Abstract: Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.

Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

Abstract: The present invention relates to ?,?-difluoroamines, fluorinating reagents comprising ?,?-difluoroamines and also processes for preparing ?,?-difluoroamines and fluorinating reagents comprising ?,?-difluoroamines.

Abstract: Fluorophores derived from photoactivatable azide-pi-acceptor fluorogens or from a thermal reaction of an azide-pi-acceptor fluorogen with an alkene or alkyne are disclosed. Fluorophores derived from a thermal reaction of an alkyne-pi-acceptor fluorogen with an azide are also disclosed. The fluorophores can readily be activated by light and can be used to label a biomolecule and imaged on a single-molecule level in living cells.

Abstract: The present invention consists on the synthesis of new products for the treatment of the iron chlorosis. These products may have improved properties regarding the currently known treatments. The new products are non-symmetrical ethylene diamino hidroxyphenyl acetic acid derivatives possessing only five coordination sites able to chelate metals.

Abstract: Pyridyldiamido transition metal complexes are disclosed for use in alkene polymerization. The ligands are tridentate with an NNN configuration.

Abstract: This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR7 group; R1 is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy; R2, R3 are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy; R4 is hydrogen, C1-C8 alkyl; R5, R6 are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl; R7 is hydrogen or straight or branched C1-C3 alkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodiu

Abstract: The present invention relates to novel organic electroluminescent compounds, and organic electroluminescent devices employing the same in an electroluminescent layer. Specifically, the organic electroluminescent compounds according to the invention are characterized in that they are represented by Chemical Formula (1) or Chemical Formula (2): provided that the total number of carbons in R1 or R2 is from 21 to 60. Since the organic electroluminescent compounds according to the invention have good luminous efficiency and excellent life property of material, organic electroluminescent devices having high color purity and luminance with very good operation life can be manufactured therefrom.

Abstract: Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.

Abstract: Triphenylamine derivatives useful as fluorophores in biology, in particular for two-photon microscopy; and compositions comprising these derivatives, to the use of these compositions and of the derivatives themselves for labelling biological molecules (or “biomolecules”) such as nucleic acids, oligonucleotides, proteins, polypeptides, plasmids, and the like, for their examination in particular by two-photon microscopy, and to biomolecules labelled with the said derivatives.

Abstract: Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.

Abstract: There is provided an organic photoconductive material that can realize an electrophotographic photoreceptor which is not only excellent in charge transporting ability but also excellent in solubility in a solvent and compatibility with a resin and moreover, which is excellent in both electric properties and durability, and the organic photoconductive material that is useful also as a raw material compound for various types of functional materials. An asymmetric bis-hydroxyenamine compound represented by the following structural formula (1aa) is provided. The compound is allowed to be contained in a charge transporting layer or a surface protective layer of an electrophotographic photoreceptor. This leads realization of the electrophotographic photoreceptor which is excellent in electric properties and durability and can stably form an image of high quality being free of an image defect such as a black spot.

Abstract: A two-photon probe for real-time monitoring of intracellular free zinc ions is provided. The two-photon probe is represented by Formula 1: wherein R is H or OCH3. The two-photon probe has high selectivity for Zn2+ and enables very effective and long-term monitoring of intracellular free Zn2+ present in the deep tissue. Further provided are a method for preparing the two-photon probe and a method for real-time monitoring of intracellular free zinc ions using the two-photon probe.

Abstract: New bicyclic derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.

Abstract: Disclosed is a method for producing a primary amine compound represented by the formula (3): wherein, Ar is as defined below , which is characterized in that a halogen compound represented by the formula (1): wherein, Ar represents an unsubstituted aromatic group such as a phenyl group, a naphthyl group, a pyridyl group, a furyl group, a thienyl group, a pyrrolyl group, an oxazolyl group, an isoxazolyl group or a pyrimidinyl group, or an aromatic group obtained by substituting such an unsubstituted aromatic group with 1-3 substituents; and X represents a halogen atom, ammonia and formaldehyde are reacted with each other, thereby obtaining a hexahydrotriazine compound represented by the formula (2): wherein, Ar is as defined above, and then the thus-obtained hexahydrotriazine compound is decomposed. By this method, a primary amine compound can be commercially advantageously produced by using a low-cost ammonia while suppressing production of a secondary amine as a by-product.

Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.

Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.

Abstract: The present invention relates to a carboxylic acid compound of formula (I): wherein R1 is H, alkyl; m is 2, 3; n is 0-2; R2 is phenyl, naphthyl, benzofuran, benzothiophene; Q is —CH2—O-Cyc1, —CH2-Cyc2, -L-Cyc3; R3a and R3b each independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGE2 receptor, specifically EP3 receptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.

Abstract: This invention relates to compounds which modulate receptors of the 5-HT2 family of receptors, and particularly to compounds which modulate 5-HT2C receptors. Compounds of the invention include agonists and selective agonists for the 5-HT2C receptor Compounds of the invention include selective agonists for the 5-HT2C receptor which exhibit significantly less or no agonist activity on the 5-HT2A receptor and/or the 5-HT2B receptor. Compounds of this invention are those of Formula I and pharmaceutically acceptable salts, esters and solvates (including hydrates) wherein variables are defined in the specification hereof.

Abstract: To provide an agent capable of controlling the degranulation reaction and/or cytokine production of mast cell and the like. The present invention provides an agent for controlling a degranulation reaction and an agent for controlling a cytokine production, comprising a substance capable of controlling an intracellular zinc ion concentration, particularly, a zinc ion, a zinc ion chelator, an agent for controlling the expression and/or function of a zinc ion-requiring protein, or an agent for controlling the expression and/or function of a zinc ion transporter, as an active ingredient.

Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.

Abstract: Substituted urea compounds useful in the treatment of diseases and C1-3alkyleneOR3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X1 is null, —O—, —S—, —CH2—, or —N(R1)—; X2 is —O—, . -£>. -, or —N(R1)—,—. . Y xs 0 or S; or =y represents two hydrogen atoms attached to a common carbon atom, —W is selected from the group consisting of heteroaryl, aryl, heterocycloalkyl, cycloalkyl, and C1-6alkyl substituted with a heteroaryl. or aryl group; R6 is —C?C—R7 or heteroaryl; R8, R9, and R10, independently, are selected from the group consisting of halo, optionally substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OCP3, CF3, NO2, CN, NC, N(R3)2, OR3, CO2R3, C(O)N (R3)2, C(O)R3, N(R1)COR3, N(R1)C(O)OR3, N(R8)C(O)OR3, N(R1)C(O)C1-3alkyleneC(O)R3, N(R1)C(O)C1 -3alkyleneC(O)OR3, N(R1)C(O)C1-3alkyleneOR3, N(R1)C(O)C1-3alkyleneNHC(O)OR3, N(R1)C(O)C1-3alkyleneSO2.

Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.

Abstract: Compounds useful to control pests are provided.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: New phosphoramide derivatives of formula (I) and the salts and solvates thereof, wherein the meanings of the various substituents are as disclosed in the description. Said compounds are useful as antiinflammatory and analgesic agents.

Abstract: The present invention relates to novel organic electroluminescent compounds, organic electroluminescent devices and organic solar cells comprising the same. Specifically, the organic electroluminescent compounds according to the invention are represented by Chemical Formula (1): wherein, R1 and R2 independently represent hydrogen, deuterium, linear or branched (C1-C20)alkyl, (C2-C20)alkenyl, (C2-C20)alkynyl, (C3-C15)cycloalkyl, tri(C1-C20)alkylsilyl, di(C1-C20)alkyl(C6-C20)arylsilyl, tri(C6-C20)arylsilyl, adamantyl, (C7-C15)bicycloalkyl or (C4-C20)heteroaryl, and the alkyl, alkenyl, alkynyl, cycloalkyl, trialkylsilyl, dialkylarylsilyl, triarylsilyl, adamantyl, bicycloalkyl or heteroaryl of R1 and R2 may be further substituted by one or more substituent(s) selected from deuterium, linear or branched (C1-C20)alkyl, (C1-C20)alkenyl, (C1-C20)alkynyl, halogen, phenyl, fluorenyl, naphthyl and anthryl.

Abstract: The present invention relates to 1-(azolin-2-yl)-amino-2-aryl-1-hetaryl-ethane compounds (I) and 1-(aminothiocarbonylamino)-2-aryl-1-hetaryl-ethane compounds (II) and their salts which are useful for combating animal pest, in particular insects, arachnids and nematodes. Furthermore, the present invention relates to a method for combating animal pests selected from insects, arachnids and nematodes, and to agricultural compositions for combating animal pests. Furthermore, the present invention relates to veterinary compositions for combating animal pests.

Abstract: Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning —X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).

Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.

Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.

Abstract: The invention relates to novel primary amine derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.

Abstract: The present invention provides a compound represented by the formula (I): wherein R1 is a C?1-6#191 alkyl group optionally substituted by a C?3-10#191 cycloalkyl group, R2 is a C?2-6#191 alkyl group, R3 is a hydrogen atom, a C?1-6#191 alkyl group or a halogen atom, and X is —OR6 or —NR4R5 wherein R4 and R6 are each independently a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R5 is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted hydroxy group, or R4 and R5 optionally form, together with the adjacent nitrogen atom, an optionally substituted nitrogen-containing heterocycle, or a salt thereof. The compound of the present invention has a superior peptidase inhibitory action and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: Alternate methods for preparing functionalized pyridyl-amine products from pyridinyl starting materials are provided herein. In addition, these alternately-prepared functionalized pyridyl-amines can be used as ligands or ligand precursors in catalytic compositions, e.g. for use in alkene oligomerization reactions.

Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, R, R1, R2, R3 and n are as defined herein or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.

Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.

Abstract: ?-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R1, R2 and R3 are each independently selected from H, halogen and OH; or R1 and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or I2; R6 is selected from —CO2—C3-4alkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl-1,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-1,2,4-oxadiazol-3-yl, 3-halomethyl-1,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-1,2,3-triazolyl, and 5-methyl-1,2,3-triazolyl; R7 and R8 are each independently Cl or I2; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein “A” is —(NR4)—, —(CR5R6)— or —O—, “B” is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and “X” is oxygen or sulfer respectively.

Abstract: One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

Abstract: The invention provides compounds and methods for treating cell proliferative diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.

Abstract: The invention relates to substituted anthranylalkyl and -cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.

Abstract: The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.

Abstract: Provided are a method of isolating a nucleic acid from a sample and a solid material for isolating the nucleic acid which can be used for the above method. The method includes contacting the sample with a bifunctional material containing an amino group and a carboxyl group at a first pH to bind the nucleic acid to the bifunctional material, the bifunctional material being positively charged at the first pH; and releasing the nucleic acid at a second pH which is higher than the first pH.

Abstract: Process for preparing imine compounds, in which a carbonyl compound is reacted with a primary amine. The imine compound obtained in this way can be reacted further with a metalalkyl and subsequently a carbonyl compound to form an imine compound.

Abstract: Substituted N-oxidanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kaposi's sarcoma, restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g.