Abstract: Compounds of formula I, 1

Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.

Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, incluidng angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

Abstract: A series of aryl piperazine compounds of the formula: 1

Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I 1

Abstract: A pharmaceutical composition is provided for topical administration of a local anesthetic agent. The composition comprises (a) a therapeutically effective amount of a local anesthetic agent and (b) a pharmaceutically acceptable, nonliposomal carrier comprised of a monohydric alcohol, a penetration enhancer, and polymer, which may be a hydrophilic polymer, a hydrophobic polymer or a combination thereof. The composition can be in the form of a gel, or it may form a film following application to a patient's body surface and evaporation of the monohydric alcohol. The composition provides rapid onset of local anesthesia as well as penetration of the active agent into the skin. Methods and drug delivery systems for administration of local anesthetic agents are also provided.

Abstract: A compound of the formula (I): 1

Abstract: The invention provides a combination of of trimebutine [2-dimethylamino-2-phenylbutyl-3, 4, 5-trimethoxy-benzoate hydrogen maleate] or its corresponding stereoisomers with an opioid analgesic for the preparation of a medicament to prevent and/or treat pain or nociception.

Abstract: A heterocyclic compound of the formula [I] 1

Abstract: Stable solid compositions comprising quinapril magnesium can be made using quinapril or an acid addition salt thereof, by reacting the quinapril or acid addition salt with an alkaline magnesium compound in the prsence of a solvent, so as to convert all or substantially all of the quinapril or acid addition salt to quinapril magnesium.

Abstract: Polymorphs Form B, Form C, and amorphous of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone, commonly known as cilostazol, have been identified. These polymorphs may be formed in pure form, in combination with each other, in combination with other polymorphs of cilostazol, or together with other pharmaceutical agents. Processes for preparing these polymorphs, and combinations of these polymorphs, as well as methods of use and unit dosages of these polymorphic forms, and their combinations, are described.

Abstract: The present invention relates to the use of farnesyl protein transferase inhibitors for preparing pharmaceutical compositions for treating advanced breast cancer.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: The present invention provides a percutaneously applicable preparation containing an antidementia medicament, wherein the antidementia medicament is incorporated a higher alcohol, a lactate of a higher alcohol, an ester of a higher fatty acid and a lower alcohol, or an ester of a fatty acid having 6-18 carbon atoms and propyleneglycol. The present invention also provides a rectum applicable preparation containing an antidementia medicament, wherein the antidementia medicament is incorporated a tiriglyceride of a fatty acid and/or a water-soluble macromolecule.

Abstract: New halogenobenzimidazoles of the formula 1

Abstract: A digestive system disease therapeutic or preventive agent containing as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: 1

Abstract: Pharmaceutical compositions for the therapy and the prevention of ulcer and dyspepsia relapses comprising as essential components the following components a) and b): component a): one or more components selected from the conventional anti-ulcer products; component b): organic compounds containing the —ONO2 function, or inorganic compounds containing the —NO group, characterized in that they are NO nitric oxide donors.

Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: 1

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1

Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula 1

Abstract: The present invention is concerned with means for stabilizing amlodipine maleate to prevent the formation of unwanted Michael adduct and with stabilized pharmaceutical compositions obtained thereby.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemiia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The invention relates to a crystal modification of the compound of the formula I 1

Abstract: Novel substituted pyrrolidine-2,3,4-trione compounds of formula I 1

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1

Abstract: A PGD2 receptor antagonist such as a compound of the formula (IA-a-5): 1

Abstract: Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C9 substituent other than keto in which the C9 keto substituent of taxol, a taxol analog, baccatin III or 10-desacetyl baccatin III is selectively reduced to the corresponding hydroxy group.

Abstract: Methods for treating smooth muscle hyperactivity, including urinary incontinence, while avoiding concomitant liability of adverse effects associated with tolterodine and the racemic version thereof are disclosed. The methods comprise administering a therapeutically effective amount of a mono-isopropyl metabolite or a parahydroxymethyl metabolite or a parahydroxymethyl mono-isopropyl metabolite of tolterodine or racemic versions thereof or a pharmaceutically acceptable salt of either metabolite. Pharmaceutical compositions in the form of tablets and transdermal devices comprising said compounds and acceptable carriers are also disclosed.

Abstract: The object of the present invention is to provide a tocotrienol derivative which is highly water-soluble and shows high bioavailability in the living body and &ggr;-CEHC delivering agent.

Abstract: An emulsion of &agr;-tocopherol, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans various routes is disclosed. Also included in the emulsion is PEGylated vitamin E. PEGylated &agr;-tocopherol includes polyethylene glycol subunits attached by a succinic acid diester at the ring hydroxyl of vitamin E and serves as a primary surfactant, stabilizer and a secondary solvent in emulsions of &agr;-tocopherol.

Abstract: A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical preparations containing it and the use of the compound in clinical conditions associated with insulin resistance.

Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same.

Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same.

Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: The present invention relates to the use of rhein or diacerhein compounds to treat and prevent vascular diseases that cause obstruction of the vascular system such as blood vessel restenosis and atherosclerosis.

Abstract: The invention relates to a process for dissolving at least one compound of low solubility in water, the said process comprising the essential step of mixing the compound of low solubility with at least one lipophilic amino acid derivative. The invention also relates to a cosmetic or dermatological composition comprising, in a physiologically acceptable medium, at least one compound of low solubility and at least one lipophilic amino acid derivative. Among the compounds of low solubility that are especially included are aminophenol derivatives, salicylic acid derivatives, 2-amino-4-alkylaminopyrimidine 3-oxide derivatives and DHEA, and also its chemical or metabolic derivatives and precursors.

Abstract: The present invention relates to a method for isolating and purifying only a certain unsaturated fatty acid in a high purity from fatty acids present in oils including vegetable oils and fish oils by means of crystallization. More particularly, the present invention relates to a method for isolating and purifying only the desired unsaturated fatty acid in a high purity from fatty acids present in oils by selectively using a urea-addition crystallization, and a cooling crystallization or a high liquid chromatography.

Abstract: Treatment of normal, non-cancerous, animal cells with an agent that depletes polyamines within the cells results in an inhibition of apoptosis when the cells are exposed to an inducer of apoptosis. This inhibition of apoptosis is not observed, or is observed to a lesser extent, in similarly treated cancerous cells. The method of the invention is useful in obtaining preferential killing of cancer cells, as opposed to normal cells, due to anti-cancer therapy.

Abstract: The present invention provides a method for treating a patient with HIV infection. The method includes administering to a patient a composition containing a therapeutically effective amount of a R-NSAID or a pharmaceutically acceptable salt or ester thereof. The composition is substantially free of S-NSAID.

Abstract: The invention concerns an aqueous solution capable of being injected by perinodular delivery or inhaled for use in the treatment of degenerative or autoimmune diseases or as immunomodulatory agent. Said solution is prepared by reacting camphor on ammonium hydroxide. The resulting product is then suspended in a saline solution. Said preparation having a basic pH is then neutralised with nitric acid. The resulting aqueous solution has pharmacological properties since it is an analogue of human cytokines, which makes it useful for treating degenerative or autoimmune diseases and/or as an immunomodulatory agent.

Abstract: The invention relates to amine compounds as well as methods and materials involved in modulating neurotransmitter reuptake. Specifically, the invention provides amine compounds, methods for synthesizing amine compounds, and methods for inhibiting neurotransmitter reuptake.

Abstract: This invention provides novel fullerene derivatives, particularly fullerene derivatives that are water-soluble, that modulate the activity of nitric oxide synthase (NOS) and/or calmodulin. The invention provides methods for modulating NOS activity and particularly provides methods for inhibiting NOS activity, by contacting one or more fullerene derivatives of this invention with cells or tissue that exhibit NOS activity. In a specific embodiment, the invention provides water-soluble fullerene derivatives that are selective inhibitors of neuronal NOS or iNOS. Preferred water soluble fullerenes have substituents that contain one or more amine groups, amine cationic groups.

Abstract: The invention relates to a process for the manufacture of colloidal particles of controlled shape, controlled size and controlled anisotropy with water-soluble block copolymer comprising at least one block of hydrophobic nature and at least one block of hydrophilic nature which can exhibit bulk organized structures and which can retain the morphology of the hydrophobic aggregates during dispersion in water. These aggregate dispersions can be used as thickening agents or as texturing agents for paints.

Abstract: This invention provides phyllosilicates and polyfunctional dispersants which can be manipulated to selectively control the viscosity of phyllosilicate slurries. The polyfunctional dispersants used in the present invention, which include at least three functional groups, increase the dispersion and exfoliation of phyllosilicates in polymers and, when used in conjunction with phyllosilicate slurries, significantly reduce the viscosity of slurries having high concentrations of phyllosilicates. The functional groups of the polyfunctional dispersants are capable of associating with multivalent metal cations and low molecular weight organic polymers, which can be manipulated to substantially increase or decrease the viscosity of the slurry in a concentration dependent manner. The polyfunctional dispersants of the present invention can also impart desirable properties on the phyllosilicate dispersions including corrosion inhibition and enhanced exfoliation of the phyllosilicate platelets.

Abstract: A dispersant of formula 1 1

Abstract: A catalyst and process for producing hydrocarbons using the catalyst is provided. The process involves contacting a feed stream comprising hydrogen and carbon monoxide with the catalyst in a reaction zone maintained at conversion-promoting conditions effective to produce an effluent stream comprising hydrocarbons. In accordance with this invention the catalyst used in the process includes at least one catalytic metal for Fischer-Tropsch reactions, preferably cobalt. The catalyst further includes a structural component, preferably a support, that includes a metal selected from the group consisting of oxides of Group 2 metals, Group 3 metals, Group 6 metals, Group 8 metals, Group 12 metals, Group 15 metals, and combinations thereof, preferably as the oxide.

Abstract: A gas-agitated multiphase reactor system that is effective for enabling maximum reactor productivity or minimizing reactor volume comprising at least two stages with or without recycle, wherein inlet gas superficial velocity is at least 20 cm/sec at Fischer-Tropsch synthesis, yielding a total syngas conversion of greater than about 90%, while syngas conversion in each reactor is less than 60%. More specifically, the total reactor volume is held to a minimum such that minimum reactor volume is less than 0.02 cubic meters total reactor volume/(kg C5+/hr production).

Abstract: A gas distribution grid for a slurry reactor includes a plurality of gas injectors horizontally arrayed across, and extending through, an otherwise gas and liquid impervious plate. The injectors have a throat open at both ends, with a gas pressure reducing bore at one end which is the entrance end and with the other end opening into an upward opening cone. Flow diverting means in the injectors prevents slurry solids from entering the throat and being attrited by the high velocity gas jet exiting the bore into the throat. It is preferred that the gas injectors not protrude above the top surface of the grid and flat space is eliminated by means such as angular fillers, to prevent solids accumulation top of the grid. A chamfer may be present at the junction of the bore and throat to prevent unrestricted expansion of the gas jet entering the throat. This is useful for injecting gas into a reactive hydrocarbon synthesis slurry in a slurry reactor, with reduced catalyst attrition and deactivation.

Abstract: A method of separating a portion of acrylonitrile-butadiene-styrene (ABS) from a mixture containing ABS and for separating a portion of ABS and polycarbonate (PC) from a mixture of plastics containing ABS and PC is disclosed. The method includes shredding and/or granulating the mixture of plastics containing ABS and PC to provide a selected particle size; dispersing the shredded mixture of plastics in a first aqueous solution having a specific gravity of 1.04±0.01 g/cc, a pH in the range of 11.5±0.8 and a surface tension of 34±4 dynes/cm wherein a first reject fraction floats and a first retained fraction sinks, separating the first reject fraction from the first aqueous solution, introducing the first retained fraction into a second aqueous solution having a specific gravity of 1.09±0.01 g/cc and a pH in the range of 11.5±0.