Abstract: Compounds of formula (I): wherein R1, R5, R6, R7, Ar, L, A, and Q are as defined in the description, and to salts thereof, to compositions containing them, to the process for preparing them, and to their use as medicinal products, in particular as anticancer agents.

Abstract: The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Abstract: Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like. A compound of the formula (I): wherein a group represented by the formula: is a group represented by the formula: and the like, R1 is carboxy and the like, R3 is —(CH2)n-N(—Y)—SO2—Ar and the like, the other symbols are as defined in claim 1.

Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.

Abstract: Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the tetrahydroindolone derivative or analogue is covalently linked to another moiety to form a bifunctional conjugate are disclosed. More specifically, methods and compositions for treating attention deficit disorder and attention deficit hyperactivity disorders in adults and children as well as mild cognitive impairment and dementia are provided.

Abstract: Provided are crystalline forms of fluvastatin sodium and processes for their preparation.

Abstract: Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole.

Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.

Abstract: The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.

Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: The present invention relates to compounds of the formula I in which R1, R2, R3, R4, X and Y have the meanings indicated in the description. These compounds have immunomodulating effects, as well as an inhibiting or regulating effect on the release of IL-1? and/or TNF-?. They can therefore be used for the treatment of diseases associated with a disturbance of the immune system.

Abstract: Novel ?-type crystal of N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide of the formula: characterized in, for example, that in powder X-ray diffractometry, it has a diffraction peak at a diffraction angle (2?±0.2°) of 18.4°. This crystal has favorable properties, such as high solubility in buffer solutions and various organic solvents, and is suitable to an active ingredient of a pharmaceutical composition for use as an antitumor agent, an activated lymphocyte suppressor or an eating enhancer.

Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.

Abstract: Provided is a condensed ring-containing compound having a condensed dicyclic group having a specific structure and carbazolyl groups and/or indolyl groups, and further provided is an organic electroluminescent device in which an organic thin film layer comprising a single layer or plural layers having at least a light emitting layer is interposed between a cathode and an anode, wherein at least one layer in the above organic thin film layer contains the condensed ring-containing compound described above in the form of a single component or a mixed component, whereby a current efficiency and a heat resistance are high, and a lifetime is very long.

Abstract: The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.

Abstract: Anti-cancer coating compositions comprising 3-hydroxymethyl-5-aziridinyl-1-1-methyl-2-[1H-indole-4,7-dione]propenol (E09) are disclosed. More specifically, the coating compositions comprise EO9 and a formulation vehicle. The formulation vehicle improves the solubility and stability of EO9. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.

Abstract: Aryl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.

Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:

Abstract: The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.

Abstract: Compounds of formula I its stereoisomers, solvates, and salts, thereof, wherein: a, b, c, d, f, n, m and Ra are defined herein are are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.

Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.

Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.

Abstract: The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.

Abstract: The invention relates to an electropolymerizable monomer, intended to be polymerized in aqueous solution, comprising a single electropolymerizable unit and an electron-donating group, characterized in that it also comprises at least one arm ionizable in aqueous solution. The invention also relates to the polymerization process, to the electroactive probe thus obtained and to the method for the detection of a target ligand in a biological sample.

Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.

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 near infrared fluorescent contrast agent comprising a compound having three or more sulfonic acid groups in a molecule, and a method of fluorescence imaging comprising introducing the near infrared fluorescent contrast agent of the present invention into a living body, exposing the body to an excitation light, and detecting near infrared fluorescence from the contrast agent. The near infrared fluorescent contrast agent of the present invention is excited by an excitation light and emits near infrared fluorescence. This infrared fluorescence is superior in transmission through biological tissues. Thus, detection of lesions in the deep part of a living body has been made possible. In addition, the inventive contrast agent is superior in water solubility and low toxic, and therefore, it can be used safely.

Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.

Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.

Abstract: This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.

Abstract: The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production of these compounds, pharmaceutical compositions containing them, and methods of using them for the prevention and/or treatment of various diseases.

Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.

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: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.

Abstract: Compounds of formula (I): are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various CNS disorders.

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune-related diseases and conditions are provided herein. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.

Abstract: Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.

Abstract: A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof.

Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.

Abstract: The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1 is e.g.

Abstract: The invention relates to a group of novel indole compounds of Formula (I): wherein: R1, R2, R4, R6, R6a, R7, R8, R9, R10, and A are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.