Abstract: Described herein are methods of treating a human patient with a newly diagnosed neuroendocrine tumor, methods of treating patients with neuroendocrine tumors with early signs of carcinoid heart disease who have not had a heart valve replacement, and methods of treating a human patient with the neuroendocrine tumor who has had a recent heart valve replacement. Administering telotristat ethyl to these patients can reduce the development of carcinoid heart disease and improve clinical outcomes.

Abstract: The present invention relates to a method for preparing a pyrrolopyridine derivative compound exhibiting antiviral activity, and a novel intermediate used therein. The preparation method of the present invention enables reaction steps to be reduced through effective process development and a high purity pyrrolopyridine derivative compound to be prepared in a high yield, and thus enables production costs to be remarkably reduced so as to be economical and to be suitable for mass production.

Abstract: The present invention relates to a method for the production of a (poly)hydroxylated pentacyclic triterpene composition including a 3-O-p-coumaroyl ester of tormentic acid from a plant suspension cell culture, to a pharmaceutical composition comprising at least 3-O-p-coumaroyl ester of tormentic acid for a use in the prevention and/or the treatment of trypanosomiasis, optionally in admixture with other (poly)hydroxylated pentacyclic triterpenes, and to 3-O-p-coumaroyl ester of tormentic acid for its use as an antiparasitic agent for the prevention and/or the treatment of trypanosomiasis, optionally in admixture with other (poly)hydroxylated pentacyclic triterpenes.

Abstract: The present invention is directed to a composition comprising a combination of thymoquinone (TQ) and one or more additional biologically active agents, wherein said biologically active agents are selected from the group consisting of carotenoids, Cannabis-related compounds and pycnogenol. In one preferred embodiment, the TQ is contained in cold-pressed Nigella sativa oil, wherein said oil is characterized by a TQ concentration of at least 1.5% (w/w) and a free fatty acid (FFA) content of 3.5% (w/w) or less. The present invention is also directed to methods for treating or preventing inflammatory conditions by means of administering these compositions.

Abstract: Crystals of (((R)-12?-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-6?,8?-dioxo-6?,8?,12?,12a?-tetrahydro-1?H,4?H-spiro[cyclopropane-1,3?-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin]-7?-yl)oxy)methyl methyl carbonate, i.e. compound of formula (1) or a solvate thereof and a preparation method therefor. The crystals include crystal form A, crystal form B, crystal form C, crystal form D, crystal form E, crystal form F, and single crystal. The crystal of the compound of formula (1) or a solvate thereof can be individually used for clinical treatment or in combination with other anti-influenza drugs such as neuraminidase inhibitors, nucleoside drugs, or PB2 inhibitors, are capable of clinically curing influenza patients quickly, and have very good activity and good bioavailability compared to existing pyridone derivatives. In addition, the stability, hygroscopicity, and storability of the crystals meet the requirements for pharmaceutical use.

Abstract: Methods of treating, suppressing, or reducing the severity of a liver cancer in a subject are described herein. The disclosed methods include administering to the subject a first amount of safranal or a pharmaceutically acceptable pro-drug thereof and administering to the subject a second amount of a TOP1 inhibitor. In some embodiments, the TOP1 inhibitor is irinotecan, topotecan, camptothecin, lamellarin D, and/or combinations thereof.

Abstract: The present invention aims to provide a high-dose formulation with improved properties of a pharmaceutical composition comprising a poorly soluble basic agent, particularly a compound represented by formula (I) or a salt thereof. The problem described above can be solved by providing a pharmaceutical composition comprising the compound represented by formula (I) or a salt thereof, a surfactant, and a basic substance.

Abstract: The present invention relates to a pharmaceutical composition comprising a tetrahydrocannabivarin (THCV), wherein the composition further comprises cannabigerol (CBG) or cannabinodiol (CBND) or a mixture thereof, for use in the prevention and treatment of overweight, preferably associated with obesitas. The pharmaceutical composition according to the invention may further comprise the following additional compounds tetrahydrocannabinol (THC), or Cannabigerol (CBG) or Cannabinodiol (CBND) or a combination thereof.

Abstract: Disclosed is a compound of formula (I): for treating or preventing a human immunodeficiency virus (HIV) infection in a mammal, for inhibiting or preventing maturation of an immature human immunodeficiency virus (HIV) to a mature HIV, and for preventing or inhibiting a human immunodeficiency virus (HIV) infection in a mammal having at least one HIV viral particle on a surface thereof.

Abstract: The present invention relates to a composition comprising at least one oxazoline, such as OX100, for inhibiting the growth of Malassezia yeasts and/or for preventing and/or treating conditions caused by Malassezia yeasts, seborrheic dermatitis, cradle cap, Malassezia folliculitis, dandruff, Pityriasis versicolor or Pityriasis capitis. The present invention also relates to a composition comprising at least one oxazoline such as OX100, at least one compound such as malic acid diester and a vegetable oil oleodistillate and/or arabinogalactan, and to the use of same for preventing and/or treating, in particular, affections caused by Malassezia yeasts, seborrheic dermatitis, cradle cap, Malassezia folliculitis, dandruff, Pityriasis versicolor or Pityriasis capitis.

Abstract: Microemulsions are described where hydrophobic liquid droplets are distributed in a continuous hydrophilic liquid phase. In relation to conventional oil-in-water (OIW) microemulsions, the described microemulsions may be thought of as modified oil-in-water (MOIW) microemulsions, where both the “oil” and “water” phases of the microemulsion are modified. The oil phase droplets of the MOIW microemulsion are modified with alcohol and can solubilize alcohol-soluble species, including nonderivatized hormones. More preferably, the modified oil phase droplets of the MOIW microemulsion directly solubilize nonderivatized hormones. The oil phase droplets of the MOIW microemulsion include DHEA, pregnenolone, and a polyphenol, where a ratio of DHEA to polyphenol is from 1:1 to 12:1 by weight. Methods of supporting and/or increasing bloodstream hormone levels in perimenopausal and postmenopausal females and improving menopausal symptoms also are disclosed.

Abstract: The present disclosure relates to oral compositions that include at least two agents selected from: agents that increase the concentration of glutamate; agents that increase dopamine production; agents that increase the concentration of brain-derived neurotrophic factor (BDNF); NMDA and/or AMPA receptor modulators; and acetylcholinesterase inhibitors. In son embodiments, a composition as provided herein includes D-glutamine present in an amount of about 20% to about 30% w/w of the composition; ginkgolide B present in an amount of about 0.1% to about 0.4% w/w of the composition; phosphatidylserine present in an amount of about 65% to about 80% w/w of the composition; and ascorbic acid present in an amount of about 0.5% to about 2.5% w/w of the composition. Such compositions are useful for improving memory and/or focus.

Abstract: The present invention relates to a compound exhibiting excellent agonist activity against melanocortin receptors. More specifically, the present invention relates to a compound of Formula 1, a pharmaceutical composition comprising the compound as an active ingredient, and a use thereof, and the compound of the present invention exhibits excellent agonist activity against melacortin-4 receptors and can be particularly useful in preventing or treating obesity, diabetes, inflammation and erectile dysfunction.

Abstract: A method for preparing nicotine. (1) The nicotinic acid alkyl ester and N-methylpyrrolidone are subjected to a condensation reaction, and then added with a strong acid to obtain 4-methylamino-1-(3-pyridine)-butanone hydrochloride. (2) The 4-methylamino-1-(3-pyridine)-butanone hydrochloride is reacted with an amino-protecting reagent to obtain an intermediate (4). (3) A chiral alcohol (5) is obtained through an asymmetric reduction. (4) The chiral alcohol (5) is converted into the nicotine through a two-step reaction.

Abstract: The present disclosure provides compounds that are inhibitors of PIKfyve kinases useful for the treatment of neurological diseases treatable by inhibition of PIKfyve. Also provided are pharmaceutical compositions containing such compounds, and methods of treatment using such compounds.

Abstract: Provided herein are pharmaceutical compositions (e.g., oral dosage formulations) comprising (S)-4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, mixture of enantiomers, tautomer, isotopolog, or pharmaceutically acceptable salt thereof, and a carrier or diluent. Also provided herein are methods of preparing and methods of using the pharmaceutical compositions.

Abstract: The present invention relates to use of biopterin compounds such as 4-Amino-(6R,S)-5,6,7,8-tetrahydro-L-biopterin or 4-Amino-(6R,S)-7,8-dihydro-L-biopterin for treating a human patient suffering from a disease condition or disorder that is associated with an increased glutamate level. The invention also relates to the use of such biopterin compounds in a method of treating or preventing glutamate excitotoxicity (glutamate storm) in a patient suffering from a condition that has the potential to result in a pathologically high glutamate level in the brain.

Abstract: Non-ionic polyether surfactants with improved resistance to hydrolysis are provided.

Abstract: Provided is a 2-heteroaryl aminoquinazolinone derivative, which is a compound represented by formula (1): or a pharmaceutically acceptable salt thereof wherein X1 represents CR1 or N, X2 represents CR2 or N, X3 represents CR3 or N, X4 represents CR4 or N, Y represents optionally substituted C1-6 alkyl, an optionally substituted C3-10 alicyclic group, an optionally substituted 4- to 10-membered nitrogen-containing non-aryl heterocycle, optionally substituted C6-10 aryl, or optionally substituted 5- to 10-membered heteroaryl, Z represents optionally substituted 6- to 10-membered heteroaryl, and R1, R2, R3, and R4 each independently represent a hydrogen atom, halogen, cyano, optionally substituted C1-6 alkyl, optionally substituted C1-6 alkoxy, or the like.

Abstract: The invention provides a method of treating cancer in a subject in need thereof, comprising administering to the subject: (a) a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or an acyl group; and (b) a PD-1 signaling inhibitor; wherein the compound of Formula I or pharmaceutically acceptable salt thereof and the PD-1 signaling inhibitor are administered in amounts which in combination are therapeutically effective. The invention further provides a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, a PD-1 signaling inhibitor and a pharmaceutically acceptable carrier or excipient.