Abstract: CDDO-compounds in combination with other chemotherapeutic agents induce and potentiate cytotoxicity and apoptosis in cancer cell. One class of chemotherapeutic agents include retinoids. Cancer therapies based on these combination therapies are provided. Also provided are methods to treat graft versus host diseases using the CDDO compounds.

Abstract: Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, 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: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.

Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.

Abstract: A composition comprises a mixture of a silicone and a solvent. The composition further comprises a drug selected from the group of retinoids, retinyls, vitamin A esters, vitamin D analogues, and combinations thereof. The composition further comprises a salt of a dialkyl sulfosuccinate, such as dioctyl sodium sulfosuccinate (DOSS). The composition yet further comprises and a solubilizer. The salt of a dialkyl sulfosuccinate solubilizes the drug. The solubilizer solubilizes the salt of a dialkyl sulfosuccinate. The composition can be topically applied to a substrate, such as skin, for delivering the drug. Drugs with a wide solubility range are soluble and compatible in the composition without separation or crystallization of the drugs occurring.

Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.

Abstract: A novel encapsulated product is provided and includes: at least one pharmaceutical; at least one compressible material; and at least one tableting material; wherein the encapsulated product is in the form of a caplet having a diameter of from about 1 millimeter to about 7 millimeters and a length from about 1 millimeter to about 7 millimeters. A method for preparing the encapsulated product is also provided.

Abstract: This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.

Abstract: A composition comprises a mixture of a silicone and a first solvent, a drug, such as a hydrophilic or lipophilic pharmaceutical agent, a salt of a dialkyl sulfosuccinate, such as dioctyl sodium sulfosuccinate (DOSS), and a second solvent, such as an alcohol. The salt of a dialkyl sulfosuccinate solubilizes the drug. The composition can be topically applied to a substrate, such as skin, for delivering the drug. Drugs with a wide solubility range are soluble and compatible in the composition without separation or crystallization of the drugs occurring.

Abstract: A muscarinic receptor antagonist is useful for the treatment or prevention of a condition associated with excess sebum production or excretion.

Abstract: The present invention belongs to the fields of pharmacology, medicine and medicinal chemistry, and provides methods and compositions for treating sexual dysfunction; more particularly, the invention relates to treatment of premature ejaculation in humans.

Abstract: A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gastrointestinal (GI) toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulcerations and/or other tissue disorders. The composition of the invention are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulsion for internal, oral, direct or topical administration.

Abstract: Acne disease states, notably acne vulgaris, are treated with naphthoic acid compounds and particularly adapalene in association/combination with light therapy.

Abstract: The invention features a method of (i) reducing the appearance of pores or oil on the skin and (ii) evening skin tone or smoothing skin by applying to an area of skin in need of such treatment a composition including an anti-acne agent, an antimicrobial agent, and a lactate.

Abstract: Dermatological compositions contain, formulated into a physiologically acceptable medium, at least one retinoid compound selected from among all-trans retinoic acid, isotretinoin, motretinide, and naphthoic acid compounds of formula (I), and salts and esters thereof: wherein R is a hydrogen atom, a hydroxyl radical, a branched or unbranched alkyl radical having from 1 to 4 carbon atoms, an alkoxy radical having from 1 to 10 carbon atoms, or a cycloaliphatic radical which is substituted or unsubstituted, and benzoyl peroxide, and also at least one anti-irritant compound selected from among 18?-glycyrrhetinic acid, and its salts and derivatives thereof.

Abstract: Methods are provided for evaluating osteoarthritis (OA), for example for diagnosing OA, to confirm a diagnosis of OA, to assess or prognose progression of OA, determining the severity of a subject who has OA, and determining a subject's risk of developing OA in the future, as are arrays and kits that can be used to practice the methods. In particular examples, the method includes determining an amount of activity (such as an amount of protein present or an amount of expression) of OA risk-related molecules, such as soluble vascular adhesion protein 1 (sVAP-1) or interleukin-15 (IL-15). Also provided are methods of identifying one or more compounds that alter the activity of an OA-related molecule, thereby identifying potential anti-osteoarthritis drugs.

Abstract: The invention provides an assay for determining whether a test agent is a COX modulator. In general terms, the assay includes: determining whether a test agent modulates binding of a PDZ-containing polypeptide to a COX PL-containing polypeptide. The PDZ-containing polypeptide may contain the PDZ domain of PDZ domain of MAGI1, TIP-1, MAST2, PSD95, or SHANK. The assays may be done in a cell-free environment or in a cellular environment, particularly using a neuronal cell. The invention finds use in a variety of therapeutic applications, including for identifying agents for use in treating cancer, pain, inflammation and neuronal conditions caused by acute insult, e.g., stroke.

Abstract: Compounds selected from: where DRUG-OH, DRUG-COOH and DRUG-NH2 are biologically active compounds; each X is independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone moiety), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO—, where y is 2-4 or 6-24 and —(CH2CH2O)zCH2COO—, where z is 2-24; each Y is independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester moiety), —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety), —CO(CH2)mO—, where m is 2-4 or 6-24 and —COCH2O(CH2CH2O)n— where n is between 2-24; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; and p is 1-6. Multi-functional compounds and drug dimers, oligomers and polymers are also disclosed.

Abstract: Dermatological disorders having an inflammatory or proliferative component, notably common acne, are treated with topically applicable pharmaceutical compositions containing about 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously formulated into topically applicable gels, preferably aqueous gels, creams, lotions or solutions.

Abstract: Pharmaceutical formulations are disclosed comprising a multi-phasic pharmaceutical composition comprising an active pharmaceutical ingredient, wherein the active pharmaceutical ingredient is in a particulate state, a solubilized state, or in both a particulate state and in a solubilized state; a solvent; a non-miscible liquid; a stabilizer, and water; wherein the pharmaceutical formulation is an oral dosage form. Such pharmaceutical formulations are capable of reducing the fed/fast variability and improving oral bioavailability to which a number of active pharmaceutical ingredients are susceptible. The pharmaceutical formulations of the invention, therefore are bioequivalent in fed and fasted states and improved oral bioavailability.

Abstract: Topical compositions containing from 0.01% to 0.09% by weight of adapalene or salts thereof are useful for the treatment or prevention of keratinization disorders, particularly acne, and additionally contain at least one gelling agent selected from among carbomers, polysaccharides, cellulose and its derivatives, copolymers of acrylate and of alkyl acrylate, copolymers of acrylamide and of sodium acrylamido-2-methylpropanesulfonate, and xanthan gum.

Abstract: This document involves methods and materials related to inhibiting cyclin D polypeptide activity. For example, this document provides methods and materials that can be used to (1) identify mammals or cells in need of cyclin D polypeptide inhibition and (2) administer an agent capable of inhibiting cyclin D polypeptide activity.

Abstract: Adapalene or pharmaceutically acceptable salt thereof is administered to an individual in need of such treatment for modulating the expression of IL-1ra by the cells of acneic epidermis.

Abstract: Fused aromatic compounds of Formula I are PPAR gamma agonists or partial agonists and are useful for weekly dosing in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

Abstract: Adapalene or pharmaceutically acceptable salt thereof is administered to an individual in need of such treatment for modulating the expression of CD1d or IL-10 in an inflammatory acneic lesion.

Abstract: Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.

Abstract: Provided is a method of treating a patient having an inflammatory disease by using a compound which inhibits the ABCC4-mediated release of leukotrienes, a medicament containing such compound and methods for screening such compounds.

Abstract: A method for producing a composition comprising nanoparticles of a biologically active compound.

Abstract: The present invention relates to the treatment of estrogen-dependent hyperproliferative uterine disorders including endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and their related symptoms by intravaginally administering at least two active agents selected from an aromatase inhibitor, an antiinflammatory agent, and a uterine-selective estrogen receptor antagonist. This combination therapy reduces local estrogen production, blocks local estrogen action, and suppresses inflammation locally, resulting in starvation of the estrogen-dependent diseased tissues, relief of related symptoms, and retardation of disease progression. Intravaginal delivery maximizes local inhibition of estrogen production without significantly affecting systemic circulating estrogen levels. This results in enhanced clinical efficacy and reduced side effects.

Abstract: The invention relates to the field of organic chemistry and medicine, in particular to virology. More specifically the invention relates to a novel chemical compound N?-{N-[3-oxo-lupan-28-oyl]-9-aminononanoyl}-3-amino-3-phenylpropionic acid of formula 1 and to pharmaceutically acceptable salts and prodrug forms thereof exhibiting an anti-viral (anti-HIV) and immunostimulating activity. A method for producing the compound of formula 1 and the use thereof for the manufacture of a medicinal agent exhibiting an anti-viral (anti-HIV) and immunostimulating activity is also disclosed.

Abstract: Provided is a fecal condition improving composition containing (a) a compound selected from the group consisting of caffeic acid, chlorogenic acid and ferulic acid, esters thereof, and pharmaceutically acceptable salts thereof, (b) a water-soluble and hardlyfermentable dietary fiber, and (c) a water-soluble and fermentable dietary fiber. The composition of the present invention is useful as a food or beverage, or a pharmaceutical for improving the fecal condition of humans or animals, more specifically, inhibiting intestinal clamping due to imbalance of the autonomic nervous system caused by psychological stress or dietary change, suppressing abdominal pain or discomfort, improving the fecal condition, and ameliorating constipation.

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: 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: Administration of adapalene in a topical medicament to a patient so as to sustain its biological response in the treatment of acne vulgaris, wherein the administration pattern of the topical medicament comprises topically applying onto the afflicted skin area a therapeutically effective amount of adapalene at least once every two days for at least 6 months.

Abstract: A combination comprising (a) at least one 6-dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol component, and (b) at least one non-steroidal anti-inflammatory drug (NSAID) component; a pharmaceutical composition and a dosage form comprising such as combination, and a method of treating pain and/or ostheoarthritis in a mammal characterized in that components (a) and (b) are administered simultaneously or sequentially to said mammal, in which component (a) may be administered before or after component (b), and in which components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.

Abstract: The present invention relates to agonists of the hTAS2R14 bitter taste receptor and its role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block hTAS2R14 bitter taste transduction or bitter taste response.

Abstract: The present invention refers to the use of at least one tricyclic diterpenes for the manufacture of a nutraceutical or pharmaceutical for the treatment, co-treatment or prevention of inflammatory disorders and/or joint disorders.

Abstract: The present invention relates to novel composition for the treatment, co-treatment or prevention of inflammatory disorders comprising an effective amount of carnosic acid 12-methylether.

Abstract: The invention relates to a composition for topical application comprising as an active ingredient a peroxide and a retinoid wherein one of said peroxide and retinoid is in the form of first microparticles comprising a solid particulate matter of the active ingredient coated by a metal oxide layer and the other of said peroxide and retinoid is present in an uncoated free form or in a coated form of the active ingredient. The invention further relates to method for treating a surface condition in a subject using said composition, a method for preparing a composition exhibiting improved stability, and a kit comprising: (a) a first composition comprising a peroxide as a first active ingredient; and (b) a second composition comprising a retinoid as a second active ingredient; at least one of said first and said second active ingredient being coated by a metal oxide layer.

Abstract: Disclosed herein is a preparation for topically delivering and localizing therapeutic agents, comprising: a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; and a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Further disclosed is an associated method of topically delivering and localizing therapeutic agents, comprising the steps of: using a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; in combination with using a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Also disclosed are various courses of treatment which comprise applying the various disclosed combinations of agents to the patient's skin.

Abstract: A process for producing a solubilized non-steroidal anti-inflammatory drug (NSAID) the process comprising the steps of: providing a mixture comprising solid NSAID and a first base which is selected from the group of bases which have a pH of at least 11 as 0.1 molar aqueous solution or dispersion, and reacting the NSAID and the first base in essentially dry state, solubilized NSAID obtainable by this process and pharmaceutical compositions comprising the same.

Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Abstract: The use of a non-steroidal anti-inflammatory drug for the treatment of nonproductive cough caused by viruses or bacteria and a combination of at least one non-steroidal anti-inflammatory drug with at least one antitussive in a formulation to treat coughs.

Abstract: This invention provides biodegradable, sustained-release pharmaceutical compositions of non-steroidal, anti-inflammatory drugs (NSAIDs) formulated with biocompatible, biodegradable tyrosine-derived polyarylates. The compositionsare particularly suitable for localized delivery of NSAIDs for various disease states. For example, implantation of the compositions at the site of surgery leads to relatively high local concentrations of the NSAID to reduce or alleviate post-surgical pain. Long term zero order release of certain NSAIDs can also be provided by with certain polymer formulations.

Abstract: Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.

Abstract: A powder comprising nanoparticles of a sparingly water-soluble drug prepared in accordance with the present invention exhibits enhanced bioavailability without generating adverse side effects caused by impurities, while the nano-particle size of the drug remains unchanged when administered. Accordingly, the powder can be useful for the development of a formulation of a sparingly water-soluble drug for oral and parenteral administration.

Abstract: Administration of adapalene in a topical medicament to a patient so as to sustain its biological response in the treatment of acne vulgaris, wherein the administration pattern of the topical medicament comprises topically applying onto the afflicted skin area a therapeutically effective amount of adapalene at least once every two days for at least 6 months.

Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from retinoid compounds—has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of retinoid compounds in a composition by at least 3-fold and as much as 10-fold or greater. The ability of the alkoxycrylene compounds to stabilize the retinoid compound is concentration dependent, with the amount of retinoid photostabilization increasing with the concentration of the alkoxycrylene compound.

Abstract: The invention provides compositions comprising sulindac, R-epimer sulindac, S-epimer sulindac, derivatives, metabolites, and structural analogs thereof which protect normal cells against damage caused by solar rays, oxidative damage, environmental factors, diseases and organisms.

Abstract: Disclosed are compositions and methods for preventing or reducing postoperative ileus and gastric stasis. Such compositions include a combination of a carrier component and a bioactive component which acts to prevent or reduce post-operative ileus. Such methods include administering atherapeutically effective amount of the composition directly to the serosal surfaces of the gastrointestinal and other visceral organs.