Abstract: The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

Abstract: Novel 1,4,8-triazaspiro[4,5]decan-2-one compounds corresponding to formula I processes for the preparation thereof, related methods of treatment and pharmaceutical formulations containing such compounds.

Abstract: The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous disease (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.

Abstract: Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R? is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to ? agonists.

Abstract: Novel imidazolopyridine 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, ECM degradation, joint degradation and/or inflammation, and others.

Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.

Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.

Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.

Abstract: The present invention relates to novel pyridine-2-carboxyamide derivatives of formula (I) useful as metabotropic glutamate receptor antagonists: wherein Y, Z, R1, R2 and R3 are as defined in the specification herein.

Abstract: To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.

Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

Abstract: Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.

Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., W is oxygen atom or sulfur atom, etc., X is halogen atom, C1-C6haloalkyl, etc., Y is halogen atm, C1-C6alkyl, etc., R1 is —CH?NOR1a, —C(O)OR1c, —C(O)NHR1d, phenyl substituted with (Z)p1, D-14, D-52, D-53, D-55 to D-59, etc., R1a is C1-C6alkyl, etc., R1c is C1-C6alkyl, etc., R1d is hydrogen atom, —C(O)R15, —C(O)OR15, etc., R2 is C1-C6alkyl, —CH2R14a, C1-C6alkynyl, —C(O)R15, —C(O)OR15, etc., further when R1 is —CH?NOR1a, —C(O)OR1c or —C(O)N(R1e)R1d, R2 may be hydrogen atom, R3 is C1-C6haloalkyl, etc., R14a is cyano, —OR25, etc., R15 is C1-C6alkyl, C1-C6haloalkyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl, etc., R25 is C1-C4alkyl, C1-C4haloalkyl, —C(O)R32 or —C(O)OR32, etc., R32 is C1-C6alkyl or C3-C6cycloalkyl, etc., Z is halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, etc.

Abstract: The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.

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

Abstract: The invention relates to methods, compositions, and uses of those compositions for making medicaments, for potentiating the beneficial effects of inhibitors of COX-1, COX-2, and 5-LOX, and reducing adverse effects, by also administering inhibitors of soluble epoxide hydrolase (“sEH”), with or without also administering one or more cis-epoxyeicosantrienoic acids. The invention further relates to the use of inhibitors of sEH as analgesics and to methods and compositions of epoxides of eicosapentaenoic acid and docosahexaenoic acid, optionally with an inhibitor of sEH, to reduce pain or inflammation or both.

Abstract: The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein X is a six-member ring selected from phenyl, pyridine, or pyrimidine; Y is H, an alkenyl, a substituted alkenyl, or alkynyl, and R is H or alkyl. Pharmaceutical compositions for treating various disorders such as cancers, the compositions including compound I are also provided.

Abstract: New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5a) and analogues thereof. The synthesis process proceeds via an ?,?-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.

Abstract: The present invention provides salt crystals of non-natural stereoisomer forms of monatin and to the use thereof.

Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, X, n, and m are as defined herein and to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them, and to methods for treating neurological and neuropsychiatric disorders.

Abstract: The present invention is concerned with duloxetine free base in crystalline form, and also novel polymorphic forms thereof.

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.

Abstract: The present invention related to a determination of a stereochemistry, a synthesis and dauer effect of 6R-(3,6-dideoxy-L-arabino-hexopyranosyloxy) heptanoic acid as a pheromone isolated from the Caenorhabditis elegance related to suppression of aging and stress. It becomes possible to develop medical substances using the pheromone relating to aging, stress, metabolism, signal transfer system in vivo, and anticancer, obesity and a suppressing agent for aging and stress.

Abstract: The addition of low concentrations of combinations of water-soluble organic salts of zinc to gels, creams, lotions or ointments can increase the ability of these products to reduce or prevent exogenous irritants from causing irritation of the underlying substrate. The addition of low concentrations of combinations of water-soluble organic zinc salts to these gels, creams, lotions or ointments also can reduce the irritation of skin or mucous membranes caused by the addition of potentially-irritating substances such as spermicides, microbicides, fungicides or other therapeutic agents to the gel, cream, lotion or ointment. The advantages of this anti-irritant approach over others, which generally employ high concentrations of single zinc salts, are the reduced potential for zinc toxicity, the reduced potential for toxicity related to zinc itself, and the preservation of the desirable biological properties of potentially-irritating therapeutic substances added to the gel, cream, lotion or ointment.

Abstract: Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.

Abstract: This invention relates to the use of compounds of the general formula (I): R?—CONH—X—NR2R3—R4—Y in which R1 represents an alkyl moiety containing 11 to 21 carbon atoms, X stands for a (CH2)n- group and n is an integer from 1 to 6, R2 and R3 independently represent an alkyl moiety with 1 to 4 carbon atoms or an hydrogen atom, Y stands for a COO— group, in cosmetic compositions, characterized in that the compound of formula (I): is prepared by reacting the oil from Theo-broma grandiflorum with an amine of the formula (II): H2N—X—NR2R3 and subsequently reaction with sodium monochloroacetic acid.

Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, R1 R2, R3, R4, R5, R6, R7, and R8 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.

Abstract: This invention provides a pharmaceutical and functional food which are made of a safe food ingredient or nutrient which has been used for a long period of time, and which have tranquilizing effect such as anti-anxiety effect, anti-depression effect, and anti-stress effect. The tranquilizer of the invention contains vitamin K as an active ingredient. Vitamin K is preferably menaquinone-4 and/or menaquinone-7. This invention also provides a supplement, health food or functional food for tranquilizing purpose that contains vitamin K as an active ingredient.

Abstract: A composition for treating hearing loss includes components that function through different biological mechanisms to provide an additive effect that is equal to or greater than a sum of the effect of the individual components. The composition includes a biologically effective amount of at least one scavenger of singlet oxygen, a donor antioxidant, a third antioxidant, and a vasodilator. A method of treating hearing loss includes the step of internally administering the composition including a biologically effective amount of the at least one scavenger of singlet oxygen, the donor antioxidant, the third antioxidant, and the vasodilator to a mammal within three days of trauma to a middle or inner ear of the mammal.

Abstract: Mixed micelles containing poly(L-histidine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of treating a warm-blooded animal with such a drug are disclosed.

Abstract: Provided are methods of treating HIV patients by administering to the patient a nutrient composition and at least one anti-retrovial drug. The method results in an increase in the patient's CD4+ cell count by at least 25% during a treatment period. The nutrient composition includes alpha lipoic acid; acetyl L-carnitine; N-acetyl-cysteine; zinc; selenium; vitamin C; bioflavinoid complex; vitamin E; one or more antioxidants selected from co-enzyme Q10 and glutathione; and one or more vitamins or minerals selected from beta-carotene, vitamin A, vitamin B1, vitamin B2, vitamin B6, niacinamide, calcium pantothenate, folic acid, vitamin B12, copper, manganese, chromium, and molybdenum.

Abstract: Aqueous dispersions of partly hydrophobic silica exhibit a smooth change in viscosity with pH over a wide pH range, without gelling or exhibiting local maxima. The dispersions have numerous uses, including use in O/W Pickering emulsions.

Abstract: The present invention relates to the field of gels. The invention also relates to an improved method for manufacturing gels. In particular the invention relates to a new class of material, fluid-bicontinuous particle-stabilized gels, and a method of making the same. The fluid-bicontinuous particle-stabilized gels comprise at least a first fluid, a second fluid, and a continuous layer of particles positioned at a continuous interface between the first fluid and the second fluid.

Abstract: A method of forming carbon nanotube-polymer composites includes the steps of forming a mixture solution including a plurality of carbon nanotubes dispersed in a co-solvent. The co-solvent includes an organic solvent and a second solvent being a short chain fluorinated carboxylic acid having a boiling point below 150° C. which is less oxidizing than nitric acid, and is soluble in both the organic solvent and water. The first polymer is mixed with the mixture solution to form a polymer including mixture. The co-solvent is removed from the polymer mixture to form a dispersed nanotube-polymer composite. The second solvent can be trifluoroacetic acid.

Abstract: A curable composition for dental use, containing a polymerizable monomer, inorganic particles (A) having irregular shapes and an average particle size of from 1.0 to 5.0 ?m, wherein the inorganic particles (A) are surface-treated with a silane coupling agent (a) represented by the formula (I): wherein R1 is a hydrogen atom or a methyl group, R2 is a hydrolyzable group, R3 is a hydrocarbon group having 1 to 6 carbon atoms, X is an oxygen or sulfur atom, p is 2 or 3, and q is an integer of from 8 to 13, and inorganic particles (B) having irregular shapes and/or spherical or nearly spherical shapes, and an average particle size of from 0.01 to 0.

Abstract: A matrix which is a polymer, plastic or polymer-wood composite includes a composition of a biocide and a processing additive therewith in the form of a free-flowing powder.

Abstract: The present invention relates to antimicrobial agents, methods for the production of these agents, and the use of these agents. The antimicrobial agent of the present invention includes a water-soluble polymer and oligodynamic metal ions which interact with counter-ions of the polymer such that the metal ions are bound to corresponding counter-ions. The water-soluble polymer controls a sustained release of the metal ions. The oligodynamic metal ions preferably include small size metal particles (e.g., nano-sized silver particles) that interact to the water-soluble polymer as well as metal ions derived from one or more water-soluble oligodynamic metal compositions (e.g., metal sulfates and/or metal nitrates). The agent may also include one or more acids, including organic acids (such as sulfates, carboxylic acids, amines, hydroxyls, nitrates, and phosphates) and/or non-organic acids (such as boric acid and dioctylborate).

Abstract: An ink composition includes: first particles which are insoluble and dispersed in an aqueous dispersion medium, a polarity of the first particles being one of positive and negative; and second particles which are insoluble and dispersed in the aqueous dispersion medium, the second particles including both a cationic group and an anionic group, the second particles having a zeta potential that changes along with a change in pH of the aqueous dispersion medium, percentage of a water-soluble component in the second particles being not higher than 5% by mass.

Abstract: What is disclosed is a plurality of prepaints which are used in any combination to produce base paints and/or colored paints of varying end-use application characteristics. Additionally, a mobile paint factory for producing a plurality of lines of architectural coatings from a plurality of prepaints en route to and/or at various locations is disclosed. The mobile paint factory may include a vehicle having a paint production system and a paint mixer located thereon. Furthermore, a method of producing a plurality of lines of user-selected architectural coatings from a plurality of prepaints en route to and/or at various locations is disclosed. The method may include: providing a mobile paint factory; prompting a user to select through the paint production system an interior or exterior application environment, a paint sheen, and a paint quality; automatically dispensing predetermined amounts of appropriate prepaints; and agitating the dispensed prepaints.

Abstract: A coating composition including an unsaturated resin selected from polyesters, alkyds or combinations thereof; an alkoxy(meth)acrylic functional monomer, and a thermoplastic compound containing active hydrogen groups; a curing agent; and a curing promoter such as at least one metal drier.

Abstract: The present invention relates to bituminous compositions suitable for use in paving applications containing water-in-oil bitumen dispersion of paving grade bitumen such as penetration-graded, viscosity-graded and/or penetration-graded varieties that is substantially free of volatile solvents and made by controlling temperature-dependent interfacial rheology through the use of selected surfactants. The invention paving compositions are suitable for use in the construction of load-bearing, high-traffic pavements at a temperature range lower than that required for conventional hot-mix bituminous paving compositions, yet with similar or superior compaction to densities property and at least equal cure rate.

Abstract: The invention concerns novel bituminous products, as well as novel aqueous emulsions of bituminous products, mixtures thereof with coated granules, useful for sealing application, building and maintaining road surfaces, sidewalks and runways, road surfaces, sidewalks, bicycle paths, parking lots and runways.

Abstract: Compositions including a polymer, a primary antioxidant, a secondary antioxidant, and a metal deactivator selected from at least one of 2,2?-oxamido bis[ethyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionate] and oxalyl bis(benzylidenehydrazide), are disclosed. The compositions can also include a light stabilizer. The compositions can be used to manufacture insulations for wire and cable. The compositions have improved long-term heat aging and also retain their color when exposed to heat. A method of making an insulation for a conductor, such as a wire or a cable, made from a composition is also provided.

Abstract: Polymer composite materials having improved gas barrier properties are generally disclosed, along with process of making the same. The polymer composite materials can include phosphonate particles, oxide particles, and combinations thereof. For example, the particles can be metal phosphonate particles, synthetic oxide particles, or combinations thereof.

Abstract: A method of decreasing the roiling resistance of a tire formed from a sulfur-vulcanized elastomeric by combining at least one diene elastomer and at least one reinforcing filler, with an effective amount of a coupling agent consisting of a combination of: 10 to 90%, of a product (I) consisting of a blend of poly(alkylphenol) polysulfides of formula: in which: R is an alkyl radical containing 1 to 20 carbon atoms; n and n? are two integers, which may be identical or different, from 1 to 8; p is an integer from 0 to 50; and 10 to 90% of a product (II) consisting of bis(triethoxysilylpropyl)tetrasulfide, to form a mixture; thereafter working said mixture; and thereafter heating said mixture to vulcanize said mixture. 90% of bis(triethoxysilylpropyl)tetrasulfide.

Abstract: The present disclosure presents materials comprising hydrogenated and/or partially hydrogenated polymerized vegetable oils. Non-limiting applications of the polymerized oils, including coatings, binders, blends, and greases are presented. Methods for forming these materials are also disclosed.

Abstract: Method for packaging a photo detector integrated circuit (IC) and a pigment filter and resulting package are described. An encapsulated package (e.g., an epoxy-encapsulated package) that includes a first surface is provided. A filter layer is then coated directly onto the first surface. The filter layer provides optical filtering properties (e.g., a predetermined filtering profile) in addition to the filtering provided by the pigment filter.