Abstract: This invention provides compounds and their pharmaceutically-acceptable salts, pharmaceutical formulations of said compounds, and methods for treating hyperglycemia associated with non-insulin dependent diabetes and for treating hyperlipidemia.

Abstract: N-(5-isoxazolyl)benzenesulfonamides and N-(3-isoxazolyl)benzenesulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. N-isoxzolyl-4-biphenylsulfonamides are particularly preferred. These compounds exhibit activity as endothelin receptor B antagonists. Methods for treating endothelin-mediated disorders, particularly inflammatory diseases, such as asthma, by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.

Abstract: Fungicidal mixtures, comprising as active components a) a compound of the formula I  its N-oxide or one of its salts where: R1, R2, R3, R4 independently of one another are: hydrogen, hydroxyl, nitro, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-haloalkylthio; R5, R6, R7 independently of one another are: hydrogen, hydroxyl, cyano, nitro, halogen, C1-C7-alkyl, C1-C7-haloalkyl, C1-C7-alkoxy, C1-C7-haloalkoxy, C1-C7-alkylthio, C1-C7-haloalkylthio, C1-C7-hydroxyalkyl, C2-C4-acyl, aryl, aryloxy, where the radicals with aryl may for their part carry one to three of the following groups: cyano, nitro, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-alkylthio and C1-C4-haloalkylthio, and b) carbamates of the formula II, in which T is CH or N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, where the radicals R may be different if n is 2, in a synergistically effective amount.

Abstract: Compounds of the Formula (I): are useful in the treatment of disorders associated with brain dopamine dysregulation.

Abstract: Compounds of the Formula (I): are useful in the treatment of disorders associated with dopamine dysregulation.

Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by ca

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

Abstract: The invention features enediynes and methods for their production and use. The enediynes of the invention have the formula: wherein R1 is a hydroxyl group or a moiety that can be replaced by a hydroxyl group in a hydrolysis reaction; each R2 is, independently, H or a monovalent hydrocarbon moiety containing between 1 and 4 carbon atoms, inclusive; R3 is a pyrrole, furan, or thiophene ring; and X is an integer between 4 and 10, inclusive.

Abstract: Indolecarboxylic acid compounds and derivatives thereof, notably 4,6-dimethoxyindole-2-carboxylic acid and derivatives thereof, are especially useful for inducing/stimulating mammalian hair growth and/or preventing/retarding mammalian hair loss.

Abstract: Taxane prodrugs comprise a taxane joined by a hydrolyzable bond to one or more oligomers that comprise a polyethylene glycol moiety. The oligomer preferably further comprises a salt-forming moiety.

Abstract: The present invention concerns an unexpected synergistic combination of known antineoplastic agents which provides unexpectedly greater efficacy than the single agents alone. Accordingly, the present invention provides a method of treating neoplasia in a subject in need of treatment, by administering to the subject an amount of paclitaxel effective to treat the neoplasia, in combination with an amount of discodermolide effective to treat the neoplasia, wherein a synergistic antineoplastic effect results. The present invention further provides a synergistic combination of antineoplastic agents, comprising an effective antineoplastic amount of paclitaxel and an effective antineoplastic amount of discodermolide.

Abstract: The invention provides a method, compounds, and compositions for inhibiting the replication or proliferation of a virus. In accordance with the invention, at least one cannabichromene derivative is exposed to the virus, a host cell, or an infected cell under conditions sufficient to inhibit the replication or proliferation of the virus.

Abstract: The present invention relates to a novel methyl analog of simvastatin, which has the ability to inhibit the synthesis of cholesterol. The compound of the present invention holds promise for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders. The invention also relates to a process for making the novel compound.

Abstract: The present invention provides a method of preventing pest feed harm on a fibrous product, a composition preventing pest feed harm on a fibrous product and uses of 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine for preventing pest feed harm on a fibrous product. The method comprises applying to a fibrous product, an effective amount of 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine. The composition comprises a carrier and as an active ingredient 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine.

Abstract: This invention is directed to a method for preventing or treating psychotic disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

Abstract: Novel methods are provided for the manufacture of 117mSn(Sn4+) DTPA. The method allows the use of DTPA, a toxic chelating agent, in an approximately 1:1 ratio to 117mSn(Sn4+) via either aqueous conditions, or using various organic solvents, such as methylene chloride. A pharmaceutical composition manufactured by the novel method is also provided, as well as methods for treatment of bone tumors and pain associated with bone cancer using the pharmaceutical composition of the invention.

Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Cytospora sp. MF 6608 (ATCC PTA-1691) is also disclosed, as well as processes for making a compound of the present invention employing the culture.

Abstract: Clear, high load water miscible emulsions of pyrethroid insecticides or triazole fungicides, as a single phase, translocatable composition which is free of xylene and alkylphenol ethoxylate surfactants and concentrate matrix for the active agricultural component at between about 5 and about 25 wt. % active concentration.

Abstract: The present invention provides a method and composition for treating skin disorders, skin pathologies and pruritus, which includes applying a compound of formula (I) in a suitable formulation to the affected area.

Abstract: Derivatives of simple carboxylic acids, particularly trisodium citrate and other citrate salts are effective agents for enhancing the production of blood clotting factors. Addition of citrate to plasma, especially at concentrations between 2 and 10% by weight, does not appreciably denature labile proteins. However, citrate is effective in inactivating or inhibiting a variety of pathogenic microorganisms. Further, the added citrate potentiates or enhances the killing of microorganisms by heat treatment. The added citrate causes a dramatic increase in the weight of cryoprecipitate that can be produced from plasma by the usual procedures. The majority of significant clotting factors are greatly concentrated in the resulting cryoprecipitate. Increasing the amount of citrate in blood bags so that the final concentration will be at least 2% by weight results in plasma that provides improved platelet concentrates because added citrate helps eliminate contaminating microorganisms.

Abstract: Methods and compositions are disclosed for prevention and/or treatment of diseases in which 5- and 12-lipoxygenase activity contributes to the pathological condition, by administration of 12-methyletradecanoic acids alone and in conjunction with other therapeutic compounds. Methods to inhibit lipoxygenase-mediated inflammations are disclosed.

Abstract: The present invention provides a highly efficient method for treating substance addiction and for changing addiction-related behavior of a mammal suffering from substance addiction. The method includes administering to a mammal an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. The present invention also provides a method of treatment of cocaine, morphine, heroin, nicotine, amphetamine, methamphetamine, or ethanol addiction by treating a mammal with an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. In one embodiment, the method of the present invention includes administering to the mammal an effective amount of a composition which increases central nervous system GABA levels wherein the effective amount is sufficient to diminish, inhibit or eliminate behavior associated with craving or use of drugs of abuse.

Abstract: Benzene butyric acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, renal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: The use of isolated or purified stilbenoid compounds including longistyline A-2-carboxylic acid as a dietary supplement to mammals suffering from elevated triglyceride levels is described. The invention also relates to the use of such stibenoid compounds in combination with other hypotriglyceridemic agents.

Abstract: The present invention relates to methods and compositions comprising a very low dose of cyclobenzaprine or metabolite thereof for preventing and treating sleep disturbances and illnesses manifested with sleep dysfunction including fibromyalgia syndrome, chronic fatigue syndrome, sleep disorders, psychogenic pain disorders or chronic pain syndromes or symptoms thereof. The present invention further relates to methods and compositions for treating sleep disturbances, chronic pain or fatigue in humans suffering from fibromyalgia syndrome, chronic fatigue syndrome, sleep disorders, psychogenic pain disorders, chronic pain syndromes using a very low dose of cyclobenzaprine.

Abstract: Facilities to convert natural gas into syncrude often are located at remote sites. At these sites and in their surrounding communities there exists demand for salable products: gasoline, distillate fuels, solvents, lubricants, etc. While it would be possible to produce these products from syncrude, the construction of such production facilities would be very expensive, and their operation would be difficult at the remote site. Fischer-Tropsch syncrude will be waxy and will also contain volatile components, complicating the shipping of both Fischer-Tropsch products from remote production sites to developed sites and salable products from developed sites to remote sites. This invention describes a safe process to both transport Fischer-Tropsch syncrude from the remote site to the developed site and supply salable products from the developed site to the remote site.

Abstract: A process for rejuvenating reversibly deactivated catalyst particles in a three-phase slurry body of gas bubbles and catalyst particles in a slurry liquid, includes passing slurry from the top down to the bottom of the body through a slurry catalyst rejuvenating means. The slurry is sequentially passed through a first gas bubble reducing zone, a catalyst rejuvenating gas contacting zone, a second gas bubble reducing zone and then a downcomer transfer zone. The gas bubble reducing, contacting and at least a portion of transfer occur in slurry body. At least part of the means is in the slurry body.

Abstract: Mechanical/chemical method and composition for de-vulcanization of rubber maintains the macromolecules, renders sulfur passive for later re-vulcanization, is cost effective, environmentally friendly and produces high quality de-vulcanized rubber to replace virgin rubber. Waste rubber is shredded, crushed and metal-removed. Modifying composition is added as the particles of shredded waste rubber are poured between two rollers that further crush the particles. The modifying composition is a mixture of (1) a proton donor that selectively breaks the sulfur bonds and renders the sulfur passive, (2) a metal oxide and (3) an organic acid that build new bonds between macromolecules for later re-vulcanization, (4) an inhibitor that prevents re-attachment of sulfur radicals with each other before the proton donor attaches itself to the sulfur and (5) a friction agent that prevents sliding of the waste rubber between the rollers. The particles are subjected to at least ten sets of rollers.

Abstract: The present invention relates to a process for preparing post-crosslinked polymer bead with increased surface area and pore volume, and suitable pore size, allowing the separation of organic compounds by post-crosslinking gel-type copolymer bead whose crosslinking degree is low and initial surface area is small, or macroporous-type copolymer bead whose crosslinking degree is high and initial surface area is intermediate in the presence of a Friedel-Crafts catalyst, and polymer beads produced thereby. Though the surface area and pore volume of polymer beads may be varied depending on physical properties of copolymer beads and Friedel-Crafts reaction conditions, the present invention provides polymer beads with larger surface area than that of commercially available polymeric adsorbents produced by the conventional method employing a porogen only.

Abstract: Flexible polyurethane, polyacrylic and polybutadiene foams can be obtained with cyclopentane as a blowing agent and are useful as coatings for leather or leather substitutes.

Abstract: A polymer composition for powder foam molding which comprises (A) a polymer having an epoxy group, (B) a peroxide having a temperature for obtaining a half-life of 10 hours of 100° C. or higher, (C) at least one of quaternary ammonium salts and quaternary phosphonium salts, and (D) a thermally decomposable foaming agent. According to the present invention, the polymer composition for powder foam molding, excellent in storage stability, capable of crosslinking and foaming in a short time, capable of giving a foam having a small compression set, excellent surface texture and little skin lack of hiding, powder of the composition, a foam obtained from the composition, a method for producing the foam, and a molded article comprising the foam.

Abstract: A urethane-modified polyisocyanurate foam obtained by reacting (A) a polyisocyanate compound component, (B) a polyol component, containing a modified phenolic resin obtained by adding 20 to 100 parts by weight of a polyhydric alcohol or its alkylene oxide adduct to 100 parts by weight of a benzylic ether type phenolic resin and heating under a reduced pressure, in an amount of at least 3 wt % to the total resin component, (C) water and (D) a foam stabilizer comprising a mixture of at least 2 silicone type surfactants having different surface tensions wherein a surfactant having a higher surface tension has a surface tension of higher than 22 dyne/cm and a surfactant having a lower surface tension has a surface tension of at most 22 dyne/cm, in the presence of (E) a urethane-forming catalyst and/or a trimerization catalyst.

Abstract: This invention relates to an improved dosing assembly (valve/feed line/liquid collecting vessel) which permits nearly immediate response time to an actuator signal. Such an assembly is used for the controlled introduction of any liquid through a valve into a collecting vessel. In particular, the inventive assembly exhibits substantially no leakage from the feed line into the liquid collecting vessel when the valve is closed and an instantaneous introduction of the feed line liquid into the liquid collecting vessel upon opening of the valve, both when a liquid possessing a surface tension of about 50 dynes/cm2 is used as the measurement standard. This assembly is particularly and preferably suited for injecting colorants into reactants for the production of polyurethane slabstock foam and permits a substantial reduction in foam waste due to low colorations during an on/off cycle.

Abstract: New, useful and surprisingly effective antiscorch compositions for utilization within polyurethane foam production methods which utilize very popular tertiary amine catalysts are provided. Such compositions require the presence of nominal yet effective amounts of organic cyclic ester materials. The ring systems of such materials appear to open during exposure to heat (during the curing process) and release carboxylic acids into the curing formulation. The tertiary amines become quenched by the carboxylic acids and thus do not exhibit heat destabilization. The resultant foams exhibit extremely low, if no, areas of excessive heating (i.e., scorch) and thus are substantially uniformly colored throughout. The processes and resultant foams are also contemplated within this invention.

Abstract: The present invention provides thick extruded foam which is extruded polyolefin resin foam having open cells, used for cushion material and packaging material and the like, which exhibits uniform physical product properties, high expansion ratio, and uniform cell diameter. The extruded open cell foam of the present invention is an extruded foam exhibiting an open cell foaming ratio of 50% or greater, the base resin whereof is principally composed of a mixed polymer consisting of 4.5 to 75 parts by weight of component A consisting of an ethylene ionomer resin, 0.5 to 30 parts by weight of component B consisting of a polyolefin resin having a melting point exceeding 120° C., and 20 to 95 parts by weight of component C consisting of one or two or more polymers selected from a group of ethylene-propylene rubbers, styrene elastomers, and polyethylene resins having melting points of 120° C. or lower (where component A+component B+component C=100 parts by weight).

Abstract: Polyurethane foams containing a syntactic phase and a cellular, non-syntactic phase are useful as reinforcing foams, such as in automotive applications. The foams are conveniently made in the reaction of a high viscosity isocyanate-reactive component and a high-viscosity polyisocyanate component, at least one of which contains a plurality of hollow microspheres.

Abstract: The invention relates to a binder for powder coating materials having an oligomeric or polymeric substructure which are curable thermally and/or by means of high-energy radiation, said binder comprising in each case terminally and/or laterally at least one vinyl ether group a) and at least one group b) which is different from the vinyl ether groups a) but is coreactive with said groups a), there being on average at least one vinyl ether group a) and one coreactive group b) per oligomer or polymer molecule. The invention also relates to powder coating materials comprising such a binder and to the use of said powder coating materials for coating surfaces, especially in the form of an automotive top coat and a coil coating material.

Abstract: The present invention relates to radiation curable aqueous polyurethane dispersions containing 0.05 to 20 wt. %, based on the weight of the non-aqueous constituents of the aqueous polyurethane dispersions, of 2,2-dimethyl-3-hydroxypropionic acid-(2,2-dimethyl-3-hydroxypropyl ester), (HPSNPG, calculated as MW 204.3). The invention also relates to substrates coated with these polyurethane dispersions, in particular to coated wood substrates with good grain enhancing properties.

Abstract: A compound and a method of forming a photopolymerizable acrylated glycidyl acrylic terpolymer resin compound is disclosed. The polymeric resin may be formed in a two-step process. A photopolymerizable acrylic hybrid polymer is suitable for forming films having glass transition temperatures from about −55 degrees C. to about 110 degrees C. A non-aromatic photopolymerizable acrylate polymer may be formed by combining, in a first step, a reactive source of epoxide ion groups. In a second step, the glycidyl acrylic terpolymer formed in the first step is reacted with a catalyst and a source of unsaturated acid or anhydride to form an acrylate polymer. A ring opening reaction is employed such that an acid or an anhydride containing a conjugated double bond forms an acrylated acrylic, an acrylated fluorinated acrylic, an acrylated silonted acrylic, or an acrylated halogenated grafted acrylic. The cure process is initiated with specific UV or visible light promotors and/or with a UV or visible light source.

Abstract: A cationic, water-soluble polymer is disclosed as an ink-jet ink resin to improve color-fastness and adhesion of an ink-jet printing ink. Also disclosed is a method for preparing the invention resin and the ink-jet ink formulation comprising same.

Abstract: A low-cost, efficient method of preparing hierarchically ordered structures by combining, concurrently or sequentially, micromolding, latex templating, and cooperative self-assembly of hydrolyzed inorganic species and amphiphilic block copolymers.

Abstract: A powder coating composition comprising metallic flakes having a leafing agent adsorbed on their surfaces, said metallic flakes being mixed with a thermosetting resin powder or deposited onto a surface of a thermosetting resin powder. A novel powder coating composition of the present invention provides a metallic coating having an excellent metallic luster.

Abstract: An aqueous resin composition comprising a polyepoxy compound represented by formula (I): wherein n represents a number of from 0.1 to 20; Z represents a single bond, an alkylidene group having 1 to 4 carbon atoms or a sulfone group; and X represents a hydrogen atom or a glycidyl group, provided that at least 10% of nX's represent a glycidyl group, and water.

Abstract: A novel process for preparing polymers having an average particle size of less than about 40 micrometers is described. The process involves dissolving a polymer in a solvent to form a solution that is introduced into an agitating aqueous medium.

Abstract: An activated, substantially water soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated poly(ethylene glycol) and the biologically active agent.

Abstract: A thermosetting weatherable powder coating composition applyable to a temperature sensitive substrate by means of electrostatic spray or fluidized bed, and curable at low temperature to form a textured surface to hide irregularities on the surface of the underlying substrate. The powder coating composition includes a hardener with a functionality of 2 or greater capable of reacting with an acid or anhydride functional group, a polymeric coreactant with a functionality of 2 or greater capable of reacting with the hardener, a carboxylic acid functional polyester and optionally, a catalyst, but no texturing agent. The polymeric coreactant is made by polymerizing an ethylenically unsaturated monomer and at least one carboxyl acid functional ethylenically unsaturated monomer or anhydride functional ethylenically unsaturated monomer, and mixtures thereof.

Abstract: An composition is provided which comprises a first component and a second component in which the first component comprises a peroxide, a liquid which comprises water, a sugar, and a solid particulate; and the second component comprises a polymer, a crosslinking agent, and a solid particulate. Also disclosed are processes for reducing fluid loss in a grouting composition and for anchoring a reinforcing member in a hole using the composition disclosed above.

Abstract: Polyolefin mouldings which have excellent stability on permanent contact with extracting media comprise, as stabilizers, a selected mixture comprising an organic phosphite or phosphonite and a specially selected group of sterically hindered phenols or a certain group of sterically hindered amines. In addition, a selected three-component mixture comprising a phosphite or phosphonite, a phenolic antioxidant and a certain group of sterically hindered amines is particularly suitable as stabilizer for polyolefin moldings which are in permanent contact with extracting media.