Abstract: A pyridine derivative exhibiting a photoelectric conversion is represented by formula (I) 1

Abstract: 1,3-Oxazoline and 1,3-thiazoline derivatives, their preparation, and their use as pesticides

Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen substituent or other substituent which undergoes substitution with a diboronic acid ester at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base.

Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.

Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.

Abstract: Electrochromic devices and materials having enhanced daylight stability are described. The materials have a redox center linked to an energy receptor site that may serve to dissipate excited state energy from the redox center, alternatively the receptor site may absorb harmful radiation prior to the absorption by the redox center.

Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.

Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel such as encephalopathies caused by the ischemia in the acute phase after the onset of cerebral infarction, cerebral hemorrhage or the like, Alzheimer's disease, etc.

Abstract: A compound of the following formula:

Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.

Abstract: Compound of formula (I): wherein: n represents 0 or 1, R1 represents hydrogen, arylalkyl, alkyl, acyl, alkoxycarbonyl, arylalkoxycarbonyl or trifluoroacetyl, R2 represents alkyl, X represents oxygen, chlorine, OR3, SR4 or NOR5, R3 represents hydrogen, alkyl, acyl, alkoxycarbonyl or arylalkoxycarbonyl, R4 represents hydrogen, alkyl or aryl, R5 represents hydrogen or optionally substituted alkyl, represents a single or double bond, Ar represents aryl or heteroaryl, its isomers and addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful as facilitators of memory and cognition and antalgic agents.

Abstract: The present invention relates to pharmaceutical compositions comprising a positive modulator of a nicotinic receptor agonist, said positive modulator having the capability to increase the efficacy of the said nicotinic receptor agonist.

Abstract: The selected sequence-directed hydrolysis of RNA under physiologically relevant conditions is described using conjugates comprising metal complexes covalently linked to oligodeoxynucleotides as hydrolysis agents. The oligodeoxynucleotide portions of the agents are selected to provide molecular recognition via the Watson Crick base pairing to the target RNA sequence to be hydrolyzed. A method is described for determining the RNA hydrolysis effectiveness of metals and ligands used to form the metal complexes useful in this invention.

Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: chelators, chelates, antibodies specific for the chelates, tracers comprising chelates conjugated to detectable labels, and immunoassays utilizing the foregoing.

Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i. e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.

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 comprises a process for preparing essentially pure 1,2-dihydro-6-alkyl-2-oxo-5-(pyridinyl)-nicotinonitriles from a crude reaction mixture containing the corresponding amide as an impurity. By "essentially pure" is meant a level of purity acceptable for orally administered pharmaceutical products, usually less than 0.1% of any single impurity. At least a stoichiometric amount of an acylating agent is reacted with the crude reaction mixture, and thereafter recovering essentially pure 1,2-dihydro-6-alkyl-2-oxo 5-(pyridinyl)-nicotinonitrile.

Abstract: The invention relates to a novel labeling reactant, suitable for labeling of a biospecific binding reactant using solid-phase synthesis. The invention further concerns new labeling methods. The novel labeling reactant has the formula (I) ##STR1## wherein -A- is a bivalent aromatic structure capable of absorbing light or energy and transferring the excitation energy to a lanthanide ion after the product made by the said solid-phase synthesis has been released from the used solid support, deprotected and converted to a lanthanide chelate;-G- is a bridge replacing a hydrogen atom in A;R is a protected amino acid residue --CH(NHX)COOH, where X is a transient protecting group, or its active ester, where said ester is e.g. an N-hydroxysuccinimido, p-nitrophenol or pentafluorophenol ester; andR' is --COOR'" where R'" is an alkyl of 1 to 4 carbon atoms, phenyl or benzyl, which phenyl or benzyl can be substituted or unsubstituted.

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: A method for the production of arylamine is described, which comprises allowing an aromatic amine to react with an aromatic halide in the presence of a copper-containing catalyst in a reaction solvent having an ionization potential of from 8.0 to 9.0 eV. According to the method of this invention, an arylamine, in particular a triarylamine or diarylamine, useful as a raw material for use in electronic materials or as an intermediate thereof can be produced with a high purity and in a high yield or at a low cost.

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

Abstract: An improved electrochromic device, the device incorporating an electrochromic medium that comprises at least three electroactive materials having absorption spectra that add together such that the color of the electrochromic medium can be pre-selected by individually choosing the concentrations of the at least three electroactive materials. The electrochromic medium generally maintains the pre-selected perceived color throughout its normal range of voltages when used in an electrochromic device. The at least three electroactive materials include at least one electrochemically reducible material (cathodic material), at least one electrochemically oxidizable material (anodic material) and at least one additional electroactive material which may be either an anodic or cathodic material. Thus, there are always three electroactive materials present in the medium, with at least two either being anodic or cathodic materials.

Abstract: The invention relates to compounds of the formula in which: Y is --CH-- or --N--; R.sub.1 is hydrogen, a halogen or a CF.sub.3, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy group; R.sub.2 is a methyl or ethyl group; R.sub.3 and R.sub.4 are each hydrogen or a (C.sub.1 -C.sub.3)alkyl; and X is:(a) a (C.sub.1 -C.sub.6)alkyl, a (C.sub.1 -C.sub.6)alkoxy, a (C.sub.3 -C.sub.7)carboxyalkyl, a (C.sub.1 -C.sub.4)alkoxy-carbonyl(C.sub.1 -C.sub.6)alkyl, a (C.sub.3 -C.sub.7)carboxyalkoxy or a (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.6)alkoxy;(b) a radical selected from (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkoxy, (C.sub.3 -C.sub.7)-cycloalkylmethyl, (C.sub.3 -C.sub.7)cycloalkylamino and cyclohexenyl, it being possible for said radical to be substituted by a halogen, hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, amino or mono- or di-(C.sub.1 -C.sub.4)-alkylamino; or(c) a group selected from a phenyl, phenoxy, phenylamino, N-(C.sub.1 -C.sub.

Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention describes a family of fluorescent indicators for metal cations. The indicators are fluorophore conjugates of pyridyl-based metal ion chelators. The indicators are very sensitive detection as quantification reagents for a variety of metals, in a variety of oxidation states, even in the presence of high concentrations of Ca.sup.2+, Na.sup.+, or K.sup.+ or other ions, such as is found in seawater, making them highly useful for assaying physiological samples, biological samples, or environmental samples.

Abstract: The invention relates to glutarimides of formula (I): ##STR1## in which Ar represents a phenyl non substituted or substituted one or more times with one of the substitutents selected from a halogen atom, a hydroxyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a (C.sub.1 -C.sub.4)alkyl, said substitutents being identical or different ; a pyridyl group; a thienyl group and X is methylene or ethylene, their salts and their enantiomers, as well as their method of preparation and their use for the preparation of the corresponding 3,3-disubstituted piperidines.

Abstract: The invention provides a complexant compound of formula IR.sup.3 S (CR.sup.1.sub.2).sub.n N(R.sup.2).sub.i (CR.sup.1.sub.2).sub.n X(CR.sup.1.sub.2).sub.n N(R.sup.2).sub.i (CR.sup.1.sub.2).sub.n SR.sup.3(I )(wherein each n, which may be the same or different, is an integer 2, 3 or 4 (preferably 2); each i, which may be the same or different, represents 0 or 1; each R.sup.3, which may be the same or different, is H or a thiol protecting group, preferably a protecting group; X is O, S, N, NR.sup.4 or a substituted phosphorus (eg. oxo substituted phosphorus), preferably S or N; each R.sup.4, which may be the same or different, is hydrogen or an optionally substituted organic group; each R.sup.1, which may be the same or different, is hydrogen or an optionally substituted organic group, or a moiety CR.sup.1.sub.2 may represents a carbonyl group or two, three or four R.sup.

Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.

Abstract: A process for preparing carboxylic acid derivatives of the formula I ##STR1## where X is OR.sup.2 or NH.sub.2,R.sup.1 is C.sub.1 -C.sub.20 -alkyl, C.sub.l -C.sub.20 -hydroxyalkyl, C.sub.3 -C.sub.12 -cycloalkyl, C.sub.4 -C.sub.12 -alkylcycloalkyl, C.sub.4 -C.sub.12 -cycloalkylalkyl, C.sub.5 -C.sub.20 -alkylcycloalkylalkyl, aryl, C.sub.7 -C.sub.20 -aralkyl, C.sub.7 -C.sub.20 -alkylaryl, a heteroaliphatic or heteroaromatic ring with 5 to 8 carbon atoms andR.sup.2 is C.sub.1 -C.sub.20 -alkyl,from carbonitriles of the formula IIR.sup.1 --C.tbd.N (II),where R.sup.1 has the abovementioned meanings, and alcohols of the formula IIIR.sup.2 --OH (III),where R.sup.2 has the abovementioned meanings, at from 50 to 300.degree. C. under from 0.1 to 350 bar in the presence of a heterogeneous catalyst, wherein the reaction is carried out in liquid phase.

Abstract: Substituted cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, serotonergic, antipsychotic, and anxiolytic agents.

Abstract: This invention relates to compositions for benzylidene- and cinnamylidene-anabaseines and methods for using these compositions for treating conditions associated with defects or malfunctioning of nicotinic subtypes brain receptors. These compositions target the alpha7 receptor subtype with little or no activation of the alpha4beta2 or other receptor subtypes.

Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.

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: The present invention relates to cyclic terpyridine-lanthanide complexes having 8 nitrogen atoms and 10 carbon atoms in the macrocycle and containing a functional group in the terpyridine moiety. The invention also relates to a process for the preparation of cyclic terpyridine-lanthanide complexes through the condensation of terpyridine hydrazines with pyridine-2,6-dialdehydes or -ketones. The compounds can be complexed with oligonculeotides and are useful in the sequence-specific cleavage of RNA.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.

Abstract: The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The invention relates to conjugated compounds of general formula (I) ##STR1## wherein X.sub.1 and X.sub.2 are, independently of one another, electron-withdrawing or electron-donating systems, and to a process for the preparation of these compounds.The invention also relates to any material which includes the compounds of general formula I and to the use of said compounds or of any material which includes them in electronic, optoelectronic, nonlinear optical and electrooptical devices.

Abstract: A new class of pyrylium salts and process for the manufacture, as well as the use of the new pyrylium salts as polycondensation components for a new class of polypyridinium salts and a new class of conducting polypyridinium salts manufactured by doping the polypyridinium salts with a conducting dopant is described. The new polypyridinium salts and their conducting doped analogs according to this invention are stable positively charged polymers resistant to base attack and are distinguished by water insolubility making them ideally suited as a metal anti-corrosion coating, stable in basic media making them ideally suited for separation membranes for anions, and as excellent, thermally and chemically stable conducting polymers when doped ideally suited for making electrically conducting materials and as redox catalysts.

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: 1,4-dihydropyridine derivatives and optically active 1,4-dihydropyridine derivatives with the following formula, having vasodilating activity based on calcium antagonism, and PAF antaognism, and methods of producing the same are disclosed: ##STR1## wherein (*) indicates a chiral center in the case of the optically active 1,4-dihydropyridine derivatives.

Abstract: Compounds of the formula (I)R.sup.1 --(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.g --H(I)in which the symbols and indices have the following meanings:R.sup.1 is B or a straight-chain or branched alkyl radical having 1 to 22 carbon atoms (with or without an asymmetrical carbon atom) in which, in addition, it is possible for one or two non-adjacent --CH.sub.2 -- groups to be replaced by --O--, --S--, --CO--, --CO--O--, --O--CO--, --CO--S--, --S--CO--, --O--CO--O--, --CH.dbd.CH--, --C.tbd.C--, .DELTA. or --Si(CH.sub.3).sub.2 --, and in which, in addition, one or more hydrogen atoms of the alkyl radical may be substituted by F, Cl, Br or CN, or is a chiral group, for example an epoxide, a dioxolane or a cyclic lactone,--(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.

Abstract: A process for synthesis of anabaseine using nicotinoyl piperidone salt having the formula ##STR1## wherein R.sub.1 and R.sub.2 are lower alkyl and M is a group I alkaline metal.

Abstract: A metalorganic complex of the formula:MA.sub.y Xwherein:M is a y-valent metal;A is a monodentate or multidentate organic ligand coordinated to M which allows complexing of MA.sub.y with X;y is an integer having a value of 2, 3 or 4; each of the A ligands may be the same or different; andX is a monodentate or multidentate ligand coordinated to M and containing one or more atoms independently selected from the group consisting of atoms of the elements C, N, H, S, O and F.The metal M may be selected from the group consisting of Cu, Ba, Sr, La, Nd, Ce, Pr, Sm, Eu, Th, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Bi, Tl, Y, Pb, Ni, Pd, Pt, Al, Ga, In, Ag, Au, Co, Rh, Ir, Fe, Ru, Sn, Li, Na, K, Rb, Cs, Ca, Mg, Ti, Zr, Hf, V, Nb, Ta, Cr, Mo, and W. A may be selected from the group consisting of .beta.-diketonates and their sulfur and nitrogen analogs, .beta.-ketoesters and their sulfur and nitrogen analogs, cyclopentadienyls, alkyls, perfluoroalkyls, alkoxides, perfluoroalkoxides, and Schiff bases.

Abstract: A compound in metal-free or metal complex form of formula (1) to (3) in which R is hydrogen or C.sub.1-30 alkyl; X is hydrogen, halogen (preferably Cl or Br) or C.sub.1-30 alkyl.

Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula (1), wherein Z1 is oxygen or sulphur, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.

Abstract: A new class of pyrylium salts and process for the manufacture, as well as the use of the new pyrylium salts as polycondensation components for a new class of polypyridinium salts and a new class of conducting polypyridinium salts manufactured by doping the polypyridinium salts with a conducting dopant is described. The new polypyridinium salts and their conducting doped analogs according to this invention are stable positively charged polymers resistant to base attack and are distinguished by water insolubility making them ideally suited as a metal anti-corrosion coating, stable in basic media making them ideally suited for separation membranes for anions, and as excellent, thermally and chemically stable conducting polymers when doped ideally suited for making electrically conducting materials and as redox catalysts.

Abstract: The invention concerns novel anabaseine-related compounds that are useful in treating certain degenerative neural diseases such as Alzheimer's and Parkinson's which apparently involve decreased function of cerebral cortical nicotinic receptors. The compounds showed activity in both in vitro and in active and passive active avoidance studies in animal models. An exemplary active compound is a 3-substituted 2,4-dimethoxy-benzylidene anabaseine.

Abstract: A polymer containing a recurring unit of a conjugated N-fluoropyridinium salt and an active material for a positive electrode, an electrolyte, a battery material for the positive electrode and a battery which use such a polymer. That polymer provides a battery material and a primary battery or a secondary battery which have high electromotive force, high energy density, high environmental acceptability, a low internal resistance in charging and discharging and strong recoverability of the electromotive force, and can be useful as a fluorinating agent.