Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize unconventional phenol derivatives as cross-coupling partners. Embodiments of the invention can be used to synthesize a variety of useful organic compounds, for example the anti-inflammatory drug flurbiprofen.

Abstract: Embodiments of the present invention are directed to heteroarylamine compounds and organic light-emitting devices including the heteroarylamine compounds. The organic light-emitting devices using the heteroarylamine compounds have high-efficiency, low driving voltages, high luminance and long lifespans.

Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease.

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.

Abstract: A problem of the present invention is to provide an economical process with minimized toxicity for producing an aromatic compound having a variety of substituents such as various alkyl groups, and the problem is solved by a process for production of an aromatic compound represented by formula (1) below, which comprises reacting a compound represented by formula (2) below with an aromatic magnesium reagent represented by formula (3a) below in the presence of an iron catalyst and a diamine compound: wherein R is an optionally substituted hydrocarbon group or a C3-C10 saturated or unsaturated ring group; A is an optionally substituted C4-C20 aromatic group or an optionally substituted heteroaromatic group; X is a halogen atom or a sulfonic acid ester; and Y1 is bromine, iodine, chlorine or a carbanion ligand.

Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.

Abstract: Provided is a novel and excellent method for treating and/or preventing benign prostatic hyperplasia, prostate cancer, and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an indole or benzimidazole derivative, where a nitrogen atom of the indole ring or benzimidazole ring is substituted with a phenyl group substituted with COOH, has a potent selective inhibitory activity against 17?HSD type 5 and may become an agent for treating and/or an agent for preventing a disease associated with 17?HSD type 5, such as benign prostatic hyperplasia, prostate cancer and the like, without accompanying adverse effects due to a decrease in testosterone; and the present invention has thus been completed.

Abstract: The present invention provides a light emitting device material which enables a light emitting device having high efficiency and excellent chromatic purity and durability using a light emitting device material containing a pyrene compound represented by formula (1), wherein any one of R1 to R10 is a group represented by formula (2), or 1 to 4 substituents is/are group(s) represented by formula (3), and a light emitting device using the same.

Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: The present invention provides a compound of the formula: Formula (I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, hypertension, and atherosclerosis, comprising administering to a patient in thereof an effective amount of a compound of Formula I.

Abstract: The present invention is related to tetrahydroindole derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

Abstract: A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.

Abstract: The invention is concerned with novel fused pyrrole derivatives of formula (I) wherein A, Ar, R1, R2, R2? and R2? and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.

Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting form hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. Such methods and reagents may also inhibit the hedgehog pathway in normal cells, e.g., where normal levels of hedgehog signalling are unwanted.

Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: Novel process for statins and its pharmaceutically acceptable salts thereof represented by general formula (I).

Abstract: Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.

Abstract: A 2-arylindole compound substituted in position 5, of formula (I): in which X, Y, Z, W, A, R and R? have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.

Abstract: Disclosed are thiol dyes of formula (1), wherein R1 is hydrogen; C1-C12alkyl; or phenyl-C1-C4alkyl; X is C1-C12alkylene; C2-C12alkenylene; C5-C10cycloalkylene; C5-C10arylene; or C5-C10arylene-C1-C10alkylene; Y is the residue of an organic dye which corresponds to the formula (1a), wherein R2 is hydrogen; or C1-C5alkyl; R3 is a radical of formula (1a1): (1a2); or (1a3); or R2 and R3 together with the linking carbon atom 1C form a 6 to 10 membered carbocyclic ring which may optionally be a condensated aromatic system and may contain one or more than one hetero atom; and R4, R5 and R6 independently form each other are hydrogen, or C1-C5alkyl; Z is H; or a thio ester group of formula (1b), wherein A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and R7, R8 and R9, independently from each other are hydrogen; C1-C12alkyl C6-C12aryl; or C6-C12aryl-C1-C12alkyl.

Abstract: The invention is directed to indoline amide derivatives as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included.

Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, al

Abstract: A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.

Abstract: It is considered that MMP-13 inhibitors contribute to the treatment or prevention against the diseases caused by or related to activity of MMP-13, especially osteoarthritis (OA). Therefore, the development of MMP-13 inhibitors has been desired. A compound represented by the general formula (I): wherein Z is 1,4-phenylene and the like; R1 is hydroxy and the like; R2 is hydrogen atom, optionally substituted lower alkyl, and the like; R12 is hydrogen atom; or R2 and R12 taken together with the adjacent carbon atom may form a ring; R3 is hydrogen atom, optionally substituted lower alkyl, and the like; R4 is halogen, lower alkyl, and the like; m is 0, 1, or 2; X is a bond, —C?C—, and the like; Y is optionally substituted phenyl, optionally substituted naphthyl, and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, L1, L2, M, n, p, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.

Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.

Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as

Abstract: Disclosed are novel compounds having the formula or a physiologically acceptable salt, amide, ester or prodrug thereof. The compounds can be used to modulate (antagonize, agonize) chemokine receptor function. Also disclosed is a method for treating a patient having an inflammatory disease and/or viral infection comprising administering an effective amount of a compound of Formula I. In particular embodiments, the invention is a method for treating a patient infected with HIV.

Abstract: There is provided a compound represented by the general formula (1): wherein Het represents an optional substituted heterocylic group A1 and A2 each independently represent —CH?, etc.; A3 represents —CH2—, etc.; R1 represents a 4-fluorophenyl group, etc.; R2 represents an alkyl group; n represents 0, 1 or 2, provided that when A1 and A2 both are —CH?, A3 represents —CH2— or —SO2—, which is an indole derivative or a mono- or diazaindole derivative that has COX-2 inhibitory activity and is useful as a pharmaceutical, such as an anti-inflammatory agent, or addition salts thereof with a pharmaceutically acceptable acid or base, or hydrates thereof.

Abstract: The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

Abstract: The invention relates to 1-(R1)-2-(R2)-3-(Y-X—NH-A- or Z-A-)-4,5,6,7-R)0.4-indoles, and their acid addition salts where the compounds are basic, wherein A is C1-4 alkylene, X is >CH2, >C?O or >C?S, and the other symbols have various defined values, and to pharmaceutical, skin-protective and cosmetic compositions which comprise them.

Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: 1

Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.

Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: 1

Abstract: A compound of formula (1) or a salt thereof, or a solvate thereof, wherein; R1 and R2 each independently represents C1-6alkoxy or halo; R3 and R4 each independently represents hydrogen, C1-6alkoxy, arylC1-6alkoxy, hydroxy, carboxyC1-6alkoxy, hydroxyC1-6alkoxy, dihydroxyC1-6alkoxy, mono- and di-(C1-6alkyl)aminoC1-6alkoxy or aminoC1-6alkoxy, and; R5 represents —NRsRt wherein Rs and Rt each independently represent hydrogen, unsubstituted or substituted C1-6alkyl, or unsubstituted or substituted heterocyclyl, a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of the compound or composition in medicine.

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R5, R6 or R7 is a group of general Formula B, wherein W is a —CH— group or a nitrogen atom, and the other substituents are as defined herein; 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 methods of preparation thereof.

Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as retinopathies or macular degeneration or other vitreoretinal diseases , inflammatory diseases, vascular leakage syndrome, edema, transplant rejection, adult/acute respiratory distress syndrome (ARDS), and the like.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: 1

Abstract: The object of the invention is a preparation for dyeing fibers, especially hair, which is prepared before use by mixing an acidic component (A1), containing at least an enamine of formula (I) or its acid addition salt of Formula (Ia) with an alkaline component (A2), containing at least one carbonyl compound and at least one primary amine, as well as a method for temporarily dyeing fibers, by means of which the coloration, obtained with the aforementioned dyeing preparation, is removed once again at any later time by a sulfite-containing decolorizing agent.

Abstract: There is provided a compound represented by the general formula (1): wherein Het represents an optionally substituted heterocyclic group; A1 and A2 each independently represent —CH═, etc.; A3 represents —CH2—, etc.; R1 represents a 4-fluorophenyl group, etc.; R2 represents an alkyl group; n represents 0, 1 or 2, provided that when A1 and A2 both are —CH═, A3 represents —CH2— or —SO2—, which is an indole derivative or a mono- or diazaindole derivative that has COX-2 inhibitory activity and is useful as a pharmaceutical, such as an anti-inflammatory agent, or addition salts thereof with a pharmaceutically acceptable acid or base, or hydrates thereof.

Abstract: The object of the present invention is a preparation for coloring fibers, which is prepared before use by mixing an acidic component (A1), containing at least one enamine of Formula (I)/(Ia) with a component (A2), containing a Schiff's base of Formula (II) as well as a method for temporarily coloring fibers, for which the coloration, obtained with the aforementioned coloring agent, can be removed once again at any time by a sulfite-containing decolorizing agent.

Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.

Abstract: An accelerated process for preparing an O-methyl phenol comprising reacting a phenol with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to another aspect, the invention provides an accelerated process for preparing an N-methyl heteroaromatic compound comprising reacting an NH-containing heteroaromatic compound with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to an additional aspect, the invention provides an accelerated process for preparing a methylated aminophenol comprising reacting an aminophenol having at least one N—H with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: The present invention relates to a process for preparing a compound of gonadotropin releasing hormone antagonists having a Formula I, in an efficient way, which involves preparation of key intermediates: 2-arylindole core; a chiral aziridine, in particular chiral nosyl aziridine; and an amine salt. The key process involves the coupling reaction of 2-arylindole and nosyl aziridine under boron trifluoride catalysis, which provides the final compound with unprecedented regioselectivity and enantioselectivity.

Abstract: The present invention comprises a new class of novel aryl and heteroaryl substituted fused pyrrole compounds useful for the prophylaxis and treatment of diseases or conditions, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. In particular, the compounds of the invention are useful for the prophylaxis and treatment of diseases or conditions involving inflammation. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of inflammation and other maladies, such as pain and diabetes, using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Cycloalkano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Abstract: The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.