Abstract: Disclosed herein are lignin-derived ionic liquids and methods for preparing them. The methods include forming a reaction mixture comprising a lignin-derived starting material, a carbonyl compound, and an amine; maintaining the reaction mixture under conditions sufficient to form a lignin-derived aminophenol; and converting the lignin derived aminophenol to the lignin-derived ionic liquid. Monomeric phenols, oligomeric phenols, and polymeric phenols can be used as lignin-derived starting materials.

Abstract: The present invention is directed to novel neuro-attentuating norketamine (NANKET) compounds according to any one of formulas (I-shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods.

Abstract: Provided herein are in vivo gelling pharmaceutical pre-formulations forming biocompatible hydrogel polymers that are polymerized in vivo and kits comprising at least one nucleophilic compound or monomer unit, at least one electrophilic compound or monomer unit, and optionally at least one therapeutic agent. The biocompatible hydrogel polymer is bioabsorbable and releases the therapeutic agent at a target site, avoiding systemic exposure.

Abstract: Provide herein are compounds with a general chemical structure of: Substituents R1 and R2 independently are H, Cl, F, Br, CH3, CF3, SH, —N(C1-3alkyl)2, —NHC(O)C1-3alkyl, or —NHC(O)C5-7cycloalkyl, substituent R3 is H or C1-3 alkyl and R4 is a bridged cycloalkene such as a bridged cyclohexene or a bridge-substituted cyclohexene. The compounds are therapeutics to treat a cancer, such as breast cancer, or metastatic cancers, to inhibit RUNX2 activity, such as protein expression, in a cancer cell and to increase survival of a subject with breast cancer.

Abstract: Process for the preparation of a compound of Formula (I), the process comprising the reaction of a compound of Formula (II) with malononitrile in the presence of a base and a palladium catalyst, Formula (II) wherein X, Y and Z, independently of each other, represent fluoro, chloro or C1-4alkyl; and L is a leaving group; with the proviso that 1 or 2 of X and Y are, independently of each other, fluoro or chloro.

Abstract: An integrated process for the production of a formaldehyde-stabilised urea is described comprising the steps of: (a) generating a synthesis gas comprising hydrogen, nitrogen, carbon monoxide, carbon dioxide and steam in a synthesis gas generation unit; (b) dividing the synthesis gas into a first synthesis gas stream and a smaller second synthesis gas stream; (c) subjecting the first synthesis gas stream to one or more stages of water-gas shift in one or more water-gas shift reactors to form a shifted gas; (d) cooling the shifted gas to below the dew point and recovering condensate to form a dried shifted gas; (e) recovering carbon dioxide from the dried shifted gas in a carbon dioxide removal unit to form a carbon dioxide-depleted synthesis gas; (f) subjecting the carbon dioxide-depleted synthesis gas to a stage of methanation in one or more methanation reactors to form an ammonia synthesis gas; (g) synthesising ammonia from the ammonia synthesis gas in an ammonia production unit and recovering the ammonia; (

Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention also relats to substantially pure compound 1 and substantially pure compound 1 salt (e.g., compound 1 hydrochloride salt and compound 1 benzenesulfonate salt). The invention further relates to methods of preparing substantially pure compound 1 and compound 1 salts.

Abstract: A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —OH, —CONH, and/or —COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —N+(R1R2R3), —NO2, —Cl, —Br, —F, or —I, and R1, R2, and R3 are independently C1-C6 alkyl; and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.

Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoholism, alcoholic steatohepatitis (ASH), non-alcoholic steatohepatitis (NASH), obesity/weight gain, anxiety, depression, post-traumatic stress disorder, inflammatory/autoimmune conditions and cancer, including metastatic cancer, advanced cancer, and drug resistant cancer of various types.

Abstract: The present invention provides inhibitors of TAK1 having formula (II), affinity resins, and fluorescent dyes and methods of using such compounds to treat various diseases or in protein isolation or purification.

Abstract: The present invention provides novel crystalline forms of Lesinurad, pharmaceutical compositions including these crystalline forms, and their use in the treatment of hyperuricemia associated with gout. Specific crystalline forms provided by the present invention include Lesinurad Forms APO-I, a hemi-methanolate, APO-II, a hemi-ethanolate, and APO-III, a co-crystal of Lesinurad and nicotinamide.

Abstract: The present invention provides aromatic 4,6-bis-trichloromethyl-s-triazin-2-yl compounds of formula (I), a process for producing para-disubstituted benzonitriles as precursor to give compounds of formula (I) and a process for the production thereof.

Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (XI): wherein Y is C1-C12 alkylene or C1-C12 alkenylene; and R8 and R12 are independently C1-C12 alkyl.

Abstract: The present invention includes crystalline forms of (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and salts thereof. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic uses of the crystalline forms.

Abstract: This invention relates to a process for the epoxidation of a tetrasubstituted alkene such as terpinolene to the corresponding epoxide such as terpinolene epoxide by reacting the tetrasubstituted alkene with peracetic acid prepared in situ from acetic anhydride and hydrogen peroxide in the presence of at least one buffering agent. Further, the invention relates to the use of an oxidizing agent comprising hydrogen peroxide and acetic anhydride for the in-situ epoxidation of a tetrasubstituted alkene.

Abstract: A composition is provided that, when utilized in combination with a coumarin anticoagulant, greatly improves the anticoagulant effects of the anticoagulant in mammalian subjects. The composition is a compound having a naphthohydroquinone ring system substantially similar to the ring system of the reduced form of vitamin K1 and has the general formula: where n is 1 or 2, where R1 and R4 are hydrogen or acyl, R2 is a hydrogen or saturated or unsaturated alkyl group with up to 6 carbons, and R3 is a hydrogen or saturated or unsaturated alkyl group with up to 6 carbons, or R2 and R3 are part of a cyclic or polycyclic ring system.

Abstract: Processes and reactor systems for biomass conversion are described. A continuous process for the conversion of carbo-hydrate-containing feed material into furanic compounds comprises a reaction step comprising subjecting said feed material to reaction conditions in a reaction medium comprising two immiscible liquid phases, including a reactive phase and an extractive phase, and a Brønsted acid as catalyst, wherein the reaction medium comprises a solid component comprising at least a part of a carbohydrate-containing fraction of said feed material.

Abstract: Disclosed is a process for the extraction of furfural which includes: (a) subjecting a composition comprising furfural, water, at least one acid and an aromatic solvent, with a boiling point higher than that of furfural, to a first separation step providing: (i) an organic phase, and (ii) an aqueous phase; (b) subjecting the aqueous phase of step (a) to a first distillation step to provide: (i) a first in top stream comprising a furfural-water azeotrope; (c) subjecting the first top stream of step (b) to a second separation step to provide: (i) a second top stream comprising a portion of the furfural-water azeotrope; (d) subjecting the second top stream of step (c) to a second distillation step to provide: (i) a third top stream enriched with the furfural-water azeotropic mixture; (e) subjecting the organic phase of step (a) to a third distillation step to provide: a fourth top stream comprising furfural.

Abstract: The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.

Abstract: The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent.

Abstract: The present invention relates to a method for the cosmetic treatment of keratin materials, in particular the skin, comprising the application of a composition to the keratin materials, such as the skin, said composition comprising a compound (I), wherein R is as defined in the description and S* is a mono or polysaccharide. In particular, the invention relates to the non-therapeutic cosmetic use of at least one compound of formula (I) as an agent for whitening, lightening and/or depigmenting keratin materials, such as the skin.

Abstract: The present disclosure provides processes for the preparation of a compound of formula: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates.

Abstract: Disclosed are methods for preparing a salt of urolithin A and, in turn, urolithin A. The methods are advantageous for the large-scale preparation of urolithin A or a pharmaceutically acceptable salt thereof.

Abstract: The present application discloses a levelling compound for electrodepositing metals.

Abstract: This invention relates to an acid labile surfactant. In particular, the surfactants of the present invention include a dioxolane or dioxane functional group which enables the surfactant to hydrolyze in an acidic environment. Surfactants of this type can be utilized to enhance protein solubilization/enzyme digestion. Following hydrolysis to destroy the surfactant (which may chromatographic issues), there are generally two components formed—a hydrophilic one, and a hydrophobic one. By altering the chemistry of the hydrolysable linker, the polarity of the hydrophobic residue can be altered, allowing it to be solubilized by significantly less organic solvent, and to minimize the potential loss of peptide material and to expand the chromatographic conditions that can be utilized.

Abstract: Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).

Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

Abstract: The present disclosure generally relates to methods of preparing nicotine and resolving R,S nicotine to enrich the (S)(?) enantiomer. The method may comprise combining N-methyl-2-pyrrolidone or a salt thereof with a nicotinate compound in the presence of a solvent and a strong base to form 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof; and reducing the 1-methyl-3-nicotinoyl-2-pyrrolidone or salt thereof in solution with Na2S2O4 to produce racemic nicotine or salt thereof. Resolving the racemic nicotine (or other enantiomeric mixture) may comprise combining the nicotine with (?)-O,O?-di-p-toluoyl-L-tartaric acid (L-PTTA).

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, W1, W2, W3, and R1-R6 are described herein.

Abstract: The invention provides a method for producing a crystal of a uracil compound with high purity by a process which can be carried out in an industrial scale. Specifically, the invention provides a method for producing a crystal of a uracil compound, wherein the method comprises dissolving a composition comprising a uracil compound represented by formula (1) in organic solvents consisting of a C3-C6 alcohol solvent and an aromatic solvent to obtain a solution, and precipitating a crystal of said uracil compound from the solution.

Abstract: Potent opioid receptor antagonists of formula (I) and their use as pharmacotherapies for treating depression, anxiety, schizophrenia, eating disorders, and addiction to cocaine, methamphetamine, nicotine, alcohol, and opiates are disclosed. More specifically, the disclosure provides potent and selective kappa opioid receptor antagonist compounds, pharmaceutical compositions of those compounds and uses of those compounds to ameliorate or treat addictions, eating disorders, etc.

Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subjuect compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.

Abstract: The present invention relates to N-((3S,4R)-1-((8-chloroquinoxalin-6-yl)carbonyl)-3-(4-fluorophenyl)piperidin-4-yl)-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-carboxamide, which is a compound that can be useful for the treatment or prevention of SPT-related diseases including congenital diseases associated with the storage of sphingolipids, such as cancer and Niemann-Pick disease, or a salt thereof.

Abstract: Provided herein are bifunctional compounds that inhibit MALT1 and/or promote targeted ubiquitination for the degradation of MALT1. In particular, provided are compounds that can bind MALT1, a protein whose activity is responsible for constitutive NF-KB signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)), and can assist in its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL), which can ubiquitinate MALT1, marking it for proteasome degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer with the bifunctional compounds, methods of promoting the degradation of MALT1, and methods of binding E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.

Abstract: The invention provides a compound as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating KIT mediated diseases.

Abstract: A compound which is a benzimidazole of formula (I): wherein X is a 5-membered heteroaryl group selected from the following: or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.

Abstract: The present invention relates to a novel compound and a composition for the prevention, alleviation or treatment of fibrosis or non-alcoholic steatohepatitis, which contains the compound as an active ingredient, and more particularly to a novel compound of Formula 1, which has an excellent effect on the prevention, alleviation or treatment of fibrosis, and to a composition for the prevention, alleviation or treatment of fibrosis or non-alcoholic steatohepatitis, which contains the compound as an active ingredient. The novel compound can regulate the activation of EMT (epithelial-mesenchymal transition) by effectively regulating the expression of snail and vimentin which are regulators of EMT, and thus can effectively prevent, alleviate or treat fibrosis. Furthermore, the novel compound has very good pharmacokinetics. In addition, the novel compound of the present invention can effectively inhibit fibrosis of liver cells, and thus can also effectively alleviate or treat non-alcoholic steatohepatitis.

Abstract: The present invention relates to a novel family of covalent kinases inhibitors, compounds of this class have been found to have inhibitory activity against members of the TEC kinase family, particularly ITK and/or TXK, BTK, TEC and/or combinations thereof. The present invention is directed to a compound of Formula I or pharmaceutically acceptable salt, solvate, solvates of salt, stereoisomer, tautomer, isotope, prodrug, complex or biologically active metabolite thereof, for use in therapy.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

Abstract: The present invention provides compounds that modulate the interaction of TCR with Nck, compositions thereof, and methods of treatment using the same.

Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, n, p, q A, B, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract: The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.

Abstract: The LIM Kinase inhibitors of Formula I and pharmaceutically acceptable salts or solvates thereof, wherein R1, R2, R3, R4, X1, X2, X3, Y1, Y2 and Z are as defined in the claims. Also, the use of LIM Kinase inhibitors of Formula I for the treatment and/or prevention of LIMK-mediated diseases.

Abstract: The present invention relates to compounds of the formula (II) wherein Ar1, R1, R2, R3, R4a, R4b and (R5)n are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (II), and especially to their use as orexin receptor antagonists.