Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.

Abstract: Disclosed are cardioversion methods for patients with either paroxysmal or persistent AFib which methods use budiodarone or a pharmaceutical composition comprising budiodarone.

Abstract: The invention relates to compounds that are useful for the prevention or treatment of TRPM3 mediated disorders, more in particular disorders selected from pain and inflammatory hypersensitivity. The invention also relates to a method for the prevention or treatment of said TRPM3 mediated disorders.

Abstract: Disclosed are methods to treat patients with AFib by monitoring their heart rhythm to determine the presence and/or the number of episodes of long duration AFib, and optionally the extent of AFib burden. Patients who meet threshold requirements are qualified for the treatment of AFib with a dosage of budiodarone. Patient monitoring is continued in order confirm that the patient is and remains responsive to budiodarone therapy including dose adjusting the patient to achieve such therapy. Subsequently, monitoring is continued to confirm that the patient remains responsive. These methods allow for treatment of the AFib and, correspondingly, reduce or delay the risk of stroke and/or congestive heart failure in the treated patient.

Abstract: Provided is a method for preventing or treating a wound or scar comprising administering to a subject in need thereof a pharmaceutical composition comprising benzbromarone as an active ingredient, wherein benzbromarone inhibits the function of heat shock protein 47 (HSP47), or inhibits the accumulation of collagen by reducing collagen overproduction cells.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: The present disclosure relates to a new salt of escitalopram and its solid state forms, processes for the preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: One embodiment of the invention provides a method for administering tasimelteon to a human patient that comprises orally administering an effective dose of tasimelteon under fasted conditions. Fasted conditions may comprise administering the tasimelteon without food, no food at least ½ hour prior to administration, no food at least 1 hour prior to administration, no food at least 1½ hours prior to administration, no food at least 2 hours prior to administration, no food at least 2½ hours prior to administration, or no food at least 3 hours prior to administration. According to such embodiments, tasimelteon may be administered, for example, at a dose of 20 mg/d. Tasimelteon may be administered where, for example, the patient is being treated for a circadian rhythm disorder or for a sleep disorder, including, for example, Non-24 Disorder.

Abstract: Disclosed in the present invention are a naphthalenesulfonamide compound, a preparation method, and an application. The naphthalenesulfonamide compound provided by the present invention can interfere with Keap1-Nrf2 binding and activate Nrf2 to relieve inflammatory damage and improve an inflammatory microenvironment, has a potential anti-inflammatory activity, and can be used for preparing an anti-inflammatory drug for inflammatory damage of various inflammation-related diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, intestinal Inflammations, rheumatoid arthritis, etc.

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: Liquid suspensions of tasimelteon and methods for their use.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: Provided are methods of enhancing bioavailability of enterally administered 5-hydroxytryptophan (5-HTP) in a subject in need thereof, said method comprising enterally co-administering low-dose carbidopa with said 5-HTP, as well as pharmaceutical formulations useful for the same. In some embodiments, the 5-HTP and/or low-dose carbidopa are provided as slow-release formulation(s).

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: A method of treating a fungal infection in a subject includes topically administering to the subject a therapeutically effective amount of a fungal iron acquisition inhibitor to treat fungal infection in the subject.

Abstract: The present disclosure provides regioselective methods for synthesizing intermediates useful in making prostacyclin. The methods include heating the compound of Formula 2 at a temperature of 180° C. to 185° C. Wherein the heating comprises irradiating the compound of formula 2 with microwave radiation.

Abstract: The present invention provides a parenteral dosage form consisting essentially of a solution filled in a container, the solution comprising amiodarone or its pharmaceutically acceptable salt and a sulfo-alkyl ether beta-cyclodextrin in an aqueous vehicle, wherein the solution has a pH in the range of about 2.4 to 3.9 and further wherein the dosage form is sterilized by subjecting the filled container to autoclaving.

Abstract: One embodiment of the invention provides a method for administering tasimelteon to a human patient that comprises orally administering an effective dose of tasimelteon under fasted conditions. Fasted conditions may comprise administering the tasimelteon without food, no food at least ½ hour prior to administration, no food at least 1 hour prior to administration, no food at least 1½ hours prior to administration, no food at least 2 hours prior to administration, no food at least 2½ hours prior to administration, or no food at least 3 hours prior to administration. According to such embodiments, tasimelteon may be administered, for example, at a dose of 20 mg/d. Tasimelteon may be administered where, for example, the patient is being treated for a circadian rhythm disorder or for a sleep disorder, including, for example, Non-24 Disorder.

Abstract: A composition in the form of an injectable aqueous solution, for which the pH is comprised from 6.0 to 8.0, includes at least: a) amylin, an amylin receptor agonist or an amylin analogue; b) a co-polyamino acid bearing carboxylate charges and hydrophobic radicals Hy, said co-polyamino acid being constituted of glutamic or aspartic units and said hydrophobic radicals Hy chosen according to formula X as defined below: c) characterized in that the composition does not include basal insulin for which the isoelectric point IP is comprised from 5.8 to 8.5. The composition also includes a prandial insulin.

Abstract: Citalopram or escitalopram, pharmaceutically acceptable salts or derivatives thereof for use in the treatment of neurodegenerative diseases The disclosure subject matter is related to the use of citalopram or escitalopram, pharmaceutically acceptable salts or derivatives thereof, in the treatment of neurodegenerative diseases that are positively influenced by the decrease of protein misfolding and/or aggregation, in particular by oral administration.

Abstract: The present invention relates to a type of aryl benzofuran amidated derivatives, the medical use thereof, and the preparation method; said derivatives have antioxidation activity, and xanthine oxidase inhibitory activity, and can be used for antioxidation and for preparing compositions, drugs and health products and treating gout and hyperuricemia.

Abstract: The present invention relates to a pharmaceutical composition for prevention or treatment of neurological diseases and mental diseases, the composition containing syringaresinol. The syringaresinol according to the present invention has an effect of reducing excitatory synaptic transmission in a central nervous system and an effect of suppressing epilepsy and activity of animals. This suppressive effect of the excitatory synaptic transmission may be effectively used for the prevention and treatment of all neurological diseases and mental diseases resulting from synapse dysfunction and synpatic excitatory-inhibitory transmission imbalance.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: The present disclosure provides regioselective methods for synthesizing intermediates useful in making prostacyclin derivatives, such as treprostinil.

Abstract: Crystal forms I and II of tasimelteon. Crystal form I: an X-ray powder diffraction spectrum using CuK? radiation and represented by a 2? angle has diffraction peaks at least at 7.2°±0.2°, 7.9°±0.2°, 10.6°±0.2°, 14.4°±0.2°, 15.9°±0.2°, 17.3°±0.2°, 21.0°±0.2°, 23.2°±0.2°, and 24.4°±0.2°. Crystal form II: an X-ray powder diffraction spectrum using CuK? radiation and represented by a 2? angle has diffraction peaks at least at 6.8°±0.2°, 12.1°±0.2°, 12.5°±0.2°, 13.1°±0.2°, 13.6°±0.2°, 13.8°±0.2°, 15.8°±0.2°, 17.0°±0.2°, 18.4°±0.2°, 20.8°±0.2°, 24.2°±0.2°, and 24.4°±0.2°. Crystal forms I and II of tasimelteon have advantages of excellent physicochemical property, good stability and solubility, and simple operation for preparation.

Abstract: Embodiments of the invention relate to the treatment of sleep disturbances in individuals with Smith-Magenis Syndrome (SMS).

Abstract: A novel technique is provided for preserving a liquid pharmaceutical preparation safely and stably. The nano-bubble water of the present invention, which is produced in the presence of a surfactant, a hydrophilic resin and/or an electrolyte and contains not less than 2.0×108 bubbles/mL of nano-bubbles, shows a superior antibacterial action, and can be used as a base of a liquid pharmaceutical preparation showing safe and stable preservation property.

Abstract: The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway.

Abstract: Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.

Abstract: Disclosed herein are compositions and methods for treating or preventing certain cancers in a subject. In certain embodiments such compositions and methods generally relate to the use of G-coupled protein receptor 40 (GPR40) agonists to inhibit the growth or induce apoptosis of certain cancer cells. The compositions and related methods disclosed herein may be used to treat subjects affected by cancers, such as melanoma, medullary thyroid carcinoma, malignant peripheral nerve sheath tumors and neuroblastoma, and to reduce the incidence of metastases in such affected subjects.

Abstract: The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway.

Abstract: The present invention provides a novel method for enhancing engraftment of haematopoetic stem cells by an ex-vivo pretreatment comprising the steps of obtaining a sample containing haematopoetic stem cells and admixing a prostacyclin analog to obtain a mixture, incubating said mixture for a period of time sufficient to stimulate G alphas-signalling in said cells and optionally and isolating said stimulated cells. Further, a composition comprising a prostacyclin analog for use in the treatment of individuals undergoing haematopoetic stem cell transplantation is provided.

Abstract: The present disclosure provides regioselective methods for synthesizing intermediates useful in making prostacyclin derivatives, such as treprostinil.

Abstract: The present invention relates to a an imide compound according to anyone of formulas Ia, Ib, Ic, or Ie wherein R1 is H or a C1-C20 optionally substituted hydrocarbon group; both R2 and R5 are a COOH group or one of R2 and R5 is a COOH group while the other substituent is H, methyl or ethyl group; R3 and R4 are independently H, or C1-C20 optionally substituted hydrocarbon group; R6 is H or a methyl group; R7 and R8 are independently H, methyl or ethyl.

Abstract: Embodiments of the invention relate to the treatment of sleep disturbances in individuals with Smith-Magenis Syndrome (SMS).

Abstract: The present invention relates to a condensed heterocyclic compound that has an enteropeptidase inhibitory effect, and use of the compound as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like. Specifically, the present invention relates to a compound represented by the formula (I) or a salt thereof, and use of the compound as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like [in the formula, each symbol is as defined in the specification].

Abstract: Compounds of Formula (I), including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV: (I).

Abstract: The present invention relates to a compound of Formula 1, and an SIRT 1 activator including, as an active ingredient, derivatives thereof or pharmaceutically acceptable salts thereof. The present invention also relates to a composition including the SIRT 1 activator for detoxification, for the improvement of metabolic disorders, for the prevention or improvement of eye diseases, or the prevention or improvement of immune diseases.

Abstract: The invention relates to fluorinated compounds and their use in the field of pathological syndromes of the cardiovascular system. Novel fluorinated benzofuran derivatives of amiodarone and pharmaceutically acceptable salts or solvates thereof and their use for the treatment of arrhythmias are described.

Abstract: It is already known that 1-(benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable acid addition salt thereof exhibits an excellent effect as an antidepressant, a psychotropic drug, an antiparkinsonian drug, and an anti-Alzheimer's disease drug. However, it has not been known at all that the compound is effective for the prevention or therapy of attention-deficit/hyperactivity disorder (ADHD). The present invention has newly found that 1-(benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable acid addition salt thereof is effective for the prevention or therapy of ADHD, and has been accomplished.

Abstract: Irreversible inhibitors of K-Ras, H-Ras or N-ras protein comprising a G12C mutation are provided. Also disclosed are methods to regulate the activity of K-Ras, H-Ras or N-ras protein comprising G12C mutation and methods to disease mediated by K-Ras, H-Ras or N-ras G12C.

Abstract: The invention relates to dronedarone or one of its pharmaceutically acceptable salts for the treatment of leishmaniasis, formulations and associations comprising dronedarone or one of its pharmaceutically acceptable salts for the treatment of leishmaniasis.

Abstract: The present invention relates to a stable, sterile, ready to administer parenteral dosage form of amiodarone or its pharmaceutically acceptable salt. Particularly, the present invention provides a stable, sterile, ready to administer parenteral dosage form of amiodarone comprising an aqueous solution comprising amiodarone or its pharmaceutically acceptable salt, an acid, and a polyol, wherein the pH of the solution is in the range of about 2.0 to 4.0, wherein the solution is filled in a plastic container and wherein the solution is free of a solubilizer.

Abstract: The invention relates to fluorinated compounds and their use in the field of pathological syndromes of the cardiovascular system. Novel fluorinated benzofuran derivatives of amiodarone and pharmaceutically acceptable salts or solvates thereof and their use for the treatment of arrhythmias are described.

Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: The invention is directed to the use of a compound of formula I, as defined herein, to a pharmaceutically acceptable salt thereof; to a pharmaceutical composition containing a compound of formula I, and to a combination of a compound of formula I with a pharmacologically effective cholinesterase inhibitor to treat a mammal, including a human, for a disorder or condition selected from the list including Alzheimer's disease, Huntington's disease, Parkinson's disease, non-Alzheimer's dementias and ALS.