Abstract: The present invention provides novel bicyclic compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.

Abstract: One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.

Abstract: Compounds of the formula (I): were synthesized. In at least one embodiment, they were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.

Abstract: The present invention relates to an isoxazoline derivative having the cyclic carboxylic acid hemiketal moiety of formula (1) for use as caspase inhibitor, a process for preparing it, and a pharmaceutical composition comprising it.

Abstract: The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.

Abstract: There are provided a novel benzofluoranthene compound and an organic light-emitting device which uses the benzofluoranthene compound, gives a blue emission hue with extremely good purity, and has an optical output with a high efficiency, a high luminance, and a long life. Specifically, there are provided a benzofluoranthene compound represented by the general formula shown below and an organic light-emitting device including a pair of electrodes including an anode and a cathode one of which is a transparent or translucent electrode material, and an organic compound layer disposed between the pair of electrodes and including a material for an organic light-emitting device containing the benzofluoranthene compound. In the general formula (1), one of X1, X2, X3, X4, X5, and X6 represents a substituted or unsubstituted fused heterocyclic group having four or less rings, and the others of X1, X2, X3, X4, X5, and X6 each represent a hydrogen atom.

Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.

Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.

Abstract: 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds and methods of using these compounds.

Abstract: The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.

Abstract: The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienopyrrole core. In some embodiments, dyes of the present invention are dithienopyrrole dyes having a dithienopyrrole core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.

Abstract: The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienofuran core. In some embodiments, dyes of the present invention are dithienofuran dyes having a dithienofuran core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.

Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.

Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.

Abstract: An organic compound is represented by general formula (1) (where R1 to R14 each independently represent a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, and R11 or R12 represents a substituted or unsubstituted fused polycyclic aromatic group.

Abstract: A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydro

Abstract: A compound of formula (I) Or its salts or pharmaceutically acceptable derivatives thereof wherein; A represents a chemical moiety with the general formula (II): X is selected from a group consisting of CH2, C(?O), CH(R5), C(R5)(R6) or C(R5)(R6)CH2; R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein; and n=1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. The compounds are useful in treating various conditions including arrhythmia.

Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.

Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.

Abstract: A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract: Substituted quinolinones of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one compound of the formula I to act on plants, their seed and/or their habitat.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.

Abstract: The invention provides compounds of formula (I), wherein Y, R, n and X are as defined in the description, a process for their preparation and pharmaceutical compositions containing them. The compounds of formula (I) inhibit the Transient Receptor Potential Vanilloid 1 (TRPV1), which plays a pivotal role in the development of post-inflammatory analgesia, therefore they can be used as analgesic and anti-inflammatory drugs.

Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract: One aspect of the invention relates to 1,8-diarylnaphthalene compounds. In certain embodiments, a compound of the invention is an N-oxide of a 1,8-diarylnaphthalene. In certain embodiments, the aryl group is an optionally substituted acridyl group. In certain embodiments, a compound of the invention is a single steroisomer. In certain embodiments, a compound of the invention is a single enantiomer. Another aspect of the present invention relates to a method of detecting the presence of an analyte in a sample by monitoring the fluorescence of a compound of the invention in a sample. In certain embodiments, the analyte is a metal ion. Another aspect of the present invention relates to a method of determining the enantiomeric purity of an analyte by monitoring the fluorescence of a compound of the invention in the presence of the analyte. In certain embodiments, the analyte is a compound that is capable of hydrogen bonding.

Abstract: Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: To provide an effective and simple process for producing 4-fluoroisoquinoline-5-sulfonylhalide or a salt thereof, and a simple method for separating for purification of the product from a by-produced position isomer thereof. The process for producing 4-fluoroisoquinoline-5-sulfonyl halide or a salt thereof, characterized in that the process includes reacting 4-fluoroisoquinoline or a salt thereof with sulfuric anhydride in the presence or absence of sulfuric acid, to thereby form 4-fluoroisoquinoline-5-sulfonic acid or a salt thereof, and, subsequently, reacting the formed sulfonic acid compound with a halogenating reagent.

Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.

Abstract: The invention relates to tetrahydroisoquinoline sulfonamide compounds (of formula (1) as defined in the specification), their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.

Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.

Abstract: An organic light emitting device having a pyrene based electron transport compound and an electron injecting and transport layer comprising the electron transport compound is provided.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.

Abstract: Compounds having the formula A-R wherein A is a hetereoaryl and R is Ia, Ib or Ic and wherein A, R, R1, R2a, R2b, R2c, R3a, R3b, R4, R5, R6, Ra, Rb, Rc, Rd, X, X1, X2 and n are as are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.

Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R3 and R4 are as defined in the specification.

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formulae: where the substituents are as described herein.

Abstract: The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.

Abstract: Disclosed are novel substituted tetrahydroisoquinoline compounds, pharmaceutical compositions containing the compounds, methods of making the compounds, and methods of using the compounds to destroy a target cell, such as a cancer cell, and to treat or prevent a cancerous condition.

Abstract: Novel trans-1,2-diphenylethylene derivatives are synthesized which can be used to form nanoparticles-monomer-nanomolecule-receptor nanosensors. These trans-1,2-diphenyl-ethylene derivatives are soluble in both water and organic solvents, highly fluorescent and can be synthesized in high yields. The trans-1,2-diphenylethylene derivatives are bonded to a nanoparticle, a nanomolecule bonded to the derivative and a receptor bonded to the nanomolecule to form a nanosensor that can be used to detect chemical and biological agents.

Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels.