Abstract: The present invention relates to a docosahexaenoic acid ester with an alcohol chosen among the group-B vitamins or provitamins, advantageously comprised by: nicotinyl alcohol of the following formula (I), panthenol of the following formula (II), and inositol of the following formula (III) or with isosorbide of the following formula (IV) or isosorbide mononitrate of the following formula (V). It also relates to a method of preparation of same, a pharmaceutical composition comprising same and the use of same in the treatment or prevention of cardiovascular disease, in particular auricular fibrillation.

Abstract: Extended release pharmaceutical compositions comprising mycophenolate sodium as the active agent, wherein the said composition exhibits a characteristic release profile when subjected to in-vitro dissolution study, and wherein said mycophenolate sodium is released in a sustained manner in-vivo for a prolonged duration in such quantities that substantially alleviates or at least reduces the chances of causing any associated gastrointestinal side effect(s) without compromising the bioavailability of the said active agent are provided. The present invention also provides process of preparing dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form. The compositions of the present invention are useful for the management such as prophylaxis, amelioration and/or treatment of immunosuppressant indicated disease(s)/disorder(s) especially for the treatment or prevention of organ, tissue or cellular allograft or xenograft rejection, e.g.

Abstract: The invention relates to fatty acid mycophenolate derivatives; compositions comprising an effective amount of a fatty acid mycophenolate derivative; and methods for treating and preventing organ rejection and autoimmune diseases such as systemic lupus erythematosus, psoriasis and multiple sclerosis comprising the administration of an effective amount of a fatty acid mycophenolate derivative.

Abstract: The present invention is directed to methods and compounds for inhibiting bacterial growth and treating a bacterial infection in a subject. These methods involve providing an inhibitor of intrabacterial pH homeostasis, including inhibitors of the Mycobacterium tuberculosis Rv3671c gene encoded membrane protease. Methods for identifying novel compounds that disrupt intrabacterial pH homeostasis and their use for inhibiting bacterial growth and treating a bacterial infection in a subject are also disclosed.

Abstract: The subject invention provides novel and advantageous materials and methods for treating neuroinflammation, neurodegenerative disease, and cerebrovascular disease by modulating TNF-? and/or nitric oxide production. Specifically exemplified herein is the therapeutic use of senkyunolide A (Sen A) and Z-ligustilide (Z-Lig), compounds isolated from traditional Chinese medicinal material Ligusticum chuanxiong (LCX).

Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.

Abstract: This invention relates to a pharmaceutical formulation containing z-butylidenephthalide and a polymer, e.g., a polyanhydride. Also disclosed is use of this formulation to treat tumor.

Abstract: The present invention is to provide skin cosmetics and anti-wrinkle agents which are excellent in reducing effect on wrinkle caused by photoaging. Skin cosmetics and anti-wrinkle agents which comprise isosorbide represented by the following formula (1).

Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.

Abstract: For use in mammals, methods for enhancing the DNA repair process, treating disorders associated with the DNA repair process, enhancing anti-tumor response and treating disorders associated with anti-tumor response. The methods generally comprise non-topical administration of purified, isolated quinic acid alkyl acid or a carboxy alkyl ester with a non-toxic carrier or diluent.

Abstract: The disclosure provides a method for isolating the bioactive component of the water-soluble extract of Uncaria tomentosa known as C-MED-100®, comprising (i) precipitating the spray drying carrier from C-MED-100®; (ii) using the resulting C-MED-100® to obtain a spotting mixture for thin layer chromatography (TLC); (iii) spotting the C-MED-100® spotting mixture on pre-run TLC plates and eluting the plates to obtain the fluorescing band with Rf=0.2-0.3; (iv) scraping off the Rf=0.2-0.3 band, eluting it in ammonia and freeze drying the eluted band to form a powder; and (v) extracting the powder with methanol to remove solubilized silica gel, concentrating the methanol solution and crystallizing the concentrated solution to obtain the bioactive component. The isolated bioactive component in vitro is a quinic acid analog, preferably quinic acid lactone.

Abstract: Skin conditioning compositions comprising a C4 to C30 monoalkyl-, dialkyl, monoalkanoyl- or dialkanoyl-substituted isohexide are found to exhibit a marked effect on skin hydration and barrier function homeostasis thereby improving skin appearances.

Abstract: Compositions and methods of treating viral infections are provided. More particularly, compositions including a combination of protease inhibitors and cytochrome p450 enzyme inhibitors are provided. Methods of using the compositions for treatment of diseases or disorders caused by a virus such as HIV infections are also provided.

Abstract: Patients having a disease associated with high level of thioredoxin system activity or a requirement for nitric oxide, e.g. large cell lymphoma or restenosis, are treated with a thioredoxin reductase inhibitor, e.g. auranofin or arsenic trioxide, and a nitric oxide donating compound, e.g. isosorbide mononitrite or isosorbide dinitrite or nitroglycerin or S-nittrosothiol. Patients having a disease associated with nitric oxide synthase overexpression or increased activity, e.g. Parkinson's disease or septic shock or pancreatic cancer, are treated with Trx/Trx reductase upregulator, e.g. aptamer that binds to thioredoxin reductase inhibitor, and agent causing depletion of nitric oxide (or adduct thereof), e.g. L-NMMA or L-NAME or minocycline or ascorbate or N-acetylcysteine.

Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.

Abstract: The present invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y and CKE have the meanings given in the disclosure, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention further relates to selectively herbicidal compositions containing 2,4,6-phenyl-substituted cyclic ketoenols and a compound which improves crop plant tolerance.

Abstract: Methods of increasing the permeability of corneal epithelium to facilitate the diffusion of agents into the collagen fibrillar network of the stroma are provided. Used in combination, these methods open the epithelium to facilitate diffusion of stabilization molecules into the stroma and dissociate bridging molecules from stromal collagen fibers, thereby priming the collagen fibrillar network for restabilization by stabilization molecules. These methods can be used to increase the effectiveness and longevity of non-invasive corneal reshaping, such as orthokeratology, for correcting myopia, hyperopia and astigmatism.

Abstract: The present invention provides delayed release pharmaceutical compositions comprising an active pharmaceutical ingredient, e.g. mycophenolate sodium, and an enteric polymer, and methods for preparing the same. Preferably, the pharmaceutical compositions do not contain a coating.

Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.

Abstract: The present invention discloses the use of L-butylphthalide of formula (I) in the manufacture of medicaments for the prevention and treatment of cerebral infarct, especially induced by focal cerebral ischemia.

Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.

Abstract: Provided is a composition for transdermal administration. The composition comprises a therapeutic agent having a net charge at skin pH and a topical penetration enhancer having a net charge at skin pH opposite the net charge of the therapeutic agent. In another aspect, a method is provided for increasing the transdermal absorption of a therapeutic agent. The method comprises forming a therapeutic composition at skin pH by combining a therapeutic agent having a net charge at skin pH with a topical penetration enhancer having a net charge at skin pH opposite the net charge of the therapeutic agent, the ratio of topical penetration enhancer to therapeutic agent being sufficient to increase absorption of therapeutic agent compared to absorption of therapeutic agent in the absence of topical penetration enhancer, and administering the therapeutic composition to a patient in need thereof.

Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.

Abstract: The present invention relates to methods and formulations for inhibiting, treating and preventing a malignant cell phenotype, cell, tumor and/or disease. Administration of nitric oxide mimetics, such as low doses, is sufficient to increase, restore or maintain nitric oxide-mediated signaling in cells so that malignant cell phenotypes, cells, tumors and/or diseases are inhibited or prevented. These methods and formulations are particularly useful in treating and preventing cancer in animals.

Abstract: The present invention relates to targets of loss of imprinting (LOI) affected IGF2 gene products in pre-malignant tissues, where methods of inhibiting those targets, including IGFR1, are disclosed to prevent tumor development in subjects at risk for developing colorectal cancer (CRC). The present invention also relates to methods of identifying increased risk in developing CRC in a subject, including methods of assessing the efficacy of a chemotherapeutic regimen. Further, the present invention relates to methods for identifying anti-neoplastic agents.

Abstract: Modified release pharmaceutical compositions comprising mycophenolate as the active agent or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof, wherein the said composition exhibits a biphasic release profile when subjected to in-vitro dissolution and/or upon administration in-vivo are provided. The composition provides a drug release in a manner such that the drug levels are maintained above the therapeutically effective concentration (EC) constantly for an extended duration of time. Further, the difference between the maximum plasma concentration of the drug (Cmax) and the minimum plasma concentration of the drug (Cmjn), and in turn the flux defined as ((Cmax?Cmjn)/Cavg) is minimal. The present invention also provides process of preparing such dosage form compositions and prophylactic and/or therapeutic methods of using such compositions.

Abstract: Isobenzofuran analogs of sclerophytin A are prepared in a highly concise fashion via an aldol-cycloaldol sequence. The analogs exhibit IC50's as low as 1 ?M in growth inhibitory studies against KB3 cells using an MTT assay. Preferred analogs have one of the following structural formulas, where R is hydrogen or a substituted or unsubstituted lower alkyl group and Ar is a substituted or unsubstituted aryl group.

Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) as defined herein, is provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy. Novel heterocyclic compounds are also provided for.

Abstract: The present invention relates to cosmetic compositions and more particularly to skin-whitening cosmetic compositions comprising senkyunolide A as an active ingredient. The present invention discloses the novel inhibitory function of senkyunolide A isolated from Cnidium officinale and Ligusticum chuanxiong on the melanocyte-stimulating hormone (MSH), and provides MSH-inhibitory compositions and skin-whitening cosmetic compositions comprising the senkyunolide A. The compositions of the present invention show significantly enhanced skin-whitening effect owing to its efficient inhibition of MSH even in lower concentration.

Abstract: This invention relates to novel hydroxyethylamino sulfonamides, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor.

Abstract: The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R1 is butyl or butyryl if R2 is hydroxyl but is butyl if R2 is hydrogen; or R1 and R2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3-(?,?-dimethylacrylyloxy)-pentylidenyl; X is a residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation.

Abstract: The present invention provides formulations comprising milnacipran or pharmaceutically acceptable salts thereof (e.g., milnacipran hydrochloride), including immediate release formulations and modified formulations, such as delayed release and extended release formulations. The present invention provides formulations with improved stability and high bioavailability. Processes for preparing the formulations as well as methods of treating conditions by administering the formulations are also described.

Abstract: The present invention is directed to a mixture of at least two different alkylated phenolphthalein ester compounds. Specifically, the present invention is directed to a mixture of at least two different compounds of formula I: wherein R1 represents a straight chain alkyl group having 1 to 11 carbon atoms; R2 represents a hydrogen atom or a group of the formula C(O)R4 where R4 is a hydrogen atom or a straight chain alkyl group having 1 to 11 carbon atoms; X2-X5 independently represent hydrogen; X6-X13 is same or different, and represents hydrogen or a straight or branched chain alkyl group having 1 to 12 carbon atoms. It further relates to a marker composition containing said mixtures dissolved in a solvent.

Abstract: The invention relates to aurones and extracts comprising them useful in the prophylactic and/or therapeutic treatment of an animal (including a human) with a phosphodiesterase (PDE) dependent disease or condition of the central nervous system, as well as methods, uses and other inventions related thereto.

Abstract: The invention relates to aurones and extracts comprising them useful in the prophylactic and/or therapeutic treatment of an animal (including a human) with an estrogen receptor (ER) related disease or condition of the animal or human body, as well as methods, uses and other inventions related thereto.

Abstract: The invention relates to nitric oxide donors of the formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: wherein A and A? are independently selected from the group consisting of H and —(X)S—Y with the proviso that at least one of A or A? is not H; wherein s is 0 or 1; X is selected from the group consisting of: —CO—, —COO—, —CONH— and —SO2— or Y is straight or branched C1-C20 alkyl chain, preferably C1-C10 alkyl chain, substituted with one or two —ONO2; or C1-C6 alkylenoxy-C1-C5 alkyl wherein the alkyl group is substituted by one or two —ONO2 groups. The invention also provides novel compositions comprising at least one compound of the invention and at least one therapeutic agent.

Abstract: The invention relates to novel benzofuran derivatives, processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.

Abstract: The invention provides a solid dosage form, e.g. a tablet, comprising mycophenolic acid or mycophenolate salt and a process for its production.

Abstract: This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1 and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Abstract: New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.

Abstract: The invention includes a method of dehydration of a sugar using a dehydration catalyst and a co-catalyst within a reactor. A sugar is introduced and H2 is flowed through the reactor at a pressure of less than or equal to about 300 psig to convert at least some of the sugar into an anhydrosugar product. The invention includes a process for producing isosorbide. A starting material comprising sorbitol is flowed into a reactor. H2 is counter flowed through the reactor. The starting material is exposed to a catalyst in the presence of a co-catalyst which comprises at least one metal. The exposing is conducted at a hydrogen pressure of less than or equal to 300 psig within the reactor and the hydrogen removes at least some of any water present during the exposing and inhibits formation of colored byproducts.

Abstract: In the present invention there are disclosed new derivatives of dianhydrohexite mononitrate corresponding to formula (I), tautomers, pharmaceutically acceptable salts, prodrugs and solvates thereof: as well as pharmaceutical compositions comprising these compounds and uses thereof.

Abstract: This invention generally relates to improvement of the body and skin appearance, for example enhancing the appearance of sagging, wrinkled, or cellulite-afflicted areas of the skin and body, through the local delivery of a nitric oxide donor, for example, using delivery vehicles such as lotions, creams, liquids, and/or transdermal patches. In some embodiments, a delivery vehicle containing a nitric oxide donor, for example, L-arginine (an important biological precursor) or its derivatives in a sufficient concentration to improve the appearance of a selected area of the body may be applied. In certain cases, one or more agents may also be included that aid in the transfer of the nitric oxide donor into the tissue, which may overcome the resistance to transfer into the skin. Non-limiting examples of suitable agents include agents able to create hostile biophysical environments, for instance, choline chloride, magnesium chloride, and/or sodium chloride.

Abstract: An anti-HIV tablet formulation comprising a core containing 0.1 to 1.5% by weight (w/w) of colloidal silicon dioxide and 0.4 to 0.9% by weight (w/w) of a lubricant, the balance of the core comprising darunavir, a disintegrant and a filler comprising a spray-dried mixture of microcrystalline cellulose and colloidal silicon dioxide, the core being optionally coated with a film coating.

Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Abstract: The present invention refers to compounds of the general formula (I) wherein R1 is hydrogen or hydroxy; R2 is butyl or butyryl if R1 is hydroxy, but R2 is butyl if R1 is hydrogen; or R3 and R2 taken together are 1-propylidene or 1-butylidene optionally substituted by hydroxy, methyl, or 3-(?, ?-dimethylacryloyloxy); the dotted line is an optional bond; X is an optionally substituted aliphatic C4-residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 and R4 are, independently from each other, hydrogen or hydroxy; and R5 is hydroxy or butyryl, for use in the treatment of disorders connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions containing such compounds, and their uses.

Abstract: The invention relates to substituted amino-thiourea compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amino-thiourea compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds. The substituted amino-thiourea compounds are defined by the following formula (I): wherein A, B, R1, R2, R3, R4, R5.1, R5.2 and R6 are defined as in the description.

Abstract: An antimicrobial composition of 3-iodo-2-propynylbutyl carbamate (IPBC) and 1,3-butylene glycol (BG) as solvent, in a defined weight ratio, preferably 9-11% IPBC and 89-91% BG, and personal care formulations including the composition in an amount of about 0.1-0.2% therein, at a pH of 4-9, is described.

Abstract: A composition comprising at least a strigolactone derivative (a) of general formula: and a fungicide compound (b) in a (a)/(b) weight ratio of from 1/1 to 1/1014; a composition further comprising an additional fungicidal compound; a method for preventively or curatively combating the pests and diseases of crops and increasing their yield by using this composition.

Abstract: The present invention relates to a fish feed comprising dioxabicyclo[3.3.0]octane derivates, in particular selected sesame lignans, and a vegetable oil or oil mixture comprising at least one 18-carbon chain omega-3 fatty acid. The dioxabicyclo[3.3.0]octane derivate will induce a desaturation and elongation of the 18-carbon chain fatty acid in the fish muscle into longer carbon chain polyunsaturated fatty acids.