Abstract: Aromatase inhibitors (AIs) are disclosed which are useful in the treatment and prevention of post-menopausal breast cancer. New AIs derived from natural products are disclosed that are evaluated for clinical utility for treating post-menopausal breast cancer and may also act as chemopreventive agents for preventing breast cancer. Several pure compounds demonstrated AI activity using a noncellular, enzyme-based microsomal and a cell-based aromatase assay. Correlations are made between structural classes with levels of aromatase inhibition. The disclosure may be utilized to direct synthetic modification of natural product scaffolds to enhance aromatase inhibition or to standardize botanical dietary supplements for increased aromatase inhibition activity.

Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; formula (I) wherein R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group -R5 or a group, -Z-Y—R5, or a group -Z-NR9R10, or a group -Z-N(R9)C(O)R11; and R3 is a lone pair, or C1-C6-alkyl; R4 is selected from one of the groups of formula (a), (b), (c) or (d); formulae (a), (b), (c), (d), Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R5 is an C1-C6-alkyl, aryl, arylalkyl; aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R6 is C1-C6-alkyl or a hydrogen atom; R7a and R7b area C1-C6-alkyl group or halogen; n and m are independently 0, 1, 2 or 3; R8a and R8b are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl and hydrogen; R8c is —OH, C1-C6-alkyl, hydroxy-C1-C6-alkyl, or a hydrogen atom; R8d is C1-C6

Abstract: A drug composition for treating type 2 diabetes and diabetic chronicity complications is disclosed. The composition is composed of mangiferin and berberine in a certain ratio.

Abstract: The present invention provides a method of modulating TGF-? activity in a subject. Methods of the present invention comprise administering to the subject an effective amount of a compound of the formula: or a salt, prodrug, tautomer, hydrate, solvate, or stereoisomer thereof, wherein a is an integer from 0 to 4; each R1 is independently hydroxy, alkoxy, halide, alkyl, cyano, nitro, amino, monoalkylamino, dialkylamino, or carboxy; R2 is aryl, cycloalkyl, alkenyl, or alkyl, each of which is optionally substituted; each of X1 and X2 is independently O, S or NR3, wherein R3 is hydrogen or alkyl; X3 is hydrogen, alkoxy, alkyl, hydroxy, halide, amino, monoalkylamino, or dialkylamino; and X4 is alkoxy, hydroxy, halide, amino, monoalkylamino, or dialkylamino.

Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).

Abstract: The present invention relates to compounds of formula I, which are functionalized phenolic compounds, and polymers formed from the same. Ar—[O—(X)p—R?]q??I Polymers formed from the functionalized phenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: Water-soluble dimethyl amino ethyl ether psoralens useful in the treatment of proliferative skin disorders, microbial infections and diseases, disorders of the blood and bone marrow of mammals and in microbiocidal compositions for sterilization of blood and blood products and surgical implants and inhibition of microbial growth in industrial applications are provided.

Abstract: Described herein are ?9-THC prodrugs, methods of making ?9-THC prodrugs, formulations comprising ?9-THC prodrugs and methods of using ?9-THC. One embodiment described herein relates to the transdermal administration of a ?9-THC prodrug for treating and preventing diseases and/or disorders.

Abstract: A composition for reducing the activity of a cervical cancer cell is provided. The composition includes at least one of the following compounds: isopsoralen, triptolide, baicalein, gallic acid, quercetin, gossypol-acetic acid, baicalin, berberine hydrochloride, and derivatives thereof in a sufficient amount to reduce the activity of the cervical cancer cell in the subject.

Abstract: This invention pertains to the discovery that a dopamine receptor agonist can activate PKA signaling and/or can act synergistically with an adenosine receptor to activate such signaling. In various embodiments, this invention exploits the synergy between the dopamine receptor pathway and an adenosine receptor pathway to provide methods of mitigating one or more symptoms produced by the chronic consumption of a substance of abuse or to mitigate one or more physiological and/or behavioral symptoms associated with cessation of chronic consumption of a substance of abuse. In certain embodiments, the methods involve administering to the mammal an effective amount of an adenosine receptor antagonist; and an effective amount of a dopamine receptor antagonist; where the effective amount of the adenosine receptor antagonist is lower than the effective amount of an adenosine receptor antagonist administered without said dopamine receptor antagonist.

Abstract: The present invention relates to compounds, compositions for use in reversing multidrug resistance in cancer cells, process for the preparation thereof and their uses in treating cancers. More particularly, the present invention relates to 3?,4?-aromatic acyloxy substituted 7,8-pyranocoumarins compounds for use in reversing P-glycoprotein overexpression mediated multidrug resistance in cancer cells, pyranocoumarins containing compositions, process for the preparation thereof and their uses in treating cancers.

Abstract: A method for treating a cell proliferation disorder in a subject, comprising: (1) administering to the subject at least one activatable pharmaceutical agent that is capable of activation by a simultaneous two photon absorption event and of effecting a predetermined cellular change when activated; and (2) applying an initiation energy from an initiation energy source to the subject, wherein the initiation energy is capable of penetrating completely through the subject, and wherein the applied initiation energy activates the activatable agent by the simultaneous two photon absorption event in situ, thus causing the predetermined cellular change to occur, wherein the predetermined cellular change treats the cell proliferation related disorder, and a kit for performing the method, a computer implemented system for performing the method, a pharmaceutical composition useful in the method and a method for causing an autovaccine effect in a subject using the method.

Abstract: The invention provides novel compounds of formula (I), (II), (III), and (IV). The invention also provides pharmaceutical compositions comprising such compounds as well as methods for treating diseases associated with opioid receptor function by administering such compounds to an animal in need of treatment. The invention also provides therapeutic methods for the use of compounds of formula (V), as well as methods for treating diseases by administering such compounds.

Abstract: Methods and compositions are provided for treating cancer, the methods including the step administering, either sequentially or simultaneously, (i) a compound of the xanthenone acetic acid group of compounds, and (ii) at least one compound selected from compounds which modulate TNF production and compounds which act on biochemical pathways leading to TNF synthesis. Compositions include a combination of (i) and (ii) above, together with acceptable pharmaceutical carriers and/or vehicles.

Abstract: The present application describes deuterium-enriched topiramate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Nutraceutical compositions derived from the fruit of the Garcinia mangostana L. or mangosteen plant and methods to make the same are provided. The nutraceutical mangosteen compositions employ novel combinations of mangosteen fruit pulp and pericarp, and can be additionally complemented by selected juice concentrates to yield a composition for improving general health and wellness in humans. The methods to make the nutraceutical compositions involve the use of a mixture comprising pericarp and inner pulp from whoe fruit of a Garcinia mangostana L. plant.

Abstract: The present invention relates to synergistic combinations of the compounds of formula I such as compounds of the xanthenone acetic acid class such as 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and NSAIDs, in particular diclofenac, which have anti-tumour activity. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing said combinations.

Abstract: A pharmaceutical composition having a cytotoxic effect to a cancer cell and a method for the same are provided. The pharmaceutical composition comprises a flavonoid compound having at least one of the following formulas: wherein B ring is a 4-oxo-cyclohexa-2,5-dienyl group, and any one of R1-R12 is one selected from a group consisting of hydrogen group, hydroxyl group, C1-C20 alkyl group, C1-C20 ether group, C1-C20 ester group, carboxyl group, halogen and sugar.

Abstract: The present invention provides a compound of Formula (I): wherein R1, R2, R3 and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C7-C14 aralkyl group and —C(?O)Rx; Rx represents an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C1-C6 alkoxy group or —NReRf; Ar1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents —(CH2)m-(L)p- or -(L)p-(CH2)m—; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents —O—, —S— or —NR5—; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical co

Abstract: The present invention relates to benzochromene derivatives of the formula I where the various parameters have the meaning indicated in the text, and to liquid-crystal media which comprise these compounds, and to the use of the media in electro-optical displays, in particular in VAN-LCDs, and to the use of the compounds and physiologically acceptable derivatives thereof as therapeutic active ingredients.

Abstract: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is a psychotherapeutic agent and the second compound is a anticonvulsant. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual with a psychotherapeutic agent and an anticonvulsant.

Abstract: The object of the present invention is to provide an antibacterial agent which has an improved antibacterial effect and a wider antibacterial spectrum than conventional antibacterial agents, and which is highly safe to human and the environment. This object is achieved with a novel substance 9-(1?,5?-dimethyl-1?-vinyl-4?-hexenyl)-4-hydroxy-7H-furo[3,2-?][1]benzopyran-7-one and an antibacterial agent comprising thereof.

Abstract: The present invention comprises compositions and methods for the treatment of liver disease, particularly treatments for infection by HCV and/or HBV. The present invention comprises antiviral compositions comprising lamiridosin, derivatives of lamiridosin or iridoids that are effective in inhibiting one or more steps in the infection of cells by HCV or HBV. Methods for treating subjects, particularly humans, infected with HCV or HBV are provided.

Abstract: The present invention relates to synergistic combinations of the compounds of formula I such as compounds of the xanthenone acetic acid class such as 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and NSAIDs, in particular diclofenac, which have anti-tumor activity. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing said combinations.

Abstract: Methods of killing mosquito larvae and controlling an adult mosquito population by using ?-mangostin, 3,6,8-yrihydroxy-2-methoxy-1,7-bis(3-methylbut-2-enyl)xanthen-9-one, or a salt, solute, hydrate or solvate thereof. Mosquito larvae are killed by contacting a lethal dose of ?-mangostin with mosquito larvae. Adult mosquito populations are controlled by treating a mosquito larvae population with a lethal dose of ?-mangostin.

Abstract: The present invention discloses morusin, a method of extracting morusin, as well as various uses in manufacturing antibacterial medicaments or oral care products or for other antibacterial uses.

Abstract: The present invention discloses hydroxy-morusin, a method of extracting hydroxy-morusin, as well as various uses in manufacturing antibacterial medicaments or oral care products or for other antibacterial uses.

Abstract: A process for separating (?)-?9-trans-tetrahydrocannabinol from a mixture of cannabinoids is disclosed. The process comprises at least one chromatographic step wherein a mobile phase passes trough a stationary phase. The stationary phase comprises a derivatised polysaccharide and the mobile phase comprises carbon dioxide.

Abstract: The invention is directed to a pharmaceutical composition of topiramate, an anticonvulsant which is useful for treating epilepsy. More specifically, the present invention provides a solid dosage formulation of topiramate intended primarily for use by pediatric patients, or for patients who have difficulty swallowing tablets. Processes for preparing the pharmaceutical composition are also described.

Abstract: A method of treating or preventing snoring, obstructive sleep apnea (OSA) and/or central sleep apnea (CSA) comprises administering a pharmacologically effective amount a salt of acetylhomotaurine (AcHT) such as calcium acamprosate (CA) to a patient. Also disclosed is the use of AcHT and CA for the manufacture of a medicament for treating or preventing snoring, OSA and/or CSA and of a diagnostic device, kit or composition; a protective patch comprising AcHT or CA; and a pharmaceutical composition comprising AcHT or CA and an agent capable of alleviating the effects of snoring OSA and/or CSA, in combined amounts effective in the treatment of snoring OSA and/or CSA, and a carrier.

Abstract: The present invention is drawn to combinations of pharmaceutical agents having similar chemical and/or pharmacological properties, wherein the combinations maximize the therapeutic effect of the drug while minimizing their adverse effects. The methods and compositions of the invention are particularly useful in the treatment of obesity and related conditions which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) or bupropion in combination with an anti-epileptic agent (e.g., topiramate, zonisamide), CB1 antagonists (e.g., rimonabant), or a 5HT2C-selective serotonin receptor agonist, (e.g., lorcaserin) for the treatment of obesity and related conditions. The invention also features kits for use in the practice of these novel therapies.

Abstract: A method of inhibiting the proliferation of a hyperproliferative mammalian cell having a multiple drug resistant phenotype utilizing an amount of a laulimalide compound effective to disrupt the dynamic state of microtubule polymerization and depolymerization to arrest cell mitosis is disclosed, together with laulimalide compounds which find use in such method.

Abstract: Methods for the treatment of a cell proliferation disorder in a subject, involving: (1) administering to the subject at least one activatable pharmaceutical agent that is capable of effecting a predetermined cellular change when activated, either alone or in combination with at least one energy modulation agent; and (2) applying an initiation energy from an initiation energy source to the subject, wherein the applying activates the activatable agent in situ, thus causing the predetermined cellular change to occur, wherein the predetermined cellular change treats the cell proliferation disorder, preferably by causing an increase or decrease in rate of cell proliferation, and a kit for performing the method, a computer implemented system for performing the method, a pharmaceutical composition useful in the method and a method for causing an autovaccine effect in a subject using the method.

Abstract: The present invention is directed to novel complexes of cyclodextrin. In particular the invention is directed to a complex of a cyclodextrin selected from the group consisting of RM-?-cyclodextrin, DM-?-cyclodextrin and TM-?-cyclodextrin, and a cannabinoid selected from the classical cannabinoid-group consisting of cannabinol, tetrhydrocannabinol and cannabidiol.

Abstract: A method of treating menorrhagia and/or dysmenorrhoea in a patient the method comprising administering to the patient an antagonist of a prostaglandin EP2 and/or EP4 receptor. Preferably the patient is a human female.

Abstract: The present invention relates to methods of treating and preventing obesity and obesity-related disorders in a subject comprising administering a neurokinin-1 antagonist and an anti-obesity agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further related to methods of treating or preventing sexual dysfunction, including male erectile dysfunction, in a subject comprising administering a neurokinin-1 antagonist and a sexual dysfunction therapeutic agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further provides for pharmaceutical compositions and medicaments useful in carrying out these methods.

Abstract: The present invention has its object to provide a specific compound derived from a naturally occurring substance, and a composition for the prevention and/or treatment of metabolic syndrome and insulin resistance syndrome which comprises that as an active ingredient, easily and efficiently. The present invention relates to a composition for the prevention and/or treatment of metabolic syndrome and a composition for the prevention and/or treatment of insulin resistance syndrome, each of which comprises, as an active ingredient, at least one compound selected from among the compound represented by the formula (1), compounds represented by the formula (4) and compounds represented by the formula (5), or a salt or ester thereof.

Abstract: The present invention relates to a method for monitoring/detecting compounds capable to regulate the transcription and/or expression of the forkhead transcription factor Foxc2, which compounds may be useful for the treatment of obesity related diseases and diabetes.

Abstract: The present invention is directed to an improved process for producing substantially pure fluorescein, as well as to substantially pure fluorescein compositions prepared by the process. The invention is particularly directed to the provision of pharmaceutical compositions for use in angiography. The substantially pure fluorescein produced by the process of the present invention is low in color, low in sodium chloride content, and substantially free of pyridine.

Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract: The present invention relates to a pharmaceutical composition comprising at least one first active therapeutic substance selected among carveol, thymol, eugenol, borneol, carvacrol, alpha-ionone, beta-ionone, as well as isomers, derivatives and mixtures thereof, and comprising at least one second active therapeutic substance that is an antiparasitic agent, in particular, an antimalarial agent. The invention is for use in the field of pharmaceutics.

Abstract: The invention provides a hair and/or scalp care composition which is a shampoo composition, comprising an anionic cleansing surfactant in an amount of from 5 to 30 wt % and visnadin. The invention also provides a hair and/or scalp care composition which is a conditioner composition, comprising a cationic conditioning surfactant in an amount of from 0.01 to 10 wt % and visnadin. The invention also a method of treating and/or preventing inflammatory skin conditions such as the scalp skin itching and flaking associated with dandruff, which method comprises topically applying a composition according to the invention to the hair and/or skin, preferably to the hair and/or scalp.

Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.

Abstract: Provided is a pharmaceutical composition for the treatment and prevention of obesity, diabetes, metabolic syndromes, degenerative diseases and mitochondrial dysfunction-related diseases, comprising: a therapeutically effective amount of a compound represented by Formula I below, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof.

Abstract: There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.

Abstract: The invention provides novel polycyclic macrolactones which can be produced, in particular, by a representative of the bacterial genus Verrucosispora. These substances are preferentially distinguished by their pharmacological effect. In particular, they exhibit an antibiotic effect. This antibiotic effect is preferably directed against Gram-positive bacteria.

Abstract: A metabolic syndrome relieving agent that is free from a problem of side effects and can be taken for a long term is provided. Bergamottin is used as an agent for relieving a metabolic syndrome. Since bergamottin has functions of activating PPAR? and PPAR?, promoting the secretion of adiponectin in adipocytes and inhibiting the generation of VLDLs in hepatic cells, it is possible to prevent or treat diseases such as insulin resistance, hyperinsulinism, type 2 diabetes, obesity, visceral fat obesity, hypertension, hyperlipemia, arteriosclerosis and the like and thus prevent or treat the metabolic syndrome. Also, as understood from the fact that citrus fruits such as a grapefruit or the like containing bergamottin have been eaten for many years, they have no problems in terms of safety and have a low calorie content, and therefore, they can be taken for a long term.

Abstract: Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

Abstract: This invention provides for the treatment of inflammatory, cancer and thrombotic disorders through the administration, in combination, of a COX2 inhibitor, low dose aspirin, and antioxidant flavanoids, flavonoids or isoflavones and at least one of these combinations will be given in a subtherapeutic amount for improved anti-inflammatory, anti-cancer, and anti-thrombotic efficacy and safety.