Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: Topically applicable cosmetic/pharmaceutical compositions contain at least one retinoid and at least one anti-irritant compound selected from among the salts of 18?-glycyrrhetinic acid and derivatives thereof, and are useful for the treatment and/or prevention of a dermatological condition or affliction related to a disorder of keratinization relating to cell differentiation and to cell proliferation, e.g. acne vulgaris.

Abstract: The present invention relates to compositions and methods for inhibition of signal transduction pathways in cancer cells. In particular, the present invention provides methods and compositions comprising Wnt and Hedgehog pathway inhibitors for reducing proliferation of adenocarcinoma cells.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.

Abstract: Provided is a method for treating a condition or disease which is one of the indications for NSAID use, which comprises administering a combination of: (a) a pharmaceutically effective amount of a NSAID, and (b) a pharmaceutically effective amount of a prostaglandin (PG) compound represented by the formula (I): to a subject in need thereof.

Abstract: A transdermal preparation for external use which contains a photosensitive NSAID and a UV blocker having a high ability to migrate into the skin. Thus, it becomes possible to ensure, in a transdermal preparation for external use containing a NSAID, the inhibition of the onset of light-induced non-immunological or immunological skin symptoms by the above-described component.

Abstract: Methods for improving pain management in a mammal, the methods comprising administering a combination of a strontium-containing compound and a second therapeutically and/or prophylactically active substance selected from the group consisting of analgesic agents, anti-inflammatory agents and palliative agents to the mammal. Pharmaceutical compositions for use in such methods, comprising a strontium-containing compound and a second therapeutically and/or prophylactically active substance selected from the group consisting of analgesic agents, anti-inflammatory agents and palliative agents.

Abstract: Novel biaryl compounds having the structural formula (I): are useful in a variety of pharmaceutical applications, whether human or veterinary, and also in cosmetics.

Abstract: A cooling composition comprising at least one compound of the Formula I in which R is selected from the group of moieties consisting of (CH2)nCOOR?; (CH2)nCONMe2; (CH2)nOR?; and CHNH2CH3; where n is 1-3 and R? is independently selected from hydrogen, methyl and ethyl; and R? is selected from the group consisting of the moieties fenchyl, D-bornyl, L-bornyl, exo-norbornyl, 2-methylisobornyl, 2-ethylfenchyl, 2-methylbornyl, cis-pinan-2-yl, verbanyl and isobornyl. The compositions are useful in providing cooling sensations to the skin or mucous membranes of the body.

Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: This disclosure ascribes new functions to derivatives of tetralin, anthraquinone, naphthylamine, tri-amino-pyrimidine, xanthen-3-one, and/or cinnamic acid (including, for example, NSC270718R, NSC117285R, NSC170008Y, NSC306711P, NSC119913X, NSC119915Z, NSC119911V, NSC119910U, NSC128437O, NSC125908P, NSC9600Q, or NSC13778J, each obtained from the Structure Diversity Set, National Institutes of Health, National Cancer Institute, Developmental Therapeutics Program). These compounds are shown to be effective inhibitors of viral essential protein kinases (such as poxvirus B1 and/or F10 protein kinases). Exemplary chemical structures for viral protein kinase (VPK) inhibitors are provided, as are methods of using such compounds, for instance, to inhibit VPK activity and/or poxvirus growth, and/or for the treatment of poxvirus infection. Also provided are pharmaceutical compositions including disclosed VPK inhibitors.

Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.

Abstract: The present invention relates to compositions, kits and methods for administration of a first component of fumaric acid ester(s), or a pharmaceutically acceptable salt thereof, and a second component which is a substance that reduces or eliminates flushing.

Abstract: A method includes (i) contacting a polymeric material with a first solvent to produce a pre-extracted polymeric material, and (ii) contacting the pre-extracted material with a solution comprising one or more therapeutic agents and a second solvent to incorporate the therapeutic agents into the pre-extracted polymeric material. The first or second solvents are the same or different.

Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: The present invention relates to the use of one or more retinoid agonists and/or antagonists comprising retinoids with selective Retinoid X Receptor (RXR) agonistic or antagonistic activity alone or in combination with one or more peroxisome proliferator activated receptor (PPAR) ligands for the manufacture of a medicament for the (preferably oral or topical) treatment (this term including prevention/prophylaxis and/or therapy) of one or more manifestations of metabolic syndrome (also known as syndrome X), also called diseases hereinafter, especially from one or more manifestations thereof selected from the group consisting of diabetes type II, obesity, dyslipidemia, hypertension and polyneuropathy, each of which can also be linked with a high risk of cardiovascular diseases. Corresponding methods, the compounds and combinations for use in the treatment of the mentioned diseases and comparable invention embodiments are also described.

Abstract: This invention relates to compositions comprising co-crystals of (?)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (?)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Abstract: This invention relates to methods and compositions for the attenuation of HIV-1 replication in human cells, and especially in human macrophages. The invention particularly concerns the use of inhibitors of P21 (CDKN1A) expression to attenuate such replication. The invention particularly concerns the use of antisense P21 oligonucleotides, siRNA and/or 2-cyano-3,12-dioxooleana-1,9-dien28-oic (CDDO) to attenuate such replication.

Abstract: Retinoids with retinoid antagonistic activities, especially Retinoid X Receptor antagonists called RXR antagonists, pharmaceutically acceptable salts and pharmaceutically acceptable esters and amides thereof, have been found to be efficacious in the treatment of inflammatory diseases of the skin and mucous membranes, and of other tissues and organs for example by topical or oral administration of RXR antagonists.

Abstract: The present invention relates to an improved method for treating a wide range of inflammatory disorders by administering a tetracycline compound together with an effective inhibitor of tetracycline absorption, such as polyvalent metals. Pharmaceutical compositions used in that method are also taught.

Abstract: Depigmenting compositions for the skin, comprise, formulated into a physiologically acceptable medium, adapalene, at least one depigmenting agent and at least one anti-inflammatory agent, and to the pharmaceutical/cosmetic applications thereof.

Abstract: The present invention provides compositions and methods for alleviating physical discomfort and/or pain-related conditions in a subject, comprising one or more ingredients that improve blood circulation, one or more ingredients that reduce pain and one or more ingredients that enhance bone health. The ingredients are selected from synthetic compounds, natural products, natural ingredients, extracts from natural ingredients, or combinations thereof. The compositions of the invention are particularly useful in alleviating musculoskeletal pain and nerve related pain.

Abstract: Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C?O or C?N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):

Abstract: The invention relates to a composition for topical application to the skin comprising effective amounts of a protease inhibitor and a cell differentiation enhancer. The composition is useful in promoting skin lipid barrier repair and maintaining the integrity of the lipid barrier. In this regard, the compositions can be used in the treatment and prevention of dry skin, and associated chrono/proto-aging conditions, in the treatment and prevention of irritation on the skin, in the treatment and prevention of UV-related damage to the skin, and in the enhancement of the retention of self-tanning.

Abstract: Disclosed is a rapidly disintegrating solid oral dosage form of a poorly soluble active ingredient and at least one pharmaceutically acceptable water-soluble or water dispersible excipient, wherein the poorly soluble active ingredient particles have an average diameter, prior to inclusion in the dosage form, of less than about 2000 nm. The dosage form of the invention has the advantage of combining rapid presentation and rapid dissolution of the active ingredient in the oral cavity.

Abstract: The conjugates of present invention are formed by the combination of rhein or their analogues with the organic bases or amino acids in molecular force between them. The methods for preparing the conjugates and their uses for manufacturing medicines in the treatment of diabetic nephrosis, recovery of gastrointestinal function and prevention of intestinal adhesion, as well as treatment of osteoarthritis, rheumatic arthritis and rheumatoid arthritis are also described. Rhein or their analogues as the left part of general formula (I) is selected from (1) the compounds of rhein or their analogues, in which one or two substituents of R2˜R3 and R6˜R7 are COOH at least two substituents of R1˜8 are —H; or (2) the rhein-containing extract derived from plants. In general formula (I), M represents nitrogen-containing organic bases or basic amino acids.

Abstract: Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.

Abstract: Compositions and methods are disclosed for treating melanoma wherein a betulinic acid derivative is the active compound in the composition to be administered. The compositions are optionally applied topically is inserted therefor.

Abstract: A composition containing 1,4-dihydroxy-2-naphthoic acid at a high concentration is obtained by intracellularly and extracellularly producing 1,4-dihydroxy-2-naphthoic acid using a bacterium belonging to the genus Propionibacterium and collecting it. This composition is efficacious in improving intestinal flora, alleviating abdominal ailments in association with the intake of milk, and preventing metabolic bone diseases.

Abstract: The present invention relates to the use of benzoic acid and/or its sodium salt in combination with saccharide(s) as active components in the manufacture of a vaginal composition for modulating vaginal flora and vaginal acidity, thereby maintaining the pH value of vaginal secretion within a range from 3.5 to 4.5; and the present invention further relates to a vaginal composition and a method for modulating and maintaining normal vaginal flora and vaginal acidity.

Abstract: The present invention relates to a topical skin care composition containing a safe and effective amount of a skin care active comprising agmatine, and its salt; a safe and effective amount of a first additional skin care active selected from the group consisting of BHT or BHA, hexamidine, cetyl pyridinium chloride, green tea catechins, phytosterols, ursolic acid, compounds derived from plant extracts, their salts and derivatives; and a dermatologically acceptable carrier for the agmatine composition. The present invention also relates to methods of using such agmatine compositions to regulate hair growth and the condition of mammalian skin. Said methods generally comprise the step of topically applying the composition to the skin of a mammal needing such treatment, a safe and effective amount of such compositions.

Abstract: A treatment is disclosed for alleviation or prevention of abnormal blood flow to various organs such as the eye, brain, kidneys, heart, feet and other tissues of organs with fine vascular networks that can lead to neurodegeneration as is seen in wet age-related macular degeneration (AMD), epilepsy and diabetes, in which an effective amount of a blood flow regulatory drug is administered to a subject in need of it. Illustrative blood flow regulatory drugs include anticoagulants and vasodilators, and their mixtures.

Abstract: The present invention is directed to dosage forms that can be used in therapeutic methods involving the oral co-administration of a combination of at least two drugs, one of which impairs gastrointestinal absorption and one of which does not. The dosage forms are designed so that the drug impairing absorption is not released into the gastrointestinal tract of a patient until after the drugs that do not impair absorption have been released and substantially absorbed. The invention may be used in treatment of migraine using a combination of triptans and NSAIDs or in the treatment of pain using a combination of NSAIDs and opioid analgesics.

Abstract: The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors. The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.

Abstract: Multifunctional, single, bilayer, and trilayer coated tablets for combination therapy are formed wherein the bioactive agents responsible for the therapeutic multifunctionality are present as a combination of a gastric acid-reducing agent, such as omeprazole and ranitidine, and at least one analgesic/anti-inflammatory agent, such as acetaminophen, naproxen sodium, ibuprofen, tolmetin, and aspirin.

Abstract: The present invention provides a method of administering adapalene for the maintenance therapy of acne vulgaris to prevent acne recurrence or reduce the severity of the acne recurrence.

Abstract: The present invention relates to an anti-aging cosmetic composition, and more particularly, the present invention relates to an anti-aging cosmetic composition containing Hibiscus esculentus extracts and at least one selected from the group consisting of oleanolic acid, ursolic acid, glycyrhetinic acid and retinol, showing high safety to skin and wrinkle-improvement effect.

Abstract: An composition and related method that prevents, inhibits and/or mitigates an allergic response by down regulating the production of IgE, down regulating the binding of IgE antibodies to receptors on cells, and/or inhibiting allergy mediators, for example, histamine, prostoglandin D2, or luekotriene C4 release. The composition comprises at least one of the following ingredients: luteolin from Perilla leaf or seed, Cinnamon, Kiwi, Picao preto, Hesperidin, Acerola cherry, Guaco, Holy Basil, Kakadu, Solamum, Rosmarinic acid, Tinospora and Aframomum. In one embodiment, the composition at least three different ingredients selected from Cinnamon, Acerola, Luteolin and Picao preto. Optionally, these ingredients can be combined with at least one of Aframomum, Rosmarinic acid, and Tinospora. The composition is administered with effective amounts to prevent, inhibit and/or mitigate allergic responses.

Abstract: A drug for inhibiting the production of matrix metalloproteinase-9 which contains leptomycin B or its derivative as the active ingredient can specifically inhibit the production of MMP-9 compared with MMP-2, furthermore, has an effect of inhibiting the production of MMP-9 even under stimulating the differentiation by adding calcium at a high concentration or adding TGF-?, and under stimulating for inducing inflammation by adding TNF-? or adding IL-2?.

Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with hydrogen peroxide or another oxidizing agent, such as arsenic trioxide that generates reactive oxygen species (ROS), significantly enhances the killing of cancer cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against cancer cells. A skin cream has been developed and used to treat skin cancer and precancerous skin growths that effectively removes the lesions with no effect on surrounding normal skin.

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract: A composition containing 1,4-dihydroxy-2-naphthoic acid at a high concentration is obtained by intracellularly and extracellularly producing 1,4-dihydroxy-2-naphthoic acid using a bacterium belonging to the genus Propionibacterium and collecting it. This composition is efficacious in improving intestinal flora, alleviating abdominal ailments in association with the intake of milk, and preventing metabolic bone diseases.

Abstract: The invention relates to an immediate release tablet capable of being chewed or disintegrated in the oral cavity, which comprises a plurality of particles in a matrix. The particles contain an active ingredient, such as ibuprofen, and a first water soluble acid having a solubility greater than about 10 g/100 mL water at 20° C.; and the matrix contains a second water soluble acid having a solubility less than about 5 g/100 mL water at 20° C.

Abstract: A method for screening for compounds or salts thereof, in particular nonsteroidal anti-inflammatory compounds or salts thereof, that are safe for gastric mucosa and cause little gastrointestinal side effects. The method uses a particular liposome to serve as a cell membrane model. The liposome encapsulates a fluorescent dye, in particular, calcein and is formed of phospholipids, such as phosphatidylcholine, phosphatidylglycerol, phosphatidylserine, and phosphatidylinositol. A test compound is allowed to react with the liposome and the leakage of the fluorescent dye from the liposome is evaluated. As a result, compounds safe for gastric mucosa, in particular, anti-inflammatory compounds can be screened.

Abstract: The present invention relates to nonaqueous preparation for percutaneous absorption prepared by laminating an adhesive layer comprising a nonsteroidal anti-inflammatory analgesic in an alkali metal salt form, and an inorganic acid which is strongly acidic compared with the nonsteroidal anti-inflammatory analgesic in a free form, together with a nonaqueous base, on a support. According to the present invention, drug-releasing characteristics and skin penetration in a nonaqueous preparation for percutaneous absorption can be improved because the addition of an inorganic acid in a nonaqueous base containing a drug in an alkali metal salt form leads to an improvement in the solubility of the drug in the base, and a good partitioning of the drug to skin surface. In addition, as the inorganic acid has no alcoholic hydroxy group in the structure, the inorganic acid does not react with the drug, therefore it causes no lowering in the stability of the drug by esterification.

Abstract: The present invention provides methods of protecting plants and other multicellular organisms from pests. The methods use substituted organic acid or substituted anthracene compounds, which act to alter the activity of one or more anion transporters in the pests. Among the pests treated are nematodes and insects. Methods of screening for such compounds are also provided.

Abstract: The present invention concerns novel derivatives of 1-phenylalkanecarboxylic acids, pharmaceutical compositions thereof, a process for their preparation and their use for the treatment and/or prevention of neurodegenerative diseases such as Alzheimer' s disease.

Abstract: A first, solid oral pharmaceutical composition includes an extended release acetaminophen, a non-steroidal anti-inflammatory drug, such as naproxen or ibuprofen, and a third drug capable of reducing gastric acid secretion, such as ranitidine or omeprazole. A second, solid oral pharmaceutical composition includes a non-steroidal anti-inflammatory drug and an agent for reducing gastric acid secretion.

Abstract: A pharmaceutical combination comprising at least a triptan and the trimebutine compound [hydrogenated maleate of 2-dimethyl-amino-2-phenylbutyl-3,4,5-trimetoxybenzoate] and an anti-inflammatory or simple analgesic for the treatment of attacks of migraine and other headaches is provided. More particularly, the present invention discloses a pharmaceutical combination comprising triptan and trimebutine for the treatment of migraine attacks. The present invention further discloses blisters and packs containing said pharmaceutical combinations.

Abstract: Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C?O or C?N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):