Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

Abstract: A compound and method for treating myocilin glaucoma using a selective Grp94 inhibitor is presented. Clearance of mutant myocilin can be promoted by selectively targeting the endoplasmic reticulum (ER) chaperone Grp94 using siRNA knockdown or small molecule inhibitors. Grp94 contributes to the intracellular accumulation of mutant myocilin. Tailored treatments aimed at disrupting the Grp94/mutant myocilin interaction can be used as a new therapeutic strategy for myocilin glaucoma. The inventors developed a compound having a general backbone structure of geldanamycin (GDA) and radicicol (RDC) in which a more hydrophobic surrogate of the quinone in GDA is linked to the resorcinol in RDC through a cis-amide bioisostere.

Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: The present invention relates to an allosteric non-inhibitory chaperone of the lysosomal acid alpha-glucosidase (GAA) for use in the treatment of a pathological condition characterized by a deficiency of the lysosomal acid alpha-glucosidase (GAA), to pharmaceutical composition thereof, to a method for increasing the activity of GAA in a subject and to a method for identifying an allosteric non-inhibitory chaperone for GAA.

Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).

Abstract: The present invention relates to dietary compositions comprising reduced level of methionine, tryptophan, all amino acids, or protein, dietary compositions comprising glycerol as a substitute for monosaccharides, disaccharides, and polysaccharides, and hypocaloric or calorie free diets with reduced level of energy, carbohydrates, or protein. Also disclosed are methods of using these compositions and diets, as well as fasting, to protect subjects against chemotherapy, radiotherapy, oxidative stress, or aging.

Abstract: Disclosed is a method comprising the administration of a 3% amino acid and 3% glycerin solution for the use of prevention and disruption of bacterial biofilms. Also disclosed is method comprising the administration of L-cysteine 0.4 g per 100 ml for the prevention and destruction of fungal biofilms.

Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.

Abstract: Several embodiments provided herein relate to histamine dosing regimens are and uses of such regimens in the restoration of histamine balance in subjects suffering from, for example, histapenia and/or histadelia. Several embodiments also relate to the use of histamine dosing regimens for the treatment and/or prevention of migraine headaches.

Abstract: Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The invention provides improved methods for coadministration of colchicine with drugs metabolized by CYP3A4 (anciently referred to as cytochrome P450 isozyme 3A4) or the P-glycoprotein transporter, but not both. The method enables non-toxic coadministration of colchicine and the second drug at their ordinary levels safely and effectively without reducing the dose or frequency for either drug.

Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2/STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines.

Abstract: The invention provides improved methods for coadministration of colchicine with drugs metabolized by CYP3A4 (anciently referred to as cytochrome P450 isozyme 3A4) or the P-glycoprotein transporter, but not both. The method enables non-toxic coadministration of colchicine and the second drug at their ordinary levels safely and effectively without reducing the dose or frequency for either drug.

Abstract: The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. The invention also relates to cosmetic or dermocosmetic compositions intended to fight skin disorders associated with said glycosylation by-products.

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 method for treating platinum drugs induced vestibulotoxicity, comprising administering a compound that impairs or prevents accumulation of platinum drugs within vestibular hair cells and/or vestibular primary neurons.

Abstract: The present invention relates to novel isocyanate and isothiocyanate compounds, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans and animals. The novel isocyanate and isothiocyanate compounds are distinguished, as compared with the known isocyanate and isothiocyanate compounds, by improved therapeutical breadth, i.e. fewer side effects while having high anti-tumor activity.

Abstract: Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.

Abstract: The present invention relates to specific analogs of combretastatin, in particular the compounds of formula (I) as described and defined herein, and pharmaceutical compositions comprising the compounds, as well as their medical use, in particular in the treatment or prevention of cancer, including multidrug-resistant cancer.

Abstract: Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.

Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: The invention relates to medicine and comprises an agent for the treatment of a viral hepatitis C, which is glutaryl histamine or a pharmaceutically acceptable salt thereof. This agent can also be administered in combination with a pegylated interferon and ribavirin. The invention further relates to a pharmaceutical composition for the treatment of a viral hepatitis C. This invention solves the problem of providing a novel agent, which is effective in the treatment of a viral hepatitis C and makes it possible to produce a sustained virologic response.

Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.

Abstract: The tablet containing (1) 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, and (2) silicon dioxide has a high content of 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof and an easily takable size as a tablet, and shows superior dissolution property.

Abstract: Some embodiments of a system or method for applying a barrier composition to a targeted skin surface can be used to as a preventative measure to reduce the likelihood of transmission of microbial entities from an external source (e.g., a floor surface or another surface) to the targeted skin surface.

Abstract: A composition and a supplement formulation includes: at least one constituent selected from the group consisting of a nitrate, a nitrite, and both; and at least one constituent amino acid selected from the group consisting of Agmatine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, Valine, Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, and Phenylalanine.

Abstract: A composition and a supplement formulation includes at least one constituent selected from the group consisting of a nitrate, a nitrite, and both, and Arginine. A method for increasing vasodilative characteristics in a human or animal includes administering to the human or animal a composition or supplement formulation including at least one constituent selected from the group consisting of a nitrate, a nitrite, and both, and Arginine.

Abstract: Embodiments relating to cream formulations as well as oxymetazoline creams and methods for treating rosacea and symptoms associated with rosacea, including, for example, papules, pustules, phymas (skin thickening), telangiectasias or erythema associated with rosacea, other skin erythemas, telangiectasias, purpura or the like, and other manifestations associated therewith; other inflammatory conditions of the skin including, but not limited to, keratosis pilaris, lupus miliaris dissemniatus faciei, eczema, dermatitis, such as contact dermatitis, atopic dermatitis, seborrheic dermatitis, nummular dermatitis, generalized exfoliative dermatitis, statis dermatitis, neurodermatitis, lichen simplex chronicus, xerosis and xerotic dermatitis, dyshidrosis and dyshidrotic dermatitis, asteototic dermatitis or other conditions characterized by sensitive skin or a disturbance of the epidermal barrier; disorders characterized by rough, dry, cracked or fissured skin, disorders characterized by hyperkeratotic skin such as ker

Abstract: Compositions and methods are provided for treating a disorder characterized by ?-synuclein dysfunction and/or altered lipid metabolism.

Abstract: A composition and a supplement formulation includes: at least one constituent selected from the group consisting of a vegetable nitrate source, a vegetable nitrite source, and both; and at least one constituent amino acid selected from the group consisting of Arginine, Agmatine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, Valine, Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, and Phenylalanine.

Abstract: A composition and a supplement formulation includes: at least one constituent selected from the group consisting of a nitrate salt, a nitrite salt, and both; and at least one constituent amino acid selected from the group consisting of Arginine, Agmatine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, Valine, Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, and Phenylalanine.

Abstract: A Nitrate or Nitrite of a Betaine Compound disclosed. Also disclosed are a composition and a supplement formulation comprising at least one constituent selected from the group consisting of a Nitrate, a Nitrite, and both; and a Betaine Compound. The composition and supplement formulation may be formulated to deliver an effective amount of the constituents to prevent the development of nitrate tolerances, to increase bioabsorption of amino acids, or to increase the vasodilative characteristics of amino acids in a human or animal.

Abstract: Composition and methods for affecting cell proliferation, metabolism or sensitization, including the potentiation of proteasome inhibitor therapy for the treatment of disease caused by deregulation of ubiquitin-proteasome systems, in a cell or subject. The composition includes a compound in combination with a ubiquitin-proteasome inhibitor. In one embodiment, the compound has the formula C42H35N5O3 and the ubiquitin-protease inhibitor is a proteasome inhibitor or an inhibitor of another component of the ubiquitin-proteasome pathway such as an E3 ubiquitin ligase. In one embodiment of the method, the compound is administered to a cell or subject and a therapeutically effective amount of a ubiquitin-protease inhibitor is also administered. In another embodiment, the compound is administered to a cell or subject to inhibit cell proliferation. In yet another embodiment, the compound is administered to a cell or subject to increase, or augment, glucose utilization.

Abstract: Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.

Abstract: An object of the present invention is to provide an antitumor aqueous solution and an anticancer agent, both of which can kill cancer cells while having virtually no effects on normal cells, and to provide methods for producing the antitumor aqueous solution and the anticancer agent. The method of the invention for producing an antitumor aqueous solution for killing cancer cells includes an aqueous solution preparation step of preparing an aqueous solution through addition, to water, of a solute containing at least one of disodium hydrogen phosphate (Na2HPO4), sodium hydrogen carbonate (NaHCO3), L-glutamine, L-histidine, and L-tyrosine disodium dihydrate (L-tyrosine.2Na.2H2O); and a plasma irradiation step of irradiating the aqueous solution with atmospheric pressure plasma generated in a plasma generation region by means of a plasma generator.

Abstract: Ophthalmic formulations are provided. The ophthalmic formulations include one or more active agents that act to optimize pupil light reflex while minimizing, or effectively eliminating, any undesired eye redness in response to application thereof. The active agents include, for example, alpha 1 antagonists, such as alpha 1a selective antagonists.

Abstract: The present invention discloses novel agents and methods for diagnosis and treatment of melanoma. Also disclosed are related arrays, kits, and screening methods.

Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.

Abstract: A nutritional supplement composition for treating nutritional deficiencies caused by a medical condition in subjects is disclosed. The present application further discloses a method of using a nutritional supplements composition for treating a subject with complications resulting from sickle cell anemia. The method comprises administering to a subject an effective amount of the nutritional supplement.

Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

Abstract: This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds in combination with substituted imidazole compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to an animal in need thereof.

Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.

Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.

Abstract: Ophthalmic products and related methods are described herein. These methods include a stabilizing composition comprising a therapeutically active agent which is separated from a liquid vehicle composition by a barrier. The barrier may be removed to allow the two compositions to mix to provide an ophthalmically acceptable liquid comprising the therapeutically active agent.

Abstract: The invention relates to a medicament for the treatment of respiratory tract diseases selected from the group including rhinosinusitis, sinusitis, tonsillitis, bronchiolitis, pneumonia, and acute respiratory distress syndrome, wherein the medicament comprises glutaryl histamine or a pharmaceutically acceptable salt thereof in an effective amount. The invention also relates to use of glutaryl histamine or a pharmaceutically acceptable salt thereof for manufacture a medicament for the treatment of a respiratory tract disease. The medicament provides potentiating the effectiveness of antibacterial therapy for the treatment of respiratory tract diseases.

Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.