Abstract: Pharmaceutical compositions comprise a nucleotide analog with a phosphonate group at a concentration effective to act as a substrate and/or inhibitor of a viral polymerase, and especially of the HCV RNA dependent RNA polymerase.

Abstract: An oxapenem compound which is, or is capable of forming, a zwitterion of formula wherein R is a C1-C8 branched or straight chain alkyl group which is substituted by a protonated nitrogen base. The compounds find particular use as high bioavailability ?-lactamase inhibitors.

Abstract: A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the eyes of the subject a non-drying antihistamine compound, such as epinastine hydrochloride, in an amount effective to reduce dry eye symptoms and stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the compound include topical administration via a liquid, gel, cream, or as part of a contact lens or a continuous or selective release device; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.

Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating colon cancer.

Abstract: Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.

Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

Abstract: The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, such as maleate salts, and to crystalline polymorphs of these salts. The invention further relates to pharmaceutical compositions of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide salts, and methods of treating disorders such as cancer using such compositions.

Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment diseases, conditions and/or disorders herein.

Abstract: Antitumour compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group.

Abstract: Novel tricyclic compounds are disclosed having the general structure of Formulas I or II: were R1, R2 and R3 are defined in the written description of the invention. The compounds are useful for the treatment or prevention of symptoms or manifestations associated with diseases or disorders affected by intracellular cytokine signaling.

Abstract: Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interferon-alfa, e.g., pegylated interferon alfa-2b, in association with a therapeutically effective amount of a CCR5 antagonist or preferably further in association with a therapeutically effective amount of at least one of ribavirin, IL-2, IL-12, pentafuside alone or in combination with a therapeutically effective amount of an anti-HIV-1 drug therapy, e.g., HAART are disclosed.

Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.

Abstract: A compound of the general formula (I): wherein R1, R2, X, Y and Z are as described in the specification.

Abstract: Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely designed in that they have a rifamycin moiety covalently linked to a linker group through the C-3 carbon of the rifamycin moiety and the linker is, in turn covalently linked to a therapeutic moiety or antibacterial agent/pharmacophore. The therapeutic moiety can be a quinolone, an oxazolidinone, a macrolide, an aminoglycoside, a tetracycline core or a structure/pharmacophore associated with an antibacterial agent.

Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more s

Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using these sodium channel blockers.

Abstract: The present invention relates to a compound represented by formula (I): where the structural variables are as defined herein. The compound is useful for promoting hydration of mucosal surfaces.

Abstract: The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer's disease.

Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.

Abstract: A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): wherein n is an integer of 0 to 3, or a pharmacologically acceptable salt thereof.

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.

Abstract: The present invention relates to optically pure S-(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.

Abstract: This invention relates to novel 8-aza-bicyclop[3.2.1]octane derivatives useful as monoamine neurotransmitter re-up-take inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: Thus, the present invention provides compounds of formula (I) The present invention further provides the use of a compound of formula (I) for the manufacture of a medicament for the treatment of a neurological disorder.

Abstract: Compounds having a selective N-type calcium channel antagonistic activity are provided. Dihydropyridine derivatives represented by the following formula: analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel, and they are used as therapeutic agents for various diseases relating to N-type calcium channel.

Abstract: Benzopyranone Compounds having the following structure: wherein R1, R2, X, Y and n are as defined herein, are disclosed. The Benzopyranone Compounds are useful for treating or preventing a bone-resorbing disease, a neoplastic disease, arthritis, a disease exacerbated by the presence of estrogen or a disease improved by the presence of estrogen, comprising administering an effective amount of a Benzopyranone Compound to a patient in need of the treating or preventing; activating the function of estrogen receptor (“ER”) in a bone cell; inhibiting the function of ER in a cancer cell; inhibiting the expression of interleukin-6 (“IL-6”) in a cell; and inhibiting the growth of a neoplastic cell, comprising contacting the cell with an effective amount of a Benzopyranone Compound.

Abstract: This invention provides compounds of Formula 1, N-oxides and suitable salts thereof wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H; C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, C3-C5 cycloalkyl, or C4-C6 cycloalkylalkyl, each optionally substituted with one substituent selected from the group consisting of halogen, CN, SMe S(O)Me, S(O)2Me, and OMe; R5 is H or Me; R6 is H, F or Cl; and R7 is H, F or Cl. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula 1, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).

Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.

Abstract: The present invention relates to novel oxazoles of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

Abstract: This invention relates, in part, to macrolide compounds, actinomycete strains for producing them, and pharmaceutical compositions containing them.

Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, and n are those defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.

Abstract: L-threo-?-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): wherein R is hydrogen, a linear or branched lower aliphatic acyl group with the acyl portion optionally substituted, an alicyclic acyl group, an aromatic acyl group with a substituent on the aromatic ring, an amino acid-derived group or a biotin derivative-derived group, having an amino substituent on the benzene ring, and salts thereof, which can easily bind to affinity column chromatography carriers as ligands of glutamate transporter proteins.

Abstract: The present invention relates to a pharmaceutical composition containing a cycloalkene compound, a salt thereof or a prodrug thereof, and a nonionic surfactant and/or a cyclodextrin derivative readily soluble in water, and a method for improving solubility, stability or coloring property of the compound, a salt thereof or a prodrug thereof.

Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel 3,4-disubstituted benzamidines and benzylamines, or a stereoisomer or pharmaceutically acceptable salt form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor Xa, factor XIa, factor IXa, and/or factor VIIa. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: This disclosure discusses problems associated with using natural gas to produce a variety of synthetic hydrocarbon products by production processes that require syngas feedstocks with varying H2/CO and (H2?CO2)/(CO+CO2) ratios. A number of gas separation membranes are used to vary the composition of the feed streams to different hydrocarbon synthesis units so that different synthetic hydrocarbon products can be produced. The process supplies syngas to an integrated hydrocarbon processing system comprising a number of hydrocarbon synthesis units. Gas (usually a portion of a raw syngas stream) is routed through the separation membrane units, multiple H2-rich and H2-lean streams are produced. These H2-rich and H2-lean streams can then be combined in a controlled fashion to produce feed streams of the desired compositions for the various hydrocarbon synthesis units. A variety of liquid synthetic hydrocarbon products can be produced from a given syngas source as required by market demands.

Abstract: A novel expandable composition and method for using the same are disclosed. The disclosed method relates to using the composition, for example, as an automotive cavity sealant. The inventive composition normally is a combination of at least one base polymer, at least one expansion or blowing agents, at least one hydrocarbon resin, at least one curing agent or catalyst and optionally at least one additives such as a supplemental polymer, colorant, tackifier, processing oil, among others.

Abstract: Surprisingly effective additive formulations for the reduction of highly undesirable yellowing or other discoloration of white, uncolored, polyurethane foam articles are provided. White polyurethane foam exhibits a susceptibility to yellowing and discoloration to a great extent, particularly in relatively short periods of time, than other types of polymeric articles. The inventive additives impart excellent low-discoloration properties over appreciable amounts of time of regular exposure to harmful elements, thereby according the pertinent industry a manner of providing white polyurethane foams for longer periods of time. Methods of producing such reliably white-colored polyurethane foams are also provided.

Abstract: A photosensitive composition comprising, (A) an oligomer or polymer containing at least one carboxylic acid group in the molecule and having a molecular weight of 200?000 or less; (B) at least one photoinitiator compound of formula I ?wherein R1 is linear or branched C1–C12alkyl; R2 is linear or branched C1–C4alkyl; R3 and R4 independently of one another are linear or branched C1–C8alkyl; and (C) a monomeric, oligomeric or polymeric compound having at least one olefinic double bond, is especially suitable for preparting photoresists, in particular color filters.

Abstract: The invention concerns dental compositions. Said composition comprises (1) a silicone crosslinkable and/or polymerizable by cation process; (2) an efficient amount of at least an initiator such as onium borate; (3) at least a photosensitizer ; and (4) a dental filler present in the composition in a proportion of at least 10 wt. % relative to the composition total weight. Said dental compositions are useful for making dental prostheses or for dental restoration.

Abstract: A mixture including a high specific gravity masterbatch pellets group (A) with specific gravity within a range from 1.8 to 3.5, and a low specific gravity masterbatch pellets group (B) with specific gravity within a range from 0.5 to 1.6. The high specific gravity masterbatch pellets group (A) comprises m different columnar masterbatch pellets, each with a different specific gravity, and the low specific gravity masterbatch pellets group (B) comprises n different columnar masterbatch pellets, each with a different specific gravity. The high specific gravity masterbatch pellets group (A) and the low specific gravity masterbatch pellets group (B) satisfy a formula (1) shown below: 0.5 ? ? ( mm - 1 ) ? ? p = 1 m ? ( Hp Sp × Rp ) - ? q = 1 n ? ( Hq Sq × Rq ) ? 12 ? ? ( mm - 1 ) ? .

Abstract: Disclosed are the following: a cement dispersant which is excellent in initial dispersibility and further in flow retainability of cement, because of using a polymer having a proper molecular weight distribution; a process for producing this cement dispersant; and a cement composition using this cement dispersant. The cement dispersant comprises a water-soluble polymer (P) as a main component, and is characterized by displaying an area proportion (a value (A?B) given by subtracting an area ratio B of a lower molecular weight side portion from an area ratio A of a higher molecular weight side portion) in the range of 13 to 60%.

Abstract: An earth-friendly tire using raw materials derived from non-petroleum resources instead of all or part of raw materials derived from petroleum resources currently used for tires. The tire is prepared by using a natural rubber instead of a synthetic rubber; an inorganic filler and/or a biofiller instead of carbon black; vegetable oil instead of petroleum oil; and natural fiber instead of synthetic fiber so that the tire comprises a non-petroleum raw material in an amount of at least 75% by weight based on the total weight of the tire.

Abstract: Disclosed is a bituminous composition that comprises a bituminous component (A), an elastomer component (B), preferably a block copolymer of a conjugated diene and a monovinylaromatic hydrocarbon, and an additive (C), wherein the additive is a compound of the general formula Ar—R—Ar??(I) wherein each “Ar” independently is a benzene ring or fused aromatic ring system of 6 to 20 carbon atoms, substituted by at least one hydroxyl group, and “R” is an optionally substituted divalent radical comprising 6 to 20 atoms in the backbone and at least one amide and/or ester group in the backbone. These compositions are disclosed to be particularly useful in the preparing and repair of roofing.

Abstract: Polyoxymethylene with improved resistance to acids, comprising A from 84 to 99.79% by weight of at least one polyoxymethylene homo- or copolymer, B from 0.1 to 5% by weight of at least one polyalkylene glycol, C from 0.1 to 10% by weight of zinc oxide, and D from 0.01 to 1% by weight of one or more nitrogen-containing costabilizers, where the total of the percentages by weight of components A to D is 100%. This polyoxymethylene is particularly advantageous when used for producing moldings for use in contact with aggressive acids or with aggressive acid-containing cleaning agents, in particular for applications in the sanitary sector or the white goods sector.

Abstract: The present invention relates to a flame retardant resin composition comprising: 100 parts by weight of a thermoplastic polyamide resin (A), 1 to 100 parts by weight of a phosphazene compound (C), and a polyphenylene ether-based resin, a polystyrene-based resin or mixture thereof (B) being present in an amount of 10 to 500% by weight based on the weight of said phosphazene compound (C).

Abstract: A liquid composition which is a precursor to a solid surface material comprises a liquid polymerizable component and two different solid particle distributions with an added polycarboxylic acid or salt retarding or preventing particle settling.

Abstract: A curable coating composition includes a polyester, a curing agent for curing the polyester, a curing catalyst, a composite solvent having at least two solvents with different dissolving powers for the polyester, and a wax incompatible with the polyester. A method for making a coated metal plate having an embossment-like texture formed from the coating composition, and the coated metal plate made thereby are also disclosed.

Abstract: This invention relates to a rubber composition prepared with reinforcement comprised of a combination of precipitated silica aggregates and pelletized rubber reinforcing carbon black composites of carbon black and organic binder of a controlled hardness and to a tire with at least one component comprised of and derived from such rubber composition in which said carbon black pellet composites are disintegrated (fragmented) in situ within said rubber composition in the presence of particulate precipitated silica and silica coupling agent. In one aspect the invention relates to a tire having a component of a rubber composition comprised of at least one conjugated diene-based elastomer and reinforcing filler comprised of a combination of precipitated silica, silica coupling agent and fragmented rubber reinforcing carbon black pellet composites, said pellets having a controlled hardness value.

Abstract: A nanostructure having at least one nanotube and at least one chemical moiety non-covalently attached to the at least one nanotube. At least one dendrimer is bonded to the chemical moiety. The chemical moiety may include soluble polymers, soluble oligomers, and combinations thereof. A method of dispersing at least one nanotube is also described. The method includes providing at least one nanotube and at least one chemical moiety to a solvent; debundling the nanotube; and non-covalently attaching a chemical moiety to the nanotube, wherein the non-covalently attached chemical moiety disperses the nanotube. A method of separating at least one semi-conducting carbon nanotube is also described.