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: 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: 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: 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.

Abstract: In some embodiments, the present invention provides methods of treating a tumor in a subject. In some embodiments, the methods may include a step of administering to the subject a therapeutic composition that comprises: (a) mycophenolic acid, an analog thereof, or a derivative thereof; and (b) at least one anti-neoplastic agent. In some embodiments, the antineoplastic agent may include at least one of 5-fluouracil (5-FU), paclitaxel, oxaliplatin, doxorubicin, etoposide, irinotecan, bleomycin, imiquimod, 13-cis-retinoic acid, and combinations thereof. In some embodiments, the relative concentrations of the mycophenolic acid, the analog thereof, or the derivative thereof, and the at least one anti-neoplastic agent correspond to their respective IC50 values.

Abstract: The object of the invention is the use of compounds comprising one or more free sulphlydryl or amino groups for preparing a pharmaceutical composition for locally binding acetaldehyde in saliva, the stomach or the large intestine, and pharmaceutical compositions comprising the said compounds.

Abstract: The present invention concerns the treatment of serotonergic dysregulation disorders and/or augmentation of serotonin levels in the brain by add-on treatments to serotonin enhancers, and slow-release formulations of 5-hydroxytryptophan (5-HTP) therefor.

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.

Abstract: Provided herein are methods for using at least one histone deacetylase inhibitor to decrease cellular DNA repair activity, methods for monitoring the decrease of cellular DNA repair activity using at least one biomarker, methods of treating cancer by using at least one histone deacetylase inhibitor to decrease cellular DNA repair activity in combination therapy, methods of combination therapy where at least one histone deacetylase inhibitor interferes with a DNA repairing mechanism involving RAD51, methods for predicting a induction time period between a first administration of at least one histone deacetylase inhibitor and a second administration of at least one other therapeutic treatment, and pharmaceutical compositions for combination therapy.

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.

Abstract: Serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.

Abstract: Methods for modulating eye damage associated with a disease or disorder, and/or damage incident to trauma including but not limited to trauma associated with ocular surgery are provided. In some embodiments, the methods include administering an effective amount of a modulator of a migration inhibitory factor (MIF) polypeptide biological activity to a subject. Also provided are methods for modulating the severity of delaying the onset of and/or inhibiting and/or preventing the development of an ocular disease, and methods for modulating the severity of delaying the onset of and/or inhibiting and/or preventing the development of scarring and/or other consequence of wound healing incident to ocular surgery, as well as modulating the survival, function, and/or differentiation of engrafted cells that can be employed as part of tissue engineering procedures to correct structural, functional, and/or cellular defects of the eye.

Abstract: Methods of using dronedarone or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the prevention of cardiovascular hospitalization or of mortality, articles of manufacture and packages related thereto.

Abstract: Provided is a simple, safe, and industrially practical method for producing a pentafluorosulfanylbenzoic acid.

Abstract: This invention relates to cosmetic and pharmaceutical preparations comprising (i) a diastereomer or a mixture of two or more diastereomers of the compound of formula (I) or (ii) a salt of a diastereomer or of a mixture of two or more diastereomers of the compound of formula (I) or (iii) a mixture of two or more salts of a diastereomer or of a mixture of two or more diastereomers of the compound of formula (I), a diastereomer, salt or a mixture as defined above as a drug for topical application and/or for the treatment of lipoatrophy; the non-therapeutic use of a diastereomer, salt or a mixture as defined above for the prevention, treatment or reduction of skin aging, especially skin wrinkles; the use of a diastereomer, salt or a mixture as defined above for the production of an orally administered non-pharmaceutical preparation.

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: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.

Abstract: A method of increasing the insulin sensitivity of a mammalian cell by contacting the cell with a protein phosphatase 2A (PP2A) inhibitor having the structure:

Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.

Abstract: This invention is based upon the discovery that a mixture of ethyl lactate and isoamyl lactate can be used to improve the penetration of active ingredients in skin care formulations through the outer layers of the stratum corneum and viable epidermis and into the dermis layer of the skin structure. The present invention more specifically discloses a method of rejuvenating skin comprising topically applying a topical formulation to the skin, wherein the topical formulation is comprised of ascorbic acid, an amino acid selected from the group consisting of phenylalanine and tyrosine, a non-toxic zinc salt, carnosic acid, ?-tocopherol, 0.01 weight percent to 20 weight percent of a mixture of ethyl lactate and isoamyl lactate, wherein the weight ratio of the ethyl lactate to the isoamyl lactate is within the range of 1:10 to 20:1, and a pharmaceutically acceptable carrier.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Abstract: A method of treating a subject at risk of or suspected of having Fragile X syndrome or autism spectrum disorder associated with abnormalities of ERK includes administering to the subject a therapeutically effective amount of at least one ERK inhibiting compound that prevents abnormalities in neuronal connectivity, a prodrug thereof that is metabolisable to form the compound, or a pharmaceutically acceptable salt thereof.

Abstract: A method for pharmacological treatment of cancers and other diseases is presented which includes the novel combination of a statin (Hmg-CoA reductase inhibitor, such as lovastatin, simvastatin, atorvastatin, cerivastatin, fluvastatin, pravastatin, or newer agents), with an interferon (such as interferon alfa-2b or others) and also including concurrent administration of selenium and calcium. The method disclosed in this invention is useful because it can prove more effective than previously known therapies for certain diseases and because its use may be more tolerable, less disfiguring, and less expensive than other methods. The method here disclosed can be readily reproduced by any person skilled in the art of treating disease.

Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.

Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.

Abstract: The disclosure relates to a pharmaceutical composition for oral administration, containing, as active principle, a benzofuran derivative having antiarrhythmic activity, in particular dronedarone and the pharmaceutically acceptable salts thereof, and at least one lipid carrier, said pharmaceutical composition being intended to be used in unit dosage form of the capsule type, in particular with a hard shell. This pharmaceutical composition and the dosage form comprising such a composition aim to limit the meal time effect following oral administration in humans. The lipid carrier allows: the solubilization of the active principle of the invention; and the shielding thereof from the negative effects of pH in the intestinal tract, thereby allowing same to be spared from the meal effect to a significant extent.

Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.

Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.