Abstract: The present invention concerns the use of methods and compositions for the treatment of cancer and other hyperproliferative diseases. In certain embodiments, methods are described for the treatment of cancer and/or hyperproliferative diseases by administration of compositions containing at least one platinum complex alone or in combination with a modulator of glutathione. In particular, the methods may be used to treat cisplatin or carboplatin resistant tumor cells.

Abstract: This invention provides compounds of formula I having the structure wherein: R1 and R2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated, acyl, or aroyl; R3, R4 are H, alkyl, cycloalkyl or —CH2-cycloalkyl; R5 is H or alkyl; R6 is H or alkyl; and wherein the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods for using these compounds to treat central nervous system disorders, including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

Abstract: This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these

Abstract: This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or phenoyl or thiophenoyl; R3 and R4 are each, independently, H, alkyl or cycloalkyl; R5 is H or alkyl; R6 is H or; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions and methods utilizing these compounds for the treatment or prevention of disorders including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, 4?- and/or 6? halo and/or alkoxy analogs, and various 5? substituents that incorporate a cyclic amine moiety.

Abstract: 1,2,4-Triazin-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: The invention provides compounds of formula (1) wherein X, R1 and R2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and bipolar disorders.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.

Abstract: Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

Abstract: The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

Abstract: This invention features opioid compounds having activity at kappa and mu receptors, methods for preparing the mu/kappa opioids, and methods for the treatment of pain or a dopamine dysregulation disease, such as schizophrenia, attention deficit hyperactivity disorder (ADHD), attention deficit hyperactivity disorder (ADD), Parkinson's disease, hyperprolactinemia, depression, and addiction.

Abstract: The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ?O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ?O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.

Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17?-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.

Abstract: The present invention provides an amorphous form of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid. This invention also provides processes for preparing the amorphous form and pharmaceutical compositions including the amorphous form.

Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R11 and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. 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.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: A sodium salt, magnesium salt, lithium salt, potassium salt, calcium salt or barium salt of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole, and a pharmaceutical composition comprising the salt. The novel salt is useful as an excellent antiulcer agent.

Abstract: The invention provides compounds of the Formula: wherein m, n, A, X, Y, Z, R1, R2, R4, R6, R7, R8, R9 and R10 are as defined herein, and pharmaceutically acceptable salts, solvates, prodrugs, single isomers or racemic or non-racemic mixture of isomers thereof. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: Novel pesticides of formula (I) wherein the substituents, R, R1, R2, R2?, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2?, T, U, X and Y are as defined in claim 1; and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).

Abstract: A method for producing an optically active 2-phenyl-2,3,-dihydroxypropyl azole derivative, which is a useful compound in various fields. An optically active ?-hydroxycarboxylic acid derivative represented by general formula (1) is used as a starting material and is allowed to react with an azole acetic acid derivative (2) to produce a new, optically active azole-alkyl ketone derivative (3). Subsequently, a new, optically active azole-methyl alcohol derivative (5) is produced by highly diastereoselective alkylation by an appropriate combination of a protective group and an organometallic reagent (4).

Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.

Abstract: The present invention relates to compositions and methods for promoting tissue regeneration, preferably neural tissue regeneration. Compositions of the invention include (i) certain diphenyl sulfides, diphenyl sulfoxides, diphenyl sulfones, and sulfide, sulfoxide and sulfones of dibenzothiophene and thioxanthene, as well as various analogues and derivatives of these compounds; (ii) one or more cells harvested from an animal or organism subsequent to the administration of a composition comprising a compound of (i); or (iii) any combination of (i) and (ii). The invention can be useful in treating decreases in neuronal function, for example from injury or disease.

Abstract: The present invention provides a compound represented by formula (I): [Formula 1] wherein n is an integer selected from 1 to 20, and R1 and R2, which may be the same or different, each represent a hydrogen atom, or a linear or branched C1-C6 alkyl group, or a salt, a prodrug or a solvate thereof, as well as a drug, a pharmaceutical composition containing the compound, and the like.

Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders in which cannabinoid receptors are involved. The compounds have the general formula (I) wherein R, R1-R4 and X have the meanings given in the specification.

Abstract: A compound represented by the general formula I: I wherein R1 represents hydrogen, etc. R2 represents NHSO2R3, etc., provided that R3 represents C1-6 alkyl, etc. R5 represents hydrogen, etc. R6 and R7 may be the same or different and each independently represents hydrogen, etc. X represents oxygen, etc. Y represents oxygen, etc. Z1 to Z6 each represents carbon, etc. n is an integer of 0 to 6 and ast1 indicates that the carbon atom is asymmetric, and *2, in the case where R5 is not hydrogen, indicates that the carbon atom is asymmetric or a salt of the compound.

Abstract: The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.

Abstract: Novel 2-pyrrolidin-2-yl-1H-indole compounds corresponding to formula (I) wherein R1, R2, R3 and R4 have the meanings given in the description, and pharmaceutical compositions containing these compounds, as well as processes for the preparation of such compounds and intermediate products of this process, and related methods of treatment.

Abstract: The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases.

Abstract: Use of escitalopram (the S-(+)-enantiomer of citalopram) or a pharmaceutically acceptable salt thereof for the preparation of a medicament useful in the treatment of neurotic disorders is provided, including anxiety states, in particular generalised anxiety disorder and social anxiety disorder, post traumatic stress disorder, obsessive compulsive disorder and panic attacks.

Abstract: Disclosed herein are carbonyl compounds of Formula I, II, or III, and others as described herein. Also disclosed are methods of treating disease, such as cancer, neurological disorders, including polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, autoimmune diseases and cardiovascular conditions, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.

Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.

Abstract: The present invention relates to novel compounds of formula (I), or a salt, solvate, or physiologically functional derivative thereof, to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Abstract: A method of treating an autoimmune disease comprising administering to the subject a treatment effective amount of a histone hyperacetylating agent, or a pharmaceutically acceptable salt thereof.

Abstract: Emulsified systems of a surfactant-stabilized, biodegradable water-in-solvent emulsion with bimetallic particles contained with the emulsion droplets are useful at removing PCBs from ex situ structures. The hydrophobic emulsion system draws PCBs through the solvent/surfactant membrane. Once inside the membrane, the PCBs diffuse into the bimetallic particles and undergo degradation. The PCBs continue to enter, diffuse, degrade, and biphenyl will exit the particle maintaining a concentration gradient across the membrane and maintaining a driving force of the reaction.

Abstract: A novel emulsion comprising a material which is stabilised by a polymer resin precursor having interface active molecules incorporated therein by reaction from poorly or non-surface active materials is disclosed. The process for producing such emulsions is likewise disclosed.

Abstract: A method and a system for drying a biomass, wet pulverized coal or combinations thereof, using heat from a Fischer-Tropsch synthesis in a heat exchanger to heat a nitrogen gas, using a flue gas in a heater to heat the heated nitrogen gas to a higher temperature, passing the twice heated nitrogen gas through apparatus to pulverize the fuel source of coal, biomass or both, forming a gas/particulate stream, filtering the gas/particulate stream in a filter to remove dried fuel feed stocks and using a blower to form a first steam and nitrogen mixture for discharge, and a second steam and nitrogen mixture for mixing with additional dry nitrogen gas for introduction to the first step of the method, at the heat exchanger.

Abstract: The invention is a reactive hot melt composition which has excellent adhesion and curing properties, and can be formulated into free-flowing pellets or beads, by using an ethylene-acrylic acid copolymer, and athylene-methacrylic acid copolymer, and/or an ethylene-acrylic acid methacrylic acid terpolymer as a component of the composition along with free radical crosslinking initiators. The incorporation of a foaming agent enables the production of compositions which are useful in space-filling applications, (i.e., as so-called “anti-flutter” compositions).

Abstract: A process for increasing the molecular weight of polyacrylates, characterized in that polyacrylates which are functionalized at least on one part of their chain ends by photoinitiator groups X are exposed to actinic radiation, so that a direct linking reaction of the polyacrylates takes place.

Abstract: UV curable, liquid, oligomeric compositions are prepared from the reaction product of a Michael addition oligomer and an isocyanate capped polybutadiene. The UV curable, liquid, oligomeric compositions can be cured in the presence of fragrances to form articles that are characterized by a controlled release of the fragrance over time.

Abstract: A method for producing a particulate polymer drag reducing agent, comprising granulating a bulk polymer DRA having an average size of greater than about 100 mm in the presence of a liquid wetting agent to form a granulated polymer DRA having an average size of from about 1 to about 100 mm. The granulated polymer DRA may then be ground to form a particulate polymer DRA having an average particle size of less than about 1 mm. The “wet” granulation process may advantageously enable one-step granulation and therefore simplified production of polymer DRAs. Examples of the liquid wetting agent include blends of glycols with water and/or an alcohol. Preferred production apparatus includes use of multiple rotary jaws for the granulation.

Abstract: The present invention discloses an organic-inorganic hybrid composition with sufficient flexibility, a high dielectric constant, which can be used as a bonding layer having a high thermal stability and high dielectric constant. The composition includes a) a high Tg epoxy resin system; b) ferroelectric ceramic particles having two particle size distributions, with one of them pertaining to a nano level; c) an electrically conductive powder, such as an electrically conductive carbon black; d) at least one macromolecular flexibilizer; e) a macromolecular dispersant; and f) additives such as a diluent, an adhesive promoter, a hardener, a hardener promoter, and an organic solvent.

Abstract: A bituminous composition which comprises a bituminous component and a block copolymer which comprises at least two blocks of a conjugated diene and at least two blocks of a monovinylaromatic hydrocarbon, being of the general formula: S1—B1—S2—B2 wherein B1 is a block of polymerized conjugated diene comprising at least 50 mole % isoprene having an apparent molecular weight of from 180,000 to 400,000, S1 and S2 are blocks of polymerized monovinylaromatic hydrocarbon having a weight average molecular weight of 12,000 to 40,000, and B2 is a block of polymerized conjugated diene comprising at least 50 mole % isoprene having an apparent molecular weight of from 15,000 to 60,000; wherein the weight ratio W of B1 over B2 is in the range of 3.0 to 12.0; and wherein the content of polymerized monovinylaromatic hydrocarbon is in the range from 10 to 35 wt. %.

Abstract: Improved tensile mechanical and dynamic viscoelastic properties of silica-reinforced sulfur vulcanized rubbers can be achieved by compounding elastomers with silica in the presence of an alkoxysilane and a catalytic amount of a strong organic base. The strong organic base acts as a catalyst to accelerate the alkoxysilane-silica reaction, especially at high compounding temperatures, resulting in rubber compounds that exhibit reduced compound viscosity, improved dispersion of silica, and reduced filler flocculation after compounding, and reduced hysteresis and improved abrasion resistance in the vulcanized product, compared to similar compounds prepared at the temperature without the strong organic base catalyst.

Abstract: The present invention relates to fibers and nonwovens made from plasticized polyolefin compositions comprising a polyolefin and a non-functionalized hydrocarbon plasticizer.

Abstract: This invention relates to a composition comprising, consisting of or alternatively consisting essentially of a stabilized furfural or glycol ester of a vegetable oil fatty acid and an antioxidant such as butylated hydroxy toluene. This invention also relates to latex film-forming compositions containing stabilized furfural or glycol esters, such as a stabilized propylene glycol monoester (PGME) mixture. This invention is also directed to methods of stabilizing furfural or glycol esters of a vegetable fatty acid by contacting the esters with an antioxidant such as butylated hydroxy toluene. This invention also includes methods of preparing film-forming compositions comprising a stabilized furfural or glycol ester, such as the stabilized PGME mixture disclosed herein.

Abstract: The present invention provides a dispersant for aqueous and non-aqueous systems which can disperse insoluble fine powders in non-aqueous liquids in a short period of time and give long-term dispersion stability to the resulting dispersions without allowing the formation of hard cake or precipitates. The dispersant is a compound of the formula wherein SO is styrene oxide; R is a C8-C22 saturated or unsaturated group; x=0-100; y=1-3; z=0-100 and s=0-100. The dispersant of the invention is also particularly effective for dispersing additives into polymers such as polyesters, polyamides, polycarbonates, polyethylene and polypropylene.