Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.

Abstract: The invention provides a methioninase inhibitor to suppress the production of methyl mercaptan that is a causative substance of a bad smell by inhibiting methioninase originated from bacteria, as well as a composition and a food or drink containing the same, wherein the methioninase inhibitor contains an extract obtained from a plant of the family Myrsinaceae, genus Myrsine, preferably Myrsine seguinii as an active ingredient; and further provides a methioninase inhibitor, as well as a composition and a food or drink containing the same, wherein the methioninase inhibitor contains as an active ingredient one or more selected from the group consisting of myrsinoic acid A, myrsinoic acid B, myrsinoic acid C, myrsinoic acid E and myrsinoic acid F; preferably the myrsinoic acid A, myrsinoic acid B, myrsinoic acid C, myrsinoic acid E and myrsinoic acid F are obtained from a plant of the family Myrsinaceae, genus Myrsine, preferably Myrsine seguinii.

Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

Abstract: Oral antidepressant formulation comprising an effective antidepressant amount of at least one pharmaceutically acceptable antidepressant active agent and an effective amount lower than 50 mg of acetylsalicylic acid, derivatives of acetylsalicylic acid, or diaspirin, for reducing the onset of antidepressant action.

Abstract: The invention relates to novel benzofuran derivatives, processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.

Abstract: The present invention pertains to the use of a compounds for the manufacture of a medicament for use in the treatment of a proliferative condition, wherein the compounds have the following formula: wherein: each of RB2, RB3, RB4, and RB5 is independently —H, —OH, or —OMe; each of R1 and R2 is independently: —H, optionally substituted C1-4alkyl, or optionally substituted C5-20aryl; RA3 is —H, —OH, —OC(?O)RE, —OS(?O)2OH, or —OP(?O)(OH)2; RE is: —H, optionally substituted C1-6alkyl, optionally substituted C3-20heterocyclyl, or optionally substituted C5-20aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

Abstract: A material for organic electroluminescence devices comprising a compound having a specific structure and an organic electroluminescence device comprising an organic thin film layer which comprises one layer or a plurality of layers comprising at least a light emitting layer and disposed between a cathode and an anode, wherein at least one layer in the organic thin film layer comprises the material for organic electroluminescence devices, are provided. The material provides the organic electroluminescence device exhibiting a great efficiency of light emission, having no defect pixels, exhibiting excellent heat resistance and having a long life.

Abstract: The invention relates to compounds of formula (I), wherein a, b, c, d, e, R1, R2, A1, A2, A3, A4, Y1, Y2, Y3, Z1, Z2, Z3, Z4 and are such as defined in claim 1, to a method for the production thereof, intermediates for the production and the thereof in the form of components in liquid crystalline media and to electrooptic display elements containing said liquid crystalline media.

Abstract: 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 3?-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, metabolic bone diseases, osteomalacia, osteopenia, secondary hyperparathyroidism, psoriasis, or other skin diseases.

Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.

Abstract: The present invention relates to modulators of metalloproteinase activity.

Abstract: 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 1?-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, secondary hyperparathyroidism, psoriasis, or other skin diseases.

Abstract: A compound represented by formula (1) or a salt thereof, and an antioxidant drug containing the compound or the salt as an active ingredient, are provided. The compound or salt exhibits effective antioxidant activity in treating ischemic organ disorders and diseases caused by oxidative cell damage, and in inhibiting retinal lesions caused by oxidation due to the effects of light.

Abstract: The present invention is directed to a method for ?N-methylation of amino acids suitable for on-resin methylation, compatible with Fmoc/tBu SPPS, and compatible with amino acids bearing protected or unprotected nucleophilic side-chains, notably Arg(Pbf), Met, Cys, and Trp. The present invention is further directed to a compound of Formula I wherein m, n, X and Y are defined as described herein.

Abstract: The present patent application is directed to novel fluoroethyl urea compounds and compositions and their therapeutic use in the treatment of pain and other conditions.

Abstract: Certain novel (dihalopropenyl)phenylalkyl substituted benzodioxolane and benzodioxane derivatives have provided unexpected insecticidal activity. These compounds are represented by formula I: where R through R10, inclusively, x, A, B, y, D, E, G and M are fully described herein. Preferred compounds of the present invention are those wherein the benzofused ring moiety is attached to the remainder of the molecule at the positions designated as 1- or 2-. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.

Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzofuran compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.

Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.

Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.

Abstract: To provide highly safe therapeutic or preventive agents for hyperuricemia, more specifically uricosuric agents, which have potent uricosuric effect and do not cause grave hepatic disorder. Medicinal compositions for the treatment or prevention of hyperuricemia or diseases caused by hyperuricemia, which contain 6-hydroxybenzbromarone or salts thereof, and pharmaceutically acceptable carriers; uricosuric agents, xanthine oxidase inhibitors, and inhibitors against the uptake of uric acid in kidney, which contain 6-hydroxybenzbromarone or salts thereof; and a process for the production of 6-hydroxybenzbromarone.

Abstract: Various divalent ligands based on khellinone derivatives are described. These derivatives can be useful in the modulation of potassium channel activity in cells, including among others Kv1.3 channels found in T-cells. The compounds may also be useful in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis.

Abstract: The invention comprises compounds of Formula 1: wherein, R1 is independently H or halogen; R2 is, for example, H or —R10—NR11R12, and wherein R10 is C1-C6 alkyl, and R11 and R12 are independently H, C1-C4 alkyl, and hydrates, solvates, salts and tautomers thereof. The invention further comprises methods for making the compounds of the invention and methods for making compounds useful in the treatment or prevention of cardiac arrhythmia from the compounds of the invention.

Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.

Abstract: The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1. These compounds may be used in the treatment of pathologies associated with insulin resistane syndrome.

Abstract: A cannabinoid receptor modulator containing a compound represented by Formula (I0) wherein, X is an oxygen atom, etc., R0 is an optionally substituted acylamino group, ring A0 is a benzene ring which may further have a substituent in addition to R0, and ring B is an optionally substituted 5-membered heterocycle, or a salt thereof or a prodrug thereof.

Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

Abstract: The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Disclosed herein are carbonyl compounds of Formula I as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.

Abstract: The invention is directed to heterocyclic indene derivatives useful for ?-amyloid plaque imaging, their radiolabeled compounds and their preparation methods. The compounds of the invention are easily labeled with radioisotopes and have high affinities to ?-amyloid depositions, thus they facilitate diagnosis of Alzheimer's disease by imaging the distribution of ?-amyloid depositions.

Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.

Abstract: The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which at least one of the groups Z1, Z2, Z3 is selected from —O—, —S—, —NH—, —N(—CH3)—, whereas the other groups Z1, Z2, Z3 have the meaning of a —CH2— group, and in which Ar is an aromatic group.

Abstract: A practical and efficient method for halogenation of activated carbon atoms using readily available N-haloimides and a Lewis acid catalyst has been disclosed. This methodology is applicable to a range of compounds and any halogen atom can be directly introduced to the substrate. The mild reaction conditions, easy workup procedure and simple operation make this method valuable from both an environmental and preparative point of view.

Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.

Abstract: Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.

Abstract: The invention relates to compounds of Formula (1) for use in modulating potassium channel activity in cells.

Abstract: The invention relates to novel heterocycles of formula (I), processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.

Abstract: A method for acylation of an aromatic compound, comprising reacting an aromatic compound and an acylating agent of the carboxylic acid type, in the presence of a Lewis acid and of a silylated reagent selected from the group consisting of halosilanes and halosiloxanes.

Abstract: An object is to provide a pyrene based compound that is good in both properties of light emission and mobility when the compound is used as a light emitting transistor element; and a light emitting transistor element wherein this specific pyrene based compound is used. A pyrene based compound represented by the following chemical formula (1) is used as a main component of a light emitting layer in a light emitting transistor element: (wherein R1 represents a group selected from a heteroaryl group which may have a substituent, an aryl group which may have a substituent except a phenyl group which does not have any substituent, an alkyl group which may have a substituent and has a main chain having 1 to 20 carbon atoms, an alkenyl group which may have a substituent, an alkynyl group which may have a substituent, a silyl group which may have a substituent, and a halogen atom.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

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: Chiral ruthenium catalysts comprising salen and alkenyl ligands are provided for stereoselective cyclopropanation, and methods of cyclopropanation are provided. The chiral ruthenium catalyst is prepared in situ by combining an alkenyl ligand, a deprotonated chiral salen ligand, and a ruthenium (II) metal. A preferred catalyst is prepared in situ by combining 2,3-dihydro-4-venylbenzofuran, deprotonated 1,2-cyclohexanediamino-N,N?-bis(3,5-di-t-butyl-salicylidene) and RuCl2(p-cymene)]2.

Abstract: Provided are an organic light-emitting compound represented by Formula 1 and an organic electroluminescent (EL) device using the same: The organic light-emitting compound has thermostability and photochemical stability in addition to superior electrical features. The organic EL device using the organic light-emitting compound has low driving voltage, high efficiency, and superior color purity.

Abstract: Dibenzo[b]perhydroheterocyclic amine compounds have shown to be particularly useful as stabilizers. The compounds may serve as antioxidants, antiozoants, heat stabilizers and ultraviolet light stabilizers and such compounds are oil soluble, thus particularly suited for use as an antioxidant in a lubricating oil composition.

Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.

Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.

Abstract: The present invention relates to the novel isolated 12–30 strain of Pestalotiopsis microspora capable of producing novel antioxidant and antimycotic agents. The present invention also relates to the novel isolated 3,5,7 trisubstituted isobenzofuranone and derivatives thereof, methods of isolating the novel isobenzofuranone from cultures P. microspora 12–30, and to novel uses of the compound as an antioxidant and antimycotic agent. The present invention further relates to a novel 1,5,7 trisubstituted 1,3-dihydroisobenzofuran and derivatives thereof, methods of isolating this novel compound from cultures of Pestalotiopsis microspora 12–30, and to uses thereof.

Abstract: A process for the preparation of prostaglandin compounds having the formula (I): wherein A is selected from the group consisting of C1–C6 alkyl groups; C7–C16 aralkyl groups wherein an aryl portion thereof is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; and (CH2)nOR? wherein n is an integer from 1 to 3 and R? represents a C6–C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; B is selected from OR? and NHR? wherein R? is C1–C6 alkyl groups; and represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.