Abstract: This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

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

Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.

Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N, wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15 wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.

Abstract: Two-phase preparation for temporally gradual administration comprising a) a phase (A) comprising water soluble vitamins and/or the corresponding provitamins, wherein phase (A) does not contain liposoluble vitamins or provitamins corresponding to liposoluble vitamins, b) a phase (B) comprising vitamins and/or the corresponding provitamins, wherein the quantity of liposoluble vitamin compounds is larger than the quantity of water soluble vitamin compounds.

Abstract: The invention provides a medical device comprising a hydrophobic analog of a medicament known to inhibit cell proliferation and migration. The invention also provides a method of treating a narrowing in a body passageway comprising placing an implantable medical device comprising a hydrophobic analog of a medicament known to inhibit cell proliferation and migration. The medicaments can be incorporated within or coated on the device. The invention further provides hydrophobic analogs of medicaments known to inhibit cell proliferation and migration.

Abstract: The invention relates to a method for inhibiting and/or preventing formation of cancer metastases and secondary malignant cancers by administration to a subject of an effective amount of a quaternary pyridinium salt of formula I wherein R? is selected from the group consisting of H, OH, CONH2, COCH3, R? is selected from the group consisting of H, CH3, R?? represents H or CH3, and X? is a pharmaceutically acceptable counterion.

Abstract: The present invention is directed to nicotinamide derivatives, and their use in treating gastrointestinal disorders.

Abstract: Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.

Abstract: Use of carboxamides of the formula (I) in which A, R1, M, Q and R are as defined in the description for controlling certain rust fungi, such as soya bean rust and coffee rust, in crop protection.

Abstract: The present invention relates to a method for treating or preventing necrotizing enterocolitis (NEC) in a human neonate in need thereof, comprising administering to the neonate a pharmaceutically effective amount of a composition comprising a poly(ADP-ribose) synthetase/polymerase (PARP) inhibitor. Also contemplated herein is an infant food or treatment composition comprising a PARP inhibitor in an amount that is 5 to 500 times greater than a daily recommended intake dosage for the PARP inhibitor.

Abstract: Compounds of the formula: wherein Ar1, Ar2, R1 and R2 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.

Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.

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

Abstract: The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.

Abstract: A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.

Abstract: The invention relates to a fungicidally active compound of the general Formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R3, R4 and R5; R1 and R2 are independently H, halo, C1-4 alkyl or C1-4 haloalkyl; and R3, R4 and R5 are each, independently, H, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 haloalkoxy, provided that at least one of R3, R4 and R5 is not H; to the preparation of these compounds, to novel intermediates used in their preparation, to agrochemical compositions which comprise at least one of the novel compounds as an active ingredient, to the preparation of the compositions and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestations of plants by phytopathogenic microorganisms, especially fungi.

Abstract: The present invention is directed to methods and kits for achieving or maintaining weight loss. These kits and methods can include administering a pharmaceutical composition comprising phentermine, topiramate and a B vitamin to a subject in need thereof.

Abstract: The invention relates to a method of attaining enhanced sexual wellness of an individual comprising administering to the genital areas of the individual, an anhydrous composition comprising a vasodilator, for example, a niacin derivative, and an acceptable carrier. The method according to the invention does not cause flushing.

Abstract: Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains and various diseases associated with the N-type calcium channels.

Abstract: An antimycobacterial combination and composition for treating tuberculosis are described. The compounds used are N-(3-[[4-(3-trifluoromethylphenyl)piperazinyl]methyl]-2-methyl-5-phenyl-pyrrolyl)-4-pyridylcarboxamide of formula (I) or a pharmaceutically acceptable non-toxic salt thereof and an amount of one or more first line antitubercular drugs.

Abstract: The instant invention relates to a combination of an EP4-receptor antagonist and an alpha-2-delta ligand, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly inflammatory, neuropathic, visceral and nociceptive pain.

Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.

Abstract: A granular, gastro-resistant product based on niacin or derivatives thereof comprises an internal part in which the niacin is substantially concentrated and an external coating, provided to cover and protect the internal part, made up of a matrix having a total weight fraction of long-chain C16-C22 saturated fatty acids of between 40% and 95% relative to the matrix. A process for the production of such a granular product is also described.

Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.

Abstract: The invention relates to 3-pyridylcarboxamide derivatives of the formula (I): wherein the various symbols are as defined in the description, compositions thereof, methods for controlling pests by applying same, and processes for their preparation.

Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.

Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.

Abstract: The instant invention describes methods of identifying compounds that modulate the activity of Sir2 enzymes. Sir2 enzymes form a unique class Of NAD+ dependent deacetylases required for diverse biological processes including transcriptional silencing, regulation of apoptosis, fat mobilization, and lifespan regulation. Sir2 activity is regulated by nicotinamide, a non-competitive inhibitor that promotes a base exchange reaction at the expense of deacetylation.

Abstract: Novel biaryl compounds having the structural formula (I): are useful in a variety of pharmaceutical applications, whether human or veterinary, and also in cosmetics.

Abstract: A chemically and physically stable, transparent, hybrid pesticide concentrate is provided for preparation of a water-based microemulsion formulation. The pesticides preferably comprise an oil-soluble pesticide component, and a pesticide component having a Lewis acid pesticide portion and a pesticide complex portion. An inactive biphasic coupling agent for the pesticide ingredients includes a solvent capable of solvating the oil-soluble pesticide component, and two organic cosolvents capable of solvating the Lewis acid pesticide portion and the pesticide complex portion pesticide ingredients, respectively. A selected emulsifier is incorporated in the concentrate. A sufficient quantity of a complexing agent is provided to maintain the electrical potential of the final concentrate at a value of about ?150 mV to about +150 mV.

Abstract: Pesticidal mixtures comprising, as active components, A) a phenylsemicarbazone compound of the formula (I), where R1 and R2 are, independently of one another, hydrogen, cyano, halogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy and R3 is C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy, or an agriculturally acceptable salt thereof, and B) a compound of the formula (II), or an agriculturally acceptable salt thereof.

Abstract: Methods for treating angina are described. A method for treating angina includes concurrently administering a compound with a therapeutic cardiovascular compound. A combination therapy employs suitable therapeutic cardiovascular compounds, such as a calcium channel blocker, a ?-adrenergic blocker, nitrates, partial fatty acid oxidation inhibitors, potassium channel activators, or a mixture thereof, in combination with a compound such as pyridoxal-5?phosphate, pyridoxic acid, pyridoxal, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, a pharmaceutically acceptable acid addition salt thereof, or a mixture thereof. The invention also includes a novel composition comprising at least one compound and nitrates, partial fatty acid oxidation inhibitors, potassium channel activators, calcium channel blockers, ?-adrenergic blockers, or a mixture thereof.

Abstract: Fungicidal mixtures comprising (1) boscalid of the formula (I) ?and (2) pyrimethanil of the formula (II) in a synergistically effective amount, methods for controlling harmful fungi using mixtures of boscalid (I) and pyrimethanil (II) and the use of boscalid (I) and pyrimethanil (II) for preparing such mixtures, compositions comprising these mixtures and also seed comprising these mixtures.

Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.

Abstract: Pesticidal mixtures comprising, as active components, 1) an 1-arylpyrazole of the formula I wherein R1 is CN, C(?O)C1-C4-alkyl, or C(?S)NH2; R2 is S(O)nR3; R3 is C1-C6-alkyl; R4 is hydrogen, halogen, amino, C1-C6-alkylamino, di(C1-C6-alkyl)amino, or 4-hydroxy-3-methoxybenzylideneamino); W is N or CR5; R5, R6 and R7 are, each independently, hydrogen, halogen, or C1-C6-haloalkyl; n is 0, 1 or 2; or its salts and 2) a compound of the formula II, or its salts, in synergistically effective amounts; use of this mixture for combating insects, arachnids, or nematodes; method for protecting plants against these pests; and method for treating, controlling, preventing or protecting a warm-blooded animal or a fish against infestation or infection by pests which comprises orally, topically or parenterally administering or applying to said animal or fish a pesticidally effective amount of this mixture.

Abstract: A pharmaceutical preparation comprising an angiotensin II receptor antagonist, a calcium channel blocker and at least one substance selected from the group consisting of a hydrophilic polymer, an acidic substance and a fluidizing agent. The pharmaceutical preparation has improved dissolution properties.

Abstract: The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein ring A, ring B, R1, R2, R3, R4, R5, m and n are as defined herein.

Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antinflammatory, antiarthritic and antiviral activity.

Abstract: A novel group of anti-inflammatory compounds are salts composed of the anion of a nonsteroidal anti-inflammatory acid drug (NSAID) and the cation N(1)-methylnicotinamide, which both anion and cation moieties alone exhibit anti-inflammatory activity, and which in this combination have advantages over the individual compounds and in comparison to commercial anti-inflammatory products. The compounds are produced in analogy to processes known in the art. They are used for the preparation of new pharmaceutical formulations with anti-inflammatory and analgesic activity. The new pharmaceutical formulations exhibit several advantageous properties over preparations of prior art.

Abstract: The present invention relates to synergistic combinations of the antifungal agent imazalil and another antifungal agent selected from the group consisting of boscalid, cyproconazole, pyraclostrobin, triflumizole, acibenzolar-S-methyl, carpropamid, fosetyl-Al, spiroxamine, tetraconazole and zoxamide for protecting plants, fruit or seeds against phytopathogenic fungi.

Abstract: The present invention is directed to N-methylnicotinamide containing food extracts, and their use in treating lipoprotein abnormalities and skin diseases and disorders.

Abstract: The invention relates to a method for the treatment or prevention of diseases or conditions associated with vascular endothelium dysfunction or liver injury comprising the administration to a patient in a need of such treatment or prevention of a therapeutically or prophylactically effective amount of a compound selected from the group consisting of: wherein R represents hydrogen atom, CH3, OH, pyridyl (C5H4N), 1-methylpyridyl (C5H4N—CH3) or pyridyl substituted with hydroxy group ((OH)C5H3N), and X represents a physiologically acceptable counterion.

Abstract: Long term weight loss can be achieved and maintained with a formulation of over-the-counter life-enhancing dietary supplements. One or more supplements stimulate the release of serotonin within the brain and one or more supplements stimulate the release of cholecystokinin into the bloodstream. The combined potentiating effect of these two mechanisms on satiety enables greater weight loss than that previously achieved by the individual mechanisms acting alone.

Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 fluoroalkyl, and —OR12; R9 is selected from H —NR13C(O)R14 and —C(O)NR10R11; R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.

Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.

Abstract: The invention relates to the use of quaternary pyridium salts of formula (1) wherein R is NH2, CH3, or N(H)CH2OH group, and X is pharmaceutically acceptable counterion, for the preparation of vasoprotective agent for the treatment or prevention of conditions or diseases associated with dysfunction of vascular endothelium, oxidative stress, and/or insufficient production of endothelial prostacyclin PGI2, in particular but not exclusively if the above coincides with hypercholes terolemia, hypertriglyceridemia or low HDL level.