Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.

Abstract: Provided are oral pharmaceutical compositions comprising sustained release or a combination of sustained and immediate release formulation of cannabinoids, a process for their preparation and methods of use thereof.

Abstract: The present invention is directed to unsaturated sphingosine compounds which are useful as therapeutic agents for the treatment of cancer and for the treatment of other diseases including diabetes and infection with intracellular bacteria. The invention is also directed to methods of using the compounds and pharmaceutical compositions comprising the compounds in treating these diseases.

Abstract: Novel methods are presented for treating Influenza by using Targeted Transient Ribosomal Inhibition (TTRI), with TTRI drugs administered by inhalation, to silence expression of every protein underlying the etiology and pathology of the influenza infection, and without adversely effecting normal cells in the lungs. The therapeutic effect is dual Antiviral and Anti-Inflammatory activity which is localized to the lungs. Pulmonary TTRI for influenza silences expression of all 10 influenza viral proteins and de novo synthesis of cytokines and leukotrienes produced in the lungs. By targeting ribosomes, TTRI is insensitive to viral mutations or human alterations to the virus. TTRI provides an off-the-shelf solution for preventing mortality from any strain of influenza.

Abstract: A pharmaceutical composition for treating disorders associated with insulin resistance is disclosed, and the composition comprises at least one inhibitor which is an effective agent to suppress endothelin-1-stimulated resistin gene expression through decreasing the endothelin-1-stimulated phosphorylation of proteins downstream of endothelin type A receptor, wherein the downstream signaling molecules comprise ERK1/2, JNKs, AKT, and STAT3 proteins, and wherein the inhibitor is selected from at least one antagonist of the endothelin type A receptor or downstream signaling proteins.

Abstract: The invention provides methods for the identification of small molecules that inhibit MUC1 oligomerization, and the functions flowing therefrom. In addition, small molecules that prevent MUC1 oligomerization are disclosed. Identified molecules will find use in treating a variety of MUC1-related inflammatory conditions, including MUC1-related cancers.

Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.

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

Abstract: The present invention relates to a combination therapy for elevating testosterone levels in male mammals in which an antiestrogen or pharmaceutically acceptable salt thereof is co-administered to the mammal with an additional therapeutic agent selected from an androgen and an aromatase inhibitor. The invention is also directed to a combination therapy for treating males with hypogonadism and disorders related thereto, including reduction of muscle mass. limitation of body performance capacity, reduction of bone density, reduction of libido, reduction of potency, reduction of benign prostatic hyperplasia and infertility.

Abstract: Biodegradable and nutritionally attractive composition comprising biocidal or antibiotic compounds and/or microbes having bio-adhesion and controlled buoyancy properties are selectively fed to an aquatic organism in open or closed water-bodies, and bioactive components are released upon contact with mucosal tissues such as gill, skin or along the digestive tract of the selected aquatic organism.

Abstract: Oncogenic Ras-driven cancer is treated with agent by interrupting pathway comprising activation of Akt by oncogenic Ras, activated Akt causing phosphorylation of eNOS at S1177 site of eNOS to provide activated eNOS in cancer cells and activated eNOS causing activation of wildtype Ras by nitrosylation thereof at C118 to provide GTP-bound activated wildtype H and N Ras. L-NAME can be orally administered to interrupt this pathway. Wortmannin can be administered intravenously to interrupt this pathway. Novel siRNAs are disclosed useful to interrupt said pathway.

Abstract: Provided are cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers include cellulose esters of formula I: wherein n of the ?-carboxyalkanoyl group, is 3, 4, 6, or 8 to provide a ?-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from: a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ?-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n=1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone.

Abstract: Compositions and methods for providing anti-diabetic and anti-hyperlipidemia benefits to diabetic subjects currently on medication but not meeting recommended targets for blood glucose, HbA1c, blood pressure and total cholesterol.

Abstract: The present application discloses new taxane analogs, intermediates and methods for producing them. The present application is also directed to pharmaceutical formulations comprising abeo-taxanes and methods of treating cancer with the abeo-taxanes.

Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.

Abstract: The present invention relates to the fields of natural medicine and medicinal chemistry, and more particularly to a 1-oxo/acylated-14-acylated oridonin derivative of a general formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and application thereof in preparation of antitumor drugs.

Abstract: A composition comprising a tetrahydrocannabinol compound, a solvent and an acid, wherein the tetrahydrocannabinol compound may be ?8 tetrahydrocannabinol, (?)-?9-trans-tetrahydrocannabinol or a side chain alkyl derivative of either compound, the solvent may be an oil or C1-C4 alcohol (e.g. sesame oil or ethanol), and the acid may be an organic acid or a mineral acid.

Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:

Abstract: The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.

Abstract: A biotechnology process that employs membrane technology for obtaining an extract rich in tannins of ellagic acid from blackberries (Rubus spp.) and from other fruits that contain these compounds, as well as to the extract obtained using this method. The method is essentially based on baromembrane technologies that allow mechanical separation and effective fractionation between the polyphenol compounds, by interactions between the physico-chemical properties thereof, the material of the membrane and the molar mass of same, thereby allowing enrichment of a fraction of the natural extract with ellagic acid tannins and modification of the content thereof in terms of anthocyanins and other compounds such as sugars and acids.

Abstract: A composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.

Abstract: Compositions useful for weight management in an animal are disclosed. The compositions comprise one or more isoflavones or isoflavone metabolites, and in some embodiments include conjugated linoleic acid, and/or L-carnitine. Also disclosed are methods useful for weight management in an animal utilizing compositions comprising one or more isoflavones, conjugated linoleic acid, and/or L-carnitine. Preferably, the compositions and methods employ a combination of one or more isoflavones, or a combination of one or more isoflavones in conjunction with conjugated linoleic acid, and L-carnitine.

Abstract: Pharmaceutical or dermo-dermo-cosmetic compositions for topical and intravaginal application for treatment of human and veterinary affections caused by anaerobic organisms or parasites comprising quassinoids or plant extracts containing these phytochemicals, in effective amounts. Such compositions can be administered topically or intravaginally to patients in need thereof in various pharmaceutical dosage forms.

Abstract: Disclosed is a pest control composition comprising at least one pyripyropene derivative of formula (I) or agriculturally and horticulturally acceptable salt thereof and at least one other pest control agent as active ingredients. The combined use of the two ingredients can provide a better insecticidal effect.

Abstract: G-protein coupled receptors are a diverse group that are the target of over 50% of marketed drugs. Activation of these receptors results in the exchange of bound GDP for GTP in the G? subunit of the heterotrimeric G-protein. The G? subunit dissociates from the ?/? subunits and both proceed to affect downstream signaling targets. The signal terminates by the hydrolysis of GTP to GDP and is regulated by Regulators of G-protein Signaling (RGS) proteins that act as GTPase Activating Proteins (GAPs). This makes RGS proteins potentially desirable targets for “tuning” the effects of current therapies as well as developing novel pharmacotherapies. The present invention provides a convenient assay for identifying modulators of RGS proteins that can be adapted for high throughput screening utilizing the colorimetric dye, malachite green, to detect free phosphate in the presence of a test compound.

Abstract: Anti-angiogenesis methods and compositions are described. The anti-angiogenic effect is provided by application of sparstolonin B or a derivative thereof to endothelial cells. The sparstolonin B or derivative thereof can inhibit angiogenesis by targeting endothelial cell cycle progression, cell migration, and chemotaxis.

Abstract: Provided herein are polymeric particles and compounds and processes that can be used to prepare polymer-based particles and methods of using those particles to localize or concentrate a subsequently delivered agent to an in vivo site.

Abstract: The present invention provides, among other things, compositions and methods of manufacturing edible soy pod fiber comprising glyceollins. In some embodiments, methods of treating overweight, obesity, prediabetes, diabetes, or gastrointestinal dysbiosis in a subject are provided comprising orally administering a composition or food product comprising edible soy pod fiber comprising glyceollins.

Abstract: Provided herein are novel crystalline forms of Compound 1. Also provided herein are compositions and methods of uses for the crystalline forms of Compound 1.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.

Abstract: This invention belongs to the chemical-pharmaceutical field. New compounds of pterocarpanquinone family presented in formula (I) according to this invention are capable to be activated by reduction generating alkylating species intracellularly. It presents selective cytotoxic effects particularly on mammalian human and nonhuman cells that divide constantly and are useful in treating diseases and dysfunctions related to the phenomenon of undesired cell proliferation. Such compounds are also effective for the treatment of diseases or dysfunctions related to high levels of TNF-? in human and nonhuman mammals.

Abstract: The present invention relates to the compounds useful in the prevention and/or treatment of tumors. More specifically the present invention relates to inhibitors of the activity of the electron transport chains and/or the mitochondrial TCA cycle in glioma-initiating cells (GICs) for use in a method for preventing and/or treating tumors presenting glioma-initiating cells (GICs) in a subject who has undergone a prior removal of a tumor glioma bulk. The present invention further provides a pharmaceutical composition containing the inhibitors of the invention and a screening method for identifying the inhibitors of the invention.

Abstract: The invention provides methods for predicting the efficacy of eribulin, an analog thereof, or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate), in the treatment of a subject suffering from breast cancer by determining the level of particular biomarkers in a sample derived from the subject.

Abstract: A method for inhibiting the production of cytokines of T helper cell type II (Th2 cell) and/or inhibiting the production of chemokines in a mammal is provided, wherein the method comprises administrating to the mammal an effective amount of an active component selected from a group consisting of a compound of formula (I), pharmaceutically acceptable salts and esters of the compound, and combinations thereof:

Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.

Abstract: A method of making an endoperoxide from a diene and oxygen in the presence of a photocatalyst having an excited state lifetime of at least 100 nanoseconds, the endoperoxide being represented by the formula: where R1 is an aryl substituted with at least one group selected from the group consisting of alkoxy, hydroxyl, halogen, carbamate, sulfonamide, silyloxy, amide, and combinations thereof or a substituted or unsubstituted heteroaryl, R2 is hydrogen, alkyl, alkynyl, or aryl, R3 is hydrogen, alkyl, alkynyl, or aryl, R4 is alkynyl or aryl, R5 is hydrogen or a substituent, R6 is hydrogen or a substituent, and A1, A2, and A3 are the same or different atoms and form a divalent group that combines with the two carbon atoms of the endoperoxide ring to form a saturated or unsaturated, substituted or unsubstituted ring system of a size of from five to six atoms.

Abstract: The present disclosure provides a dual-action pest control formulation for controlling rodents and arthropods, the formulation including: a rodenticide; an insecticide; an optional attractant; and a carrier matrix. The present disclosure also provides a method of controlling rodents and arthropods, the method including: applying the dual action pest formulation to a target area.

Abstract: A novel polyisoprenylated tetracyclic xanthone, named garciesculentone B, isolated from Garcinia esculenta Y. H. Li is disclosed in the present invention. This compound is shown to have significant cytotoxicity against various cancer cells. In addition, garciesculentone B is shown to have antimigration effect on various cancer cells such as human esophageal carcinoma cell. The experimental data supports that this compound is useful for developing into an anticancer drug.

Abstract: The present invention relates to a composition which comprises as an active ingredient coumestrol or a bean extract containing coumestrol, whereby adipocyte differentiation is inhibited, the immune system of the body is improved, toxic substances are purged, and neurodegenerative disorders are prevented or improved.

Abstract: The present invention relates to a composition which comprises as an active ingredient coumestrol or a bean extract containing coumestrol, whereby adipocyte differentiation is inhibited, the immune system of the body is improved, toxic substances are purged, and neurodegenerative disorders are prevented or improved.

Abstract: The present invention relates to a composition which comprises as an active ingredient coumestrol or a bean extract containing coumestrol, whereby adipocyte differentiation is inhibited, the immune system of the body is improved, toxic substances are purged, and neurodegenerative disorders are prevented or improved.

Abstract: This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.

Abstract: Nutraceutical compositions for improved administration of important phytochemicals from pomegranate to a human or animal. More particularly, enables oral or enteral dosage forms containing phytochemicals from pomegranate for administering on a routine basis. In at least one instance the natural contents of a pomegranate are encapsulated into a pill form or concentrated juice that provides for more efficient administration than eating a pomegranate but contains the same key ingredients present in the fruit. Enables the recipient to receive the benefits of the fruit but allows for the dosages to be taken in pill or concentrated juice form. Composition is chemically similar or equal to a natural pomegranate but is in a powder, pill or concentrated liquid form.

Abstract: The invention provides methods of treatment of metabolic syndrome with HSP90 inhibitors, particularly HSP90? inhibitors. The invention provides methods of diagnosis and monitoring of metabolic syndrome using HSP90, particularly HSP90?, expression and activity level.

Abstract: Dermal fibroblasts permanently loose their ability to synthesize elastin, the major component of elastic fibers, shortly after puberty. This progressive loss of elastic fibers cannot be replaced, resulting in the physical signs of aging. The present invention provides methods and compositions containing the polyphenols ellagic acid and/or tannic acid for protection against degradation of cutaneous elastic fibers by the elastolytic enzymes. The use of ellagic acid and/or tannic acid increased the overall deposition of elastic fibers in healthy and damaged skin cells. The protection of both intra-tropoelastin and extra-cellular mature elastic fibers from proteolytic enzymes by ellagic acid and tannic acid caused an increase in the net deposition of elastic fibers. Therefore, embodiments of the present invention provide methods and composition for the treatment of skin and prevention and treatment of degradation of dermal elastic fibers.

Abstract: Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.

Abstract: Described herein are compounds, compositions, and methods for treating HIV and related diseases.

Abstract: Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Abstract: The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.

Abstract: Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.