Abstract: Compositions are provided that are useful for the preparation of a medicament. The compositions comprise granules having a layer of sodium picosulphate coated on potassium bicarbonate. Additional granules having a layer of magnesium oxide coated on a core of citric acid are also provided. The two types of granules may be combined to obtain mixtures (preferably homogeneous or substantially homogeneous mixtures) of the two types of granules, which are useful, e.g., as pharmaceutical compositions.

Abstract: Molecules having a spacer unit, linker and recognition unit(s) are used for the treatment of various diseases, disorders and conditions. The compounds are useful in treating infectious diseases and diseases, disorders or conditions related thereto. Further, the methods for treating diseases, disorders or conditions involve recognition and binding of carbohydrate structures.

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: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.

Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.

Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.

Abstract: The present invention relates to a stable liquid oily ready-to-use formulation comprising an active pharmaceutical ingredient, which has hydrophobic and/or lipophilic properties and/or which exhibits stability problems in aqueous environments. The present invention further relates to a method for preparing said formulation, and said formulation for use in the medical treatment of particular patient groups.

Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Abstract: This invention relates to a method of mitigating side effects of non-steroidal anti-inflammatory drugs, specifically to administration of a pyridine derivative to mitigate and/or prevent prostaglandin e2 reducing side effects of non-steroidal anti-inflammatory drugs. Also provided is the use of a pyridine derivative in the preparation of a medicament for the reduction of said side effects of non-steroidal anti-inflammatory drugs, and a pharmaceutical composition comprising a non-steroidal anti-inflammatory drug and a pyridine derivative.

Abstract: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Abstract: A compound of formula (I): in which R1-R8, A, B, X, Y, m, and n are as defined herein. Also disclosed is a method for detecting a cancer cell using a compound of formula I.

Abstract: Pharmaceutical formulations and methods of using thereof for the treatment and prevention of pulmonary arterial hypertension are provided. The formulations contain one or more agents to simultaneously reduce ADMA levels in a patient and reduce inflammatory processes in the pulmonary vasculature of a patient. The formulations contain a therapeutically effective amount of cerivastatin, a cerivastatin analog, or a pharmaceutically acceptable salt, prodrug, clathrate, or solvate thereof in a carrier suitable for pulmonary administration.

Abstract: Compounds produced by combining imino sugars and creatine are herein disclosed. The compounds being in the form of a creatine imino sugar amides and produced by the disclosed methods; protecting the guanidine group of creatine and then activating the protected creatine with DCC and reacting it with an imino sugar, followed by removal of the guanidine protecting groups. The resulting creatine imino sugar amides have enhanced stability in solution as compared to related esters. In addition, specific benefits are conferred by the imino sugar in addition to, and separate from, the creatine substituent. Methods of preparation and use of these compounds are also disclosed.

Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

Abstract: A derivative of ?-carboline alkaloid harmine, 10,12-diheptanoyl-11-hydroxy-3-methyl-?-carboline, prepared by a Friedel-Crafts acylation of harmine is reported as a novel potent antitubercular drug.

Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.

Abstract: The present invention relates, in general, to glaucoma and, in particular, to a method of preventing or treating glaucoma using statins.

Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.

Abstract: Disclosed are an antitumor preparation comprising a combination of (1) a combination drug of tegafur/gimeracil/oteracil potassium, (2) at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof, and (3) cis-oxalate(1R,2R-diaminocyclohexane)platinum(II); a kit comprising a combination of pharmaceutical compositions for treating cancer in a mammal, comprising: (a) a combination drug of tegafur/gimeracil/oteracil potassium in a therapeutically effective amount; (b) a composition containing at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof in an amount effective for enhancing antitumor effects, and (c) a composition containing cis-oxalate(1R,2R-diaminocyclohexane)platinum(II) in an amount effective for enhancing antitumor effects; and a method for treating cancer.

Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I), and methods of treating conditions associated with the activity of p38 kinase.

Abstract: A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.

Abstract: A pharmaceutical composition is provided comprising a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier. The embodiments of the pharmaceutical compositions can have lipid lowering properties, or alternatively can have properties that can treat oxidative stress, by decreasing inflammation or inflammatory processes contributing to neurodegenerative diseases. A method of lowering lipid levels in an individual is also provided, comprising administering to the individual in need of such treatment a pharmaceutical composition including a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier, wherein lipid levels are decreased.

Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: A composition for regenerative treatment of cartilage disease, which comprises a PDE4 inhibitor as an active ingredient, specifically a composition comprising a PDE4 inhibitor and a biocompatible and biodegradable polymer is provided, which composition, when formulated into a form suited to administer locally to affected cartilage region, such as microsphere preparation, can provide a pharmaceutical composition showing an excellent effect in regenerative treatment of cartilage.

Abstract: A composition for reconstruction, replacement or repair of damaged or diseased biological tissue comprising an extracellular matrix (ECM) composition that includes an ECM scaffold component derived from a mammalian source and at least one additional bioactive component selected from the group consisting of a statin and a chitin derivative.

Abstract: Methods for the treatment of Angelman Syndrome autism spectrum disorders are provided. The methods comprise administrating to a subject an agent that increases the expression of or increases activity of, ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) at neuronal synapses.

Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein R1, R2, R3 and n have the significance given in claim 1.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: Disclosed is a compound represented by the general formula shown below, which can bind to a retinoid X receptor (RXR), which is one of nuclear receptors, and exhibit an agonistic or antagonistic action. [Wherein, R1 is selected from the group consisting of an alkyl group, an alkenyl group, an alkynyl group and an aryl group. R2 is selected from the group consisting of an alkoxy group, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. W is NR3 or CR3; and R3 is selected from a hydrogen, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. X1 and Y1 are selected from CH or N. X2 and Y2 are selected from CH, CR4 or N. R4 is selected from an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen, a nitro group and an amino group. Z is selected from a carboxylic acid, a carboxylate ester or a hydroxamic acid, which is bound directly or via an alkyl group, an alkenyl group or an alkynyl group.

Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: This invention provides compositions and methods of inhibiting, suppressing, or treating a tendinous or musculoskeletal soft tissue injury. The invention further provides a method of ameliorating symptoms associated with a tendinous or musculoskeletal soft tissue injury. Additionally, the invention provides methods for evaluating the risk of developing a tendinous or musculoskeletal soft tissue injury.

Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Abstract: The present invention inter alia provides a method, and use thereof, of diagnosing and/or predicting atherosclerosis or CVD by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control and has identified specific lipid markers that are more specific and sensitive in detecting and predicting atherosclerosis and CVD than currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, preventing and/or treating atherosclerosis or CVD. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of atherosclerosis or CVD.

Abstract: A coating on a balloon of a medical device is provided. The coating comprises a drug and a polymer. Also provided are methods of forming and using the coating.

Abstract: Methods and compounds for the treatment or prevention of oxidative damage in a mammalian subject. The treatment and/or prevention may be on inhibiting heme-induced lipid peroxidation. Also discloses are methods and compounds for treating or preventing isoprostane-mediated tissue damage.

Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

Abstract: The invention generally relates to methods of treating a patient having, and/or at risk of, cardiovascular or cerebrovascular disorders. Such methods may include administering a MetAP2 inhibitor at a dose that does not substantially modulate angiogenesis.

Abstract: Subject of the invention is a method for the production of a cyanopyridine, comprising the steps of (a) providing a column comprising an absorber section and a stripping section, the absorber section being positioned above the stripping section, such that liquid which passed the absorber section enters the stripping section, (b) feeding a gaseous phase comprising the cyanopyridine into the column, (c) contacting the gaseous phase with an aqueous solution in the absorber section, such that at least a portion of the cyanopyridine is dissolved in the aqueous solution, (d) stripping the aqueous solution obtained from the absorber section in step (c) with a stripping gas in the stripping section, and (e) eluting an aqueous solution comprising the cyanopyridine from the bottom of the column. Another subject of the invention is a device for carrying out the invention.

Abstract: Methods are provided for treating disorders associated with mGlu receptors by simultaneously inhibiting at least two mGluRs belonging to at least two different groups. In one embodiment, there are provided methods for treating a disorder associated with mGlu receptors 2, 3, and 5, including administering to a subject in need thereof an effective amount of at least one antagonist which modulates mGluR2, mGluR3, and mGluRS. The disorders treated by the method include, for example, nicotine addiction, cocaine addiction, and depression.

Abstract: An NSAID formulation for encapsulation into a soft gel capsule with increased stability, concentration and bioavailability of the NSAID. The preferred NSAIDS are naproxen, ibprofen, indomethacin and diclofenac, which are provided in both an acidic and basic form in the fill formulation. The pH values of fill formulations may be adjusted without additional process steps. A process for increasing the achievable concentration of an NASAID pharmaceutical ingredient in a fill composition for dosage units is also provided. The highly concentrated NASAID formulation permits a reduction in the fill volume or dosage unit size or an increase in concentration of the NSAID in each dosage it.

Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.

Abstract: Compositions and methods for managing or treating chronic pain are provided. More particularly, methods are provided for managing or treating chronic pain by administering to a patient in need thereof an effective amount of propofol or a propofol derivative having limited anesthetic properties. Methods of modulating HCN channel gating are also provided. Pharmaceutically acceptable compositions for, e.g., modulating HCN channel gating are further provided.

Abstract: Compound of formula (I) wherein W, X, Y, Z is —C(R1)? or N; R1 is hydrogen or alkyl, V is N or C (i.e.

Abstract: The present application relates to substituted enaminocarbonyl compounds of the formula (I) in which A, B, D, R1 to R3 are each as defined in the description, to processes for preparation thereof and to the use thereof for controlling animal pests.

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).

Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.

Abstract: A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.

Abstract: Compositions of flupirtine for management of neuropathic or inflammatory pain optionally including one or more other analgesics including opiates, NSAIDS and other active agents in immediate and controlled release forms. Methods and systems for administration of these compositions.