Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.

Abstract: A novel liquid crystalline carbonate and the mixture containing the same: wherein R3 is an alkyl (H2n+1Cn) or an alkenyl (H2n?1Cn) group, each of 1 to 12 carbon atoms, the ring A is laterally unsubstituted benzene or pyridine or pyrimidine or trans-substituted cyclohexane ring, symbol r is 0 to 2; the lateral substituents: X2, X3, X4 and X5 in the benzene rings represent independently hydrogen or fluorine or chlorine atoms, X1 is hydrogen or fluorine atom and simultaneously at least one of the substituents: X2, X3 and X4 is fluorine or chlorine atoms, Y is an alkyl or an alkyloxy or an alkenyl or an alkenyloxy group, each of 1 to 12 carbon atoms or hydrogen or fluorine or chlorine atom or NCS group are described.

Abstract: A renewable adsorbent enabling to adsorb cesium selectively and efficiently, and to reuse cesium by eluting adsorbed cesium, and its manufacturing method are provided. Polyethylene (PE)/polypropylene (PP) based non-woven fabric may be exposed with electron beam, PE/PP based non-woven fabric to which electron beam was exposed is contacted to the monomer solution containing acrylonitrile (AN), dimethyl sulfoxide (DMSO), Tween80 (polyoxyethylene sorbitan monooleate) as a surfactant, and AMP (ammonium molybdophosphate n-hydrate) as an inorganic ion exchanger, and then the inorganic ion exchanger (AMP) is supported directly by the non-ionic graft chain.

Abstract: The present invention provides glucosinolate and isothiocyanate compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents.

Abstract: A novel liquid crystalline carbonate and the mixture containing the same: wherein R3 is an alkyl (H2n+1Cn) or an alkenyl (H2n?1Cn) group, each of 1 to 12 carbon atoms, the ring A is laterally unsubstituted benzene or pyridine or pyrimidine or trans-substituted cyclohexane ring, symbol r is 0 to 2; the lateral substituents: X2, X3, X4 and X5 in the benzene rings represent independently hydrogen or fluorine or chlorine atoms, X1 is hydrogen or fluorine atom and simultaneously at least one of the substituents: X2, X3 and X4 is fluorine or chlorine atoms, Y is an alkyl or an alkyloxy or an alkenyl or an aikenyloxy group, each of 1 to 12 carbon atoms or hydrogen or fluorine or chlorine atom or NCS group are described.

Abstract: The present invention relates to photo-crosslinkable liquid crystal monomers with optical activity. The liquid crystal monomers contains one chiral center with an acrylate group or terminal diacrylate groups, and terminal dibenzene rings are introduced in order to extend its hard segment for the purpose of getting a wider liquid crystalline phase. By introducing the liquid crystal monomers, the room temperature nematic liquid crystal or the cholesteric liquid crystal may have a better mutual solubility and a wider, steadier structure of liquid crystal.

Abstract: Compositions including a comb polymer and an Fe(III)-complexing agent X selected from the group consisting of thiocyanates, condensed phosphates, amines, amino acetic acids, oxycarboxylic acids and compounds of the formula (V). The invention also relates to a method for stabilizing comb polymers in the presence of Fe(III) using such Fe(III)-complexing agents X.

Abstract: A process for producing an essential oil. The essential oil can be white mustard essential oil. The white mustard essential oil can include a moisture sensitive isothiocyanate compound. The moisture sensitive isothiocyanate compound can be 4-HBITC. The essential oil can be produced from mustard seed, which can comprise a precursor sinalbin and myrosinase enzyme. The mustard seed can be reduced into a powder. Activation of the myrosinase enzyme by using a water solvent and a promoter to form a slurry can be performed, wherein the myrosinase enzyme catalyzes the production of an essential oil comprising an isothiocyanate from the sinalbin precursor.

Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.

Abstract: Novel sulfate ester agents and the use of those agents for treating gastroesophageal reflux disease (GERD) are described, exemplary agents being of the formula: wherein X is —OCH2— or —CH2O—; Y is a group pendant from X comprising at least one —OSO3R4 moiety, wherein R4 is H or a pharmaceutically acceptable cation; n is an integer from 1-3; and R1 and R2 are each independently selected from the group consisting of —H, a halogen with an atomic number from 9 to 53, —SO3R4, —NCS, —NCO, —NH(CO)—OR3, —NH(CS)SR3, —NH(C═NH)OR3, —NHCOCH2Cl, —NHCOCH2Br, —NHCO—CH═CH2, —NHC(O)—CF3, wherein R4 is H or a pharmaceutically acceptable cation.

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

Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.

Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.

Abstract: A method for analyzing an objective substance, comprising reacting a labeled probe with an objective substance on a biological sample, said probe comprising a label substance of the formula (I): wherein A1 is an aromatic group, R1 is a hydrogen or —COCH2COCnF2n+1 and n is an integer of 1-6, which is bonded to a probe selected from the group consisting of nucleic acid, nucleic acid binding protein, low molecular ligand and receptor for ligand (except antibody) to give a fluorescent complex, reacting the complex with an objective substance on a biological sample and assaying fluorescence of the resultant fluorescent complex, a labeled nucleic acid probe and a labeled nucleotide. According to the method of the present invention, defects such as hindrance of fluorescence due to contaminant substance, low sensitivity and the like can be resolved, thereby enabling analysis on a tissue.

Abstract: A method for analyzing an objective substance, comprsing reacting a labeled probe with an objective substance on a biological sample, said probe comprsing a label substance of the formula (I): wherein A1 is an aromatic group, R1 is a hydrogen or —COCH2COCnF2n+1 and n is an integer of 1-6, which is bonded to a probe selected from the group consisting of nucleic acid, nudeic acid binding potein, low molecular ligand and receptor for ligand (except antibody) to give a fluorescent complex, reacting the complex with an objective substance on a biolgical sample and assaying fluorescence of the resultant fluorescent complex, a labeled nucleic acid probe and a labeled nucleotide. According to the method of the present invention, defects such as hindrance of fluorescence due to contaminant substance, low sensitivity and the like can be resolved, thereby enabling analysis on a tissue.

Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.

Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.

Abstract: Bis-oxime derivatives of the formula I ##STR1## W is oxygen or sulfur, and the other substituents defined as follows: R.sub.1 =hydrogen, C.sub.1 -C.sub.4 alkyl; cyclopropyl;R.sub.2 =hydrogen, C.sub.1 -C.sub.6 alkyl; halo(C.sub.1 -C.sub.6) alkyl; C.sub.2 -C.sub.6 alkoxyalkyl; C.sub.3 -C.sub.6 cycloalkyl; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; cyano; C.sub.1 -C.sub.6 alkoxycarbonyl; C.sub.1 -C.sub.6 alkyl-S(O).sub.n ; substituted or unsubstituted aryl-S(O).sub.n ; C.sub.1 -C.sub.6 alkoxy; substituted or unsubstituted aryloxy; substituted or unsubstituted heteroaryloxy; unsubstituted or mono- to trimethyl-substituted heterocyclyl; substituted or unsubstituted aryl-C.sub.1 -C.sub.6 alkyl; substituted or unsubstituted heteroaryl-C.sub.1 -C.sub.6 alkyl;R.sub.3 =hydrogen; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl having 1 to 5 halogen atoms; C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.2 -alkyl; unsubstituted or mono- to trihalo-substituted C.sub.1 -C.sub.6 alkenyl; C.sub.

Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.

Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR.sup.4 ; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl; X is halogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, nitro or cyano; and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R.sup.1 is unsubstituted phenyl at least one of R.sup.2 and R.sup.3 is other than hydrogen or methyl.

Abstract: A method for preparing (R)X.sub.m-p A.sub.p by reacting (R)X.sub.m and MA in N-methylpyrrolidone and recovering the by-product MX as a precipitate wherein:X is halide;R contains from 1 to 8 carbon atoms, can be substituted or unsubstituted, and is straight or branched chain alkyl, cycloaliphatic, aralkyl, alkylene, alkenyl, alkenylene, alkynyl or alkynylene with the proviso that X is not attached to a carbon atom having a double bond;A.sup.- is a monovalent anion soft base selected from the group consisting of halide different from X, SCN.sup.-, SH.sup.-, SO.sub.3 H.sup.-, R.sub.2 PO.sub.4.sup.-, PF.sub.6.sup.-, and [SP(Z) (OR.sup.1).sub.2 ].sup.- wherein R.sup.1 is lower alkyl and z i sulfur or oxygen;M is an alkali metal or NH.sub.4.sup.+ ;m is an integer from 1 to 3 with the proviso that m is 1 or 2 when R has one carton; andP is an integer from 1 to m.

Abstract: Process for the introduction of functional or functionalizable substituents para to the amino group in 2-aminophenols and 3-aminophenols. The process proceeds in one step, with substitution occurring selectively at the position para to the amino group. Consequently, the reaction is surprisingly straightforward, with very little or no contamination by isomeric by-products. The process comprises reaction of (a) an aminophenol having an open para position to the amino function, with (b) an unhindered non-enolizable aldehyde, and (c) a thiol or sulfinic acid which acts as a nucleophile. In preferred embodiments, the process is conducted at a temperature of from about 50.degree. C. to about 100.degree. C., and in the presence of a polar solvent. The reaction is promoted by an acid having sufficient acidity to protonate the amino group of the aminophenol. Preferably, the acid promoter is a mineral acid, and it is present in an amount at least substantially equivalent to the amount of aminophenol reactant.

Abstract: This invention is directed to a method for treating helminthiasis in an animal which method comprises administering to an animal in need thereof an anthelmintically effective amount of a compound of the Formula (I): ##STR1## wherein Z is oxygen or sulfur;R.sup.1 is hydrogen or lower alkyl; andR.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen, halo, lower haloalkyl, lower alkoxy, lower haloalkoxy, nitro, cyano, halophenoxy, haloalkylphenoxy, thiocyano or isothiocyano, provided that R.sup.2 and R.sup.3 cannot simultaneously be hydrogen and that R.sup.4 and R.sup.5 cannot simultaneously be hydrogen; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions formulated therewith. This invention is also directed to novel anthelmintically active benzenepropanamides of Formula (I) wherein Z is oxygen.

Abstract: Process for the introduction of functional or functionalizable substituents para to the amino group in 2-aminophenols and 3-aminophenols. The process proceeds in one step, with substitution occurring selectively at the position para to the amino group. Consequently, the reaction is surprisingly straightforward, with very little or no contamination by isomeric by-products. The process comprises reaction of (a) an aminophenol having an open para position to the amino function, with (b) an unhindered non-enolizble aldehyde, and (c) a thiol or sulfinic acid which acts as a nucleophile. In preferred embodiments, the process is conducted at a temperature of from about 50.degree. C. to about 100.degree. C., and in the presence of a polar solvent. The reaction is promoted by an acid having sufficient acidity to protonate the amino group of the aminophenol. Preferably, the acid promoter is a mineral acid, and it is present in an amount at least substantially equivalent to the amount of aminophenol reactant.

Abstract: Acrylates of the general formula ##STR1## where R.sup.1 and R.sup.2 independently of one another are each C.sub.1 -C.sub.8 -alkyl, X is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, haloalkyl, cyano or nitro, W is unsubstituted or alkyl-substituted, saturated or unsaturated C.sub.1 -C.sub.10 -alkylene, Y is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, an unsubstituted or substituted C.sub.4 H.sub.4 chain which is fused to the benzene radical, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, NO.sub.2, ##STR2## where R' and R" independently of one another are each hydrogen, alkyl, alkoxy, alkylthio or cycloalkyl, or are phenyl which is unsubstituted or substituted by alkyl, halogen or alkoxy, m is 0 or 1, n is from 1 to 4 and Z is oxygen, sulfur, SO or SO.sub.2, and fungicides containing them.

Abstract: Process for the preparation of aryloxy-benzoic acids containing a sulphonamide group by the direct reaction of a phenoxy-benzoic acid with a sulphonamide, in the presence of a halogenating agent such as P(O)Cl.sub.3.

Abstract: Disclosed herein are thiocyanopyrimidine derivatives represented by the following general formula: ##STR1## wherein R means an alkyl group having 1-3 carbon atoms and X denotes a halogen atom, their production process, and agricultural and horticultural fungicides containing same as active ingredients. The compounds of this invention can provide ideal agricultural and horticultural fungicides, since they exhibit outstanding fungicidal activities against plant pathogens led by late blight and downy mildew, their toxicity to animals are low and they are not phytotoxic.The compounds of this invention can be obtained by reacting pyrimidine derivatives represented by the following general formula: ##STR2## with thiocyanates while using an organic acid as a solvent. Good results can be obtained particularly when formic acid is used as a solvent.

Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.

Abstract: Chlorophosphines or thiophosphinic acid chlorides of the general formulae RPCl.sub.2, R.sub.2 PCl or R.sub.2 P(.dbd.S)Cl are made from feed materials selected from hydrogen-functional primary or secondary phosphines or secondary phosphine sulfides, where R stands for identical or different, linear or branched, substituted or unsubstituted alkyl radicals having from 1-16 carbon atoms, aryl radicals, aralkyl radicals or alkylaryl radicals having from 6-9 carbon atoms or cycloalkyl radicals having from 5-10 carbon atoms. To this end, the feed materials are reacted with phosphorus pentachloride, or with chlorine gas in the presence of phosphorus trichloride at temperatures within the range -78.degree. to +145.degree. C. It is possible for two radicals R to be linked together by one or two substituted or unsubstituted hydrocarbon chains having from 1-4 carbon atoms.

Abstract: Acrylates of the general formula ##STR1## wherein R.sup.1 and R.sup.2 independently of one another are each C.sub.1 -C.sub.8 -alkyl, X is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, haloalkyl, cyano or nitro, W is unsubstituted or alkyl-substituted, saturated or unsaturated C.sub.1 -C.sub.10 -alkylene, Y is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, an unsubstituted or substituted C.sub.4 H.sub.4 chain fused to the benzene radical, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, NO.sub.2, aralkyloxy, ##STR2## and R' and R" independently of one another are each hydrogen, alkyl, alkoxy, alkylthio or cycloalkyl or are each phenyl which is unsubstituted or substituted by alkyl, halogen or alkoxy, and n is from 1 to 4, and fungicides containing them.

Abstract: There are described compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z is 1H-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation.