC).

Abstract: Provided is a method capable of preparing high-purity aliphatic isocyanate, particularly, xylylene isocyanate in a high yield in a simple manner without an additional separate process, wherein when aliphatic isocyanate is prepared using phosgene, a side-reaction inhibitor capable of inhibiting side-reactions is introduced during phosgenation.

Abstract: The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of misfolded proteins.

Abstract: A radiation-sensitive resin composition includes a first polymer including a first structural unit that includes a first acid-labile group; a radiation-sensitive acid generator; and a compound represented by formula (1). n is 1 or 2. R1 represents a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms in a case in which n is 1. R1 represents a divalent organic group having 1 to 20 carbon atoms in a case in which n is 2. R2 represents a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms. E represents a group represented by formula (i). R2 and E may taken together represent a ring structure having 3 to 20 ring atoms together with the nitrogen atom. X represents a divalent organic group having 1 to 20 carbon atoms. R3 represents a second acid-labile group.

Abstract: A novel onium salt having formula (1) and a resist composition comprising the same as a quencher are provided. When the resist composition is processed by photolithography using high-energy radiation, there is formed a resist pattern which is improved in LWR and CDU. In formula (1), R1, R2 and R3 each are a C1-C20 monovalent hydrocarbon group which may contain a heteroatom exclusive of fluorine, and Z+ is a sulfonium, iodonium or ammonium cation.

Abstract: A method for preparing an enone compound of formula (I) is disclosed. Furthermore, the enone compound of formula (I) obtained by the method may be used alone, or in combination with a washing agent, a cleaning agent, an insect repellant agent, a pharmaceutical agent, a fragrance, a pro-fragrance, or combinations thereof.

Abstract: The present invention discloses a method for preparing 2,3-dichloro-5-trifluoromethylpyridine, comprising at a temperature of 100˜150° C. and a pressure of 0.5˜5.0 MP, in presence of at least one catalyst selected from supported metal chloride, supported zeolite molecular sieve and supported heteropolyacid, 2-chloro-5-trifluoromethylpyridine reacts with chlorine gas to obtain 2,3-dichloro-5-trifluoromethylpyridine. The preparing method provided by the present invention has advantages such as high selectivity of desired product, high utilization rate of chlorine gas, moderate process condition, simple operation and less three wastes. The present invention also discloses a preparing method for preparing 2-chloro-5-trifluoromethylpyridine, which is capable of reducing unit consumption, reducing separation cost, and improving safety compared to the prior art.

Abstract: The present invention relates to quinoline derived small molecule inhibitors of nicotinamide N-methyltransferase (NNMT), the preparation thereof and uses thereof. Formula (I).

Abstract: The present invention relates to a compound shown in formula (II) or a pharmaceutically acceptable salt thereof and an application of the same in preparing a drug for treating a disease related to angiotensin II receptor type 2 (AT2R).

Abstract: The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt:

Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

Abstract: The present invention concerns a process for the preparation of firocoxib, i.e. 3-(cyclopropylmethoxy)-5,5-dimethyl-4-(4-methylsulfonylphenyl)-furan-2-one, comprising steps (a)-(g), wherein the process provides for step (d) of the reaction of a new intermediate, i.e. 2-methyl-1-[4-(methylsulfanyl)phenyl]-1-oxopropan-2-yl (acetyloxy)acetate (compound VII) in the same organic solvent of step (a) in the presence of a catalyst and a phase transfer catalyst solution in the same organic solvent with hydrogen peroxide.

Abstract: A process is provided for making esters of FDCA, in which an aqueous feed comprising glucaric acid is first reacted with a high boiling first alcohol in the presence of an acid catalyst and with removing water during the reaction, to form a first product mixture comprising a first ester of FDCA and the high boiling first alcohol, then unreacted high boiling first alcohol is removed from the first product mixture. The first ester of FDCA and the high boiling first alcohol is then transesterified with a lower boiling second alcohol selected from the group consisting of methanol, ethanol, isopropanol and n-propanol, to form a second product mixture comprising a second ester of FDCA with the lower boiling second alcohol, and the second ester of FDCA with the lower boiling second alcohol is recovered.

Abstract: Provided are compounds that generate a peroxide when they react with ozone in the presence of water. Additionally, alkyne compounds reactive with a free radical, a reactive oxygen species (ROS) or another reactive species are provided. Also provided are enol ether, enamine, and vinal thioester compounds reactive with a free radical, a strong acid, a reactive oxygen species (ROS) or another reactive species. Additionally provided are compounds reactive with a free radical, an ROS or another reactive species. The compounds comprise a conjugated moiety operably joined to an alkene moiety and a resonance-transmitting moiety, wherein the resonance-transmitting moiety transmits an electron through the conjugated moiety to the alkene moiety, which reacts with the free radical, an ROS or another reactive species. Also provided are methods of decomposing a free radical, an ROS or another reactive species. The methods comprise contacting the free radical or ROS with any of the above compounds.

Abstract: The present invention relates to nebivolol synthesis method and intermediate compound thereof. Specifically, the present invention relates to a method for synthesizing nebivolol, intermediate compound thereof, and a method for preparing the intermediate compound.

Abstract: The present invention includes a method for obtaining a higher purity cannabinoid solvent extract from a plant which comprises cannabinoids and/or terpenes. A solvent extraction is performed on the optionally dried plant material, followed by a step of removing high molecular weight impurities by a cooling step. Following the cooling step, the precipitate is removed and a higher quality filtrate is obtained which contains higher levels of purity of cannabinoids and/or terpenes than the starting solvent extract. The methods of the invention also include a method for obtaining crystallized THCa, which comprises obtaining a filtrate by the methods disclosed herein, or obtaining a solvent extract, and allowing crystallization of the THCa to occur. The filtrate, crystallized THCa, and residual filtrate remaining after crystallization of THCa can be used as starting materials for products that include cannabinoids and/or terpenes.

Abstract: A medicinal agent for the prevention and/or treatment of diseases caused by EP4 receptor activation is disclosed. A compound having antagonistic activity against the EP4 receptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EP4 receptor for the prevention and/or treatment of diseases caused by EP4 receptor activation.

Abstract: A highly efficient, Z-selective ring-closing metathesis system for the formation of macrocycles using a stereoretentive, ruthenium-based catalyst supported by a dithiolate ligand is reported. This catalyst is demonstrated to be remarkably active as observed in initiation experiments showing complete catalyst initiation at ?20° C. within 10 min. Using easily accessible diene starting materials bearing a Z-olefin moiety, macrocyclization reactions generated products with significantly higher Z-selectivity in appreciably shorter reaction times, in higher yield, and with much lower catalyst loadings than in previously reported systems. Macrocyclic lactones ranging in size from twelve-membered to seventeen-membered rings are synthesized in moderate to high yields (68-79% yield) with excellent Z-selectivity (95%-99% Z).

Abstract: The present invention generally relates to electrochromic compounds and the uses thereof, particularly to series of fluoroalkyl 3,4-dioxythiophene compounds and their electrochromic polymers or co-polymers. Both compositions and process for manufacturing thereof are in the scope of this invention.

Abstract: The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.

Abstract: Described are imino-azacycle-benzamide compounds compounds that inhibit WDR5 and associated protein-protein interactions, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.

Abstract: The present invention relates compounds of Formula (A) as H3R antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of Histamine 3 Receptor (H3R) functions. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to H3R functions in humans.

Abstract: Provided herein are amino isoquinolinyl amide and sulfonamide compounds that affect the function of kinases and other proteins in a cell and that are useful as therapeutic agents. In particular, these compounds are useful in the treatment of eye diseases such as glaucoma and retinal diseases, as anti-inflammatory agents, for the treatment of cardiovascular diseases, and for diseases characterized by abnormal growth, such as cancers.

Abstract: The present disclosure relates to an improved process for the preparation of a sulfonamide structured kinase inhibitor, namely N-(2?,4?-difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1?-biphenyl]-3-yl)cyclopropanesulfonamide (1A) and pharmaceutically acceptable salts thereof. Compound of formula (1A) is a selective inhibitor of FGFR/VEGFR kinase families and is useful in the treatment of cancer.

Abstract: The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula A: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula A, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.

Abstract: The invention provides compounds of formula (I), stereoisomers and pharmaceutically acceptable salts thereof: (I) wherein A1 to A4, R1 and RP are as defined herein. Such compounds are suitable for use in the treatment or prevention of diseases or conditions which are mediated by the activation of lactate dehydrogenase A (LDHA), for example cancer.

Abstract: Compounds, and compositions, methods, and uses thereof, are described herein for treating neurodegenerative diseases and disorders. In particular, vasopressin receptor modulators, and compositions, methods and uses thereof, are described herein for treating neuropsychiatric aspects of neurodegenerative diseases such as Huntington's Disease, Parkinson's Disease, and Alzheimer's Disease.

Abstract: New compounds of formula I are described: The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.

Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.

Abstract: The present invention relates to a polymorphic form of masitinib mesylate, processes for its preparation, pharmaceutical compositions comprising it and their medical use.

Abstract: The present application provides bifunctional compounds of Formula (I): which act as protein degradation inducing moieties for EGFR and/or a mutant thereof. The present application also describes methods for the targeted degradation of EGFR and/or a mutant thereof through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to EGFR and/or a mutant thereof which can be utilized in the treatment of disorders modulated by EGFR or a mutant thereof.

Abstract: The present invention provides compounds which are selective allosteric inhibitors of TMLR, TMLRCS, LR, LACS containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

Abstract: The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.

Abstract: Disclosed are compounds according to Formula (I), and related pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I).

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising to substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.

Abstract: Fused compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. Wherein R1, R2, R2a, R3, R3a, R4, and R4a are defined herein.

Abstract: Provided are crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide which are stable and show excellent oral absorbability. The crystals are Form II crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2?±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.

Abstract: New compositions of matter useful for the treatment of human diabetes and cancers comprise the reaction products of thymoquinone and harmaline or harmaline-like compounds, such as ?-carboline compounds, and the derivatives, solvates, prodrugs, isomers, and tautomers of such compounds.

Abstract: New compositions of matter useful for the treatment of human diabetes and cancers comprise the reaction products of thymoquinone and harmaline or harmaline-like compounds, such as ?-carboline compounds, and the derivatives, solvates, prodrugs, isomers, and tautomers of such compounds.

Abstract: Derivatives of relebactam, therapeutic methods of using the derivatives of relebactam, particularly in combination with ?-lactam antibiotics and pharmaceutical compositions thereof are disclosed. The derivatives of relebactam are suitable for oral administration.

Abstract: Described herein are compounds that are farnesoid X receptor agonists, 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 farnesoid X receptor activity.

Abstract: The present invention provides improved methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.

Abstract: The invention relates to pharmaceutical compositions comprising 4-((6bR,10aS)-3-methyl -2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-1-(4 -fluorophenyl)-butan-1-one, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

Abstract: Bridged compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. wherein R2, R3 R4, R5 and R6 are defined herein.

Abstract: The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.

Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.

Abstract: The present disclosure provides substituted pyrrolidine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.