Abstract: Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R1 is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3? are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocarbonyl, whereas R3 and R3? do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.

Abstract: The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.

Abstract: The present disclosure concerns compounds of formula (I) and pharmaceutically acceptable salts, hydrates, solvates, pharmaceutically acceptable derivatives, pro-drugs, tautomers and/or isomers thereof.

Abstract: Substituted 5,6,6a,11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds, and processes for the production thereof, pharmaceutical compositions containing these compounds and the use thereof in treatment methods and for the production of pharmaceutical preparations for specific indications, in particular for the treatment of pain.

Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.

Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

Abstract: Novel compounds of formula (I), wherein D, W, X, Y, T and R1 have the meanings cited in claim 1, are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumors

Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject.

Abstract: The invention relates to novel 1,4-dihydro-1,4-diphenylpyridine derivatives of formula (I) wherein the variable groups are as defined in the text and claims. Processes for their preparation, pharmaceutical compositions containing them, and methods of treatment of inflammatory processes, expecially chronic obstructive pulmonary diseases, using them are also disclosed and claimed.

Abstract: Novel compounds (I) and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy wherein Ar is a group of formula a) or b).

Abstract: This invention provides compounds of Formula I, N-oxides and salts thereof wherein A, B, R1 through R5, R7 through R9, X and Y are as defined in the disclosure. 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 I. Also disclosed are compositions for controlling an invertebrate pest comprising the compounds of Formula I.

Abstract: The present invention relates to a pharmaceutical composition comprising an insulin sensitizer and a diuretic which can prevent or treat side effects such as edema, cardiac enlargement, body fluid retension or hydrothorax caused by administration of an insulin sensitizer.

Abstract: The invention relates to novel compounds of Formula (I) or a salt, solvate or prodrug thereof, wherein A, R1, R2, R3, n and m are described in the specification, useful in the treatment of a disease or condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to methods for preparing compounds of Formula (I) and their use as medicaments in the treatment of diseases mediated by glucokinase.

Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A—(B)b0—(C)c0—NO2 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R—T1—, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from anminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.

Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein —N-HET is, for example, (Ic) or (If) wherein R1 is, for example, halogen or a (1–4C)alkyl group which is substituted by one substituent selected from, for example, hydroxy, (1–4C)alkoxy, amino, cyano or azido; Q is selected from, for example, Q1 wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

Abstract: Provided are process for the preparation of valsartan and the precursors thereof.

Abstract: Compounds of the formula in racemic or enantiomeric forms wherein the substituents are as defined in the application. Useful for treating acromegalia, hypophyseal adenomas or endocrinic gastroenteropancreatic tumors.

Abstract: A compound is disclosed, which is useful in treating a mammal having a disease-state characterized by thrombotic activity. The compound is of the following formula: wherein A, B, R1, R2, R3 and R4 are as defined herein or an isomer or isomeric mixture thereof or a pharmaceutically acceptable salt thereof.

Abstract: A compound represented by the formula (1): wherein R1—X— indicates that 1 to 4 R1—X— groups are present which may be the same or different, the ring A is a saturated or unsaturated 5-membered heterocyclic ring, X is a single bond, a group represented by the formula: —N(R3)—, —O— or —S—, or the like. R1 is a hydrogen atom, a halogen atom, a nitro group, a carboxyl group, a substituted or unsubstituted alkyl group, or the like, R2 is a hydrogen atom, a halogen atom, a nitro group, a carboxyl group, a substituted or unsubstituted alkyl group, or the like, and R3 is a hydrogen atom, a substituted or unsubstituted alkyl group, or the like; a prodrug of said compound, or a pharmaceutically acceptable salt of said compound or prodrug is a useful compound as a therapeutic agent for diseases for which Rho kinase is responsible.

Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5a and R5b is C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5a and R5b may also be hydrogen, aryl, Het1, Het2; R6 is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms.

Abstract: The present application describes monocyclic and bicyclic lactams and derivatives thereof of Formulae Ia–e: wherein one of one of T1 and T2 is carbonyl, thiocarbonyl, or sulfonyl or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and pharmaceutical compositions comprising such compounds, the compounds having the following formula: wherein R1 and R2 each represent hydrogen, or a protecting group of the amino group; R3 represents hydrogen, or a protecting group of the hydroxyl group; R4 represents a lower alkyl group; n is 1 to 6; X represents oxygen or nitrogen, which is unsubstituted or substituted with a lower alkyl group; Y represents ethylene; Z represents a C1–C10 alkylene; R5 represents an aryl group; and R6 and R7 each represents hydrogen; provided that when R5 represents hydrogen, then Z represents a group other than a single bond or a straight chain C1–C10 alkylene group.

Abstract: The invention provides conjugates of cis-docosahexaenoic acid and pharmaceutical agents useful in treating noncentral nervous system conditions. Methods for selectively targeting pharmaceutical agents to desired tissues are provided.

Abstract: The present invention provides a TNF-? production inhibitor containing a kavalactone as an active ingredient, which inhibitor has high safety, exerts an excellent effect of inhibiting TNF-? production, and is useful as a drug or an animal drug for preventing, ameliorating, or treating diseases such as cachexia attributed to cancer or infectious diseases, chronic rheumatoid arthritis, inflammatory diseases, osteoarthritis, systemic lupus erythematosus (SLE), rejection during bone marrow transplantation, multiple organ failure, AIDS, meningitis, hepatitis, and type-II diabetes. The present invention also provides a preventive, ameliorating, or therapeutic agent for diseases caused by abnormal production of TNF-?, the agent containing a kavalactone as an active ingredient.

Abstract: A formulation is described comprising paracetamol, niflumic acid or a pharmaceutically acceptable salt or ester thereof and a pharmaceutically acceptable excipient.

Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I.

Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-?, such as rheumatoid arthritis, graft rejection, cachexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease or HIV infection.

Abstract: A method to treat an animal, including a human, having a solid tumor. The method provides a lipophilic lathyrogen. The method administers a therapeutically effective amount of the lipophilic lathyrogen within the solid tumor.

Abstract: The present invention describes novel methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for improving kidney functions, such as urine output, and treating symptoms associated with kidney malfunction or failure. The invention also relates to kits for the improvement of kidney functions and the treatment of symptoms associated with kidney malfunction or failure, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.

Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention relates to the use of biguanide derivatives of general formula I below: in which: the groups R1 and R2 represent, independently of each other, a hydrogen atom, a C1–C7, alkyl group, a cycloalkyl group, a heterocycle, a C2–C7 alkenyl group, an aryl group, an aralkyl group, an aryloxyalkyl group or a heteroaryl group, or R1 and R2, taken together, represent a C2–C7 alkylene which may contain one or more hetero atoms, and the group R3 represents a primary, secondary or tertiary amine, or pharmaceutically acceptable salts thereof, to manufacture a medicinal product with cicatrizing action, the said medicinal product being in a pharmaceutical form for topical use.

Abstract: Antiobestic agents and health foods containing as the active ingredient substances having an effect of adsorbing bile acid in the digestive tract, an effect of inhibiting intestinal circulation or an effect of inhibiting the absorption of exogenous lipids typified by pharmaceutically acceptable anion exchange resins. In particular, antiobestic agents and health foods characterized by lowering body weight and/or visceral fat content without reducing food intake.

Abstract: The invention relates to the use of substituted bicyclo[3.3.1]nonan-2,4,9-triones, especially clusianon and clusianon derivatives, as pharmaceutical active ingredients or medicamentous active ingredients, especially for producing medicaments for the prophylactic and/or therapeutic (curative) treatment of tumour or cancer diseases, and of viral diseases. The above-mentioned compounds can be used in cytostatic agents and antiviral agents (virostatic agents). They are especially used as inhibitors of topoisomerases and telomerases and as regulators during the MAP kinase signal transduction and can thus intervene on a cellular scale in the mechanism for multiplication of tumour or cancer cells and viruses.

Abstract: The invention relates to the use of treosulfan as a conditioning agent before allogenic transplantation of bone marrow or haematopoietic stem cells, whereby treosulfan is administered, either as single effective agent, or in combination with other chemotherapetic agents or immunosuppressant agents.

Abstract: Method for continuously removing the unreacted butene-1, and optionally other volatile components, from a polymeric solution obtained by liquid phase (co)polymerization of butene-1, the method comprising the steps of: subjecting the polymeric solution to heating and mixing conditions such that a mixture is formed consisting substantially of: (1) a polybutene melt containing entrapped butene-1 and (2) supercritical gaseous butene-1; subjecting the above mixture to a sequence of devolatilization steps operating at decreasing pressures.

Abstract: Black polyurethane foams that exhibit higher strength black colorations without the need for concomitant increases in black colorants therein are provided. Such a resultant jetter black foam article is possible through the unexpectedly effective introduction of small amounts of certain toner compounds or combinations that exhibit specific measurable appearance characteristics. Such toners exhibit at least one absorption peak within a specific range of wavelengths (e.g., from about 560 to 610 nm) and specific ranges of half-height bandwidths (from 40 to 130 nm). Furthermore, such a compound or combination of compounds, is preferably liquid in nature (at room temperature) or in dispersion form and may thus be easily incorporated within target polyurethane precursor compositions for admixture with either black pigments (or dispersions thereof), black polymeric (liquid) colorants, or both.

Abstract: An expandable material and articles incorporating the same are disclosed. The material includes a polymeric admixture; a blowing agent; a curing agent; a tackifier; and optionally, a filler or fiber.

Abstract: Radiation-curable resins containing a carbonyl-hydrogenated ketone-aldehyde and/or a ring-hydrogenated phenyl-aldehyde resins, and a process for preparing them.

Abstract: There is provided a process for forming a light emitting polymer comprising photopolymerization of a reactive mesogen having an endgroup which is susceptible to photopolymerization e.g. by a radical polymerization process. Also provided are methods for using the light emitter in displays, backlights, electronic apparatus and security viewers.

Abstract: The present invention relates to a process for the production of a cellular composite, and to the resultant cellular composites. This process comprising (A) preparing a mixture of a polyisocyanate, water, and, optionally, one or more additives; (B) adding this mixture under low shear mixing to inorganic hollow microspheres; (C) completely filling a mold with the mixture; and (D) heating the mold containing the mixture to a temperature of from 100 to 280° C., thereby forming the composite.

Abstract: The present invention relates to a thiol compound derivative represented by the following formula (1), a curable composition containing the derivative, and a molded product made of the composition.

Abstract: A non-xenoestrogenic phosphorus-containing stabilizer for organic materials is disclosed wherein the stabilizer is selected from the group consisting of phosphorus-containing compounds of the structures wherein y in an integer of from 6 to 20, and where Z is a linking group, m is 0 or 1, n is an integer of at least 2, the asterisks are independently selected terminal groups, R1, R2, R3, R4, R5, R6, R7, and R8 are independently selected from the group consisting of hydrogen, alkyl groups, aralkyl groups, or halogen groups and Q is selected from the group consisting of where R11, is alkyl or aralkyl, and

Abstract: The present invention provides a (meth)acrylic resin composition, in which thermal degradation when processing is inhibited and discoloring hardly occurs, which could not be obtained in the conventional (meth)acrylic resin composition containing (meth)acrylic resin prepared by suspension polymerization. More specifically, the present invention relates to a (meth)acrylic resin composition comprising 100 parts by weight of a methyl methacrylate polymer obtained by suspension polymerizing 50 to 100% by weight of methyl methacrylate and 50 to 0% by weight of a monomer copolymerizable therewith, 1 to 200 parts by weight of a copolymer having a multi-layer structure and 0.02 to 10 parts by weight of a fatty acid metallic salt.

Abstract: Compositions comprising a polymer and an exfoliated metal phosphonate are provided. Processes for making such polymer compositions and articles formed from such polymer compositions are also provided. Compositions according to the invention are useful in polymer applications in which barrier properties are of concern, such as in plastic food and beverage containers.

Abstract: An agglomerate comprising fine primary particles of an inorganic compound except for silica is provided, satisfying dp50: the average particle diameter [?m] of the agglomerate measured by Microtrac-FRA, a laser analysis type particle size distribution measurement apparatus, ?: the value calculated by dividing the difference between the particle diameter d90 of cumulative 90% minus sieve particles of the agglomerate and the particle diameter d10 of cumulative 10% minus sieve particles of the agglomerate calculated by the Microtrac-FRA, Sw: the BET specific surface area [m2/g] of the agglomerate, St: the tensile strength [MPa] required to break the agglomerate with the particle diameter 4 ?m, and, Sta: the tensile strength [MPa] required to break 30% of the particle diameter of the agglomerate with the particle diameter 4 ?m, both St and Sta being measured by a micro compression testing machine manufactured by Shimadzu Corporation.

Abstract: This invention relates to a composition for repairing metallic articles which in its initial state is in the form of an adhesive, self-supporting putty, capable of being molded including 5–15% by weight of a sacrificial binder containing at least one acrylic resin and volatile solvent. The invention also relates to a kit for the composition and methods for repair.

Abstract: A tire tread comprising a rubber composition based on (phr: parts by weight per hundred parts of elastomer): (i) a diene elastomer; (ii) more than 50 phr of an inorganic filler as reinforcing filler; (iii) between 2 and 15 phr of an (inorganic filler/diene elastomer) coupling agent; (iv) between 1 and 10 phr of a methylene acceptor, and (v) between 0.5 and 5 phr of a methylene donor. This tread has, after mechanical running-in of the tire for which it is intended (“auto-accommodation”), a rigidity gradient which increases radially from the surface towards the inside of the tread. Use of such a tread for the manufacturing or recapping of tires. Tires comprising a tread according to the invention, in particular of the snow or ice type (“winter” tires).

Abstract: Disclosed are elastomeric compounds including an elastomer and a silicon-treated carbon black, and optionally including a coupling agent. The elastomeric compound exhibits poorer abrasion resistance in the absence of a coupling agent, lower hysteresis at high temperature and comparable or increased hysteresis at low temperature compared to an elastomer containing an untreated carbon black. A variety of elastomers and formulations employing such elastomers are contemplated and disclosed. Elastomeric compounds incorporating an elastomer and an oxidized, silicon-treated carbon black are also disclosed. Also disclosed are methods for preparing elastomers compounded with the treated carbon black.