Abstract: Process for the preparation of amino acid derivatives of the general formula I where R1-R4 are as defined herein, from the corresponding malonic acid monoester amides of the general formula II  by Hofmann degradation using a hypohalite in an aqueously basic medium, which comprises carrying out the reaction in the presence of an alcohol or amine and using the hypohalite in amounts of from 1.0 to 1.5 equivalents and the base in amounts of from 0.8 to 4.0 equivalents per mole of starting material II.

Abstract: A method of preparing carbamates of the general formula RR′—N—CO2—R″ by reacting an amine with carbon dioxide and an organic electrophile in an anhydrous solvent in the presence of a cesium base, whereby carbamate synthesis is accomplished in good yield at mild temperatures, either in solution or on a solid support, and wherein R, R′, and R″ are hydrogen, alkyl of 1-18 carbon atoms, silyl, phenyl, benzyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, allyl, or heterocycle, which are widely used as industrial products, and as intermediates in organic synthesis.

Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds.

Abstract: The present invention provides a compound that includes an active therapeutic agent attached to a blocking moiety that is sensitive to the catalytic action of molecules having retro-aldol and retro-Michael catalytic activity, methods for making such compounds and methods of converting such compounds to active therapeutic agents using molecules having aldolase activity.

Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: Novel herbicidal compounds are provided having the formula (I) 1

Abstract: The present invention relates to a scaleable process for the oxidation of carbon-boron bonds with Oxone®.

Abstract: The invention relates to novel processes for preparing differentially protected lysine derivatives via a novel p-anisaldehyde Schiff base intermediate and the intermediate prepared therein.

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: The invention concerns an isocyanate composition at least partially masked, characterized in that it is masked by at least two agents, one of which at least has a non-carbon carboxylic function. The invention is applicable to organic synthesis.

Abstract: 2,3-Di-substituted trans olefinic N-heteroaromatic or urido propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: A polymeric furanone magenta colorant is disclosed that contains a furanone magenta chromophore having a furanone adduct, the adduct containing at least one alkoxylated phenyl radical, the chromophore further being derived from at least one aromatic aldehyde having a para-nitrogen and containing electron donating groups selected from the group consisting of alkyls, cycloalkyls, and oligomers or polymers derived from alkyleneoxy or aryleneoxy moieties. The colorant can be utilized in resins, waxes and inks.

Abstract: A process for producing (2R, 3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S, 3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S, 3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S, 3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S, 3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound, furthermore treating said compound with an inorganic base. An intermediate for the production of an HIV protease inhibitor can be produced from L-phenylalanine.

Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a &agr;v&bgr;3, &agr;v&bgr;6, &agr;5&bgr;1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: An adhesive paste, free of water, based on a reaction product of a polyisocyanate component and a co-reactant selected from the group consisting of a polyol, a monofunctional fatty derivative component and mixtures thereof, wherein the reaction product contains moisture reactive isocyanate groups.

Abstract: Unique masked isocyanates well suited for formulation into a variety of coating compositions, for example paint powders, are prepared by condensing an isocyanate with a ring-hydroxylated aromatic compound bearing at least one substituent which comprises a carbonyl or nitrile functional group and the apparent melting point of which being at least 30° C.

Abstract: A process for preparing N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride of the following formula (I), is to react N-[1-(S)-ethyoxy carbonyl-3-phenylpropyl]-L-alanine with XCOOR, wherein X is halogen atom, R is C1-C6 alkyl, to obtain a N-alkoxycarbonyl compound, then reacting with an acyl group activation reagent, finally contact with water. The compound of formula (I) is a key intermediate of ACE inhibitors.

Abstract: A phenylacetylene derivative represented by the formula [I]: {wherein X is a halogen atom, a C1-C6 alkyl group, a C2-C6 alkoxy group, a C2-C6 haloalkyl group, etc., n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkynyl group, a C2-C6 alkynyl group, a C1-C6 alkoxy group, etc., A is a C1-C6 alkylene group which may be branched, G is an oxygen atom, a sulfur atom or a —NR3— group; R3 is a hydrogen atom or a C1-C6 alkyl group, and Y is a hydrogen atom, a C1-C10 alkyl group, said group may be substituted by a halogen atom, a hydroxyl group or a C1-C6 alkoxy group], a C2-C6 alkenyl group, etc.; and an agricultural/horticultural fungicide containing the same as the active ingredient.

Abstract: The present invention concerns alkyl esters of &bgr;-amino acid derivatives which are useful in the synthesis of taxol and analogs.

Abstract: The invention provides novel isocyanate-based compounds. Such novel compounds can be used in essentially all applications where conventional isocyanate-based compounds are employed. In other words, the novel isocyanate-based compounds can be used in the making of liquid and powder coating compositions, adhesives, rigid and moldable plastics and foams. The isocyanate-based compounds of the present invention include a polyfunctional isocyanate compound which is at least partially blocked with at least one of the following: a polyhydroxy aromatic compound, or a mixture of a polyhydroxy aromatic compound and a hydroxy-functional ester compound. The present invention further provides compositions which include the aforementioned novel isocyanate-based compound as a component. These compositions can be in the form of liquid coating compositions, powder coating compositions, powder slurry coating compositions, plastic compositions, adhesive compositions, or polymeric foam compositions.

Abstract: The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) 1

Abstract: Carbamates of the formula I where the substituents have the following meanings: Z is methoxy, NH2, NHCH3, N(CH3)2, CH3, C2H5, CF3 or CCl3, X and Y are identical or different and each is hydrogen, F, Cl, Br, CF3, CN, NO2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring, R1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O—CO2-alkyl, A is —O—, —S—, —CR2═CR3—, CHR2—O—, —CHR2—S—, —CHR2—O—N═C(R4)—, —CR2═N—O—, —O—N═C(R4)—, —C≡C—, —CHR2—CHR3—, —CHR2—O—CO—, —O—CHR2— or a single bond, B is substituted or unsubstituted and is alkyl, alke

Abstract: The present invention relates to novel 2-aryl-3-hydroxy-&Dgr;2-cyclopentene-1-one derivatives of the formula (I) in which A, B, D1, D2, G, W, X, Y and Z are each as defined in the description, to processes for their preparation and to their use as herbicides and pesticides.

Abstract: A novel class of tripeptide &agr;-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M1—AA—AA—AA—CO—NR3R4.

Abstract: A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.

Abstract: Phenylcarbamates of the formula I where: R1 is C1-C4-alkyl; R2 is cyano, nitro, trifluoromethyl, halogen, C1-C4-alkyl and C1-C4-alkoxy; m is 0, 1 or 2, where the radicals R2 may be different if m is 2; R3 is hydrogen, cyano, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl; R4, R5 and R6 are each as defined in claim 1, and salts thereof, a process and intermediates for preparing these compounds and compositions comprising them for controlling animal pests and harmful fungi are described.

Abstract: Alternative equilibrium modifiers for use with aldoxime extractants, such as hydroxyl aryl aldoxime extractants, employed in the process for extraction of metal values, particularly copper values, in the extraction from aqueous solutions, in which the extractant and modifiers are employed in an organic solvent phase, the solvent being a water insoluble, water immiscible hydrocarbon solvent, such as a kerosene.

Abstract: The invention concerns a compound of formula (I) in which m is to 0 or 1 Iso is the (poly)isocyanate radical (after elimination of an isocyanate function); R10 is selected among: a negative charge; a hydrocarbon-based radical (i.e. a residue containing hydrogen and carbon atoms) having a carbon as it binding point [i.e. the atom carrying the open bond ]; R11 is selected among: a negative charge. The invention is applicable to organic synthesis.

Abstract: The present invention relates to novel 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) in which A, B, G, X, Y and Z have the meaning given in the description, to processes for their preparation and to intermediates for this purpose. The compounds of the formula (I) are used as pesticides and herbicides.

Abstract: A pharmaceutical composition for inhibiting cysteine protease which comprises a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an acyl group; R.sup.2, R.sup.3 and R.sup.4, same or different, are a bond, an amino acid residue or a group of the formula:--Y--R.sup.5 --in which R.sup.5 is a group resulting from imino group removal from an amino acid residue;Y is --O--, --S-- or --NR.sup.6 -- in which R.sup.6 is a hydrogen atom or a lower alkyl group;A is ##STR2## Z is a hydrogen atom, an acyl group or an optionally substituted hydrocarbon group; n is 1 or 2;provided that when n is 1, then A is ##STR3## and Y is --S-- or --NR.sup.6 --, and, at least one of R.sup.2, R.sup.3 and R.sup.4 is the formula --Y--R.sup.5 --, provided that when further all Y are --NR.sup.6 --, at least one of the amino acid residues is not bound to amhydrogen atom at the .alpha.-carbon thereof but substituted via carbon;provided that when n is 2 and Z is an aldehyde group, then R.sup.

Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.

Abstract: Polymerizable liquid-crystalline compounds of the formula IZ.sup.1 --Y.sup.1 --A.sup.1 --Y.sup.3 --M--Y.sup.4 --A.sup.2 --Y.sup.2 --Z.sup.2 IwhereZ.sup.1 and Z.sup.2 are radicals containing reactive groups via which polymerization can be effected,Y.sup.1 -Y.sup.4 are a single chemical bond, oxygen, sulfur, --O--CO--, --CO--O--, --O--CO--O--, --CO--NR--, --NR--CO--, --O--CO--NR--, --NR--CO--O-- or --NR--CO--NR--, where at least one of the groups Y.sup.3 and Y.sup.4 is --O--CO--O--, --O--CO--NR--, --NR--CO--O-- or --NR--CO--NR--,A.sup.1 and A.sup.2 are spacers having 2 to 30 carbon atoms in which the carbon chain may be interrupted by ether oxygen, thioether sulfur or by nonadjacent imino or C.sub.1 -C.sub.4 -alkylimino groups,M is a mesogenic group,R is C.sub.1 -C.sub.4 -alkyl,and compositions comprising them are distinguished by favorable liquid-crystalline phase-temperature ranges and can be used in optical display devices and in cholesteric liquid-crystalline colorants.

Abstract: The invention relates to chiral ferrocenyls of formula (I) ##STR1## wherein R.sub.a is --P(R.sub.10 R.sub.11) or --SR.sub.12 ;R.sub.b is --P(R'.sub.10 R'.sub.11), --SR'.sub.12, --CH.dbd.NR.sub.12, --CH.sub.2 --NH--R.sub.12 or --CH.sub.2 --O--P(R.sub.10 R.sub.11); and the other substituents are as defined in claim 1,which may be used as ligands for transition metal catalysts in enantioselective reactions.

Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: The patent describes ketobenzamides of the formula ##STR1## where R1, R2, R3, R4, X and n have the meanings given in the description, and their preparation. The novel compounds are useful for controlling disorders.

Abstract: Disclosed is a process for the preparation of N-aryl amine compounds, comprising reacting an amine compound with an arylating compound in the presence of a base and a transition metal catalyst under reaction conditions effective to form an N-aryl amine compound, the transition metal catalyst comprising a Group 8 metal and P(t-Bu).sub.3 as a ligand, and wherein the ratio of the ligand to the Group 8 metal is in the range of about 3:1 to about 0.25:1, and wherein the reaction temperature is less than 100.degree. C. The process of the present invention provides a useful general method of N-arylation for the manufacture of pharmaceuticals, polymers, and the like.

Abstract: Compounds having the formula: ##STR1## wherein R is hydrogen or CO.sub.2 CH(CH.sub.3).sub.2, useful as intermediates in the preparation of the miticide bifenazate, methods for their preparation, and methods for the preparation of bifenazate.

Abstract: This invention relates to the chemical synthesis of N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester using peptide coupling methods. The coupling reaction is conducted by condensation of an activated derivative of novel N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester or by enzymatic coupling of N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester. This invention also relates to novel N-(3,3-dimethylbutyl)-L-aspartic acid, derivatives thereof and the preparation thereof. The activated derivative of N-neohexyl-L-aspartic acid may be an anhydride, mixed anhydride, active ester or an intermediate activated derivative thereof.

Abstract: Carbamates of the formula I where the substituents have the following meanings:Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.

Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: The present invention is directed to a polymeric vehicle, the formulated coating composition and a coating binder made from the polymeric vehicle and a method for making the polymeric vehicle where the polymeric vehicle includes a phenol blocked isocyanate having reactive aliphatic hydroxyl groups. The phenol blocked isocyanate may be made from a phenolic ester alcohol having at least one aliphatic hydroxyl group and one phenolic hydroxyl group.

Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.

Abstract: A process for synthesizing aromatic urethanes, which entails:a) reacting an organic carbonate, in an amount which is equal to or greater than a stoichiometric amount, with an aromatic amine at a temperature of 00 to 190.degree. C.; andb) recovering the aromatic urethane from the reaction mixture, wherein step a) is carried out by maintaining reaction alcohol in an amount of from 10 to 40 mol % based on a total quantity of alcohol coproduced during the reaction.

Abstract: Stabilizer precursors and preformed stabilizers having induced unsaturation, and prepared from low intrinsic unsaturation-containing polyoxyalkylene polyether polyols may be used to form polymer polyols of higher solids content, lower viscosity, and superior filterability and particle size than polymer polyols prepared from stabilizers derived from polyols having higher intrinsic unsaturation, even when the latter are coupled to form high molecular weight stabilizers.

Abstract: The invention provides compounds of formula (I) and (II) wherein X and Y are independently chlorine, bromine, iodine, a mesyl group CH.sub.3 SO.sub.3 or a tosyl group OSO.sub.2 phenyl (wherein phenyl is optionally substituted by 1, 2, 3, 4 or 5 substituents independently selected from C.sub.1-4 alkyl, halogen, cyano or nitro; R.sup.1 and R.sup.2 are independently 1 to 4 optional substituents; Z.sup.1 and Z.sup.2 are each independently --O-- or --NH--; R.sup.3 is hydrogen, t-butyl or allyl; Z.sup.3 is a hydrocarbyl group such as carboxyethyl, optionally containing heteroatoms, and physiologically acceptable derivatives thereof. The compounds can be converted in situ into nitrogen mustard agents by the actions of enzymes such as carboxypeptidase or nitroreductase and are useful for the treatment of cancer.

Abstract: Phenylenediamines represented by general formula (1): ##STR1## wherein R represents an alkyl group or an optionally substituted aralkyl group, X.sup.1 represents a hydrogen atom or a halogen atom, and X.sup.2 represents a halogen atom; salts thereof, and a process for preparing the same. The compounds are useful as intermediates for synthesis of pyridonecarboxylic acid derivatives useful as antibacterial agents.

Abstract: The invention concerns hydrazonoacetic acid amides of general formula (I), a process for producing them, and the use of the said amides as pesticides. In the formula shown, the following meanings apply: A stands for a simple bond or optionally substituted alkylene; Q stands for oxygen or sulphur, R.sup.1 stands for optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl; R.sup.2 stands for hydrogen or optionally substituted alkyl, cycloalkyl, cycloalkenyl, aryl or heterocyclyl; R.sup.3 and R.sup.4 are identical or different and each stand for hydrogen or optionally substituted alkyl or cycloalkyl; R.sup.2 and R.sup.3 together with the nitrogen atom to which they are bound form an optionally substituted heterocyclyl ring; R.sup.5 stands for optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl.