Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: The invention relates to the use of a compound of formula (I): for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-&bgr;1.

Abstract: The invention relates to the use of N-substituted indole-3-glyoxylamides of the general Formula I and to pharmaceutical compositions having antitumor action.

Abstract: The invention relates to a process for preparing constant-weight thrombin inhibitors of the formula I where n is 0, 1, 2, and tautomers thereof, wherein an aqueous solution of the active substance is spray dried.

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.

Abstract: Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally subs

Abstract: Bisimino-substituted phenyl compounds of the formula I where the substituents have the following meanings: X is a group A or B  where # denotes the bond with the phenyl ring and Ra is halogen, alkyl or alkoxy; Y is halogen, alkyl, haloalkyl or alkoxy; n is 0, 1 or 2, it being possible for the radicals Y to be different if n=2; R1 is alkyl; R2 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl; R3 is hydrogen, alkyl, haloalkyl or substituted or unsubstituted phenyl; R4 is ═CRbRc or ═N—ORd where Rb, Rc independently of one another are hydrogen, alkyl or substituted or unsubstituted phenyl; and Rd is one of the radicals mentioned under R2. Processes and intermediates for their preparation, and their use.

Abstract: The invention features a method for treating a patient having a cancer or other neoplasm, by administering to the patient (i) a benzimidazole or a metabolite or analog thereof; and (ii) pentamidine or a metabolite or analog thereof simultaneously or within 14 days of each other in amounts sufficient to inhibit the growth of the neoplasm.

Abstract: The present invention relates to a pharmaceutical composition for the hepatoprotection and treatment of liver diseases comprising as an active ingredient a dihydroxyphenyl derivative represented by the following formula (1), pharmaceutically acceptable acid addition salt or stereochemical isomer thereof together with a pharmaceutically acceptable inert carrier: in which in which A, B, D and E are defined as described in the specification.

Abstract: Pharmaceutical compositions containing arglabin and arglabin derivatives are described. The compositions can be in unit dosage form and are useful for the treatment of cancer in humans.

Abstract: This invention describes the novel use of alkyl, alkoxyl, halogenyl, or hydroxy substituted dicinnamoylquinides as therapeutic agents for enhancing adenosine levels in the brain and peripheral organs. These agents are particularly useful in treating human diseases or conditions that benefit from acute or chronic elevated levels of adenosine, such as reperfusion injury, coronary or cerebral ischemia, coronary vasoconstriction, paroxysmal supraventricular tachycardia, hypertension, wound healing, diabetes, inflammation, or sleep disturbances. They can also be used to protect normal cells from chemotoxicity in patients undergoing cancer therapy, and reverse the behavioral effects of caffeine intake.

Abstract: The present invention provides compositions and methods for lowering plasma Lp(a) levels in humans. The present invention provides compositions and methods for lowering the risk factors for cardiovascular diseases. Moreover, this invention provides therapeutic alternatives to current pharmaceutical interventions for the lowering of cholesterol, LDL-cholesterol, triglycerides and other metabolic risk factors.

Abstract: The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by wherein R is alkyl or aryl, the compound is trans-across the epoxide ring, OX is a carbonyl (═O) or hydroxy group (OH) and R′ is a H, alkyl or aryl group. The invention further provides methods of identifying patients at increased risk for hypertension, comprising assaying for epoxide hydrolase activity in a urine sample from the patient. In particular, the assays comprise determining the amount of dihydroxyeicosatrienoic acids (DHETs), determining the amount of epoxyeicosatrienoic acids (EETs) in said sample, or determining the amount of both DHETs and EETs in said sample.

Abstract: The invention relates to the formulation of deltamethrin as water-dispersible granules which comprise wetting agents, dispersants, solid inert substances and one or more acids in an amount sufficient to adjust the pH of the mixture to a value in the range from 1 to 7. The granules are particularly useful for controlling animal pests.

Abstract: Methods of using propionoyloxymethyl propionate (“POMP”) and butyroyloxymethyl butyrate (“BOMB”) are disclosed. Methods of treating cancer using these compounds are disclosed. The compounds are effective in the inhibition of histone deacetylase.

Abstract: The present invention provides compositions and methods for maintaining cardiac function by administering dichloroacetate (DCA) in combination with an inotrope.

Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as naphthoic acid derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokine may for example be stromal cell-derived factor (SDF)-1, and the relevant chemokine receptors may for example be corresponding chemokine receptor (CXCR-4). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of 3-Hydroxy-2-naphthoic acid in the treatment of disease.

Abstract: The invention provides methods of treating erectile dysfunction comprising the step of placing within the fossa navicularis of the patient an effective erection-inducing amount of a prostaglandin E1 composition of a semi-solid consistency, as well as suitable applicators. The composition comprises prostaglandin E1, a penetration enhancer, a polysaccharide gum, a lipophilic compound, and an acidic buffer system. The penetration enhancer is an alkyl-2-(N,N-disubstituted amino)-alkanoate ester, an (N,N-disubstituted amino)-alkanol alkanoate, or a mixture of these. The lipophilic compound may be an aliphatic C1 to C8 alcohol, aliphatic C2 to C30 ester, an aliphatic C8 to C30 ester, or a mixture of these. The composition includes a buffer system capable of providing a buffered pH value for said composition in the range of about 3 to about 7.4.

Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.

Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

Abstract: Provided is a process for reducing CO2 emissions generated by a Fischer-Tropsch GTL facility. The process includes introducing a synthesis gas into a Fischer-Tropsch reactor and performing a Fischer-Tropsch process to produce a Fischer-Tropsch product and CO2. At least a portion of the CO2 from the Fischer-Tropsch reactor is fed into at least one of a feed stream being fed to a synthesis gas formation reactor, producing the synthesis gas, or the synthesis gas being fed into the Fischer-Tropsch reactor. In addition, naphtha is obtained from the Fischer-Tropsch product and is fed into a naphtha reformer. Naphtha reforming is conducted, generating hydrogen by-product and C6-C10 product. At least a portion of the hydrogen by-product, generated during naphtha reforming, is fed into the feed stream, converting at least a portion of the CO2 in the feed stream into additional CO. Finally, the additional CO is converted into hydrocarbons in the Fischer-Tropsch reactor.

Abstract: This invention relates to ion exchange resins that have a reduced amount of physically adsorbed organic compounds, as well as methods of producing and using such resins. In particular, the amount of extractable total organic carbon on the resins may be less than about 200 parts per trillion by wet weight, as measured using gas chromatography/mass spectrometry. This invention also relates to methods of treating water that use such resins.

Abstract: There are disclosed: (1) a container comprising a foamed olefin resin, wherein weight W (g) and content volume V (ml) of the container satisfy the following expression (1): W(g)/V(ml)≦0.055  (1), and (2) a process for producing the container by a blow molding method.

Abstract: The invention relates to the use of surface-active photoinitiators of formula I the units being arranged randomly or in blocks, and wherein n is a number from 1 to 1000; m is a number from 0 to 100; p is a number from 0 to 10,000; x is the number 1, or, when n is 1, x may also be the number 2; A1 and A2 are, for example, C1-C18alkyl; or A1 and A2 together are a single bond; R1, R2 and R3 are, for example, each independently of the others C1-C18alkyl, phenyl or C5-C8cycloalkyl; R4 is, for example, unsubstituted or substituted C1-C18alkyl, unsubstituted or substituted phenyl or C5-C8cycloalkyl; IN, when x is 1, is a radical of formula when x is 2, is a radical of formula R13 and R14 are, for example, each independently of the other C1-C12alkyl; Y is, for example, —(CH2)a—O—; X is OR15 or N(R16)(R17); R15 is, for example, hydrogen or C1-C4alkyl; R16 and R17 are, for example, hydrogen or C1-C12alkyl; X1 has, for example, one of the meanings o

Abstract: The objective of the present invention is to provide a production method by which a polymer of a functional group-terminated vinyl monomer can be easily and practically produced. Further, it is another object of the present invention to provide a functional group-terminated vinyl polymer which is useful as a material for the production of various functional products. The first aspect of the present invention is concerned with a production method of a functional group-terminated vinyl polymer comprising a step of synthesizing a halogen atom-terminated vinyl polymer by the radical polymerization reaction of a vinyl monomer in the presence of a halogen compound and a step of introducing a functional group to a terminus by substituting a functional group-containing group for the terminal halogen atom of said vinyl polymer.

Abstract: A low-viscosity dental material contains a non-settling nanoscale filler. Improvements of the mechanical properties of the dental materials, including the abrasive resistance and the compressive strength are provided. Furthermore, the dental materials have increased resistance to microleakage and have increased bond strengths. The filler forms a stable sol with low-viscosity dental materials and the filler may be prepared by surface treatment of fillers having a primary particle size of from about 1 to about 100 nanometers.

Abstract: A solvent-based water- and oil-repellent agent composition, which contains a graft copolymer having a repeating unit derived from a vinyl monomer having a perfluoroalkyl group and a repeating unit derived from a polymerizable cyclic acid anhydride and an organic solvent, has high product stalibity and high dilution stability and can give high water- and oil-repellency.

Abstract: Vulcanized ethylene-propylene-diene (EPDM) rubbers are disclosed that are particularly suited for use in dynamic applications as a replacement for natural rubber parts. The ethylene-propylene-diene rubbers exhibit excellent thermal and oxidative resistance while displaying tensile strength and dynamic fatigue resistance comparable to similar compounds based on natural rubber. The ethylene-propylene-diene rubbers comprise a high molecular weight EPDM, a processing oil, a carbon black, and a cure system containing sulfur, tetramethylthiuram-disulfide and 2-mercaptobenzothiazole.

Abstract: Self crosslinking aqueous polymer dispersions containing hard and soft copolymers containing polymerized units of a conjugated diene, a vinyl aromatic compound, an organic carboxylic acid and/or anhydride, and at least one crosslinker may be included in consolidated nonwoven constructions. The consolidated nonwoven construction is useful as a base material such as a bituminized roofing mat.

Abstract: An emulsion-polymerized addition copolymer formed from a monomer mixture comprising ethylenically unsaturated monomers, including from more than 4 to 15 wt % based on the weight of said mixture of at least one ethylenically unsaturated carboxylic acid functional monomer, and from 0.05 to 5 wt % based on the weight of said mixture of at least one polymerizable surfactant monomer comprising hydrophobic and hydrophilic functional groups, wherein said hydrophobic functional group comprises a polymerizable group within it, is useful as a binder in an ink jet ink having improved print quality.

Abstract: A humidity responsive control device consists of a package having at least one face that is a permeable to liquid and gases and water vapor and is formed by mixing together a) 5 to 50% by weight of a hygroscopic polyacrylate and/or PVA polymer, b) 10 to 60% of porous silica minerals such as vermiculite and perlite, c) 5 to 50% of an absorbent such as zeolite or activated carbon for small molecules such as ammonia and d) 5 to 60% by weight of an aqueous emulsion of a mixture of an active ingredient of one or more of a bacteriocidal, fungicidal or odor masking compounds. The device is effective at eliminating and masking odors under varying humidity conditions.

Abstract: A process for preparing an epoxy group-containing curable polyphenylene ether (PPE) resin. The process involves introducing an epoxy group-containing functional group to the terminal end of PPE (Mn>3000) by modifying the hydroxy and ester groups on the terminal end. Thus, a curable PPE resin (Mn>3000) including an epoxy group on the terminal end can be obtained. The modified PPE resin contains epoxy groups and has high glass transition temperature.

Abstract: Disclosed are a fatty acid esters composition of a polyglycerine containing more than 70% of a fatty acid monoester which is defined by a specified analysis method, a process for the preparation thereof, a process for the preparation of a highly-purified fatty acid esters composition of a polyglycerine, and a highly-purified fatty acid esters composition of a polyglycerine having an oxirane oxygen concentration of below 100 ppm which is defined by a specified analysis method. The fatty acid esters compositions of a polyglycerine are useful as additives for a variety of food-stuffs, additives for a variety of thermoplastic resins, and as additives for a variety of cosmetics or detergents.

Abstract: An aqueous semi-continuous emulsion polymerization process for producing bimodal polymer particles in volumes large than a single batch size is provided. A bimodal polymer composition prepared by the process of carrying out an aqueous semi-continuous emulsion polymerization is also provided.

Abstract: Emulsifier free fluoropolymer manufacturing method in which (a) a mixture of an oxidizing agent and reducing agent is used to start the polymerization and where one or the other but not both, are further added during polymerization, or (b) an oxidizing metal ion is added to start polymerization and where additional oxidizing metal ion is added during polymerization.

Abstract: The invention provides metallocene catalyst systems for the controlled polymerization of alkenes to a wide variety of polyolefins and olefin coplymers. Catalyst systems are provided that specifically produce isotactic, syndiotactic and steroblock polyolefins. The type of polymer produced can be controlled by varying the catalyst system, specifically by varying the ligand substituents. Such catalyst systems are particularly useful for the polymerization of polypropylene to give elastomeric polypropylenes. The invention also provides novel elastomeric polypropylene polymers characterized by dyad (m) tacticities of about 55% to about 65%, pentad (mmmm) tacticities of about 25% to about 35%, molecular weights (MW) in the range of about 50,000 to about 2,000,000, and have mmrm+rrmr peak is less than about 5%.

Abstract: A catalyst system useful for polymerizing olefins is disclosed. It comprises an activator and an organometallic complex. The complex includes a Group 3-10 transition or lanthanide metal and a 1,3-bis(arylimino)isoindoline or 1,3-bis(heteroarylimino)isoindoline ligand. Activities of the Group 8-10 catalyst systems rival or exceed those of late transition metal bis(imines). The resulting polyolefins typically have high molecular weights, broad molecular weight distributions, and a high degree of crystallinity, which makes them valuable for film applications.

Abstract: A process for polymerizing propylene is disclosed. The propylene is polymerized with a catalyst system which comprises an activator and a [1,2-b]indenoindolyl Group 4-6 transition metal complex having open architecture. The process has high catalyst activity and gives high molecular weight elastomeric polypropylene.

Abstract: A new class of methylene-bridged metallocenes of formula (I), wherein M is a transition metal of group 3, 4, 5, 6, lanthanide or actinide; X is a monoanionic sigma ligand; R1 can be alkyl, cycloalkyl, aryl, alkylaryl or arylalkyl radicals; R2 can be halogen, alkyl, cycloalkyl, aryl, alkylaryl or arylalkyl radical; p is 0-3; m is 0-2; and n is 0-4. Furthermore, the corresponding ligands, a new process for their preparation and catalysts systems containing said methylene-bridged metallocenes are described.

Abstract: A catalyst system useful for polymerizing olefins is disclosed. The catalyst system comprises an activator and an organometallic complex that incorporates a Group 3 to 10 transition metal and at least one chelating, dianionic triquinane ligand. The cis,syn,cis-triquinane framework is generated in three high-yield steps from inexpensive starting materials, and with heat and light as the only reagents. By modifying substituents on the triquinane ligand, polyolefin makers can control catalyst activity, comonomer incorporation, and polymer properties.

Abstract: This invention provides a method for syntheses of new electroluminescent conjugated polymers modified with high electronegative heterocyclic groups (such as 1,3,4-oxadiazole-diyl, 1,3,4-thiadiazole-diyl, and 1,2,4-triazole-diyl). These electroluminescent polymers (homopolymers, statistical copolymers or block coplymers) are obtained by polymerization of bis(halomethyl) arenes modified with heterocyclic groups via the Wessling precursor route, Gilch side chain route, Wittig reaction or Wittig-Hornor reaction. By a proper selection of the monomers and their ratios in the polymerization, the emissive polymers (fully conjugated or limited conjugating length) covering the full visible range even extending to the near-IR range can be prepared. The polymeric light emitting diodes (PLED) with these materials as emissive layer or electron transport layer have high external quantum efficiency and can be used as indicators and displays for cellular phones, pagers, portable computer, wristwatch, toys, etc.

Abstract: Highly cross-linked, maroporous/mesoporous polymer monoliths are prepard using supercritical carbon dioxide (scCO2) as the solvent and porogen for the polymerisation of monomers having more than one polymerisable group, at a monomer concentration in CO2 of more than 40 vol %. The procedure allows the direct formation of dry, solvent-free, macroporous/mesoporous cross-linked monoliths with large surface area and well-controlled pore size distribution.

Abstract: This invention discloses a process for synthesizing an amine functionalized monomer that comprises (1) reacting a secondary amine with a 2,3-dihalopropene to produce a vinyl halide containing secondary amine having a structural formula selected from the group consisting of wherein R and R′ can be the same or different and represent allyl, alkoxyl or alkyl groups containing from 1 to about 10 carbon atoms, and wherein X represents a halogen atom, and wherein m represents an integer from 4 to about 10, and wherein X represents a halogen atom; and (2) reacting the vinyl halide containing secondary amine with a vinyl magnesium halide to produce the monomer having a structural formula wherein R and R′ can be the same or different and represent alkyl, allyl or alkoxyl groups containing from 1 to about 10 carbon atoms, and wherein m represents an integer from about 4 to about 10.

Abstract: The present invention relates to a process for the preparation of random copolymers of propylene with c2-c10 &agr;-olefins, carried out in the presence of a catalyst comprising: A) A solid component comprising a titanium compound supported on mgcl2 in active form and an electron-donor compound; b) An alkyl-al compound, and c) An electron-donor compound selected from the group of 1,3-diethers. The copolymers obtained using the said process show, for an equivalent content of &agr;-olefin, a lower content of xylene-soluble fractions when compared with the copolymers obtained with the catalysts of the prior art.

Abstract: The present invention provides a polyimide resin, a resin composition, an adhesive solution, a film-state joining component, and an adhesive laminate film soluble in a solvent having excellent heat resistance and adhesion, capable of bonding and curing at relatively low temperatures.

Abstract: In the method for solid-phase drying or solid-phase polymerizing a polyamide of the present invention, the polyamide that is stored for 20 days or longer after the production thereof until subjected to the solid-phase drying or the solid-phase polymerization under the specific conditions is used as the starting material. By storing the polyamide under the specific conditions of the present invention, the resultant solid-phase dried or solid-phase polymerized polyamide with a low yellowness is obtained even if 20 days or more time has lapsed after the starting polyamide is produced until it is subjected to the solid-phase drying or solid-phase polymerization.

Abstract: The invention relates to high purity fluoropolymers and processes for making such materials. These polymers are particularly suited for applications in the semiconductor industry. The process comprises removal of unstable polymer end groups by fluorination and removal of heavy metal impurities by extraction with an aqueous acid medium.

Abstract: Cyclic peptides of formula I are potent and selective antagonists of melanocortin-4 receptors, and as such are useful research tool for the determination of the physiological roles of the MC-4 receptor, as well as for the diagnosis, treatment or prevention of disorders or diseases mediated through the MC-4 receptor.

Abstract: The activation of cyclin dependent kinase 5 (Cdk5) depends on the binding of its neuronal specific activator Nck5a. The minimal activation domain of Nck5a has been experimentally determine comprise acid residues 150 to 291 of the protein. It has been demonstrated that a 28 residue peptide encompassing amino acid residues Ala 146 to Asp 173 of Nck5a is capable of binding Cdk5 and hence resulting in the inhibition of its Kinase activity. Additionally, this peptide could also inhibit Cdk2 with a similar potency as it does to Cdk5. The direct competition experiments showed that the Nck5a inhibitory peptide does not compete with Nck5a for Cdk5 or cyclin A for Cdk2. Steady state kinetic analysis indicated that the Nck5a peptide acts as a non-competitive inhibitor of Cdk5/Nck5a complex with respect to its substrate.