Abstract: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: A compound of the formula (I) wherein the variables X1 to X5, R1 to R7 including R3?, E, q, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed

Abstract: A bis(5-aryl-2-pyridyl) compound represented by formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbyl group or a substituted or unsubstituted aromatic heterocyclic group, and X is a group selected from the group consisting of moieties having formulas (2) to (5): wherein, in formula (2), m is an integer of 1 or 2; in formula (3), n is an integer of 1 to 6; and in formula (4), R is hydrogen or a lower alkyl group and p is an integer of 1 to 6.

Abstract: The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.

Abstract: Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: All multiple myeloma cell lines examined showed constitutively active I?B kinase (IKK), I?B? phosphorylation and constitutively active NF-?B. Curcumin, a chemopreventive agent, suppressed constitutive I?B? phosphorylation through inhibition of IKK activity and downregulated NF-?B. Curcumin also downregulated expression of NF-?B-regulated gene products such as I?B?, Bcl-2, Bcl-xL, cyclin D1 and interleukin-6. Consequently, curcumin suppressed multiple myeloma cell proliferation and arrested cells at the G1/S phase of the cell cycle. Curcumin also induced apoptosis and chemosensitivity to vincristine. Overall, results presented herein provide a molecular basis for the treatment of multiple myeloma patients with this pharmacologically safe agent.

Abstract: The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.

Abstract: A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3–5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5.

Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.

Abstract: The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential

Abstract: The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell proliferative disorders.

Abstract: The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.

Abstract: Cell adhesion inhibitors can interact with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. An inhibitor including a polyethylene glycol moiety can have advantageous pharmaceutical properties.

Abstract: The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: Substituted 3-(benzoylureido)thiophene derivatives, processes for preparing them and their use The invention relates to compounds of the formula I where the radicals are as defined, and their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.

Abstract: The present invention relates to the bioactivity of taxanes isolated from the leaves of Himalayan Yew tree Taxus wallichiana against human cancer cell lines grown in-vitro and subsequent identification of brevifoliol [1] as anticancer agent useful in the treatment of various types of cancer in humans

Abstract: Compositions and methods are disclosed which greatly improve the shelf-life of pesticidal agents and especially insecticides. The tendency of the composition to segregate from the solid components is minimized, which improves uniformity throughout the product.

Abstract: Antimicrobial system which comprises a cationic surfactant, derived from the condensation of fatty acids and esterified dibasic amino acids, according to the following formula (I), where: X is Br, Cl or HSO4R1: is linear alkyl chain from an saturated fatty acid, or hydroxyacid from 8 to 14 atoms of carbon bonded to the ?-amino acid group through amidic bond. R2 is a linear or branched alkyl chain from 1 to 18 carbon atoms or aromatic. R3: is Formula (II), where n can be from 0 to 4, and at least one antimicrobial agent characterised for its enhanced activity.

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: The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions.

Abstract: Compositions and methods for coating surfaces of MLS gasket layers are disclosed. The process includes applying a coating precursor on at least one surface of one or more of the layers, and curing the coating precursor by exposure to radiation. Disclosed coating precursors include those containing an acrylated oligomer and a photoinitiator, which can polymerize in response to ultraviolet or electron beam radiation.

Abstract: In ink containing a colorant, a humectant, a penetrant, water, and a water-soluble substance that is condensation-polymerized in the absence of the water (e.g., hydrolyzable silane compound), the surface tension of the ink at 25° C. before the water-soluble substance is condensation-polymerized is set to 20–50 mN/m, or the ink further contains a fluoroalkyl monoalcohol whose boiling point is lower than 100° C.

Abstract: Provided are a nanoporous organic polymer and preparation method thereof, and its application for catalyst. More particularly, provided is a nanoporous organic polymer composite comprising a mesoporous molecular sieve having micropores within mesopore walls, and an organic polymer impregnated within the micropores of the molecular sieve and coated on the wall surfaces of the molecular sieve. Also, provided is a method for preparing a nanoporous organic polymer composite comprising preparing a mesoporous molecular sieve having micropores within mesopore walls; impregnating an organic monomer diluted in solvent into the molecular sieve; and polymerizing the molecular sieve impregnated with the organic monomers to form organic polymers within the micropores and on the wall surfaces of the mesoporous molecular sieves. Further, provided are properties of catalytic reaction of the material as applicable representative examples of the nanoporous organic polymer.

Abstract: The invention provides a polyester block copolymer composition (R) obtained by thermally-processing a polyester block copolymer composition (Q) obtained by melt-mixing 100 parts by weight of a polyester block copolymer (P) with 0.1–5 parts by weight of an epoxy compound (C) having one or more epoxy groups under an inert gas atmosphere and not less than 102° C. in a solid phase, and further, at a temperature lower than a melting point of the polyester block copolymer composition (R) obtained.

Abstract: Elastomers are formed from castor oil and/or ricinoleic acid estolides and a polyester formed from an epoxidized vegetable oil such as ESO and a polycarboxylic acid such as sebacic acid, optionally in the presence of a peroxide initiator, or include crosslinked reaction products derived from ricinoleic acid or castor oil estolides, epoxy group-containing compounds such as epoxy resins and/or epoxidized vegetable oil, epoxy hardeners such as polyamine and polycarboxylic acid hardeners, thermally activated free radical initiators such as peroxides, and optionally but preferably include fillers such as limestone or wood flour. The elastomers can be prepared using a two-step, solvent-less procedure at elevated or ambient temperatures. These predominantly “all-natural” elastomers have physical properties comparable to conventional petroleum-based elastomers and composites and exhibit good flexibility, resiliency, abrasion resistance and inertness to hydrolysis.

Abstract: Dyed poly(trimethylene terephthalate) fibers having a lightfastness of 4 or higher after approximately 480 kJ incident UV radiation, and processes for preparing the fibers, are provided. The fibers are useful in automotive applications and other uses wherein UV absorption is likely.

Abstract: A thermoplastic flame retardant resin composition according to the present invention comprises: (A) about 40˜95 parts by weight of a styrenic resin; (B) about 5˜60 parts by weight of a polyphenylene ether, (C) about 0.1˜40 parts by weight of a rubber modified polystyrene resin containing about 40˜65% by weight of a rubber and about 0.1˜8% by weight of acrylonitrile based on 100 parts by weight of the sum of (A) and (B); and (D) about 5 to 30 parts by weight of an aromatic phosphoric acid ester compound based on 100 parts by weight of the sum of (A) and (B).

Abstract: A biodegradable polyesteramide and preparation method, having a formulation that contains (a) a diacid: 30%˜70% by weight (b) a diol: 10%˜50% by weight (c) an amide: 5%˜70% by weight (d) a diamine: 10%˜70% by weight (e) a branching agent: 0%˜10% by weight (f) a catalyst: an organic compound containing tin, 0 ppm˜50 ppm total proportion by weight (g) an antioxidant: an aromatic antioxidant, 0%˜5% by weight. A polycondensation reaction proceeds under nitrogen protection, and at a temperature of 140° C.˜270° C., and under this reaction temperature a vacuum polycondensation reaction proceeds for 4–6 hours, whereupon the biodegradable polyesteramide is acquired having a melting point of 125° C.˜130° C., a stretchability strength of 19˜28 Mpa, a fracture tensibility ratio of 80%˜300%. Under conditions where PH=12 and at a temperature of 80° C. complete degradation can be realized.

Abstract: A carboxylic ester of the formula in which A is —(CH2)x— where x=1–10, a process for its preparation which esters are useful lubricated and plasticizers for high molecular polymeric thermoplastics.

Abstract: A tire for vehicles includes a tread having a vulcanized polymeric base including at least one reinforcing filler dispersed in the polymeric base; an amount of extractable residue of at least one vulcanization accelerator, containing at least one carbon atom bound to at least two sulfur atoms, from 0.5% to 1.8% by weight based on a total weight of the tread; an amount of at least one activator, expressed as equivalents of zinc oxide, not higher than 2% by weight based on the total weight of the tread; and an amount of combined sulfur lower than 2.5% by weight based on the total weight of the tread. A tread for vehicle tires, a vulcanizable rubber composition for the manufacture of such a tread, and a vulcanizing system, all related to the tire for vehicles, are also disclosed.

Abstract: A thermoplastic resin composition (Y) characterized by comprising (A) 20 to 64.9 wt % one or more ethylene copolymers comprising an ethylene/?-olefin copolymer, (B) 35 to 70 wt % metal hydroxide, and (C) 0.1 to 30 wt % grafted ethylene polymer. The resin composition has excellent flame retardancy and has satisfactory pliability/flexibility and excellent tensile properties. It is suitable for use as an insulating material or sheath for electric wires. Also provided are: a polymer composition (Z) having high flame retardancy, characterized by comprising relative to (AA) 100 parts by weight of a polymer such as a thermoplastic polymer or thermosetting polymer, in the ratio of (BB) 50 to 250 parts by weight of a metal hydroxide, (E) 0.1 to 40 parts by weight of a triazine ring containing compound, and (F) 0.1 to 40 parts by weight of a polyhydric alcohol; and a molded object obtained from the polymer composition. These are suitable for use as an insulating material or sheath for electric wires.

Abstract: The invention relates to polymer modified inorganic particles with a layer structure with an average particle diameter of 5 nm to 20,000 nm, containing 20 to 5000 mass % interlamellarly, in relation to the anhydrous inorganic particle, of a mixture of aminoplasts and water. These polymer modified inorganic particles are produced by swelling the inorganic particles with aldehydes and then reacting the inorganic particles with multifunctional C1–C30 amino compounds. The invention also relates to plastic containing polymer modified particles with a layer structure and to semi-finished products and moulded material produced from the same.

Abstract: An optical material is a mixture of materials comprising a first material having a refractive index of not more than 1.45 for the d-line and a second material having an Abbe's number, indicating wavelength dispersion in the visible region, of not more than 25. A relation between the refractive index for the d-line (nd) and the Abbe's number (?d) is defined as follows: nd??6.667×10?3?d+1.70.

Abstract: A surface tension control agent for coating materials includes a fluorine-containing (meth)acrylate copolymer obtained by copolymerizing a fluorine-substituted alkyl (meth)acrylate monomer (A), an alkyl (meth)acrylate monomer (B), and a hydroxyl group- or ether group-containing alkyl (meth)acrylate monomer (C), such that the ratio of (A) to {(B)+(C)} is 3–60 parts by weight to 40–97 parts by weight.

Abstract: High-solids binder combinations comprising polyisocyanates, special lactone-based polyols and polyacrylate-polyols, a process for preparing such binders, and their use for producing coatings. The lactone-based polyols include ?-caprolactone-based polyols having an average hydroxy functionality ?2 and a number-average molecular weight of from 119 to 2000 g/mol. The polyacrylate resins are prepared by copolymerizing optionally functional polybutadienes, aromatic monomers, hydroxyalkyl esters of acrylic or methacrylic acid having primary hydroxyl groups, aliphatic esters of acrylic or methacrylic acid and C1 to C8 monoalcohols, ?,?-unsaturated C3–C7 monocarboxylic or dicarboxylic acids or of one or more monoesters of maleic acid or fumaric acid and C1 to C14 monoalchols.

Abstract: A stabilizer composition is described and comprises a 3-arylacrylate, a polymeric compound with molecular weight at least 2000, bearing, on a polymeric framework, side groups having amine functions, where all of the substituents in the ?-position to the amine nitrogen atom are other than hydrogen, and comprises a sterically hindered phenol. The stabilizer composition is particularly suitable for stabilizing thermoplastic polyurethane with respect to light, oxygen, and heat.

Abstract: Disclosed is a UV curable coating composition comprising a (methyl)acryloxy or vinyl functionalized silane, silica and acrylate oligomer containing at least two acrylate groups.

Abstract: The invention is based on the discovery of useful combinations of fully cross-linked thermoplastic vulcanizates with styrenic block copolymers. The new combinations of the invention can provide a synergistic effect. Specifically, the compositions formed thereby can be both softer and more elastic than would be expected on the basis of the properties of the individual components. Such compositions can be used in numerous applications, including, for example, any application for which a soft material with very good recovery is desired.

Abstract: Melt blended HDPE compositions for single and dual wall corrugated HDPE pipe and associated fabricated and molded fittings and accessories with enhanced physical properties and processing and environmental stress crack resistance (ESCR) characteristics and associated blend methods are disclosed in which virgin or recycled homopolymer and/or copolymer HDPE resin components are blended. The invention discloses methods for 1) selecting and determining the relative weight fractions of the HDPE blending components that provide specific physical properties and processability of HDPE blended compositions associated with density and melt index respectively and specific values of environmental stress crack resistance (ESCR) associated with specific molecular parameters and 2) for determining from molecular parameters, the ESCR of linear polyethylene resins and blended compositions within a class having similar densities.

Abstract: A water-absorbent resin composition excelling in an absorption capacity under pressure, a first transition of initial absorption, and the small amount of rewet is provided. It comprises a water-absorbent resin obtained by aqueous solution polymerization and by reversed-phase suspension or reversed-phase emulsion polymerization and shows a CSF of not less than 20 g/g or an AAP of not less than 20 g/g or an SFC of not less than 10 (unit: 10?7×cm3×s×g?1). The gaps among resin particles owing to the difference in shape form optimum gap widths for the sake of capillarity. The resin composition consequently formed, therefore, manifests such excellent properties without the influences of a surfactant or an emulsifier.

Abstract: The invention relates to highly flowable propylene block copolymers that comprise 50 to 80 wt.-% of a propylene homopolymer and 10 to 70 wt.-% of a propylene copolymer having 5 to 50 wt.-% of a C2–C8 alk-1-ene polymerized into it that is different from propylene, and that are obtainable from the gaseous phase by a two-step polymerization by means of a Ziegler-Natta catalyst system. In a first polymerization step, the propylene is polymerized at a pressure of 10 to 50 bar, a temperature of 50 to 100° C. and an average dwelling time of the reaction mixture of 0.3 to 5 hours in the presence of at least 2.0% by volume, based on the total volume, of hydrogen. The propylene homopolymer obtained in said first polymerization step is transferred together with the Ziegler-Natta catalyst system into an intermediate container, expanded for 0.01 to 5 minutes to less than 5 bar and maintained at a temperature of 10 to 80° C.

Abstract: The present invention provides a vinyl polymer with an epoxy group terminally introduced therein and an epoxy resin composition comprising (A) an epoxy resin and (B) a vinyl polymer which has a main chain produced by living-radical polymerization and has a reactive functional group at a main chain terminus. A flexible epoxy resin composition can be obtained using these compounds. The invention further provides an epoxy resin composition-having an epoxy group at a main chain terminus thereof.

Abstract: Various novel block cationomers comprising polyisobutylene (PIB) and poly(2-dimethylamino)ethyl methacrylate) (PDMAEMA) segments have been synthesized and characterized. The specific targets were various molecular weight diblocks (PDMAEMA+) and triblocks (PDMAEMA+-b-PIB-b-PDMAEMA+) with the PIB blocks in the DPn=50–200?(Mn=3,000–9,000 g/mol) range connected to blocks of PDMAEMA+ cations in the DPn=5–20 range. The overall synthetic strategy for the preparation of these block cationomers comprised four steps: 1) Synthesis by living cationic polymerization of mono- and di-allyltelechelic polyisobutylenes, 2) End group transformation to obtain PIBs fitted with termini capable of mediating the atom transfer radical polymerization (ATRP) of DMAEMA, 3) ATRP of DMAEMA and 4) Quaternization of PDMAEMA to PDMAEMA+I? by CH3I. Kinetic and model experiments provided guidance to develop convenient synthesis methods.

Abstract: Provided are a high melting point copolymer prepared by heat-polymerizing cyclopentadiene and/or dicyclopentadiene and a vinyl-substituted aromatic compound, wherein a use amount of a solvent in heat polymerization is 0.1 time or more and less than 0.5 time based on the mass of the whole monomers, and the copolymer has a softening point falling in a range of 100 to 135° C., and a hydrogenated copolymer obtained by hydrogenating the above high melting point copolymer. The hydrogenated copolymer of the present invention is suitably used as an adhesion-providing resin having a high softening point for a hot melt adhesive.

Abstract: A process for modification of a polymer comprising modifying a polymer (A) capable of decomposing by carbon radicals present in the molecule thereof using a compound (B) having a nitroxide radical in the molecule thereof and a radical initiator (C) in a ratio of (B)/(C) (molar ratio) of at least 0.7, whereby organic groups derived from the nitroxide radicals are introduced into the polymer and a modified unhalogenated butyl rubber obtained therefrom.

Abstract: The present invention relates to heterofunctional copolymers of glycerol and polyethylene glycol, conjugates of these heterofunctional copolymers with bioactive agents, nanoparticles, hydrophobic polymers and/or lipids; and to compositions containing these conjugates.

Abstract: A process for preparing an aqueous styrene-butadiene polymer dispersion by free-radical aqueous emulsion polymerization of a monomer mixture M containing from 40 to 80% by weight of styrene as monomer M1, from 20 to 60% by weight of butadiene as monomer M2, and from 0 to 40% by weight, based on 100% by weight of monomers, of ethylenically unsaturated comonomers M3 other than styrene and butadiene by a monomer feed technique in the presence of from 0.05 to 0.5% by weight, based on 100% by weight of monomers, of at least one hydrocarbon HC having 6 to 20 carbon atoms selected from compounds which on abstraction of a hydrogen atom form a pentadienyl radical or a 1-phenylallyl radical and ?-methylstyrene dimer comprises raising, at a point in time when at least 70% of the monomers to be polymerized have been supplied to the polymerization reaction, the concentration of butadiene in the monomer feed for a period of at least 1% of the total feed time by at least 10% by weight, based on monomers in the feed.

Abstract: Ethylene and optional comonomers are polymerized in the presence of an organozinc compound and a catalyst system to produce an ethylene polymer. The catalyst system comprises a bridged indenoindolyl Group 3-10 transition metal complex and an activator. The organozinc compound is used in an amount effective to increase the polymer bulk density compared with that observed in the absence of the organozinc compound. The organozinc compound can also narrow the particle size distribution of the polymer and the wt. % of polyolefin chunks produced. The operability of processes utilizing bridged indenoindolyl metal complexes is enhanced while maintaining desirably high polyolefin molecular weights.

Abstract: A 3+ metal complex for coordination polymerization of olefins is disclosed. The precursor metal complex is stabilized by a anionic multidentate ligand and at least two monoanionic ligands. The multidentate ligand and the transition metal form a metallocycle having at least five primary atoms, counting any ?-bound cyclopentadienyl group in the metallocycle as two primary atoms. Olefin polymerization is exemplified.