Abstract: Resveratrol ferulate compounds and compositions.

Abstract: The present invention provides for methods of treating and preventing cardiac hypertrophy. Class I HDACs, which are known to participate in regulation of chromatin structure and gene expression, have generally been considered as pro-hypertrophic in their action. However, the present invention demonstrates that inhibition of certain Class I HDACs should be avoided in the treatment of cardiac hypertrophy, thereby pointing toward selective, and not global, inhibition of Class I HDACs. In particular, the present invention provides for selective inhibition of HDACs 1 and/or 2, and the avoidance of inhibition of HDAC3.

Abstract: Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

Abstract: A compound of formula (I) wherein Y is oxygen or sulfur, and X1, X2 and X3 are independently of each other hydrogen, halogen, hydroxy or linear or branched (C1-6)-alkoxy, or hydroxy-(C1-6)alkyl or (C1-6)alkoxy-(C1-6)alkyl, mono- or dihalogenated (C1-6)-alkyl, amino(C1-6)-alkyl, hydroxy(C1-6)-alkyl, with one of the two provisos that: (1) at least of X1, X2 and X3 is other than hydrogen, and (2) X2 is other than hydroxy, when X1 and X3 are hydrogen.

Abstract: The present invention provides compounds, and compositions comprising these compounds, which have immunomodulatory activity and/or anti-inflammatory activity.

Abstract: The present invention provides processes for making and forms of solid dispersions of pharmaceutical active ingredients.

Abstract: The present invention provides compositions and methods for treating glaucoma, ocular hypertension, and age-related macular degeneration. More specifically, the present invention describes the use of agents that down-regulate expression of tanis and/or p21Waf1/Cip1/Sd1 genes to treat such disorders of the eye.

Abstract: The invention provides solid dispersions of at least one insoluble active pharmaceutical ingredient, pharmaceutical dosage forms comprising the solid dispersions, and methods of manufacturing same. In an embodiment, a solid dispersion of the present invention includes a plurality of coated particles comprising inert particles with a coating, wherein the coating comprises an insoluble active pharmaceutical ingredient dispersed in a hydrophilic polymer, and wherein the inert particles comprise nonpareils; and a plurality of granules comprising an insoluble active pharmaceutical ingredient with at least one pharmaceutically acceptable excipient. In an embodiment, the insoluble active pharmaceutical ingredient in the coating and the insoluble active pharmaceutical ingredient of the granules are the same type. A solid dispersion of the present invention may optionally be encapsulated in capsules or compressed into a tablet.

Abstract: The invention concerns novel polyunsaturated compounds of formula (I) wherein: R1 represents a R?1, -A-R?1 group, R?1 being selected from —COOH, —COOR3, —CONH2, —CONHR3, —CONR3, R4, —CHO, —CH2OH, —CH2OR5, and A represents a C2-C16 alkylene, alkenylene or alkynylene; R2 represents: an optionally substituted aryl group or an optionally substituted heteroaryl group; a sugar residue or, a fatty acid residue optionally branched and/or substituted preferably at the chain terminus and particularly by hydroxy, acetoxy radical or by an optionally protected amino radical; a —OC—(CH2)n CO-tocopheryl (alpha, beta or gamma or delta) group, with 2 $m(F) n $m(F) 10; a —R?2—O—R6 group, wherein R?2 is an optionally substituted arylene group or an optionally substituted heteroarylene group, and R6 represents a hydrogen atom, a straight or branched optionally substituted C1-C16 alkyl, a straight or branched optionally substituted C2-C16 alkenyl, or a straight or branched C2-C16 alkynyl group, an optionally substituted tocophery

Abstract: The present invention relates to a stable pharmaceutical composition of a poorly water-soluble drug with a view to increasing its solubility and bioavailability. The present invention relates to a solid dispersion of a poorly water-soluble drug.

Abstract: Embodiments of the invention generally relate to pharmaceutical compositions containing at least one caffeic acid compound and methods for the topical treatment of proliferative and inflammatory skin disorders such as plaque psoriasis, atopic dermatitis, and other disorders. In some embodiments, the topical treatment includes applications of the pharmaceutical composition containing at least one caffeic acid compound or a mixture of caffeic acid compounds such as caffeic acid ester compounds, caffeic acid amide compounds, analogues thereof, derivatives thereof, salts thereof, or mixtures thereof. The pharmaceutical composition or topical dosage may contain the caffeic acid compound at a concentration by weight within a range from about 0.01% to about 20%, preferably, from about 0.1% to about 15%, preferably, from about 1% to about 10%, more preferably, from about 3% to about 7%, and more preferably, from about 4% to about 6%.

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: The present invention relates to substances which can be used as cosmetic ingredients, especially for skin whitening and as cosmetic agents against signs of ageing skin. The present invention also relates to the use of such substances for the manufacture of a medicament for the treatment of disorders related to the pigmentation of the skin. The invention furthermore relates to specific substances.

Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.

Abstract: The invention concerns compositions comprising substituted 1,3-diphenylprop-2-en-1-one derivatives designed for therapeutic use. The inventive compositions are useful in particular for preventing or treating cardiovascular diseases, syndrome X, Ia restenosis, diabetes, obesity, hypertension, inflammatory diseases, cancers or neoplasms (benign or malignant tumors), neurodegenerative, dermatological diseases and disorders related to oxidative stress, for preventing or treating the effects of ageing in general and for example skin ageing, in particular in the field of cosmetics (occurrence of wrinkles and the like).

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

Abstract: Methods of treating, inhibiting, or ameliorating gout, including chronic acute (refractory) gout, pseudogout, or drug-induced gout, in a human subject in need thereof, comprising administering to a subject in need a therapeutic amount of an interleukin 1 (IL-1) antagonist, wherein the incidence of a gout flare is reduced or inhibited.

Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed lipoxins, generated from the interaction between a dietary omega-6 polyunsaturated fatty acid (PUFA) such as arachidonic acid (AA), oxygenases and the analgesic aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy containing derivatives of AA containing compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- and tri-hydroxy derivatives of AA (lipoxins, aspirin-triggered epi-lipoxins) that diminish, prevent, or eliminate NV, hemangiogenesis and/or angiogenic condition(s) of corneal tissue. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.

Abstract: The present invention provides a pharmaceutical composition comprising a combination of an Hsp 90 family protein inhibitor and at least one compound, the said pharmaceutical composition wherein the Hsp 90 family protein inhibitor is a benozoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl, or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like], or a prodrug thereof; or a pharmaceutically acceptable salt thereof, and the like.

Abstract: Benzolipoxin analogs, methods of their preparation and pharmaceutical compositions containing the compounds are provided. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease and abnormal cell proliferation.

Abstract: The invention relates to organic compounds having the ability to reduce or suppress the onset of skin irritation induced by extraneous cause selected from the group of 2-heptylcyclopentanone, 2-ethoxynaphthalene; 2-methoxynaphthalene; 1-methoxy-4-(prop-1-enyl)benzene; 1-(cyclopropylmethyl)-4-methoxybenzene; wherein X, Y, and R1 to R11 have the same meaning as given in the description. Furthermore the invention refers to compositions for topical application to the skin comprising them. It further relates to a method of reducing or suppressing the formation of skin irritation.

Abstract: It is intended to reinforce the anti-fungal, anti-viral and anti-bacterial activities of alkyl gallates, and to provide a new technology and means which allow the solubilization of the alkyl gallates in water. A pharmaceutical composition of alkyl gallates of the present invention is characterized by containing (A) an alkyl gallate in which the carbon number of the alkyl group is in the range of 5 to 16 and (B) another alkyl gallate in which the carbon number of the alkyl group is smaller than that of (A). Preferably, the carbon number of the alkyl group of the alkyl gallate (B) is in the range of 2 to 7, and the composition further contains (C) at least one member selected from an alkali metal salt, boric acid, sodium borate and an organic salt.

Abstract: Disclosed is an amide compound represented by the formula (1) below, which has excellent plant disease controlling activity. In the formula, X1 represents a fluorine atom or a methoxy group; X2 represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group or the like; X3 represents a halogen atom, a C1-C4 alkyl group or the like; Z represents an oxygen atom or a sulfur atom; and A represents an A1-CR11R12R13 group, an A2-Cy1 group or an A3-Cy2 group, wherein A1 represents a CH2 group or the like, A2 represents a single bond, a CH2 group or the like, A3 represents a C1-C3 haloalkyl group, a C2-C4 alkenyl group or the like, Cy1 represents a C3-C6 cycloalkyl group substituted with a C1-C6 alkoxy group or the like, Cy2 represents a C3-C6 cycloalkyl group which may be substituted with a halogen atom or the like, R11 and R12 independently represent a C1-C4 alkyl group, and R13 represents a halogen atom, a hydroxyl group or the like.

Abstract: Aspirin (ASA) triggers a switch in the biosynthesis of lipid mediators, inhibiting prostanoid production and initiating 15-epi-lipoxin generation, through the acetylation of cyclooxygenase II.

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: An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye. There are provided an agent for promoting proliferation of a meibomian gland epithelial cell or a corneal epithelial cell, containing a PPAR? or ? agonist as an active ingredient, as well as an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye, containing a PPAR? or ? agonist as an active ingredient.

Abstract: The present invention provides an enhanced gelling agent composition comprising a mixture of an anionic surfactant and a coupling agent. The invention also describes compositions in gel form comprising: (a) a solvent selected from the group consisting of polar solvents, non-polar solvents and combinations thereof; and (b) a gelling agent in an amount sufficient to impart gelation to the composition, the gelling agent being a mixture comprising an anionic surfactant and a coupling agent. The gels of the invention may be substantially anhydrous or may optionally contain water as part of the formulation.

Abstract: A method for treating irritable bowel syndrome (IBS) is included. The method includes the step of administering a fibric acid derivative to a patient diagnosed with IBS in order to alleviate the symptoms associated with IBS.

Abstract: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.

Abstract: It has been discovered that polyphenols are effective as a co-pharmaceutical in combination with traditional dual drug therapies of catecholamines and decarboxylase inhibitors for the treatment of Parkinson's disease. Accordingly, a method of treating Parkinson's disease comprising administering to a subject suffering from Parkinson's disease a pharmaceutical composition comprising at least one catecholamine, at least one decarboxylase inhibitor, and at least one polyphenol is provided.

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 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: Provided is a method of treating hypertension, which comprises administering an effective amount of a compound represented by the following formula (1) or (2): wherein, R1 and R2 are the same or different and each independently represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxyalkyl, aryl, alkylaryl, aralkyl, or acyl, R3 represents hydroxyl, ester bond residue, or amide bond residue, R4 represents ester bond residue or amide bond residue, or a pharmaceutically acceptable salt thereof (except ferulic acid).

Abstract: Methods of treating, inhibiting, or ameliorating gout, including chronic acute (refractory) gout, pseudogout, or drug-induced gout, in a human subject in need thereof, comprising administering to a subject in need a therapeutic amount of an interleukin 1 (IL-1) antagonist, wherein the incidence of a gout flare is reduced or inhibited.

Abstract: Compositions are provided comprising a lipophilic active compound, e.g., a human or veterinary drug or a nutraceutical, interwoven with a polymeric matrix formed by two or more polymers, wherein one of the polymers is an amphiphilic polymer and the other polymer is either an amphiphilic polymer with a different hydrophobic-hydrophilic balance or a hydrophilic polymer, and the active lipophilic compound has modified physicochemical properties. The composition forms colloidal nanodispersion upon contact with aqueous media.

Abstract: antiperspirant compositions comprise an antiperspirant active and a carrier oil in which the carrier oil comprises an aromatic ester oil obeying the general formula: R1—CO2—X—Y—R2 in which R1 and R2 each represent a phenyl group, X represents an alkylene group containing from 2 to 4 carbons including at least one pendant alkyl group and Y represents a bond, or an ether or ester linkage.

Abstract: Provided are cosolvent evaporation methods and compositions for improving the solubility of hydrophobic compounds, including therapeutic agents such as anticancer drugs, polyene antibiotics, antilipidemic agents, and hydrophobic compounds used in various industries, and/or for reducing the toxicity of certain hydrophobic therapeutic agents, especially polyene antibiotics, in particular, Amphotericin B (AmB), and therapeutics such as paclitaxel, tamoxifen, an acylated prodrug or an acylated cis-platin, by incorporating these agents within micelles comprising an amphiphilic block-forming copolymer.

Abstract: The invention provides novel omega-3 oil liquid formulations of fenofibrate. These formulations can be substantially free of any food effect, effective in small volumes, and readily bioavailable. Notably, because the formulations of the invention contain an omega-3 oil as the major ingredient, they not only provide anithypercholesterolemic and antihypertriglyceridemic effects due to the fenofibrate active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof.

Abstract: The present invention relates to the use of a ginger extract on its own or in combination with pharmaceutical compositions for inhibiting human drug transporters for positively influencing the oral bioavailability and pharmacokinetics of active substances.

Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes, to pharmaceutical compositions comprising them and to the processes for the preparation of these compounds.

Abstract: Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.

Abstract: The present invention provides crystalline solid and amorphous forms of (?)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (?)-halofenate.

Abstract: The present invention relates to a combination of a peroxisome proliferator activated receptor (PPAR) activator and a benzoquinone and their use in treating and/or preventing disorders characterized by endothelial dysfunction, such as cardiovascular disease, strokes and myocardial infarction. According to a preferred embodiment of the invention the benzoquinone or precursor thereof is a ubiquinone or precursor thereof, more preferably, coenzyme Q10 or a precursor thereof, and the PPAR activator is a fibrate or a thiazolidinedione, more preferably fenofibrate.

Abstract: The present invention relates to compositions containing a) at least one monoacyl lipid; b) at least one diacyl glycerol and/or tochopherol; and c) at least one fragmentation agent; and optionally an active agent. The compositions are capable of self-dispersing to provide colloidal non-lamellar particles upon contact with an aqueous fluid. The invention additionally provides a method for forming non-lamellar particles from such compositions, and pharmaceutical formulations containing the compositions, plus non-lamellar particles formable from the compositions.

Abstract: The present invention is directed to fibrate compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The fibrate particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: Disclosed herein are methods for treating mucositis (e.g., Alternaria-activated mucositis) that involves the direct mucoadministration of an active agent that is antifungal and antibacterial in an amount and for a duration effective to treat mucositis.

Abstract: The compound represented by the following formula (1): wherein A, B, R1, R2, R3 and Z are as defined in the specification is analogous to shogaol and gingerol useful in the fields of foods, medicines, quasi-drugs, cosmetics, etc., and more highly active in tyrosinase activity inhibition, etc. than shogaol and gingerol.

Abstract: A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z? are defined herein.

Abstract: The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has ?3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.