Abstract: The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2A receptor activity. Such conditions include, but are not limited to, diseases of the central nervous system such as depression, cognitive function diseases and neurodegenerative diseases such as Parkinson's disease, senile dementia as in Alzheimer's disease or psychoses and stroke. The compounds of the present invention may also be employed for the treatment of attention related disorders such as attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD), extra pyramidal syndrome, e.g.

Abstract: The present invention relates to benzimidazole carboxamides of formula I, the use of the compounds of formula I of as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of pharmaceutical compositions and methods of treatment, comprising administering said pharmaceutical compositions to a patients.

Abstract: The invention relates to an improved pharmaceutical or dietary composition in form of an aqueous syrup, consisting essentially of (a) vitamins recommended for consumption by children or young adults, (b) a suitable calcium source, (c) at least one dibasic amino acids, (d) taurine, (e) at least one solubilizer, (f) at least one additional agent selected from the group consisting of sweetening agents, flavoring agents, flavor enhancers, preservatives, antioxidants, co-solvents, and (g) water.

Abstract: The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.

Abstract: A process for the production of a composition comprising a water-insoluble opioid which comprises the steps of: a) providing a mixture comprising: i) a water-insoluble opioid, ii) a water soluble carrier, and iii) a solvent for each of the opioid and the carrier, and b) spray-drying the mixture to remove the or each solvent and obtain a substantially solvent-free nano-dispersion of the opioid in the carrier.

Abstract: The present application discloses a pharmaceutical composition for treating Parkinson's disease and psychotropic intoxication/abusive potential, which contains a morphinan compound.

Abstract: The present invention relates to imidazopyridine derivatives of the Formula I and, therapeutically acceptable salts thereof which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the treatment of gastrointestinal inflammatory diseases. In further aspects, the invention relates to the compound of the invention for use in therapy; to processes for preparation of such new compound; to pharmaceutical compositions containing the compound of the invention, or a therapeutically acceptable salt thereof, as active ingredient; and to the use of the compound of the invention in the manufacture of medicaments for the medical use indicated above.

Abstract: Compounds of formula I processes for their preparation and pharmaceutical compositions comprising them.

Abstract: The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.

Abstract: The invention provides heteroarylene substituted 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, A, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract: A methylphenidate solution and associated methods of administration and production, which includes methylphenidate and at least one organic acid dissolved in a solvent system, where the solvent system includes at least one non-aqueous solvent. The solvent system may include water. The non-aqueous solvent can include, but is not limited to polyols and glycols and associated mixtures thereof. Pharmaceutical additives such as flavorings, colorants, buffers, preservatives and mixtures thereof may be optionally added to the methylphenidate solution.

Abstract: This invention provides a compound of formula (I): wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, R2 represents an alkyl group having from 1 to 4 carbon atoms, R3 represents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula —C(R4)(R5)— (in which R4 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R5 represents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

Abstract: An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability.

Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):

Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for determining ?-amyloid levels in a subject are described.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: The present invention relates to benzimidazole derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical compositions and methods of treatment, comprising administering said pharmaceutical compositions to patients.

Abstract: The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R1 represents methyl, R2 represents methyl or a fluorine atom and R3 represents a fluorine atom.

Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.

Abstract: Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.

Abstract: The present invention relates to anti-viral uses of leflunomide product, alone or in combination with other anti-viral agents, or in combination with a pyrimidine such as uridine.

Abstract: The present invention relates to novel diphenylurea derivatives useful as chloride channel blockers. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The present invention relates to new compounds of formula I, wherein P, Q, X1, X2, X3, X4, R1, R2, m and p, are as defined as in formula I, or, salts, solvates or solvated salts thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.

Abstract: The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

Abstract: The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate.

Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.

Abstract: Disclosed herein are analogs of Salinosporamide A, having the Formula I as follows: Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.

Abstract: Agent for the depletion of an unwanted protein population from the plasma of a subject, which agent comprises a plurality of ligands covalently co-linked so as to form a complex with a plurality of the proteins in the presence thereof, wherein at least two of the ligands are the same or different and are capable of being bound by ligand binding sites present on the proteins, wherein the agent is a non-proteinaceous agent other than a D-proline of the formula wherein R is the group R1 is hydrogen or halogen; X is —(CH2)n—; —CH(R2)(CH2)n—; —CH2O(CH2)n—; —CH2NH—; benzyl, —C(R2)?CH—; —CH2CH(OH)—; or thiazol-2,5-diyl; Y is —S—S—; —(CH2)n—; —O—; —NH—; —N(R2)—; —CH?CH—; —NHC(O)NH—;—N(R2)C(O)N(R2)—; —N[CH2C6H3(OCH3)2]—; —N(CH2C6H5)—; —N(CH2C6H5)C(O)N(CH2C6H5)—; —N(alkoxyalkyl)-; N(cycloalkyl-methyl)-; 2,6-pyridyl; 2,5-furanyl; 2,5-thienyl; 1,2-cyclohexyl; 1,3-cyclohexyl; 1,4-cyclohexyl; 1,2-naphthyl; 1,4-naphthyl; 1,5-naphthyl; 1,6-naphthyl; biphenylen; or 1,2-phenylen, 1,3-phenylen and 1,4-phenylen, wher

Abstract: This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or a branched alkylene group, B ring and C ring are selected from a benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle compound, D is —(CH2)(n+1)—, —(CH2)—O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— wherein a D ring is connected with the carbon atom composing the C ring, E is selected from an oxygen atom or a sulfur atom, P is a phosphine atom, R1˜R7, wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle, R1, R2 and R3 are not a hydrogen atom if the B ring is a benzene ring and may be the same or different and are substituents, R8 and R9 are may be the same or different and are substituents, R10 is an alkyl group, n and m are 0-10 and o is 0-2.

Abstract: Compounds having a general formula X-(A)n-Y, wherein: n varies between 6 and 20; X denotes a hydrogen atom, an RaCO, RaOCO, RaNHCO or RaSO2 group, Ra being an alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl group, the groups being substituted or not, on condition that X is different from H when n is equal to 6; A denotes either a group having formula (I) or (II), wherein Ri is a hydrogen atom, an amino acid side chain, an alkyl, alkenyl, alkynyl, aryl, aralkyl or heteroaryl group, said groups being substituted or not, i being an integer of between 1 and n; Y is an NRbRc, Rb and Rc group having the same meaning as given earlier for Ra. The compounds are used for the preparation of medicaments that are intended to treat bacterial, fungal or cytotoxic diseases and, in particular, fungal infections, such as aspergillosis and candidiasis, and resistant bacterial infections.

Abstract: The invention relates to any isolated or synthetic compound and, in particular, to compounds having formula which can: modulate the cell specification of neural stem cells, promote the differentiation and subsequent survival of differentiating glial cells and neurones, and promote the differentiation of oligodendrocyte precursor cells into mature oligodendrocytes. In addition, the inventive compounds can reduce the inflammatory component of diseases that affect the nervous system, for example, by reducing activation of the microglia an/or astrocytes and/or by reducing reactive gliosis. The invention also relates to the methods of preparing such compounds and to the use of same in the preparation of a pharmaceutical composition that is intended for the prevention or treatment of diseases that affect the nervous system. More specifically, the inventive compounds have general formula.

Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases in a human subject whereby a subject is administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative. In some embodiments, the administration of analogs or derivatives of carotenoids may inhibit and/or ameliorate the occurrence of diseases in subjects. In some embodiments, analogs or derivatives of carotenoids may be water-soluble and/or water dispersible. Maladies that may be treated with analogs or derivatives of carotenoids embodied herein may include diseases that provoke or trigger an inflammatory response. In an embodiment, asthma may be treated with analogs or derivatives of carotenoids embodied herein. In an embodiment, administering analogs or derivatives of carotenoids embodied herein to a subject may control or affect the bioavailability of eicosanoids. In an embodiment, atherosclerosis may be treated with analogs or derivatives of carotenoids embodied herein.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The invention relates to a composition for topical use containing at least one oxidation sensitive hydrophilic active principle and at least one maleic anhydride copolymer, comprising one or more maleic anhydride comonomers and one or more comonomers selected from the group consisting of vinyl acetate, vinyl alcohol, vinylpyrrolidone, olefins containing from 2 to 20 carbon atoms, and styrene, in a physiologically acceptable medium containing an aqueous phase. The invention also relates to the use of a maleic anhydride copolymer as defined above for stabilizing an oxidation-sensitive hydrophilic active principle, in particular in the aqueous phase.

Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: The present invention relates to the inhibition of melanogenesis with para-aminobenzoic acid (PABA) and its use in treating melanotic cancer.

Abstract: A composition for use as a medicament, functional food or nutritional product is described which comprises at least one lipid wherein the lipid provides greater than 35% total energy of the composition. A preferred embodiment comprises a n-6/n-3 fatty acid ratio of about 2/1 to 7/1. In addition, a method of preparing the composition; use of the composition in the manufacture of a medicament, functional food or nutritional product; and a method of treatment or treatment or prevention of sepsis or inflammatory shock which comprises administering an effective amount of the composition are described.

Abstract: Therapies are for treating patients in need of nitroglycerin therapy and allow increased dosage, postponement of tolerance and preconditioning, without exacerbating or causing hypotension. Methods for determining cross-tolerance, nitroglycerin effectiveness and dose are also disclosed. Composition for intravenous administration of nitroglycerin does not contain ethanol or contains less ethanol than conventional compositions.

Abstract: A crude oil simulant is disclosed that is an emulsion of an organic continuous phase, an aqueous dispersed phase, and an emulsifier. To enhance the biodegradability rate of the simulant various strains of bacteria can be added to the aqueous phase. Nutrients can be added to the aqueous phase to increase activity of the bacteria. The components of the simulant of the invention can be mixed under high shear conditions such as 1,000-12,000 reciprocal minutes. The emulsion based oil simulants can be prepared on-site and can be readily tailored to simulant a wide variety of crude oils under various conditions.

Abstract: An improved process for the production of ultralow density, high specific surface area gel products is provided which comprises providing, in an enclosed chamber, a mixture made up of small particles of material suspended in gas; the particles are then caused to aggregate in the chamber to form ramified fractal aggregate gels. The particles should have a radius (a) of up to about 50 nm and the aerosol should have a volume fraction (fv) of at least 10?4. In preferred practice, the mixture is created by a spark-induced explosion of a precursor material (e.g., a hydrocarbon) and oxygen within the chamber. New compositions of matter are disclosed having densities below 3.0 mg/cc.

Abstract: There is provided an acidic zirconia sol having compatibility of particle properties and binding properties, and a production method of the same. The present invention relates to a production method of an acidic zirconia sol containing zirconia particles having a particle diameter of less than 20 nm in a content of 10 to 50% by mass, based on the mass of all zirconia particles including: a first process in which an alkaline zirconia sol (A) and a zirconium salt (B) are mixed in a mass ratio (Bs/As) ranging from 0.2 to 5.0 of a mass of a solid content (Bs) which is converted into an amount of ZrO2 in the zirconium salt (B) to a mass of a solid content (As) which is converted into an amount of ZrO2 in the alkaline zirconia sol (A); and a second process in which the resultant mixture is reacted at 80 to 250° C. to produce an acidic zirconia sol.

Abstract: The present invention relates to cross-linked polyolefin aerogels in simple and fiber-reinforced composite form. Of particular interest are polybutadiene aerogels. Especially aerogels derived from polybutadienes functionalized with anhydrides, amines, hydroxyls, thiols, epoxies, isocyanates or combinations thereof.

Abstract: The invention provides reinforced aerogel monoliths as well as fiber reinforced composites thereof for a variety of uses. Compositions and methods of preparing the monoliths and composites are also provided.

Abstract: Rigid polyurethane foams are made using a polyol component that includes toluene diamine-initiated polyols containing specified levels of oxyethylene groups. Foams made from these polyols have low k-factors and excellent demold expansion values.

Abstract: The invention relates to polyurethane foams comprising oligomeric polyols. In embodiments of the invention, the polyurethane foams comprise the reaction product of: (a) a polyisocyanate; and (b) an active-hydrogen containing composition comprising an oligomeric polyol having a hydroxyl number of about 45 to about 65 mg KOH/g, a number average hydroxyl functionality (Fn) of less than about 2.7, and about 40% weight or greater oligomers. The polyurethane foams of the invention may be slabstock foams or molded foams. Also disclosed are low odor polyols and polyurethane compositions.

Abstract: Disclosed is a photosensitive resin composition. The composition comprises [A] an alkali-soluble resin, [B] a photoactive compound and [C] a solvent. The alkali-soluble resin is a copolymer including at least one structural unit with an aziridine group. The composition exhibits good storage stability, high sensitivity, high UV transmittance, high residual film ratio, improved coating uniformity and excellent pattern-forming properties. Further disclosed is an organic insulating film formed using the composition. The organic insulating film has excellent resistance to solvents and chemicals.

Abstract: This invention includes a wettable biomedical device containing a high molecular weight hydrophilic polymer and a hydroxyl-functionalized silicone-containing monomer.

Abstract: Prepolymers comprising at least one block of Formula II and terminated with a polymerizable ethylenically unsaturated radical are useful in hydrogel materials are disclosed: wherein n, R, R1, R2 and X+ are as defined herein.

Abstract: Disclosed are ophthalmic device materials having improved light transmission characteristics. The materials contain a combination of certain UV absorbers and blue-light absorbing chromophores.