Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

Abstract: Provided is a method of treating inflammatory bowel disease comprising administering a pharmaceutical composition comprising a 6-aminopyridin-3-ol compound or a pharmaceutically acceptable salt thereof as an active ingredient to a subject, which inhibits colitis in a model of inflammatory bowel disease, and accordingly, they may be suitable for use as a drug for the prevention or treatment of inflammatory bowel disease.

Abstract: A series of substituted 3H-imidazo[4,5-c]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, W and X are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention provides a compound having the structure: wherein R1 is halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5) R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-5 alkyl-aryl, or C1-5 alkyl-NH-aryl; Ar1 is phenyl or thiophene; wherein when Ar1 is phenyl, then R1 is other than —C(?O)—NR5R6, where one of R5 or R6 is phenyl or quinoline and the other of R5 or R6 is hydroxyalkyl, or where one of R5 or R6 is quinoline and the other of R5 or R6 is H; and wherein when Ar1 is phenyl, then R1 is other than —NR5—C(?O)—R6, where one of R5 is H and R6 is quinoline, or a pharmaceutically acceptable salt thereof.

Abstract: A phosphorescent transition metal complex especially suitable as sensor for hydrogen peroxide in cells, in particular in mitochondria in live cells, includes a metallic central atom, which is a transition metal, a first ligand with at least one pyridine ring, and a second ligand having at least one pyridine ring and at least one structural component selected from the group of 1,2-diketone moiety and an arylboronate moiety. A method for preparing the metal complex is also disclosed as well as a method of detecting hydrogen peroxide in cells by incubating cells with the transition metal complex. The metal complex shows advantageous intense and long-lived phosphorescence accompanied by exceptional cellular localization properties. The metal complex is highly photostable and highly selective towards hydrogen peroxide, thus, especially suitable for detecting mitochondrial H2O2.

Abstract: The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.

Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.

Abstract: The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.

Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. Under such circumstances, the development of novel agricultural and horticultural insecticides is desired. The present invention provides an amide compound represented by the general formula (I): (wherein A1, A2 and A3 each represent a nitrogen atom or a CH group, R1 represents an alkyl group, R2 and R4 each represent a haloalkyl groups, R3 represents an alkyl group, and m represents 0, 1 or 2) or a salt thereof; an agricultural and horticultural insecticide and microbicide comprising the compound or a salt thereof as an active ingredient; and a method for using the insecticide and microbicide.

Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5- to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].

Abstract: A compound for an organic photoelectric device is represented by Chemical Formula 1, and an organic photoelectric device, an image sensor, and an electronic device include the same.

Abstract: The present invention discloses oxindole compounds and a single step, one pot reaction for the synthesis of oxindole derivates via a solvent free Passerini reaction of isocyanides, isatins and carboxylic acids.

Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.

Abstract: The present application relates to novel 3-aryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.

Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract: The invention features therapeutic compositions comprising agents useful for the treatment or prevention of pruritis, and methods useful for identifying such agents.