Abstract: In the present disclosure, doxycycline-inducible astrocyte-specific HIV Tat transgenic mice (iTat), a surrogate HAND model, were treated with PNU-125096, a positive allosteric modulator of ?7 nicotinic acetylcholine receptor (?7 nAChR) and effects on Tat-induced behavioral impairments and neuropathologies were observed. This disclosure shows that PNU-125096 treatment significantly improved locomotor, learning and memory deficits of iTat mice while inhibited glial activation and increased PSD-95 expression in the cortex and hippocampus of iTat mice. ?7 nAChR knockout eliminated the protective effects of PNU-125096 on iTat mice. In addition, inhibition of p38 phosphorylation by SB239063, a p38 MAPK-specific inhibitor, exacerbated Tat neurotoxicity in iTat mice. These findings demonstrated for the first time that ?7 nAChR activation led to protection against HAND and suggest that ?7 nAChR and PNU-125096 hold significant promise for development of therapeutics for HAND.

Abstract: Disclosed herein are methods of elevating brain extracellular 5-hydroxytryptamine (5-HTExt) and of treating psychiatric conditions and neurological disorders using continuous intravenous infusion of 5-hydroxytryptophan (5-HTP). The methods can be provided for treatment of acute suicidal ideation and/or acute worsening of a mood disorder. The methods can provide rapid onset of therapeutic effect while also having low incidence of acute or moderate adverse effects. Also described herein are compositions for use in the methods, including stable 5-HTP compositions for use in preparing infusate solutions.

Abstract: The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.

Abstract: A method for producing acetic acid can improve the life of a silver-substituted ion exchange resin for removing organic iodine compounds in acetic acid. In a carbonylation process of a methanol method, an acetic acid distillation step has at least one distillation step of carrying out the purification of an acetic acid stream under conditions of a column bottom temperature of a distillation column of less than 175° C., a nickel base alloy or zirconium is used as a material of the distillation column in the distillation step, and as metal ion concentrations in a charging mixture of the distillation column in the distillation step, an iron ion concentration is less than 10,000 ppb by mass, a chromium ion concentration is less than 5,000 ppb by mass, a nickel ion concentration is less than 3,000 ppb by mass, and a molybdenum ion concentration is less than 2,000 ppb by mass.

Abstract: Pharmaceutically active benzofuran compositions for the treatment of mental disorders or for mental enhancement, including for entactogenic therapy. The present invention also includes benzofuran compounds, compositions, and methods for generally modulating central nervous system activity and treating central nervous system disorders.

Abstract: An object of the present invention is to provide a method for producing an unsaturated carboxylic ester, wherein the risk of polymerization blockage is reduced and the required equipment cost and workload involved are kept low while maintaining a high conversion rate in an esterification reaction of unsaturated carboxylic acid. This object can be achieved by a method for producing an unsaturated carboxylic ester, which includes performing an esterification reaction using a reactor packed with a solid catalyst, wherein unsaturated carboxylic acid and alcohol are continuously fed to the reactor from an inlet thereof to form a fluid of the reaction solution in the reactor, and the vaporized organic solvent is continuously fed to the reactor from the inlet or a part near the inlet of the reactor.

Abstract: The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof.

Abstract: The invention provides novel regimens for treatment of neurodegenerative disorders utilising methylthioninium (MT)-containing compounds. The regimens are based on novel findings in relation to the dosage of MT compounds, and their interaction with symptomatic treatments based on modulation of acetylcholinesterase levels.

Abstract: The disclosure provides compounds. In certain embodiments, compounds of the disclosure are capable of inhibiting a mammalian SHMT, such as human SMHT1 and/or SHMT2. Compounds of the disclosure have numerous uses.

Abstract: The present disclosure relates to pharmaceutical formulations comprising imatinib or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing a disease using the formulations.

Abstract: The present invention relates to the field of laboratory-scale sample preparation, which describes a methodology for the specific isolation of tetraprotic naphthenic acids, called ARN acids, from residual naphthenate deposits from petroleum production. The method consists of cleaning the naphthenate deposit, converting the naphthenate salts to naphthenic acids and isolating the ARN acids from the other organic acids, using a silica-based sorbent material with aminopropyl functional groups, previously selected for an efficient elution of different functional groups and polarities.

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: Methods and compositions for treating a lysosomal movement associated disease in an animal, in which the position of lysosomes can influence disease progression, comprising administering an effective amount of a first lysosome migration inhibitor or a pharmaceutically acceptable salt, solvate, clathrate, stereoisomer, enantiomer or prodrug thereof.

Abstract: The present invention relates to a process for preparing a (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (S,R)-(2), wherein R1 represents a monovalent hydrocarbon group having 1 to 6 carbon atoms, and a bold wedged bond represents the absolute configuration, and a (1R,2S)-(2-acetoxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (R,S)-(3), wherein R1 is as defined above, a hashed wedged bond represents the absolute configuration, and Ac represents an acetyl group, the process comprising: subjecting a (1RS,2SR)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (RS,SR)-(2), wherein R1 is as defined above, and a hashed unwedged bond represents a relative configuration, to a kinetic resolution reaction with a lipase in the presence of vinyl acetate to obtain the (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound ((S,R)-(2)

Abstract: The disclosure relates to methods for treating or preventing a sleep disorder by administering a compound of formula (1)(1), or a compound of formula (1A), (1B), (1C), (1D), (1E), or (1F) to an animal in need of such treatment. In certain embodiments, such compounds effectively treat or prevent a sleep disorder in the animal, while producing reduced side effects compared to previously available compounds.

Abstract: The present invention belongs to the technical field of fine chemicals and relates to a new crystalline form of tefluthrin, a preparation method therefor and the use thereof. The preparation method specifically comprises: taking an amorphous tefluthrin or a solid tefluthrin other than the tefluthrin as described in the present invention as a raw material, firstly preparing the raw material into an amorphous substance at room temperature, and then allowing the amorphous substance to cool to 5° C. to ?24° C. to obtain a white or light yellow solid, i.e., a new crystalline form of tefluthrin.

Abstract: The present disclosure relates to methods of treating neurological or psychiatric diseases or disorders, such as schizophrenia. Compound 1, or a pharmaceutically acceptable salt thereof, is an antipsychotic agent with a non-D2 mechanism of action. Adverse events associated with antipsychotic agents that target the D2 dopamine receptor can be reduced by treating disorders with Compound 1, or a pharmaceutically acceptable salt thereof.

Abstract: In the embodiments, an aqueous hydrochloric acid solution instead of hydrogen chloride gas and solid triphosgene instead of phosgene gas may be used in the process of preparing a diisocyanate from a diamine through a diamine hydrochloride. In addition, the embodiments provide processes for preparing a diisocyanate composition and an optical lens of high quality in which the content of water, the content of cations, or the content of an aromatic compound containing 3 or more of chlorine (Cl) in the organic solvent used in the reaction of a diamine hydrochloride composition and triphosgene is adjusted to a specific range.

Abstract: This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

Abstract: Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.