Abstract: Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

Abstract: The present invention relates to the use of aminothiazole derivatives of Formula I of as inhibitors of PAI-1, and to novel classes of aminothiazole derivatives, their synthesis and their use as inhibitors of PAI-1. It has been discovered that compounds of Formula I: or a solvate, hydrate or a pharmaceutically acceptable salt thereof, wherein Y, Ar1, Ar2, R1, R2, Z, m and n are described in the specification, inhibit plasminogen activator inhibitor-1 (PAI-1). These compounds can be used in the prophylaxis or for the treatment of thrombosis, angina pectoris, cerebral infarction, myocardial infarction, pulmonary infarction, intra-atrial thrombus in atrial fibrillation, deep venous thrombus, disseminated intravascular coagulation syndrome, diabetic complications, restenosis and stroke.

Abstract: A compound of the formula XXV(H) wherein the substituents are defined as set forth in the specification which are useful intermediates for the production of derivatives of 2-(iminomethyl)-amino-phenyl having inhibitory activity on NO-synthase enzymes.

Abstract: In accordance with the present invention, it has been discovered that PPAR&ggr; is expressed consistently in each of the major histologic types of human liposarcoma. It has further been discovered that maximal activation of PPAR&ggr; with exogenous ligand (a thiazolidinedione or derivative thereof) promotes terminal differentiation of primary human liposarcoma cells. It has still further been discovered that RXR-specific ligands are also potent adipogenic agents in cells expressing the PPAR&ggr;/RXR&agr; heterodimer, and that simultaneous treatment of liposarcoma cells with a thiazolidinedionyl moiety (a PPAR&ggr;-selective class of compounds) and an RXR-specific ligand results in an additive stimulation of differentiation. Accordingly, according to the invention, there have been identified compositions which are useful for the treatment of liposarcomas.

Abstract: Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotropin releasing factor (CRF) antagonists.

Abstract: The present invention relates to methods for inhibiting bone resorption in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of an EP4 receptor subtype antagonist.

Abstract: The invention is directed to methods and compositions that can be used in the treatment of headaches. In particular, methods and compositions are described involving the combination of a long-acting NSAID and a 5-HT agonist. Included among the long-acting NSAIDs are cyclo-oxygenase-2 inhibitors.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: Compounds, known as heteroarotinoids, having varying abilities to inhibit growth of certain cancerous cells, induce normal cell differentiation, and induce apoptosis or death of cancerous cells, of the general formula: in which: Ar and Ar′ denote aryl substituents, and wherein at least one of said aryl substituents comprises an aromatic ring having at least one heteroatom in a fused, partially saturated ring; W denotes O or S; and Q denotes H or i-C3H7.

Abstract: Farnesyl diphosphate analogs, specifically the 3-substituted alcohol precursors of the diphosphate analogs, 3-allylfarnesol and 3-vinylfarnesol, are potent inhibitors of mammalian protein fanesyltransferase (FTase). 3-allylgeranylgeraniol is a highly specific cellular inhibitor of protein geranylgeranylation (GGTase I). Furthermore, these compounds are able to efficiently block the anchorage-dependent growth of ras transformed cells. While 3-allylfarnesol inhibits protein farnesylation in situ, 3-vinylfarnesol instead leads to the abnormal prenylation of proteins with the 3-vinylfarnesyl group. In a similar manner, treatment with 3-allylgeranylgeraniol inhibits protein geranylgeranylation while 3-vinylgeranylgeraniol restores protein geranylgeranylation in cells.

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an &agr; bonds, the solid triangle represents a &bgr; bond, the wavy segments represent &agr; or &bgr; bond, dashed lines represent a double bond or a single bond R, , R1, R2 and R3 are as defined in the specification.

Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.

Abstract: Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is I and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.

Abstract: The present invention deals with the certain novel esters derived from specific cyclic ether containing alcohols. These products have surprising hydroalcoholic solubility and a very desirable skin feel, making them ideal candidates for use in products like after shave preparations.

Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B; R1, R2, R3, R4 and R5 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds, a method for treating or preventing Type II Diabetes Mellitus.

Abstract: A &ohgr;-substituted phenyl-prostaglandin of formula (I), a process for the preparation thereof, a mediciament comprising it as active ingredient (all symbols have the same meaning as described in the specification). The compounds of the formula (I) bind strongly in PGE2 receptor (especially subtype EP4) and therefore are useful for the prophylaxis and/or treatment of immune diseases (autoimmune diseases (amyotrophic lateral sclerosis (ALS) etc.), post-transplantation graft rejection, etc.), asthma, abnormal bone formation, neurocyte death, pulmopathy, hepatopathy, etc. They are also related to sleeping disorders and platelet coagulations, and therefore they are also applicable to these diseases.

Abstract: Tannate compositions consisting of carbetapentane tannate and pyrilamine tannate, which are effective when administered orally for the symptomatic relief of coryza associated with the common cold, sinusitis, allergic rhinitis, unproductive cough and upper respiratory tract conditions, are disclosed.

Abstract: An aqueous insecticide composition consisting essentially of acetic acid and at least one additional acid selected from the group consisting of citric acid, malic acid and ascorbic acid.

Abstract: The present invention contains halogenated 2-amino-3,4 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: Rosacea is treated by application of a composition containing lipoic acid and/or a lipoic acid derivative such as dihydrolipoic acid, a lipoic or dihydrolipoic acid ester, a lipoic or dihydrolipoic acid amide, a lipoic or dihydrolipoic acid salt, and mixtures of any of these. Preferred compositions further comprise &agr;-hydroxy acids or acid derivatives such as glycolic and/or lactic acid. Other embodiments also contain fatty acid esters of ascorbic acid such as ascorbyl palmitate, and/or tocotrienol.

Abstract: A topical composition for delivering an effective amount of a pharmaceutically acceptable drug, including laureth-4, propylene glycol, dimethylsorbide, and a pharmaceutically acceptable diluent is described as an improved drug delivery composition. Further, a method of transepithelial delivery of a drug to a human by topical application to the skin of a human of a composition including laureth-4, propylene glycol, dimethylsorbide, a pharmaceutically acceptable diluent of water and ethanol and an effective amount of a pharmaceutically acceptable drug has beneficial delivery effects.

Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.

Abstract: A compound of the formula: wherein Ar is an aromatic group; X and Y are a bivalent group selected from —O—, —S—, —CO—, —SO2—, —NR8—, —CONR8—, SO2NR8 and —COO— (wherein R8 is H, a hydrocarbon group or acyl), or a bivalent C1-6 aliphatic hydrocarbon group which may contain one or two above bivalent groups; R1 and R2 are H or C1-6 alkyl, or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring; and ring A is a monocyclic aromatic ring, or a salt thereof or a prodrug thereof exhibits an excellent inhibitory activity of the production and/or the secretion of amyloid-&bgr; protein.

Abstract: The present invention relates to new uses of S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate, (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by therapeutic agents, radiation treatment or diabetes. In particular, the invention provides a method for treating neurotoxicity and nephrotoxicity associated with the administration of chemotherapeutic agents.

Abstract: Aqueous germicidal compositions comprising a phenolic compound and a phenate and methods of treating animal skin with the compositions are provided. The compositions have a pH of from about 6-10 and comprise from about 1-2% by weight of a phenolic compound and a quantity of phenate to give a phenolic compound to phenate weight ratio of from about 0.81:1 to 10,000:1.

Abstract: Methods and compositions for improving sleep in individuals with sleep disorders or other conditions which interfere with normal sleep via administration of a NO-mimetic are provided.

Abstract: The invention relates to fine emulsions comprising at least one W/O emulsifier and at least one hydrophilic component, and to a process for their preparation. The fine emulsions are obtainable by converting a W/O preemulsion comprising at least one W/O emulsifier into an O/W fine emulsion by adding at least one hydrophilic component and, where appropriate, changing the temperature. Suitable W/O emulsifiers are preferably sorbitol esters. The fine emulsions are preferably spray emulsions for cosmetic and pharmaceutical applications.

Abstract: Process and economic advantages are achieved by the integration of a Fischer Tropsch process for hydrocarbon liquids production as a retrofit in an installation for the production of ammonia fertilizer from fossil fuel derived syngas. Utilization of most of the CO and part of the H2 in the syngas stream during Fischer-Tropsch synthesis as the first step in the integrated process produces hydrocarbon products while the F-T effluent containing unreacted hydrogen gas at the necessary ratio of H2/N2 is used in the second step of ammonia synthesis. The overall product slate as appropriate for maximum economic performance of the installation is thus achieved.

Abstract: A catalyst, which can be used in the Fischer-Tropsch process, and contains cobalt oxide having crystals with an average size ranging from 20 to 80 Å supported on an inert carrier of alumina. A preparation process for the catalyst and a Fischer-Tropsch process utilizing the catalyst are also provided.

Abstract: A continuous method for making foams having uniform and/or small cell sizes and articles made with these foams are described. The method allows for adjusting or controlling cell size and cell size distribution by controlling temperature and/or blowing agent concentration. The foams feature small and/or uniform cell sizes and may be comprised of amorphous thermoplastic polymers, pressure sensitive adhesive compositions, and immiscible thermoplastic polymer compositions. A method for coextruding the foams is also described.

Abstract: A foam composition that includes a vehicle and surface-modified nanoparticles disposed in the vehicle. The individual nanoparticles having a particle diameter of less than about 100 nanometers.

Abstract: To provide a type of phenol foam characterized by the fact that the phenol foam is formed by using a hydrocarbon as the foaming agent. The phenol foam has excellent heat-insulating performance, high compressive strength and other mechanical strengths, improved brittleness and is friendly to the environment of the earth.

Abstract: In a process for producing flexible polyurethane foams by the reaction known per se of polyisocyanates with compounds containing at least two hydrogen atoms which react with isocyanate, the reaction is carried out in the presence of cyclic or heterocyclic compounds containing at least one reactive hydrogen atom.

Abstract: Low-density hydrophilic flexible polyurethane foams are prepared by reacting organic and/or modified organic polyisocyanates (a) with a polyetherol mixture (b) and, if required, further compounds (c) having hydrogen atoms reactive toward isocyanates, in the presence of water and/or other blowing agents (d), catalysts (e) and, if required, further assistants and additives (f), by a process in which the polyetherol mixture (b) consists of b1) at least one difunctional or polyfunctional polyetherol based on propylene oxide and/or butylene oxide and ethylene oxide, having an ethylene oxide content of more than 40% by weight, based on the total amount of alkylene oxide used, an OH number of from 20 to 120 mg KOH/g and a proportion of primary OH groups of more than 20% and b2) at least one difunctional or polyfunctional polyetherol based on propylene oxide and/or butylene oxide and, if required, ethylene oxide, the ethylene oxide content being not more than 40% by weight, and having an OH number of more than 25 m

Abstract: A method for making an energy-absorbing foam having a density that is less than about 7 pcf that exhibits excellent strength properties and that is particularly suitable for automobile bumper applications. The invention is also directed to the energy-absorbing foam made with the method.

Abstract: Azeotrope-like compositions of 1,1,1,3,3-pentafluoropropane and at least one hydrocarbon selected from the group n-pentane, iso-pentane, cyclopentane, n-hexane and iso-hexane are provided. The compositions of the invention are useful in the preparation of polyurethane and polyisocyanurate foams.

Abstract: A continuous method for making foams having uniform and/or small cell sizes and articles made with these foams are described. The method allows for adjusting or controlling cell size and cell size distribution by controlling temperature and/or blowing agent concentration. The foams feature small and/or uniform cell sizes and may be comprised of amorphous thermoplastic polymers, pressure sensitive adhesive compositions, and immiscible thermoplastic polymer compositions. A method for coextruding the foams is also described.

Abstract: The present invention relates to polyol mixtures which are suitable for the preparation of rigid polyurethane foams and comprise addition products of alkylene oxide on aromatic di- or polyamines, and rigid foams prepared with these polyol mixtures.

Abstract: A method of reducing the flow viscosity of a polyacrylate composition, which comprises adding a) to a polyacrylate, a polyacrylate copolymer, a polyacrylate mixture or a mixture of polyacrylates and polyacrylate copolymers having an average molecular weight of more than 500000 g/mol b) a polyacrylate, a polyacrylate copolymer, a polyacrylate mixture or a mixture of polyacrylates and polyacrylate copolymers having an average molecular weight of less than 500000 g/mol, component (b) possessing functional groups crosslinkable by UV irradiation.

Abstract: An ink-jet ink is provided including an ink jet vehicle and a colorant. The vehicle includes at least 35% by weight radiation curable material, based on the total vehicle weight. The vehicle may but does not necessarily include a thickener. The vehicle is a paste or a solid at 20° C. and has a viscosity of less than 25 centipoise between 40° C. and 130° C.

Abstract: Disclosed are hyaluronate-containing hydrogels having angiogenic and vascularizing activity and pre-gel blends for preparing the hydrogels. The hydrogels contain a cross-linked matrix of a non-angiogenic hyaluronate and a derivatized polysaccharide material, in which cross-linking is effected by free-radical polymerization. Kits for preparing the hydrogels are also disclosed.

Abstract: A radiation-curable inkjet composition for forming 3-D models or images comprising a semi-crystalline or crystalline, low-shrinkage, radiation-curable oligomeric material, a photoinitiator, and a diluent, said inkjet composition having a viscosity of between about 10 to about 50 cps at at least one temperature between 50 to 140° C.

Abstract: An alkylsiloxane-containing epoxy resin composition can suitably be used as water-repellent agent or a water-repellent coating to be advantageously applied to areas that are apt to be brought into contact with solutions and substances containing one or more than one components that can damage the film forming property and the adhesion of an ordinary water-repellent agent. The resin composition comprises at least an alkylsiloxane-containing epoxy resin having two or more than two alkylsiloxane groups and two or more than two cyclic aliphatic epoxy groups in a molecule and a cationic polymerization catalyst.

Abstract: A photo-curable resin composition for sealing material, which is superior in the photo-curing performance and in the prompt curing property and is better in the adhesive property, in the resistance to moisture permeation and in the heat resistance, the photo-curable resin composition comprising (A) a compound having oxetane ring, (B) a photoinitiator for cationic polymerization and (C) a silane coupling agent, wherein the composition has a viscosity in the range from 0.01 to 300 Pa.s at 25° C.

Abstract: A method is provided for incorporating a foaming agent into mixtures of particulates and then forming a foam within the mixture to increase the flowability of the particulates. A method is also provided for excavating solid particulates, incorporating a foaming agent into mixtures of solid particulates, and then forming a foam within the mixture to increase the flowability of the particulates. The particulates can be transported through pipelines or boreholes. Examples of particulates include, but are not limited to, mine tailings, ores, sand, coal, soils, clays, silts, aggregates, and mixtures thereof.

Abstract: An ink jet ink composition comprising from about 0.5% to about 30% by weight of a pigment, a carrier and a dispersant, the dispersant comprising an anionic derivative of an ethoxylated alkylphenol-formaldehyde resin, the ratio of dispersant:pigment being from about 0.1:1 to about 5:1.

Abstract: The invention provides, in a first embodiment, a blocking wax composition. The blocking wax comprises from about 50 to about 90 weight percent of a water-soluble continuous phase and from about 10 to about 50 weight percent of a discontinuous solid phase filler that is substantially inert to the continuous phase. The invention further provides a method for mounting a contact lens blank for machining.

Abstract: The invention is directed to a polymer-clay nanocomposite material comprising a melt-processible matrix polymer and a layered clay material having decreased levels of extractable material, such as extractable salts of organic cations. This invention is also directed to processes for preparing polymer-clay nanocomposites, and articles or products produced from nanocomposite materials.