Abstract: A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-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: A process for the preparation of 2-(4-methylphenyl)benzoic acid C1-6alkyl esters by reaction of a sulfonic derivative of formula wherein R is C1-6alkyl and R1 is optionally perfluorinated C1-6alkyl or optionally substituted C1-6aryl, with a 4-methylphenylzinc halide.

Abstract: 4-Haloalkylnicotinonitriles having the formula (I) 1

Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.

Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.

Abstract: A process of preparing 4-substituted pyridine compounds via pyridine betaine compounds.

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C4-C20 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino and Y stands for benzylene or phenylene and R2 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, C1-C4 alkyl, hydroxyalkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl, nitro, amino, ca

Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicides.

Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.

Abstract: There is disclosed a process for producing a nitrile compounds by ammoxidation of a carbocyclic or heterocyclic compound having organic substituent(s) by reacting the compound with ammonia and an oxygen-containing gas, wherein unreacted ammonia is recovered from the reaction product gas and recycled to the reaction system.

Abstract: Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.

Abstract: There is disclosed a process for producing a nitrile compounds by ammoxidation of a carbocyclic or heterocyclic compound having organic substituent(s) by reacting the compound with ammonia and an oxygen-containing gas, wherein unreacted ammonia is recovered from the reaction product gas and recycled to the reaction system. In the first process of the present invention, the ammoxidation is conducted by vapor-phase catalytic reaction in the presence of a fluid catalyst containing at least one metal oxide selected from the group consisting of vanadium oxide, molybdenum oxide and iron oxide while controlling a water concentration of a gas fed to a reactor to 12% by volume or lower by adjusting a water content of the recovered ammonia by distillation, thereby avoiding deterioration in activity of the catalyst due to recycle of the recovered ammonia. As a result, it is possible to stably obtain the aimed product at a high yield for a long period of time.

Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,

Abstract: 2-, 3- or 4-arylpyridines are prepared by reacting a halopyridine with an aryl Grignard compound, where the halogen is chlorine or bromine, in the presence of a palladium catalyst of the formula (IV)

Abstract: Pyridine derivatives of the formula I and their salts, their preparation, and their use for controlling animal pests and harmful fungi.

Abstract: Described are processes for the large, commercial scale production of USP grade nicotinamide, wherein the USP grade product is isolated using novel strategies which minimize product waste, and avoid the need for crystallizations and/or ameliorate complications arising in crystallization strategies. Preferred processes involve the processing of nicotinamide reaction crudes over both cation exchange and weak base resins and the subsequent recovery of USP grade nicotinamide by simple evaporation.

Abstract: A process for preparing amidines and their salts with inorganic or organic acids comprises reacting the corresponding nitrile with ammonia, C1-C6-alkylamine or hydrazine in the presence of a mercaptocarboxylic acid and in the presence or absence of an in-organic or organic ammonium salt.

Abstract: The process according to the invention can be illustrated by way of example by the following equation: The monosodium salt of the 3-cyano-2-hydroxy-5-fluoropyrid-6-one (cf. Formula (I)) and/or tautomers thereof are preferably employed in the process according to the invention. The use of a basic catalyst enables significantly lower amounts of chlorinating agent to be employed in the chlorination according to the invention than is necessary, for example, for chlorination of the free dihydroxy compound according to EP-A 333 020. Furthermore, the product 2,6-dichloro-5-fluoronicotinonitrile is obtained in a high purity and high yields after hydrolysis, which is not the case if the conditions according to EP-A 333 020 are applied. Basic catalysts which can be used for the process according to the invention are, for example, organic bases, for example aliphatic and aromatic amines and amides, and also inorganic bases, for example basic compounds of nitrogen and phosphorus and salts thereof.

Abstract: A process for preparing thiopyridines of the formula I where the substituents are as defined in the description.

Abstract: The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I): ##STR1## that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: A process for the production of 3-cyanopyridine by ammoxidation of 2-methyl-1,5-pentanediamine to form 3-cyanopyridine, optionally carried out as an oxidative ammonolysis process.

Abstract: Compounds of formula I, N-oxides or salts, thereof ##STR1## in which q is 0, 1 or 2A is CH and D is N.sup.+ R.times.1/n Q.sup.n- or A is N and D is N.sup.+ R.times.1/n Q.sup.n- or A is CH or N and D is Nor A is N.sup.+ R.times.1/n Q.sup.n- and D is N, R is CR.sup.6 R.sup.7 D.sup.a R.sup.8,Q.sup.n- is an inorganic or organic anion, n being 1, 2, 3 or 4;X is NH, O or S(O).sub.q, (q is 0, 1 or 2); and the R groups have various meanings as defined in the claims are useful pesticidal, especially insecticidal activity.

Abstract: The present invention relates to certain 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medicinal therapy, particularly in the treatment or prophylaxis of glucocorticoid dependent diseases or symptoms.

Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.

Abstract: Pyridylacetic acids of the formula I ##STR1## wherein X is NOCH.sub.3, CHOCH.sub.3 and CHCH.sub.3 ;Y is oxygen or NR.sup.a ;R is cyano, nitro, trifluoromethyl, halogen, alkyl and alkoxy;m is 0, 1 or 2;R.sup.1 is hydrogen or alkyl;R.sup.2, R.sup.3 and R.sup.4 are hydrogen, cyano, nitro, hydroxyl, amino, halogen, unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl and hetaryl, each of which is bonded directly or via --O--, --S-- or --N--,R.sup.4 is furthermore CR.sup.d .dbd.NOR.sup.e ;or a salt thereof, processes and intermediates for their preparation and their use for controlling harmful fungi or pests.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are independently H, C.sub.2 -C.sub.6 acyl or halo-substituted benzoyl; and R.sup.3 is --C(O)O--C.sub.1 -C.sub.6 alkyl, C(O)OH, CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R.sub.2 is acetyl and R.sup.3 is methoxycarbonyl, R.sup.1 is not H; and that when R.sup.3 is CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, R.sup.1 and R.sup.2 are H.The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.The present invention further relates to a process for producing the compounds of the formula (I).

Abstract: This invention relates to a solid catalyst having the following formula for preparing nitrites and its preparation, in particular which contains molybdenum and phosphorus, etc. as main component which can improve the conversion and the selectivity in case of using as a catalyst during the process for preparing a heteroaromatic nitriles.Mo.sub.x P.sub.y O.sub.z X Ywherein,Mo is molybdenum;P is phosphorus;O is oxygen;X is ammonium salt or ion;Y is water; andx,y and z are respectively a number of atom, wherein y/x is 0.01.about.5 and z is 0.01.about.10.

Abstract: The invention relates to new combinations of dihydropyridines of the general formula (I) ##STR1## in which R.sup.1 to R.sup.5 have the meaning indicated in the description, for the prevention and treatment of vascular disorders, in particular of cardiovascular and cerebrovascular disorders, containing dihydropyridines having calcium antagonist activity, acetylsalicylic acid nitroesters and vitamins, and, if appropriate, also further auxiliaries or active compounds.

Abstract: The present invention relates to phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 and [sic] CHCH.sub.2 CH.sub.3 ;R.sup.1 is hydrogen and [sic] C.sub.1 -C.sub.4 -alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, C.sub.1 -C.sub.4 -alkyl and [sic] C.sub.1 -C.sub.4 -alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, C.sub.1 -C.sub.1 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino;R.sup.4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen,R.sup.5 is hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, C.sub.1 -C.sub.10 -alkylcarbonyl, C.sub.2 -C.sub.10 -alkenylcarbonyl, C.sub.3 -C.sub.

Abstract: An ammoxidizable compound is reacted with an ammonium salt, especially an inorganic ammonium salt, in the presence of a source of oxygen and an ammoxidation catalyst at 100 to 700.degree. C., preferably 200 to 700.degree. C., in order to produce cyano compounds of the formula R--CN, in which R is H or an organic group.

Abstract: A pyridine-2,3-dicarboxylic acid diester of the formula Va ##STR1## where the radicals R.sup.2 and R.sup.4 have the meanings set out in the specification and where R.sup.8 is a C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.5 -alkenyl or C.sub.3 -C.sub.5 -alkynyl radical, which may be substituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkoxy.

Abstract: Dyestuffs of the formula whereinD is the radical of a carbo- or heterocyclic diazo component,X represents O, NH, NT, NCOT, NCCH.sub.2 T or NSO.sub.2 T,and the other substituents have the meaning given in the description, are preferably suitable, if m=n=l=o, for dyeing and printing hydrophobic synthetic fiber materials and mixtures thereof with naturally occurring fiber materials.

Abstract: This invention relates to a process for the preparation of highly active and selective ammoxidation catalyst of formula (VO).sub.2 P.sub.2 O.sub.7, TiO.sub.2 or (VO).sub.2 P.sub.2 O.sub.7, Al.sub.2 O.sub.3, which process comprises refluxing a vanadium source in the presence of alcohols; adding a source of phosphorous to form vanadyl pyrophosphate hydrate (VO).sub.2 H.sub.4 P.sub.2 O.sub.9 or (VO).sub.2 P.sub.2 O.sub.7.2H.sub.2 O; Physical mixing of (VO).sub.2 H.sub.4 P.sub.2 O.sub.9 with oxides selected from titania or alumina, and heating the resultant mixture in the presence of air at a temperature in the range of 300-600.degree. C. for a period in the range of 1 to 10 hours; and the use of said ammoxidation catalyst in the preparation of heteroaromatic nitrites.

Abstract: Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Abstract: The present invention provides a process for preparing biaryl compounds comprising reacting an arylmetal reagent selected from arylmagnesium reagents and aryllithium reagents with an arylhalide in the presence of a catalyst system comprising a catalyst selected from nickel catalysts and palladium catalysts and a cocatalyst selected from zinc cocatalysts and cadmium cocatalysts. The present invention specifically provides a process for the preparation of 2-(4'-methylphenyl)benzonitrile comprising reacting a 4-methylphenylmagnesium reagent with a 2-halobenzonitrile in the presence of a catalyst system comprising a catalyst selected from nickel catalysts and palladium catalysts and a zinc cocatalyst.

Abstract: Process for cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates.In a process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates under palladium catalysis in the presence of at least one water-soluble complex ligand, the reaction medium comprises an aqueous and an organic phase and the palladium is added in the form of a palladium compound soluble in the organic phase.Polycyclic aromatic compounds can thus be prepared economically and in very good yields and simultaneously very high purity, in particular without contamination by the complexing ligands.

Abstract: A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II wherein R.sup.1 is selected from hydrido, halo, alkoxy, haloalkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R.sup.2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R.sup.5 and R.sup.6 are one or more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R.sup.5 and R.sup.6 is substituted with alkylsulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.

Abstract: This invention relates to a process for the preparation of highly active and selective ammoxidation catalyst of formula (VO).sub.2 P.sub.2 O.sub.7 ,TiO.sub.2 or (VO).sub.2 P.sub.2 O.sub.7, Al.sub.2 O.sub.3, which process comprises refluxing a vanadium source in the presence of alcohols; adding a source of phosphorous to form vanadyl pyrophosphate hydrate (VO).sub.2 H.sub.4 P.sub.2 O.sub.9 or (VO).sub.2 P.sub.2 O.sub.7.2H.sub.2 O ; Physical mixing of (VO).sub.2 H.sub.4 P.sub.2 O.sub.9 with oxides selected from titania or alumina, and heating the resultant mixture in the presence of air at a temperature in the range of 300-600.degree.C. for a period in the range of 1 to 10 hours; and the use of said ammoxidation catalyst in the preparation of heteroaromatic nitrites.

Abstract: A system provides an oxygen-bearing gas and gaseous reactant stream to a fluidized bed reactor using a sparger to entrain the oxygen-bearing gas into the reactant gas stream. A feed line couples the sparger to the reactor's fluidized bed and introduces the reactant gas stream and entrained oxygen-bearing gas directly into contact with the fluidized bed. A controller controls and maintains both the amount of oxygen-bearing gas and the gaseous reactant above an upper flammability limit, preferably with a safety margin of at least 10%.

Abstract: A method of producing cyanopyridines by means of the catalytic reaction of methylpyridines with ammonia and oxygen at elevated temperature using catalysts consisting of compounds of the elements antimony, vanadium, silicon, titanium and oxygen and compounds of one or more of the alkali metals as well as a method of producing the catalysts and the catalysts themselves.

Abstract: A class of substituted 1,2,3,6-tetrahydropyridine derivatives are disclosed that are ligands for dopamine receptor subtypes within the body. These compounds are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.

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. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention relates to a process for the dehydration of amides to nitrites which comprises carrying out the dehydration in the presence of an adduct of sulphur trioxide and an amine as the dehydrating reagent in a basic reaction mixture. Thereby, for example, aliphatic, aromatic and heteroaromatic amides are dehydrated to the corresponding nitrites, such as 5-carbamoyl-4-methyl-oxazole to 5-cyano-4-methyl-oxazole, a valuable intermediate in the synthesis of pyridoxine.

Abstract: A process for the preparation of nitriles of formula ##STR1## wherein X is CH or N, and R.sub.1 and R.sub.2 are each independently of the other hydrogen, chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, CN, phenyl, phenoxy, dimethylamino, piperidyl, morpholinyl or pyrrolidyl, or R.sub.1 and R.sub.2 together form a fused benzene ring, by reacting an aldehyde of formula ##STR2## with hydroxylaminosulfate in the presence of a tertiary amine base of formula ##STR3## wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen, methyl or ethyl, R.sub.5 is branched C.sub.3 -C.sub.5 alkyl or phenyl, and R.sub.6 and R.sub.7 are methyl or ethyl,in the temperature range from 100.degree. to 160.degree. C., while distilling the released water of reaction off concomittantly at a pressure in the range of 0.02 to 1.5 bar, with subsequent removal of the ammonium salts, and isolating the nitrile so obtained by customary methods.