Abstract: Subject of the invention is a method for the production of a cyanopyridine, comprising the steps of (a) providing a column comprising an absorber section and a stripping section, the absorber section being positioned above the stripping section, such that liquid which passed the absorber section enters the stripping section, (b) feeding a gaseous phase comprising the cyanopyridine into the column, (c) contacting the gaseous phase with an aqueous solution in the absorber section, such that at least a portion of the cyanopyridine is dissolved in the aqueous solution, (d) stripping the aqueous solution obtained from the absorber section in step (c) with a stripping gas in the stripping section, and (e) eluting an aqueous solution comprising the cyanopyridine from the bottom of the column. Another subject of the invention is a device for carrying out the invention.

Abstract: Subject of the invention is a method for the production of a cyanopyridine, wherein (A) a gaseous reaction product comprising the cyanopyridine is produced in a reactor, (B) the gaseous reaction product is quenched with water in a column (2) and a gaseous phase is obtained, which is depleted from at least a portion of the cyanopyridine, (C) the gaseous phase is transferred to a condenser, in which a condensate is obtained, and the gaseous phase is depleted from at least a portion of the water, and (D) the gaseous phase from the condenser is passed through at least one heat exchanger. Another subject of the invention is a device for carrying out the invention.

Abstract: A ?-conjugated aromatic ring-containing compound represented by the formula (1) below is relatively stable and useful as a light-emitting material for light from blue-violet region to red region. [In the formula, R1-R6 independently represent a hydrogen atom or the like; A and D independently represent a pyridine ring, pyrimidine ring, pyridazine ring, pyrazine ring, furan ring, pyrrole ring, pyrazole ring, imidazole ring, thiophene ring, benzothiadiazole ring, thieno[3,4-b]pyrazine ring, furo[3,4-b]pyrazine ring, 6H-pyrrolo[3,4-b]pyrazine ring or the like; a1, a2 and a3 independently represent 0 or 1; and n1 and n2 independently represent an integer of 1-5.

Abstract: The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor.

Abstract: The invention concerns benzamide compounds of Formula (I), wherein R1a, R1b, R1c, R2, R3, R4, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).

Abstract: The invention relates to novel 3,4-dihydropyrimidin-2(1H)-one derivatives having the formula processes for their preparation, and their use in compositions, and in the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract: The invention relates to a facile synthesis of a series of 2-(4?-alkoxyphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): wherein CnH2n+1 is a linear alkyl group having 2-12 carbon atoms. The synthesis of the liquid crystalline 2-(4?-alkoxyphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkoxyphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then, the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4?-alkoxyphenyl)-5-cyanopyridine.

Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.

Abstract: The present invention relates to a Compound of the formula (I), wherein X represents CN, COOR, wherein R represents hydrogen or a carboxyl protecting group, CONR?2, wherein R? represents hydrogen or a carboxyl protecting group, or nitro; R1, R2, R3, R4, R5 independently of each other represent hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; Y represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C7-C13 alkaryl, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; and wherein the stereochemically unspecified double bonds in the above formula (I) represent either the E,E; E,Z; Z,E or Z,Z configuration.

Abstract: The present invention relates to inhibitors of 11-?-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alky groups, and optionally having hydroxyl and/or alkoxyl groups substituents.

Abstract: The invention relates to a method for the manufacture of cyanopyridines from methylpyridines by their conversion with ammonia and oxygen and catalysts suitable therefor which contain further transition metals in addition to vanadium and phosphorus.

Abstract: The present invention relates to liquid-crystalline mixtures and to novel compounds therefor, and to the use thereof in nematic liquid-crystal displays having positive dielectric anisotropy, such as, for example, STN or IPS displays, which are characterised in that they comprise one or more compounds of the formula (I) in which R1, A1, A2, Z1, Z2, n are as defined in claim (1).

Abstract: The invention relates to 2-(pyridin-2-yl)-pyrimidine compounds of general formula (I) and their use for controlling pathogenic fungi and as plant protection products that, as an active constituent, contain compounds of this type: In general formula (I), k represents 0, 1, 2, 3; m represents 0, 1, 2, 3, 4 or 5; n represents 1, 2, 3, 4 or 5; R1, independent of one another, represents halogen, OH, CN, NO2, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, C2-C4 alkenyl, C2-C4 alkynyl, C3-C8 cycloalkyl, C1-C4 alkoxy-C1-C4 alkyl, amino, phenoxy, which is optionally substituted by halogen or C1-C4 alkyl, NHR, NR2, C(Ra)?N—ORb, S(?O)pA1 or C(?O)A2, or two radicals R1 bound to adjacent carbon atoms can, together, also represent a group —O-Alk-O—, wherein Alk represents a linear or branched C1-C4 alkylene, and 1, 2, 3 or 4 hydrogen atoms can also be replaced by halogen; R2 represents C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, hydroxy, halogen, CN or NO2; whereby R2 can also represent

Abstract: A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.

Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: There is provided a process for stereoselectively producing E-form of 3-acyloxyacrylonitrile compound (3) or Z-form which comprises reacting 3-oxopropionitrile compound (1) with an acid chloride (2), characterized in that the reaction is conducted with removal of hydrogen chloride, or by using an organic base or an inorganic base, to thereby regulate the stereostructure of the product; a process for producing the compound (1) characterized by reacting acetonitrile compound (5) with an aromatic ester compound (6) by use of an alkali metal alkoxide in a hydrocarbon solvent while removing alcohol formed as a by-product by azeotropic distillation in a separating tank; and a process for isomerizing E-form of 3-acyloxyacrylonitrile compound to Z-form thereof by use of an organic base.

Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.

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: The present invention relates to a process for preparing optionally substituted aromatic or heteroaromatic nitriles starting from haloaromatics. These are reacted in a copper-catalysed reaction with potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III) in the presence of heteroaromatic amines.

Abstract: The present invention relates to liquid-crystalline mixtures and to novel compounds therefor, and to the use thereof in nematic liquid-crystal displays having positive dielectric anisotropy, such as, for example, STN or IPS displays, which are characterised in that they comprise one or more compounds of the formula (I) in which R1, A1, A2, Z1, Z2, n are as defined in Claim (1).

Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: A process for producing cyano substituted arene boranes is described. The compounds are useful intermediates to pharmaceutical compounds using the cyano group as a reactant.

Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.

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 present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?zHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1 , 2 or 3, or anions selected from the group of [(Rf1SO2)2N]? anions or anions selected from the group of [BFwRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.

Abstract: The present invention provides certain substituted 1,4-dihydropyridine compounds, including pure enantiomeric forms and pharmaceutical formulations thereof. These compounds provide for elevation of ?-MyHC protein levels and ?-MyHC mRNA levels, and most frequently these same compounds provide simultaneous lowering of ?-MyHC protein levels and ?-MyHC mRNA levels. Thus, these compounds may be used alone or in conjunction with other drugs to treat heart failure.

Abstract: The invention relates to a facile synthesis of a series of 2-(4?-alkylphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): wherein Cn is a linear alkyl having 1-12 carbon atoms. The synthesis of the liquid crystalline 2-(4?-alkylphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkylphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4?-alkylphenyl)-5-cyanopyridine.

Abstract: The present invention relates to new compounds of formula (I) wherein R1 to R9, X, p and n are defined as in claim 1, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.

Abstract: The invention relates to a facile synthesis of a series of 2-(4?-alkoxyphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): wherein CnH2n+1 is a linear alkyl group having 2-12 carbon atoms. The synthesis of the liquid crystalline 2-(4?-alkoxyphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkoxyphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then, the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4?-alkoxyphenyl)-5-cyanopyridine.

Abstract: The invention concerns benzamide compounds of Formula (I), wherein R1a, R1b, R1c, R2, R3, R4, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).

Abstract: The invention relates to novel substituted pyridyl ketones of the formula in which A, R, X, Y, Z and n are as defined in the disclosure, to processes for preparing these novel substances, and to their use as crop treatment agents, in particular as herbicides. The invention further relates to novel intermediates of the formulae and to processes for their preparation.

Abstract: The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: To provide a method for producing a 3-substituted 2-chloro-5-fluoro-pyridine or its salt in high yield from a readily available material through a short process under mild reaction conditions using a reagent which is easy for handling and simple in the reaction operation. Namely, a method for producing the following compound (2) or its salt which comprises selectively reducing a chlorine atom at the 6-position of the following compound (1) or its salt, is provided. Further, a method for producing the following compound (4) or its salt which comprises substituting a Z1 group of the following compound (2) or its salt obtained by the reduction reaction, by a Z2 group, is provided. Here, Z1 is —CO2R1, etc., and R1 is a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group. Z2 is a group different from Z1 and is —CO2R5, etc., and R5 is an alkyl group, an alkenyl group, an aryl group, an aralkyl group or a cycloalkyl group.

Abstract: A process is described for catalytically preparing optionally substituted aromatic or heteroaromatic nitrites of the general formula (I) Ar—CN ??(I) by reacting the corresponding aryl halides of the general formula (II) Ar—X ??(II) in which X is chlorine, bromine, iodine, triflate, nonaflate, mesylate or tosylate and Ar is an optionally substituted aromatic or heteroaromatic radical, characterized in that the reaction is performed in the presence of a palladium compound, a phosphine of the general formula (III) or (IV) where R is an alkyl radical and R?, R? and R?? are each an alkyl radical or an aryl radical or heteroaryl radical and A is an alkylene or arylene radical, and potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III), optionally in a solvent and optionally with addition of a base.

Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked sulfonamides of heterocyclic thioesters.

Abstract: The invention relates to a facile synthesis of a series of 2-(4?-alkylphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): wherein Cn is a linear alkyl having 1-12 carbon atoms. The synthesis of the liquid crystalline 2-(4?-alkylphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkylphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4?-alkylphenyl)-5-cyanopyridine.

Abstract: A four-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of the formula: starting from 2-methyl-5-ethylpyridine. 1-(6-Methylpyridin-3yl)-2-[4-(methylsulfonyl)phenyl]ethanone is an intermediate for preparing inhibitors.

Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic esters and amides.

Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.

Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.

Abstract: Disclosed herein is a process for the preparation of a compound of the formula (II): or a salt thereof, wherein X is halogen; each Y, which may be the same or different, is halogen, haloalkyl, alkoxycarbonyl or alkylsulphonyl, and n is 0 to 3; which process comprises treating a compound of the formula (III): with a cyanide source and a catalyst selected from the group consisting of a tetraalkyl ammonium salt and a tetraalkyl phosphonium salt in an aqueous solvent or without solvent, wherein: X is halogen; each Y, which may be the same or different, is halogen, haloalkyl, alkoxycarbonyl or alkylsulphonyl: and n is 0 to 3; and wherein the cyanide source is hydrogen cyanide, an alkali metal cyanide, an alkaline earth metal cyanide or an optionally substituted ammonium cyanide.

Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

Abstract: This invention relates to novel compositions and uses of N-heterocyclic carboxylic acids and carboxylic acid isosteres for treating a vision disorder, improving vision, treating memory impairment or enhancing memory performance in an animal.

Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.

Abstract: There is provided a fluorine-containing resin composition which is used for nonlinear optical material and comprises (I) a fluorine-containing prepolymer and (II) an organic compound exhibiting a second- or higher-order nonlinear optical effect, in which the fluorine-containing prepolymer (I): (1) is a non-crystalline polymer having a fluorine content of not less than 25% and (2) has a carbon-carbon double bond in a polymer side chain or at an end of a polymer trunk chain and also there is provided a nonlinear optical waveguide device produced from the fluorine-containing resin composition. A suitable nonlinear optical material having a stable structure with a nonlinear substance is produced, and an excellent nonlinear optical waveguide device is produced by relatively simple steps while maintaining transparency in a near infrared region.