Abstract: Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase, their processes for production as well as their use as medications for treating various diseases are described.

Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.

Abstract: The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described. Indenoisoquinolones substituted at C-11 are prepared by McMurry reactions of 11-ketoindenoisoquinolones with aldehydes.

Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.

Abstract: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound having said structural formula.

Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.

Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian Factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, where; X is —C(R4)? or —N?; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independently hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is —C(R4)?,R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.

Abstract: Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.

Abstract: The present invention provides an ?-2A/?-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof. The present invention further provides a pharmaceutical composition that contains a pharmaceutical carrier and a therapeutically effective amount of an ?-2A/?-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof.

Abstract: An object of the present invention is to provide a medicament and method which is useful for prevention and/or therapy of arterial wall injury.

Abstract: Constrained paclitaxel derivatives include a bridge extending from the C-3? phenyl to either the C4 or -3 positions. Many of the constrained paclitaxel derivatives provide activity comparable or superior to the natural product paclitaxel.

Abstract: The present invention relates to Diphenylethylene Compounds and compositions comprising a Diphenylethylene Compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more Diphenylethylene Compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more Diphenylethylene Compounds. The present invention further relates to articles of manufacture and kits comprising one or more Diphenylethylene Compounds.

Abstract: Compounds of the formula having anti-tumor activity, wherein R1 and R2 are as described herein

Abstract: The subject invention pertains to materials and methods for the prevention and treatment of gastrointestinal diseases, including inflammatory bowel diseases such as Crohn's disease and ulcerative colitis. Therapeutic compositions of the invention include compositions that can neutralize hydrogen peroxide, such as reducing agents and oxidizing agents. In one embodiment, a therapeutic composition of the invention comprises a reducing agent such as sodium thiosulfate. Therapeutic compositions of the invention can optionally include compounds with antibacterial activity, compositions that inhibit bacterial adherence to cells and tissue, compositions that inhibits epithelial lipid peroxidation, compositions that add viscosity to a solution, compositions that inhibit most cells, and/or compositions that help to seal or repair tight junctions between cells of the colonic epithelium of the gastrointestinal tract. Methods of the invention include administration of compounds or compositions of the invention.

Abstract: Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.

Abstract: A fungicide can be provided by using, as an active ingredient, a diamine derivative of the following general formula (1): wherein R1 to R7 represent a specific substituent such as an alkyl group with 1 to 6 carbon atoms, and R8 represents an aryl group, which may be substituted or a heteroaryl group, which may be substituted.

Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteonaimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention. In particular, the invention relates to treatment of viral infections using terphenyl derivatives.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

Abstract: Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.

Abstract: Novel biaromatic vitamin D analogues have the general formula (I): and are suited for a wide variety of pharmaceutical applications, whether in human or veterinary medicine, and also for cosmetic applications.

Abstract: The present invention relates to the synthesis of fluorinated forms of alkyl phenol compounds and their subsequent use as pharmaceutical agents. More specifically, alkyl phenol compounds are fluorinated to increase compound volatility such that the compound may be administered to a mammal, such as a human being, by inhalation. The invention also provides an inhaler (or vaporizer), that can be used for administration of the volatile derivatives of fluorine-substituted alkyl phenol compound. Further, different derivatives of fluorine-substituted alkyl phenol compound can be also administered by other routes as described in this document.

Abstract: Stable rare earth tris (organophosphate) solutions comprise a rare earth tris (organophosphate) and a hydrocarbon solvent. From about 2% to about 10% rare earth element, preferably from about 3% to about 8%, is present in the solutions. The rare earth tris (organophosphate) solutions are stable from precipitation of the rare earth tris (organophosphate) for at least about fifteen (15) days, preferably for at least about twenty (20) days and most preferably at least about thirty (30) days. A process for preparing these solutions is described herein. A stabilizing additive, acid, glycol or mixtures thereof, is utilized to inhibit precipitation. The molar ratios of free acid, glycol and/or water to the rare earth element are controlled to inhibit precipitation.

Abstract: A composition of matter comprising anionic clay having the general formula [M2+1-xM3+x(OH)2]x+(x/n)An?·yH2O??(I) or [M1+M3+2(OH)6]1+(1/n)An?·yH2O;??(II) where M1+ is a mono-valent metal; M2+ is a divalent metal; and M3+ is a trivalent metal; A is an inorganic or organic anion, chosen such that the rule of charge neutrality is obeyed; n is an integer; x is any rational number between 0 and 1; and y is any rational number between 0 and 10; where the anionic clay is in the form of particles having a volume weighted mean particle size diameter of less than 500 nm. Stable colloidal dispersions comprise such anionic clay particles having a volume weighted mean particle size diameter of less than 500 nm dispersed in a liquid medium.

Abstract: A blowing agent blend for making thermoplastic polymer foams comprises methyl formate. The blowing agent blend can further comprise at least one co-blowing agent. The co-blowing agent is either a physical co-blowing agent (e.g. an inorganic agent, a hydrocarbon, a halogenated hydrocarbon, a hydrocarbon with polar, functional group(s), water or any combination thereof), or a chemical co-blowing agent, or combinations thereof. The thermoplastic polymer foam can be an alkenyl aromatic polymer foam, e.g. a polystyrene foam. The blowing agent blend can comprise any combination of methyl formate and one or more co-blowing agents. The methyl formate-based blowing agent blends produce stable foams for various applications, including containers, packaging systems, as well as insulation boards and building materials. A process for the preparation of such foams is also provided.

Abstract: A composition comprising one or more radiation curable monomers and/or oligomers and one or heat stable composition comprising at least one radiation-curable alpha, beta-ethylenically unsaturated compound, at least one phenolic stabilizer, and at least one non-phenolic stabilizer selected from the group consisting of hydroperoxide decomposers and free radical traps. The compositions and methods are useful in applications such as radiation curable ink jet systems where viscosity is reduced by heating.

Abstract: The invention relates to a mixture for the application of a polymeric coating to a substrate. Said mixtures comprises water and optionally an organic solvent, at least one water-dispersible radically polymerizable compound, at least one water-dispersible polymerizable crosslinking compound and at least one water-dispersible compound which forms free radicals upon exposure to actinic radiation. The radically polymerizable compound cannot fully set with the free radicals formed on irradiation at room temperature, but rather comprises further reactive bonds, which lead to further or complete setting with the crosslinking compound. The invention further relates to a method for application of a non-adhesive corrosion protection layer to a substrate, by application of a mixture to the surface of a metallic or polymeric substrate, drying the mixture and irradiation of the applied coating with actinic radiation of such an intensity and for such a period that a solid, hard, tough coating is formed.

Abstract: A denture liner which includes a hydrophobic polymer component, a plasticizer component and an adhesive component. A method for making this denture liner and a denture liner kit are also provided. The compositions have improved consistency and are useful in prosthodontics, including formulating denture liners for the compositions have a glass transition temperature lower than the lower of an ambient temperature at which the liner is applied and a temperature inside the oral cavity. Phthalate-free embodiments, as well as kits are also described.

Abstract: Embodiments of this invention comprise a pigment comprising one or more substantially spherical-shaped beads, wherein each substantially spherical-shaped bead comprises one or more high aspect ratio particles encapsulated within an encapsulating material. Embodiments also comprise a resinous composition comprising said pigment. Yet further embodiments comprise a method of preparing said pigment via suspension polymerization.

Abstract: The invention relates to a method for treating a mineral filler by means of a polydialkylsiloxane and a fatty acid, the hydrophobic fillers thus obtained, and the application thereof in polymers for the manufacture of films and notably “breathable” films.

Abstract: The present invention relates to a process for preparing dry polymer granules having increased minimum ignition energy, lowered to unchanged maximum explosion pressure, lowered explosion strength (Kst) coupled with reduced dusting levels by drying a mixture including one or more emulsion polymers and one or more surfactants having HLB values between 10 and 25.

Abstract: The invention relates to addition compounds suitable for use as wetting agents and dispersants and obtainable by reacting monofunctional or polyfunctional aromatic epoxides with polyoxyalkylenemonoamines having a number-average molecular weight of >400 g/mol, one primary or secondary amino group and at least 4 ether oxygen atoms per molecule, from 90 to 100% of the epoxide groups of the starting material having undergone reaction, the weight fraction of aromatic groups in the addition compounds being not more than 50% and the addition compounds containing per molecule at least one amino group on which salts can be formed, or being present as a salt. The invention also relates to a process for preparing the addition compounds, to their use as wetting agents and/or dispersants and to pigments or fillers coated with the addition compounds and to pigment pastes which comprise pigments, binders and the addition compounds of the invention.

Abstract: A reworkable conductive adhesive composition, and method of making such, comprising an epoxy based conductive adhesive containing conductive metal filler particles dispersed in a solvent-free hybrid epoxy polymer matrix. In an additional embodiment an improved method of removing cured conductive polymer adhesives, disclosed here as thermal interface materials, from electronic components for reclamation or recovery of usable parts of module assemblies, particularly high cost semiconductor devices, heat sinks and other module components.

Abstract: A composition for microsurfacing of pavement is described. The composition includes a polymer-modified emulsion asphalt oil, water, cement, and crushed aggregate. The crushed aggregate includes a first portion having an L.A. abrasion resistance which is higher than an L.A. abrasion resistance of a second portion of the crushed aggregate.

Abstract: The present invention relates to thermoplastic polyamide moulding compositions which contain at least one copolyamide with at least 20% by weight polyamide 12 components and at least one aprotic compound selected from the group of N-alkylated, cyclic carboxylic acid amides with 5 to 7 ring elements and/or of urea derivatives, the alkyl rests of which are linear at the nitrogen or which form a linking of the two N-atoms, and a process for production of the moulding compositions. The thermoplastic polyamide moulding compositions are distinguished by the fact that no solid deposits are formed during thermoplastic conversion.

Abstract: A process for obtaining a grafted diene elastomer having functional groups along the chain, a rubber composition containing this grafted elastomer and having in particular improved hysteresis properties in the cross-linked state, a preparation process for this composition, a tire tread made from this composition and a tire of reduced rolling resistance which incorporates this tread. A process for obtaining this grafted elastomer includes a radical grafting reaction carried out in solution or without a solvent by means of a reagent of the mercaptan type to graft functional groups on to the chain of a starting elastomer. The starting elastomer is treated with an antioxidant having at least one aromatic amine function before the grafting reaction, so that the grafted elastomer has a macrostructure which is practically identical to that of the starting elastomer.

Abstract: Provided is an acrylic pressure sensitive adhesive composition excellent in pressure sensitive adhesive characteristics and removability and a pressure sensitive adhesive tape using the acrylic pressure sensitive adhesive composition. An acrylic pressure sensitive adhesive composition containing an acrylic polymer obtained by at least copolymerizing a (meth) acrylic acid alkyl ester with an alkyl group having 2 to 14 carbon atoms and a carboxyl group containing unsaturated monomer copolymerizable with the (meth) acrylic acid alkyl ester, and tackifier resins, wherein the tackifier resins are respective resins each containing a natural product as a raw material, include at least 4 kinds of the resins different in a molecular structure from one another and a content of each of the tackifier resins is in the range of 5 parts by weight or more and 20 parts by weight or less relative to 100 parts by weight of the acrylic polymer.

Abstract: Organic thiol compounds based on pentaerythritol and dipentaerythritol are described herein. More specifically, the compounds of the present invention are mixed esters of pentaerythritol and dipentaerythritol having at least one sulfhydryl group and preferably a plurality of sulfhydryl groups as well as at least one non-thiol-containing group. The organic thiol compounds are utilized to plasticize and/or heat stabilize halogen-containing polymer compositions especially poly(vinyl chloride) compositions. The compositions are substantially free or free of metal-based stabilizers, Lewis acids and terpenes. The compounds of the present invention are ideally utilized in polymers normally susceptible to deterioration and color change which can occur during processing of the polymer or exposure of the polymer to certain environments and surprisingly also serve as excellent plasticizers.

Abstract: Disclosed herein are a novel thermoplastic material and a golf ball utilizing the thermoplastic material. The golf ball (10) preferably comprises a core (12), a cover (16) and optionally a boundary layer (14). At least one of the core (12), cover (16) or boundary layer (14) of the golf ball (10) comprises the thermoplastic material. The thermoplastic material comprises a partially to highly neutralized blend of a copolymer, a metallocene-catalyzed alpha-olefin with a softening comonomer, and a fatty acid or fatty acid salt.

Abstract: A water absorbent polymer with reduced residual monomer content is prepared using silver ions and/or colloidal silver.

Abstract: A mixture of sinterable powders for rapid prototyping, comprising a powdered polymer base and material of a substantially glassy type in the form of microflakes, optionally with the addition of a material of a substantially glassy type in the form of microspheres, powdered aluminum and/or powdered graphite.

Abstract: A hose material for a fuel cell which is superior in both of low extraction property and electrical isolation, and which also has excellent mechanical properties, and also a hose manufactured using the hose material. The hose material comprises: (A) an ethylene-propylene copolymer; (B) hydrophobic silica; (C) a peroxide crosslinking agent; and (D) carbon black.

Abstract: Methods are provided for making a solution masterbatch containing a diene elastomer in an organic solvent and a reinforcing silica filler dispersed therein, comprising the steps of (a) mixing a precipitated silica having an average particle size substantially equivalent to an average particle size of a powdered silica, with a diene elastomer in a first organic solvent; and (b) desolventizing the mixture to form a solution masterbatch preparation. The use of such desolventized solution masterbatches in vulcanizable rubber compounds results in excellent processing characteristics with improved dispersion of fillers, including polymeric nanoparticles. The compounds also demonstrate improved properties, including reduced hysteresis.

Abstract: A novel food coating substance comprising a plasticizer-free aqueous copolymer poly(vinyl ester) dispersion of emulsion polymer, emulsifier, protective colloid and optionally other stabilizers is outstandingly suitable for the surface treatment or surface coating of hard cheese or semi-hard cheese, but also of meat products, fruits, nuts or seed material.

Abstract: An improved coating composition for use in providing a glossy finish to various objects comprises from about 80 to about 92 percent by weight of an acrylic emulsion polymer; and from about 5 to about 12 percent of a glycol ether. The composition also includes from about 1 to about 3 percent by weight of a polyethylene wax emulsion; up to about 1% by weight petroleum distillate; and the balance is water. About 3 to about 5 parts by volume of the concentrate is mixed with from about 2 to about 4 parts by volume of water. The composition is sprayed onto the object to be coated.

Abstract: A composition is for use with fabricating a ceramic composite stiffening member that defines a T-section. The stiffening member includes a web portion, at least one flange portion, a radius region disposed between the web portion and the at least one flange portion, and a skin member that is secured to the at least one flange portion and the radius region. The composition is a pliable mixture of refractory particles, plasticizers, silica-yielding polymers, and solvents that is applied along the radius region.