Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.

Abstract: N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.

Abstract: Compounds of the formula I: wherein Rx is cyano or bromo; R1 is halo; R2 is C114 C3 alkyl, and pharmaceutically acceptable salts and prodrugs thereof have activity as antiretrovirals.

Abstract: A starting product for the preparation of COX-2 inhibitors, notably the compound 1-(6-methylpyridine-3-yl)-2-[(4-(methylsulfonyl)phenyl]ethanone of the formula (I): A method for making the compound.

Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: The present invention is directed to substituted N?-(arylcarbonyl)-benzhydrazides, N?-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein Ar1, Ar2, and R1–R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: The present invention relates to compounds of formula (I) that are novel VR1 antagonists useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.

Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.

Abstract: Methods are provided for the construction of unsymmetrical biaryl compounds and alkylated aromatic compounds from arylnitriles using a nickel or palladium catalyzed coupling in which the catalyst has at least one phosphine or phosphite ligand.

Abstract: The invention relates to a process for the preparation of a compound of formula (V), according to the following scheme: wherein the various substituants are as defined in the description

Abstract: A process for preparation of heteroaromatic nitrile from the corresponding alkyl pyridine is disclosed. The process comprises contacting the alkyl pyridine with ammonia and an oxygen source in the presence of a catalyst comprising an active component comprising of oxide of vanadium and antimony and a promoter provided on a support.

Abstract: Compounds of formula (I), wherein the substituents R1, R2, R3, R4 and Z and the suffixes n and m are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomers of those compounds are suitable for use as herbicides.

Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.

Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.

Abstract: There are provided novel compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease, CNS disorders and pain.

Abstract: The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.

Abstract: The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Ar′ and Ar are independently optionally substituted aryl or optionally substituted heteroaryl, provided that the ring structure of said optionally substituted heteroaryl comprises not more than two nitrogen atoms; and R11 is hydrogen; or alkyl, cycloalkyl, aryl or heteroaryl, each of which is optionally substituted. The present invention also relates to the discovery that compounds having Formula V are activators of caspases and inducers of apoptosis. Therefore, the compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: A process for the manufacture of an improved vanadium antimony oxide oxidation or ammoxidation catalyst which comprises heat treating the catalyst at a temperature above 780° C. in the presence of an oxygen enriched environment. Such catalysts are useful in processes for the ammoxidation of a C3-C5 paraffinic hydrocarbon to its corresponding &agr;-&bgr;-unsaturated nitrile, the ammoxidation of propylene with NH3 and oxygen to acrylonitrile, the ammoxidation of methylpyridine with NH3 and oxygen to make cyanopyridine, the ammoxidation of m-xylene with NH3 and oxygen to make isophthalonitrile, and the oxidation of o-xylene to make phthalic anhydride.

Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.

Abstract: The invention relates to a process for the preparation of aromatic nitriles form halogenoaromatics or aryl perfluorosulfonates and alkali metal cyanides in the presence of palladium catalysts, zinc, and polyethers.

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

Abstract: The invention concerns a method for hydrocyanation of ethylenically unsaturated organic compounds into compounds comprising at least a nitrile function. More particularly, it concerns a method for hydrocyanation of organic compounds comprising at least a ethylenical bond by reacting hydrogen cyanide, in the presence of a catalytic system comprising a transition metal and an organophosphorus ligand. The organophosphorus ligand is a compound with monophosphanorbornadiene structure. The invention concerns in particular hydrocyanation of butadiene into adiponitrile.

Abstract: The present invention relates to 2-aryl-5-trifluoromethylpyridines of the formula I 1

Abstract: The invention relates to a process for the preparation of a compound of formula (I): wherein Y and n are as defined in the description.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.

Abstract: The compound of the formula 1

Abstract: The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I): 1

Abstract: A reactor for producing a nitrile compound from a carbon ring or heterocyclic compound having organic substituents by a gas phase reaction using a fluidized catalyst bed with ammonia and a gas containing oxygen. In a cylindrical fluidized catalyst bed having a diameter of 2.0 meters or greater, partial vaporization-type cooling tubes (the cooling medium is partially vaporized in the tubes) and complete vaporization-type cooling tubes (the cooling medium is completely vaporized in the cooling tubes) are disposed in a specific arrangement. Water containing ionic SiO2 in 0.1 ppm or smaller and having an electric conductivity of 5 &mgr;S/cm or smaller is used as the cooling medium for the complete vaporization-type cooling tubes. The temperature of the reaction is easily stabilized and uniform distribution of temperature is obtained in the fluidized catalyst bed. Stable continuous operation is achieved for a long time in a commercial scale apparatus.

Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or solvate of either entity, wherein R4 is a guanidinyl moiety and the other substituents are as defined in the text, are urokinase inhibitors.

Abstract: The present invention relates to a fungicide containing a novel benzoylpyridine derivaitive or its salt. The present invention provides a fungicide containing a benzoylpyridine derivative represented by formula (I) or its salt: wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cyclo(alkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may he esterified or amidated, or at substitutable amino group; n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2 is a substitutable alkyl group, it substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.

Abstract: A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.

Abstract: The invention discloses certain N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

Abstract: Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.

Abstract: The invention relates to novel 2-hetaryl-3,4-dihydro-2H-pyrrole derivatives of the formula (I) in which Hetaryl represents substituted heterocyclyls and Ar represents substituted phenyl, to a plurality of processes for their preparation and to their use as pesticides.

Abstract: A compound of the formula (I), wherein R1 is hydrogen, halogen, carbymoyl, cyano, formuly, or lower alkyl optionally substituted with halogen, amino or a protected amino, R2 is hydrogen, halogen, cyano or lower alkoxy, R3 is phenyl or pyridyl, each of which is substituted with lower alkoxy, and R4 is lower alkoxy; provided that either R1 or R2 is hydrogen, then the other is other than hydrogen, or its salts, which are useful as a medicament.

Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or solvate of either entity, wherein R4 is a guanidinyl moiety and the other substituents are as defined in the text, are urokinase inhibitors.

Abstract: Novel sulphones of formula I are disclosed: 1

Abstract: The invention provides dicarboxylic acid-substituted heteroaryl derivatives of the formula

Abstract: 1

Abstract: Novel agents acting as co-factors for replacement of NAD(P)+/NAD(P)H co-enzyme systems in enzymatic oxido-reductive reactions. Agents mimicking the action of NAD(P)+/NAD(P)H system in enzymatic oxidation/reduction of substrates into reduced or oxidized products. A method for selection and preparation of the mimicking agents for replacement of NAD(P)+/NAD(P)H system and a device comprising co-factors for replacement of NAD(P)+/NAD(P)H system.

Abstract: The invention relates to a process for the preparation of aromatic nitrites from halogenoaromatics or aryl perfluorosulfonates and alkali metal cyanides in the presence of palladium catalysts, zinc, and polyethers.

Abstract: The present invention relates to pharmaceutical compositions comprising and methods of using an N-linked urea or carbamate of a heterocyclic thioester for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance.

Abstract: There is disclosed a genus of compounds and pharmaceutical compositions that are protective for mitigating damage associated with tissue ischemia, particularly stroke (CNS ischemia), and ischemia of the myocardium. The present invention further provides a method for treating tissue damage caused by ischemia. Lastly, the present invention provides a method for treating tissue damage caused by providing a compound that inhibits the cytotoxic activity of 3-aminopropanal.

Abstract: 4-Substituted-3-substituted-amino-cyclobut-3-ene-1,2-diones having the Formula (I): 1

Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.

Abstract: Compounds of general formula (1) are described: 1

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.