Abstract: The present invention relates to a method of treating or preventing the visual function loss in optic nerve in a subject after crush injury by using 4-(Phenylsulfanyl)butane-2-one (4-PSB-2). The present invention has the ability of enhancing the protection effect of RGCs, preserving the visual function in optic nerve after crush injury, recovering the visual function loss, attenuating apoptosis in optic nerve after injury, and inhibiting the inflammatory responses in optic nerves after ON injury.

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: The present invention provides effective and safe medicaments for the treatment of connective tissue diseases of the skin, particularly with respect to the treatment of cutaneous forms of Lupus Erythematous. The medicaments comprise as the therapeutically active ingredient a beta2 adrenoceptor agonist. The invention furthermore relates to dermatological compositions without skin sensitization properties and which contain enantiomerically pure or enriched R-enantiomers of a beta2 adrenoceptor agonist.

Abstract: Sweetness receptor antagonists represented by formula (I): wherein each symbol is described herein, are useful for the prophylaxis or treatment of metabolic syndrome, diabetes, obesity and the like.

Abstract: The present invention relates to methods of treating overactive bladder and the symptoms associated therewith, for example, urinary urgency, frequency of mictruitions, nocturia, and urgency urinary incontinence. One treatment method according to the present invention comprises treatment with the beta-3 adrenergic receptor agonist solabegron. Another treatment combination according to the invention comprises solabegron, and a muscarinic receptor antagonist which results in a synergistic effect on the symptoms associated with OAB.

Abstract: Disclosed herein are methods for treating cancer comprising administering at least one immune checkpoint inhibitor and at least one Retinoic Acid Receptor or Retinoid X Receptor active agent.

Abstract: Methods and compositions are provided for increasing the anaerobic working capacity of muscle and other tissues. Also provided are compositions formulated for the sustained release of free beta-alanine. Also provided is a dietary supplement formulated, for example, as a solid food product, an edible suspension, liquid or semi-liquid as described herein.

Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

Abstract: The present invention relates to a tall oil fatty acid which is modified by saponification for use in the prevention of growth of harmful bacteria in the animal digestive tract and/or in the prevention of intestinal disorders. The invention further relates to a feed supplement and a feed composition comprising tall oil fatty acid which is modified by saponification.

Abstract: Use of polyunsaturated fatty acid derivatives as medicaments or functional foods. The present invention relates to the use of 1,2-fatty acid derivatives in the treatment or prevention of common diseases whose etiology is based on alterations (of any type) of the cell membrane lipids, for example, changes in levels, in the composition or in the structure of these lipids. In addition, for diseases in which the regulation of lipid composition and of the structure of the membranes (or proteins that interact with membranes) causes the reversion of pathological state.

Abstract: This invention is related to a novel sugar-like chemical composition and its use for diabetes therapy. Particularly, the present invention teaches the use of monosaccharide-like glycylated sugar alcohol compounds to block or reduce sugar absorption in diabetes patients, so as to prevent the risk of hyperglycemia symptoms. Glycylation of sugar alcohols is a totally novel reaction that has never been reported before. Therefore, the novelty of the present invention is that for the first time glycylated sugar alcohols not only was found but also was found to be useful for treating Diabetes mellitus. In addition, the present invention teaches a method for producing these glycylated sugar alcohols. In sum, the present invention includes not only a kind of novel sugar-like chemical compositions and its use for treating diabetes but also a state-of-the-art protocol and methodology for producing such a novel composition via glycylation of sugars and sugar alcohols.

Abstract: The concentrated liquid diet disclosed is a concentrated liquid diet having a total amount of a medium-chain fatty acid having 8 carbon atoms and a medium-chain fatty acid having 10 carbon atoms included as constitutive fatty acids of a triglyceride being 2.5 to 8.0 g per 100 kcal of the energy of the concentrated liquid diet, the concentrated liquid diet having in the total mass of the medium-chain fatty acid having 8 carbon atoms and the medium-chain fatty acid having 10 carbon atoms the rate of the medium-chain fatty acid having 10 carbon atoms being no less than 60% by mass, and the rate of the medium-chain fatty acid having 8 carbon atoms being no greater than 40% by mass.

Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of cytopathic diseases. Cytopathic diseases may be caused by a variety means such as viral infections like HIV and AIDS in a mammalian subject. The methods and compositions of the invention are effective for inhibiting de novo HIV infection, upregulating viral expression from latent provirus, inhibiting HIV-induced cytopathic effects, down regulating the HIV receptor, increasing ThI cytokine expression, and decreasing Th2 cytokine expression. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent such as those used in HAART protocols or therapeutic agents used to treat opportunistic infections due to HIV in mammalian subjects.

Abstract: The present invention relates to a composition for preventing or treating a psychiatric disorder comprising a phenyl carbamate compound and a method for preventing or treating a psychiatric disorder therewith. The present invention provides anti-anxiety activity and protections against seizure and bipolar disorder, such that it may be effectively used for preventing or treating various psychiatric disorders related to mood disorder or resulting convulsion.

Abstract: The invention is directed to a method of treating bipolar disorder in a subject, comprising administering a therapeutically effective amount of a carbamate compound, or pharmaceutically acceptable salt or amide thereof.

Abstract: The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and an anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein R1 is a hydrogen atom, an alkyl group and the like, R2, R3, and R4 are the same or different and each is a hydrogen atom, an alkyl group and the like, R5 and R6 are the same or different and each is a hydrogen atom, a halogen atom and the like, m is 0 or 1, R is a halogen atom, a cyano group, a nitro group, a phenyl group optionally substituted by an alkyl group and the like, an alkyl group and the like, Ar1 is a phenyl group, a naphthyl group, a pyridyl group, a pyrazolyl group, or the like, each of which is optionally substituted by a halogen atom, a cyano group, a nitro group, alkyl group and the like, and W is —O—, —S—, —SO2—, or —N(R7)— wherein R7 is a hydrogen atom, a (C1-C6)alkyl group and the like, or a pharmacologically acceptable salt thereof.

Abstract: The invention relates to doxepin, pharmaceutically acceptable salts and prodrugs of doxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.

Abstract: The invention disclosed herein generally relates to low-dose oral doxepin pharmaceutical formulations and the use of these formulations to promote sleep.

Abstract: The present invention relates to epicatechin for use in the prevention or reduction of symptoms of an allergic disorder and/or an allergic reaction. The invention further relates to epicatechin for said use in the form of food, food product, food supplement or pharmaceutical products.

Abstract: The invention relates to a method of treating or preventing seborrheic keratosis. The method comprises locally applying to a subject in need thereof artemisinin and/or one or more structurally related compounds. Also disclosed are topical formulations comprising artemisinin and/or one or more structurally related compounds.

Abstract: The present invention includes compositions and methods for the treatment of skin conditions by administration of a cyclolignan such as picropodophyllin and/or a derivative, metabolite, analog, prodrug, pharmaceutically acceptable salt, or hydrate thereof.

Abstract: There is provided the use as reducing agents of alpha-hydroxycarbonyl compounds capable of forming cyclic dimers. There is also provided corresponding methods of reducing reducible compounds, particularly reduction-activated prodrugs. Examples of the alpha-hydroxycarbonyl compounds used are dihydroxyacetone, glycolaldehyde, glyceraldehyde, erythrose, xylulose, erythrulose or 3-hydroxy-2-butanone.

Abstract: Provided is a composition for use in treating a skin condition, the composition comprising: (a) a first component comprising a substituted or unsubstituted diindolylmethane compound; and (b) a second component comprising a substituted or unsubstituted retinoid compound.

Abstract: Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of an active compound having the chemical structure: where n=1-4 and X is selected from the group consisting of hydrogen, lithium sodium, potassium, rubidium, cesium and francium.

Abstract: Roflumilast crystals have been shown to increase in size during storage. The size of the roflumilast crystals can affect the bioavailability and efficacy of a pharmaceutical composition. The growth of roflumilast crystals can be inhibited during storage by including hexylene glycol in the composition. The resulting composition has improved bioavailability and efficacy and can be used to inhibit phosphodiesterase 4 in a patient in need of such treatment.

Abstract: Provided is a sustained-release preparation containing pioglitazone or a salt thereof as an active ingredient and showing superior sustainability. A sustained-release preparation containing pioglitazone or a salt thereof, which shows a dissolution ratio of pioglitazone of average 25-58% at the 2-hour time point, and average 60-100% at the 4-hour time point, in a dissolution test according to the 50 rpm USP Paddle Method and using pH 2.0 KCl/HCl buffer at 37° C. as a test solution.

Abstract: Crystalline forms of 5-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

Abstract: Provided herein are methods for inhibiting osteolysis or treating osteoporosis in a subject in need thereof, the method including administering to the subject at least one RON inhibitor. The osteolysis may be caused by a condition selected from the group consisting of cancer, inflammation, and cyst. The condition may include a bone tumor or a tumor located in bone. The subject may have been diagnosed with bone cancer. The inhibitor may be ASLAN002. The inhibitor may be OSI-296. The inhibitor may be selective or specific for RON. The inhibitor may not depend on the function of RANKL or TGF?.

Abstract: An acetic acid ester compound represented by the following formula (I) or a salt thereof, wherein R represents optionally substituted deuterated lower alkyl, is disclosed.

Abstract: The invention concerns a storage stable pharmaceutical preparation comprising oxycodone and naloxone for use in pain therapy, with the active compounds being released from the preparation in a sustained, invariant and independent manner.

Abstract: A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]-heptanedicarboxyimide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.

Abstract: This invention relates to the new use of the compound 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-?]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide (orvepitant) or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing it and one or more therapeutic agents for the treatment of chronic cough, including chronic refractory cough and to combinations for such a use.

Abstract: Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.

Abstract: This disclosure relates to the uses of compounds that target an interaction between CHFR and PARP1. In certain embodiments, the disclosure relate to treating cancer by administering a mitotic inhibitor such as a taxane and a vinca alkaloid in combination with a compound that inhibits CHFR and PARP1 interactions, such as 5-((1-benzyl-1H-indol-3-yl)methylene)-1-(3,4-dimethylphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione, derivatives or salts thereof, optionally in further combination with a third anti-cancer agent.

Abstract: Methods of treating a head and neck cancer are disclosed.

Abstract: A tau aggregation inhibitor can sufficiently inhibit a tau protein from aggregating in cells. The inhibitor includes a 4-substituted catechol structure compound, having, at position 4 of its catechol ring, an electron-donating substituent R other than a hydrocarbon group, or a salt thereof. The 4-substituted catechol structure compound is preferably 4-aminocatechol or 1,2,4-benzenetriol. Examples of tauopathies to which this inhibitor is applicable include AD, Down's syndrome, frontotemporal dementia, cotricobasal degeneration (CBD) and progressive supranuclear palsy (PSP).

Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.

Abstract: Disclosed are pharmaceutical compositions comprising brimonidine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.

Abstract: Disclosed are pharmaceutical compositions comprising brimonidine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.

Abstract: The present invention provides a method of using arylpiperazine derivatives for treating attention deficit hyperactivity disorder (ADHD). The method comprises a step of administering to a patient in need thereof an effective amount of a compound of Formula 1, which is an arylpiperazine derivative.

Abstract: Disclosed are compounds of general formula (I): and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.

Abstract: The invention relates to pharmaceutical compositions for emergency contraception, to the use of levonorgestrel in combination with COX inhibitors for the preparation of pharmaceutical compositions for the stated purpose, and to a method for preparing these pharmaceutical compositions.

Abstract: Topical pharmaceutical compositions are described comprising, based on the total weight of the composition: a) 0.01 to 0.2 wt. % of mometasone furoate, b) 5 to 18 wt. % of hexylene glycol, c) 20 to 40 wt. % of water, and d) 25 to 70 wt. % of an oil phase. Said compositions are stable and can be safely and easily applied over large surface areas of the skin in an acceptable way by the general patient population for the treatment or prevention of psoriasis, atopic dermatitis (atopic eczema) and other skin disorders or diseases.

Abstract: An inventive composition including an amount of sugar or sugar alcohol, an amount of alkalizing agent, and an amount of vehicle; whereby the inventive composition is formulated for transdermal administration to alleviate one or more disorder symptoms, for example neurogenic pain, or to treat one or more disorders, for example neurogenic inflammation.

Abstract: The disclosure provides an oral antiviral supplement composition comprising a lysine, an ascorbic compound, a flavonoid glycoside, a threonine, and a pyridoxine. The disclosure also provides a method of reducing viral replication in a cell comprising treating a virus-infected cell with a composition of the disclosure. The disclosure further provides a method for the treatment and prophylaxis of a viral infection in a patient comprising administering a composition of the disclosure.

Abstract: The present invention provides a method for the treatment of immune mediated or immune related diseases or disorders, infectious diseases, metabolic disorders and cancer in mammalian subjects. This method comprises the administration of a naturally occurring, mammalian intermediary metabolite or T cell receptor ligand, preferably a glucosylceramide, to a mammalian subject. In a preferred embodiment, such mammalian subjects are human beings.

Abstract: The present invention generally relates to concentrated natamycin suspension formulations for inhibition of fungal growth. Specifically, the present invention relates to stable suspension concentrate formulations comprising from about 25% to about 48% w/w natamycin, from about 0.1% to about 10% w/w of an anionic surfactant selected from the group consisting of polyelectrolyte polymers, modified styrene acrylic polymers, dioctyl sodium sulfosuccinates, sodium salts of naphthalene sulfonates, and combinations thereof, and water. The formulations of the present invention contain natamycin as particles which are on average less than 11 microns in diameter and the formulations have a viscosity of less than 1400 centipoise at 21 degrees Celsius.

Abstract: The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m?-X]p-L; (iii) AFA-[X-(L)n?]q; or (iv) (AFA)m?-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m? is 1 to 10; p is 1 to 10; n? is 1 to 10; and q is 1 to 10, provided that q? and n are not both 1; and m? is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.