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

Abstract: The invention relates to thiazolidinones of general formula (I) their production and use as inhibitors of polo-like kinases (Plk) for treating various diseases.

Abstract: Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.

Abstract: A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(?O), C(?S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hy

Abstract: The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4 H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

Abstract: Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.

Abstract: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist.

Abstract: The present invention provides a compound of the formula: (Formula I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, comprising administering to a patient in thereof an effective amount of a compound of Formula I.

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 and/or thrombin, as well as a process for its preparation and intermediates therefor.

Abstract: The present invention relates to the use of the compounds of general formula 1 wherein the groups R1, X and Y may have the meanings given in the claims and in the specification, for preparing a pharmaceutical composition for the treatment of COPD (chronic obstructive pulmonary disease), as well as new compounds of general formula 1 and processes for preparing them.

Abstract: The present invention relates to a compound of formula (I) having CCR2 receptor antagonistic properties, particularly anti-inflammatory properties.

Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is a hydrogen atom or the like; R2 is NHSO2R3 or the like; R3 is a (C1-C6)alkyl group or the like; R5 is a hydrogen atom or the like; R6 and R7 may be the same or different and are each independently a hydrogen atom or the like; X is an oxygen atom or the like; Y is an oxygen atom or the like; Z1 to Z6 are a carbon atom or the like; n is an integer of 0 to 6; *1 is an asymmetric carbon atom; and *2 is an asymmetric carbon atom when R5 is other than a hydrogen atom.

Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.

Abstract: The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke.

Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.

Abstract: Disclosed and claimed herein are e,e,e malonic acid/acetic acid tri-adducts of buckminsterfullerene of the general formula C60R3, wherein each R is independently selected from groups of the formula ?CR1R2 wherein each R1 and R2 is independently selected from the group consisting of —H and —COOH, provided, however, that at least one of the R1's and R2's is a hydrogen. Processes for preparing and uses of the same for treating neuronal injury and for life-extension are also disclosed and claimed herein.

Abstract: Biomacromolecules such as proteins are inactivated by hydrophobic ANSA derivatives of the formula: wherein R1 and R2 are hydrophobic or affinity groups and R3 is selected from the group consisting of aminoacyl groups and peptidyl groups upon nitrosation. ANSA derivatives can be designed to selectively kill tumor cells and various pathogens, including bacteria, viruses, and fungi.

Abstract: Aromatic derivatives of aliphatic diamines are effective in ameliorating conditions characterized by unwanted calcium ion channel activity, especially T-type and N-type channels. These conditions include, for example, stroke and pain.

Abstract: The present invention provides an antiallergic agent comprising, as an active ingredient, at least one of a tomato extract, tomato pericarp, naringenin chalcone or its derivatives, tricaffeoylquinic acid or its derivatives and dicaffeoylsuccinylquinic acid or its derivatives; a histamine-release inhibitor or a leukotriene-release inhibitor; and a medicament, food, drink or cosmetic comprising the antiallergic agent, the histamine-release inhibitor or the leukotriene-release inhibitor mentioned above; and a method for producing an antiallergic agent comprising extracting raw material tomato with a solvent.

Abstract: Methods and apparatuses for comminuting and stabilizing small particles are provided. In one embodiment, an apparatus moves an organic compound dissolved in a solvent to form a suspension of particles in a first fluid stream and moves the suspension in a second fluid stream, wherein the second fluid stream is oriented and positioned with respect to the first stream to cause shearing between the streams and mixing of at least some of the particles in the first and second streams.

Abstract: A process for the preparation of a catalyst which comprises activating a catalyst precursor comprising a cobalt compound and a support with a gas comprising at least 5 mol % of a hydrocarbon.

Abstract: The present invention relates to a recycling method of a mixed waste of polyester and polyamide (hereinafter, referred to as “mixed waste”) in which polyesters including polyethylene terephthalate and polyamides are inseparable from one another. In accordance with the recycling method of the present invention, it is possible to prepare a solid block polymer having an acid value of 1 to 150 mgKOH/g, a weight average molecular weight of 3,000 to 50,000 and a softening point of 10 to 150° C., or a liquid polyester-amide block polymer composition having good compatibility, solubility and dispersibility. In addition, the polymer having an acid value of more than 20 mgKOH/g is reacted with a basic compound to form a neutralized salt which is then used to prepare a water-soluble polyester-amide block polymer composition.

Abstract: The invention provides a polyurethane foam manufactured from a polyisocyanate and a polycarbonate polyol. Moreover, the invention provides a method of manufacturing the polyurethane foam manufactured from a polyisocyanate and a polycarbonate polyol, comprising mixing the polyisocyanate and polycarbonate polyol together and foaming same.

Abstract: A method of preparation of a cross-linked hydrogel by graft copolymerisation, said method comprises the steps of preparing an aqueous solution comprising one or more hydrophilic polymers, a cross-linking agent and a photoinitiator comprising a water-soluble peroxydisulphate, subjecting said solution to irradation and obtaining the cross-linked hydrogel, wherein the hydrophilic polymers are saturated and the cross-linking agent acts as a co-catalyst of cross-linking. The hydrogel is fast to produce and has low toxicity. The hydrogel may be suitable for use in medical devices such as dressings and the like.

Abstract: The invention relates to the acyl- and bisacylphosphine derivatives according to formula (I), wherein Y represents O, S, NR3, N—OR3 or N—NR3R4, Z represents O, S, NR3, N—OR3, N—NR3R4 or a free pair of electrons, and FG represents a leaving group and the remaining groups are defined as in the description. The invention further relates to a method for the production of the inventive derivatives and to their use.

Abstract: Liquid printing inks for flexographic and/or gravure printing comprise solvents, colorants, if required additives, and, as a binder, at least one hyperbranched polymer having functional groups. Printing lacquers for priming unprinted print media or overcoating printed print media comprise solvents, if required additives, and, as a binder, at least one hyperbranched polymer having functional groups. Such hyperbranched polymers are used for the preparation of printing inks and of printing lacquers.

Abstract: Provided are a thermoplastic resin composition, a thermoplastic resin molded product and an outside plate part of a vehicle capable of improving both characteristics of heat resistance and impact resistance while being compatible with each other. The thermoplastic resin composition contains: 65 to 86.5 mass % of a polyamide resin component (A), 13 to 25 mass % of an acid modified elastomer component (B), and 10 mass % or less of an olefin-based resin component (C) and/or 8 mass % or less of a filler component (D), wherein a dispersion phase of a core-shell type particle structure that is formed from the acid modified elastomer component (B) serving as a shell phase and the olefin-based resin component (C) and/or the filler component (D) serving as a core phase is dispersed in a matrix phase formed from the polyamide resin component (A).

Abstract: A sheath composition and a cable using the sheath composition are disclosed. The sheath composition contains a polyolefine resin and flame-retardant particles containing a metal hydrate. The flame-retardant particles are provided with a coating layer on the surfaces thereof and have a volume average particle diameter in a range from 1 to 500 nm.

Abstract: The flame retardant thermoplastic resin composition of the present invention comprises (A) 45˜95 parts by weight of a polycarbonate resin; (B) 1˜50 parts by weight of a rubber modified vinyl graft copolymer; (C) 0˜50 parts by weight of a vinyl copolymer; (D) 1˜30 parts by weight of a mixture of organic phosphorous compounds consisting of (d1) 1˜50% by weight of a oligomeric compound of cyclic phosphazene and (d2) 99˜50% by weight of an oligomeric phosphoric acid ester compound, per 100 parts by weight of the sum of (A), (B) and (C); and (E) 0.05˜5 parts by weight of a fluorinated polyolefin resin per 100 parts by weight of the sum of (A), (B) and (C).

Abstract: An alkali metal or alkaline earth metal salt of sulfonic acid of polyphenylene ether oligomer is useful as a modifier for thermoplastic resins, typically as a flame retardant, compatibilizing agent or antistatic agent.

Abstract: The invention provides a process for improving the storage stability of aqueous composite-particle dispersions and of aqueous formulations comprising them.

Abstract: An additive for imparting flame retardancy with an organic resin is provided. This additive does not use environmentally harmful halogen or phosphorus flame retardant which also adversely affects the performance of the product, and this additive satisfies severe flame retardancy requirements at the level equivalent to those employing such flame retardants. Also provided are a flame retardant polycarbonate resin composition adapted for use in producing a product having excellent mechanical properties, moldability, and outer appearance as well as an article molded therefrom. The additive for imparting flame retardancy with an organic resin comprises a silicone compound having phenyl group bonded to silicon atom, an alkali metal sulfonate salt group or an alkaline earth metal sulfonate salt group bonded to silicon atom via a hydrocarbon group (optionally containing a hetero atom), and siloxane bond.

Abstract: A thermoplastic composition comprises a polycarbonate, an ionizing radiation stabilizing additive, and a poly-substituted aromatic compound of formula: wherein X is an aryl group; Y is a non-hydrogen substituent group, a is 1 to 4, b is 0 to 4, a+b is less than or equal to 4, and c is 0 or 1; and wherein the amounts and identities of the polycarbonate, ionizing radiation stabilizing additive, and poly-substituted aromatic compound are selected such that a molded article having a thickness of 3.18 millimeters and comprising the thermoplastic composition has, after exposure to gamma radiation at 83 kGy and when measured according to ASTM D1925-70, an increase in yellowness index (dYI) of less than or equal to 50, when compared to the unexposed thermoplastic composition.

Abstract: A polyvinyl alcohol polymer film includes a polyvinyl alcohol polymer and a plasticizer selected from the group consisting of ethylene glycol, glycerin, propylene glycol, diethylene glycol, diglycerin, triethylene glycol, tetraethylene glycol, and trimethylolpropane. The amount of the polyvinyl alcohol polymer eluted when a 10 cm square of the polyvinyl alcohol polymer film is left in 1 liter of water of 50° C. for 4 hours is from 1 to 100 ppm. The film has only a small number of defects and is useful as raw material for producing a polarization film.

Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.

Abstract: The invention provides reagents and methods for conjugating a polymer specifically to the ?-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the ?-amine of a polypeptide having a cytokine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.

Abstract: The invention relates to methods for producing crosslinked polyvinyl acetals, according to which a polyvinyl alcohol (A1) containing carboxyl groups is crosslinked by (i) reacting the polymer (A1) with at least one polyaldehyde of formula R9(CHO)n, and (ii) at least partly esterifying groups of formula (1) and formula (4a) with each other, said steps being performed in any order. The invention further relates to methods for producing crosslinked polyvinyl acetals, according to which a polyvinyl alcohol (A2) is crosslinked by (i) reacting the polymer (A2) with at least one compound of formula (6), (ii) adding at least one compound of formula (4b), (iii) adding a polyaldehyde of formula (5), and (iv) at least partly esterifying groups of formula (1) and structural units derived from the compound of formula (4b) with each other, the radicals R7, R8, R9, R10, and R11, and the index n being defined as indicated in the description.

Abstract: The present invention relates to a two-component epoxy adhesive composition comprising a) a first component comprising a first epoxy resin and a second epoxy resin, the second epoxy resin being flexibilized by an elastomer, and b) a second component comprising at least one amine compound with one or more primary and/or secondary amino groups, said amine compound having a molecular weight of less than 450 g/mol. The ratio of the total number of amino groups of the amine compound to the total number of epoxy groups of the epoxy resins is 0.01:1 to 0.5:1. The mixing of the two components a) and b) results in a wash-off resistant composition. Said wash-off resistant composition results upon heat-curing in a crash-stable structural adhesive.

Abstract: The present invention provides hardenable coating compositions, comprising: a first compound selected from the group consisting of polyacids, polyanhydrides, salts thereof and mixtures thereof, and a second compound having two or more active hydrogen groups. When used as a roll coating composition, the first compound preferably has a low average molecular weight and an acid number greater than about 100. The hardenable coating composition preferably has an extended open time and can be rapidly cured to a substantially tack-free state in less than about one minute at 200° C. Coated articles and methods of coating are also provided.

Abstract: The invention relates to novel multimodal polyethylene polymers comprising a low molecular weight fraction and a high molecular weight fraction, and having a MFR5 of greater than 0.10 g/10 min and less than or equal to 0.22 g/10 min, and a density of greater than equal to 952 kg/m3. The invention also relates to uses of the novel polymers in the production of polymeric articles, especially pipes.

Abstract: A process for crosslinking polymers employs a silane crosslinker which, upon hydrolysis, produces a reduced quantity of volatile organic compound.

Abstract: A plug flow reactor having an inner shell 27 surrounded by outer shell 21 and having at least one annular flow passage 35 therebetween can be used to prepare compositions, including polymers. The plug flow reactor also includes inlet port 36, an outlet port 37 and a plurality of exchanger tubes 26 wherein the exchanger tubes are in fluid communication to the at least one annular flow passage. Polystyrene and high impact polystyrene can be prepared using the reactor.

Abstract: A liquid sealing agent used for automobile parts, electric parts, various kinds of machine parts and the like exhibits good oil resistance, heat resistance, adhesiveness and flexibility. A vinyl polymer has at least one crosslinkable silyl group and can yield a cured product exhibiting an oil resistance superior to that of a cured product from a reference polymer obtained by replacing the repeating unit thereof with butyl acrylate alone, in any one item of the immersion test according to JIS K 6258 for the land use 3-5 lubricating oil specified in JIS K 2215.

Abstract: Provided herein is a copolymer that includes a soft block (A) and a hard block (B) comprising a tyrosine di-peptide. The copolymer can be any of AB, ABA or BAB type block copolymers. The soft block can include a PEA polymer.

Abstract: Polymers made by transition metal catalyst systems comprising a bulky noncoordinating anion (NCA) as cocatalyst component. In comparison to polymers containing a conventional NCA, these polymers show a considerably lower dielectric loss, making them suitable for insulation applications such as for power cable.

Abstract: A one-pot polymerization process of preparing long chain branching polymers is provided. Also described is a “T” reagent that serves as a link between main and side chains of an inventive long chain branching polymer. A “T” reagent has at least two functionalities, serving as both co-monomer and chain transfer reaction agent. Optionally, a copolymerization reaction between an alpha-olefin and “T” reagent takes place initially to incorporate some “T” molecules in the polyolefin main chain, and the incorporated “T” units then behave as chain transfer agents for reacting with the propagating polyolefin chains to form side chains. In a particular embodiment, a polymerization process for preparing long chain branching polyethylene (LCBPE) and long chain branching polypropylene (LCBPP) is detailed.

Abstract: This disclosure relates to olefin polymerization processes for polymerizing ethylene, higher alpha-olefin comonomer and at least one diene, especially vinyl norbornene (VNB), and especially processes for producing amorphous or semi-crystalline polymers such as ethylene propylene diene (EPDM).

Abstract: An ethylene terpolymer wax comprising from 40 to 95% by weight of units of ethylene, from 0.1 to 40% by weight of units of at least one anhydride of a C4-C10-dicarboxylic acid having at least one ethylenic C—C double bond, and from 0.1 to 40% by weight of units of at least one ester of the formula I where R1 is selected from hydrogen, C1-C10-alkyl, C3-C12-cycloalkyl or C6-C14-aryl and R2 is selected from C1-C10-alkyl, C3-C12-cycloalkyl or C6-C14-aryl, having a molecular weight Mw of up to 20000 g/mol.