Abstract: A compound of the formula (I): wherein R1 represents an amino group which may be substituted; R2 represents a carboxy group which may be esterified or amidated; R3, R4, R5 and R6 each represent a hydroxy group which may be protected; Q represents an aryl group which may be substituted; or a salt thereof is disclosed. The compound (I) possesses ant-Helicobacter pylori activity, and is useful in the prevention or treatment of various diseases associated with Helicobacter bacteria, such as duodenal ulcer, gastric ulcer, chronic gastritis and cancer of the stomach.

Abstract: Described is a composition which is suitable for removing adhering substances, such as (synthetic) resins, paint lacquers, polymer foams and mastics by means of forming a dispersion. The composition comprises at least one amphoteric compound and optionally a surfactant substance.

Abstract: The present invention relates to compositions and methods of preparing amino acid chelates that are electrically neutral and free of interfering ions. The composition is prepared by reacting in an aqueous solution a calcium oxide and/or hydroxide, an amino acid, and a soluble metal sulfate salt at a ratio sufficient to allow substantially all of the ions present in solution to react forming a metal amino acid chelate and an essentially inert calcium sulfate, and wherein the metal amino acid chelate has a ligand to metal molar ratio from 2:1 to 3:1.

Abstract: Compounds of the formula I as defined, and their pharmaceutically acceptable salts are VLA-4 antagonists which are useful in inhibiting cell adhesion and in the therapeutic or prophylactic treatment of inflammatory and autoimmune diseases, particularly inflammatory airways diseases. They are particularly useful in reducing post-surgical inflammation, especially that resulting from transplant surgery.

Abstract: A compound of formula wherein the substituents are defined as in the specification and salts or hydrates thereof is disclosed as well as a method of treating disorders associated with the inactivation or excessive degradation of cholecystokinin.

Abstract: A method is described for producing saturated dicarboxylic acids with a chain length of C6 to C21 or the corresponding diamidic dicarboxylic acids from fatty acid cleavage of unsaturated fatty acids or the bis-fatty acid diamides of these unsaturated fatty acids by oxidative ozonolysis and subsequent separation and purification of the dicarboxylic acids, whereby after oxidative ozonolysis, the reaction products are dissolved at a high temperature in a carboxylic acid or a mixture of several carboxylic acids with a medium chain length of C6 to C12 or esters of short-chain alcohols of these carboxylic acids as the recrystallization solvent.

Abstract: The present invention provides a method and composition for treating or preventing pathogenic effects in a mammal caused by intracellular calcium overload, comprising administering to a mammal a mixture of sodium co-transport dependent amino carboxylic acids or their physiologically acceptable salts in an amount sufficient to substantially saturate sodium-dependent amino carboxylic acid transport mechanisms of a cell's plasma membranes. Administration of these amino carboxylic acids can advantageously treat or prevent cell lysis and irreversible cell damage caused by intracellular calcium overload, especially in mammals suffering from a disease condition associated with or resulting from insufficient tissue oxygenation.

Abstract: The present invention provides illudin analogs of the general formula (I): where R1 is (CH2)n—X—Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7 membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2 (C1-C4)alkyl, O—(C5-C12)aryl or —S—(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).

Abstract: This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral bidentate phosphine ligands with cyclic ring structures which could be used to restrict conformational flexibility of the ligands and thus the efficiency of chiral transfer can be enhanced through the ligand rigidity.

Abstract: Disclosed is a process for the oxidation of sulfonamides to sulfonyl imines using chromium (IV) dioxide as the oxidant.

Abstract: This invention is directed to a process for making a salt of a carboxylic acid. The process comprises contacting a catalyst with an alkaline mixture comprising a primary alcohol. In one embodiment, for example, the catalyst comprises a metal support (preferably a metal sponge support) coated with copper. The support comprises at least about 10% (by weight) non-copper metal, and the copper-containing coating comprises from about 0.005 to about 0.5 grams of copper (per gram of said metal support). In another embodiment, the catalyst comprises a metal support (preferably a metal sponge support) coated with silver. The support comprises at least about 10% (by weight) non-silver metal, and the silver-containing coating comprises from about 0.005 to about 0.5 grams of copper (per gram of said metal support). In another embodiment, the catalyst comprises at least about 15% (by weight) non-copper metal, and at least about 10% (by weight) copper.

Abstract: Treatment of the anxiety disorders and insomnia in humans may be accomplished by administering gabapentin in an effective amount.

Abstract: A process for making 6-aminocaproic acid by hydroformylating 3-pentenenitrile to produce 3-, 4-, and 5-formylvaleronitrile (FVN mixture), oxidizing the FVN mixture to produce 3-, 4-, and 5-cyanovaleric acid; hydrogenating the resulting product to produce 6-aminocaproic acid, 5-amino-4-methylvaleric acid, and 4-amino-3-ethylbutyric acid; and isolating 6-aminocaproic acid from the reaction product. The resulting 6-aminocaproic acid can be cyclized to produce caprolactam.

Abstract: An improved process for the preparation of non-hygroscopic salts of L(−)-carnitine, in which the characterizing step comprises heating a mixture comprising L(−)-carnitine inner salt and a fumaric acid or tartaric acid.

Abstract: An industrially advantageous method of producing &bgr;-halogeno-&agr;-aminocarboxylic acids is provided. Methods are also provided of producing optically active N-protected-S-phenylcysteines having high optical purity and of intermediates thereof, respectively, in which the above production method is utilized. A method of producing &bgr;-halogeno-&agr;-aminocarboxylic acids or salts thereof is disclosed which comprises halogenating the hydroxyl group of a &bgr;-hydroxy-&agr;-aminocarboxylic acid (in which the basicity of the amino group in &agr;-position is not masked by the presence of a substituent on said amino group) or a salt thereof with an acid with a halogenating agent.

Abstract: A method for the production of polyasparagine is provided wherein the polyasparagine is prepared by ammonolysis of polysuccinimide in liquid ammonia, acting both as a solvent and as a reactant, wherein the polysuccinimide can be any polysuccinimide, such as linear, branched or cross-linked, wherein the polyasparagine produced has high %N content and is neutral as opposed to anionic or cationic.

Abstract: The present invention relates to methods for the synthesis of chiral non-racemic products, e.g., enantiomerically-enriched hemiesters, from prochiral starting materials, e.g., meso anhydrides. The present invention also relates to catalysts for the aforementioned methods, and methods for synthesizing these catalysts.

Abstract: The present inventintion relates to the formation of an amido ester having the formula:

Abstract: Osmium-catalyzed aminohydroxylation reactions are accelerated and expanded in scope by the use of olefinic substrates having ionic groups, either anionic or cationic. The use of ionic groups on olefinic substrates also extends the aminohydroxylatable positions of unsaturations to include &agr;,&bgr;, &bgr;,&ggr;, and &ggr;,&dgr; positions, with respect to such ionic groups. A mechanism for the disclosed acceleration and extension is provided.

Abstract: A composition consisting of the reaction product of a halogenated carboxylic acid, an amine, and optionally a fatty acid. The composition has biocidal properties and enhances pigment dispersibility.

Abstract: This invention is directed to a process for making an iminodiacetic acid compound from a monoethanolamine compound having the following formula: 1

Abstract: Disclosed are prodrugs as follows: (I) a prodrug of the formula where A is a sulfur or a selenium, and R is a mono- di- or oligo-saccharide; (II) a prodrug of the formula where A is sulfur or selenium, R′ is a sugar, or ═O, and the R″ groups are hydrogen, alkyl, alkoxy, carboxy; (III) a conjugate of an antioxidant vitamin and a thiolamine or selenolamine; (IV) a prodrug of the formula where A is sulfur or selenium, and R′ is a sugar, or an alkyl or aryl group, or ═O, and R‡ is an alkoxy, or an amine group; (V) a prodrug of the formula R is COOH or H, and R′ is a sugar or ═O.

Abstract: Process for preparing an aqueous mixture of &egr;-caprolactam and 6-aminocaproic acid and/or 6-aminocaproamide which involves, as the reductive amination step, contacting 5-formylvaleric acid and/or an alkyl 5-formylvalerate in water as solvent with hydrogen and an excess of ammonia in the presence of a ruthenium on carrier, as a catalyst, wherein the carrier is titanium oxide, zirconium oxide, graphite or carbon and the catalyst also contains at least one of the metals of group 8-11, or a compound of these metals. The aqueous mixture can be used to prepare &egr;-caprolactam.

Abstract: The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: Process for producing an optically active ester by reaction of a racemic alcohol with an optically active amino or tartaric acid derivative, a process for producing an optically active alcohol by hydrolysis of the optically active ester, a process for converting an alcohol into a ketone by oxidation, a method for stably storing an optically active ketone, and a new optically active amino acid ester and a new optically active tartaric acid ester.

Abstract: A peptide derivation of the formula (I) or its pharmaceutically acceptable salt or hydrate thereof is disclosed. These compounds have superior ability over thyroid stimulating hormone (TRH) and its derivatives to activate the central nervous system, such as, for example, sustained acetylcholine releasing action, anti-reserpine action and locomotor increment.

Abstract: The invention provides compounds and processes for synthesis of peptide nucleic acids (PNA). The compounds include temporary amino protecting groups that are base-labile, and protection groups for the exocyclic amino function of the nucleotide base that is compatible with the base-labile amino protecting group. Cleavage of an oligomer comprising these compounds from a solid support can be achieved using weak or medium strength acids.

Abstract: R-(−)-carnitine is prepared by (a) conversion of (S)-3-hydroxy-4-butyrolactone [1] to alkyl (S)-4-halogen-3-hydroxy-butyrate [2] by reaction with a linear or branched C1-C7 alcohol (b), substitution of a CN group for the halogen of compound [2] to yield the alkyl ester of (R)-4-cyano-3-hydroxybutyric acid [3], (c) conversion of alkyl ester [3] to yield (R)-4-cyano-3-hydroxybutyramide [4], (d) cyclization of compound [4] to yield (R)-5-(cyanomethyl)-2-oxazolidone [5] via conversion of the amide function to isocyanate, (e) hydrolysis of compound [5] to yield (R)-4-amino-3-hydroxybutyric acid [6], and finally (f) methylation of the amino group of compound [6] to yield the end product (R)-carnitine.

Abstract: Disclosed are a novel process for preparing D-alloisoleucine and an improved process for epimerizing L-isoleucine to prepare D-alloisoleucine. In the former process, (2S, 3S)-tartaric acid derivative of formula I below; wherein R stands for a hydrogen atom, a C1-C3 lower alkyl group, lower alkoxy group, chlorine atom, bromine atom and nitro group; and “n” is a number of 0, 1 and 2; is combined with an epimer mixture of L-isoleucine and D-alloisoleucine in a reaction medium to form a complex of D-alloisoleucine and the compound of formula I. The precipitated complex is decomposed by putting it in an alcohol to isolate D-alloisoleucine. In the latter process, L-isoleucine is suspended in an inert solvent which does not substantially dissolve amino acids, and epimerized in the presence of C1-C5 saturated lower fatty acid and salicylaldehyde.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: R-(−)-carnitine is prepared by (a) conversion of (S)-3-hydroxy-4-butyrolactone [1] to alkyl (S)-4-halogen-3-hydroxy-butyrate [2] by reaction with a linear or branched C1-C7 alcohol (b), substitution of a CN group for the halogen of compound [2] to yield the alkyl ester of (R)-4-cyano-3-hydroxybutyric acid [3], (c) conversion of alkyl ester [3] to yield (R)-4-cyano-3-hydroxybutyramide [4], (d) cyclization of compound [4] to yield (R)-5-(cyanomethyl)-2-oxazolidone [5] via conversion of the amide function to isocyanate, (e) hydrolysis of compound [5] to yield (R)-4-amino-3-hydroxybutyric acid [6], and finally (f) methylation of the amino group of compound [6] to yield the end product (R)-carnitine.

Abstract: A compound Wherein x, y, and z are integers from 0 to 3; and the (poly)ethereal amine is at least one selected from compounds of formula II1 through II5:

Abstract: Methods, compositions, and devices for alleviating the problems of toxic discharge of aldehydes present in waste streams are disclosed. The methods relate to reducing neutralized aldehydes wherein the neutalized aldehydes are formed by treating aldehydes with amino acids and thereinafter are reduced. These reduced, neutralized aldehydes do not revert back to toxic aldehydes, but form amino acids and thus allow waste containing aldehyde to be more environmentally safely disposed.

Abstract: A process for producing N-formylleucine includes reacting leucine with formamide, precipitating the N-formylleucine, once the reaction is complete, at a temperature of approximately 0° to 40° C., by mixing the reaction medium with water and an acid, so that the final pH of the mixture is approximately 2 to 3, wherein the amount of water used in between approximately 1.5 and 5 parts per part by weight of starting formamide.

Abstract: Haloacetoamido, benzoic acid derivatives having anti-tumorigenic activity are inclosed. Examples of the haloacetoamido, benzoic acid derivatives include 3-chloroacetoamido, benzoylurca, 3-bromoacctoamido, benzoylurea, 3-todoacetoamido, benzoylurca, ethyl-3-chloroacetoamido, benzoate, ethyl-3-bromoacetoamido, benzoate and ethyl-3-iodoacetoamido, benzoate. Intermediates for synthesizing the derivatives, along with method of making and using the derivatives, are also provided.

Abstract: A calcium amino acid malic acid chelate complex for fortification of oleagnious foods which is stable, bioavailable, and palatable is disclosed. Further, oleaginous foods fortified with the calcium amino acid malic acid chelate complexes of the present invention are also disclosed. The calcium amino acid malic acid chelate complex is prepared by reacting a calcium source, an amino acid ligand, and malic acid in an aqueous environment.

Abstract: An aminopolycarboxylate is described, which is represented by the following formula (1): 1

Abstract: Water-soluble dodecandioates wherein the cationic moiety is selected from the group comprising the cations of basic aminoacids (e.g. lysine) and choline and orally or parenterally administrable compositions containing same, are disclosed.

Abstract: The present invention discloses the use, in the manufacture of a preventive and therapeutic drug of a brain disease, of a compound represented by formula (1): CH2═CH—CH2—S(O)n—R  (1) [wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside. The drug of the present invention for ameliorating brain diseases, inhibiting reduction of brain neurons and promoting branching of neurites, is useful for the prevention and treatment of brain diseases such as dementia in association with degeneration and sloughing of brain neurons.

Abstract: Disclosed are &agr;-amides of L-amino acids that produce fragrance or attenuate or mask malodor. In particular, threonine amides, glycine amides, serine amides, and alanine amides can be used in the invention. Such &agr;-amides of L-amino acids are useful for generating pleasant fragrances or attenuating or masking malodor upon cleavage of the &agr;-amides of L-amino acids by bacteria in axillae. The &agr;-amides of L-amino acids can be incorporated into skin treatment compositions and personal care products, such as deodorants, body sprays and antiperspirants, and used in methods for producing fragrance or attenuating or masking malodor.

Abstract: A method for the production of a salt of carboxylic acid by catalytic dehydrogenation effected by reacting the corresponding primary alcohol in aqueous solution with an alkaline hydroxide in the present of a copper catalyst, in which, before the catalytic dehydrogenation, the mass of the reagents comprising the said aqueous solution of a primary alcohol is subjected to a deoxygenation stage in order to remove or reduce the level of dissolved molecular oxygen. The deoxygenation stage is preferably carried out by bubbling an inert gas or by adding a reducing agent.

Abstract: Aliphatic primary alcohols, including aliphatic primary alcohols possessing one or more oxygen, nitrogen and/or phosphorus heteroatoms that may be atoms substituting for carbon atoms in the alkyl group or component atoms of substituents on the alkyl group, were converted into salts of carboxylic acids by contacting an alkaline aqueous solution of the primary alcohol with a catalyst comprising cobalt, copper, and at least one of cerium, iron, zinc, and zirconium. Diethanolamine, for example, was converted to sodium iminodiacetate by treatment in an aqueous medium containing sodium hydroxide with a catalyst that was obtained by reducing a mixture of cobalt, copper, and zirconium oxides with hydrogen.

Abstract: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.

Abstract: 1,2-Bis-adducts of stable hindered nitroxide compounds with substituted ethylenes are prepared by reacting two equivalents of nitroxyl compound with an ethylenically unsaturated compound such as styrene or an acrylate ester. These adducts are very effective inhibitors to prevent the premature polymerization of ethylenically unsaturated monomers when such monomers are distilled, processed or stored.

Abstract: Disclosed a process for preparing substantially enantiomerically pure 3-amino-3-cyclopropylpropanoate esters, i.e., esters of 3-amino-3-cyclopropylpropanoic acid (3-cyclopropylalanine esters or 3-CPA esters) by a 5-step process wherein cyclopropanecarboxaldehyde (CPCA) is reacted with malonic acid and a source of ammonia to obtain 3-cyclopropylalanine (3-CPA); esterifying the 3-CPA; contacting the 3-CPA ester with a substantially enantiomerically pure acid selected from tartaric acid, dibenzoyltartaric acid and mandelic acid to obtain a diastereomeric salt of the 3-CPA ester and the acid; recrystallization of the salt to substantial diastereomeric purity; and neutralizing the salt to afford the substantially enantiomerically pure 3-CPA ester.

Abstract: A compound of the formula wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

Abstract: An additive for an admixture of a cement composition, especially, a retarder of a cement composition, capable of exhibiting excellent retardation effect with a smaller addition amount and easily controlling the retardation time by adjusting the addition amount. An admixture of a cement composition, comprising a cement and at least one iminodiacetic acid or salt thereof represented by formula (I): wherein the M groups each independently represents a hydrogen atom, an alkali metal atom, an ammonium group or a substituted ammonium group; Y represents a divalent alkyl group having from 1 to 5 carbon atoms and the divalent alkyl group may be substituted by a hydroxyl group or a COOM group wherein M represents a hydrogen atom, an alkali metal atom, an ammonium group or a substituted ammonium group; and W represents a hydrogen atom, a hydroxyl group or a COOM group wherein M represents a hydrogen atom, an alkali metal atom, an ammonium group or a substituted ammonium group.

Abstract: An optically active 1-phenylethylamine is reacted to a phosphine oxide carboxylic acid of a racemic modification shown by the following general formula (2): and a produced diastereomeric salt is separated using the difference in solubility against a solvent, which is subsequently decomposed by acid, so as to free and separate an optically active phosphine oxide carboxylic acid.

Abstract: Compounds of formula 1 wherein R4 is an ester or thioester group, and R, R1, R2 and R3 are as defined in the specification are inhibitors of rapidly dividing tumour cells.

Abstract: Catalyst for dehydrogenating amino alcohols to aminocarboxylic acids or ethylene glycol (derivatives) to oxycarboxylic acids, said catalyst containing zirconium, copper and possibly an additional metal, whereby the cited metals are precipitated as hydroxides, washed, dried, calcined, and reduced, preparable in that zirconium hydroxide is precipitated from an aqueous zirconium salt solution using a base until a pH of 4 to 10 is attained, the aqueous solution of a copper salt and possibly of an additional salt is added to the zirconium hydroxide suspension, and by adding further base copper hydroxide and possibly the hydroxide of the metal contained in the additional salt is precipitated until a pH of 8 to 14 is attained, the suspension obtained is filtered, washed, dried, calcined in air at 450 to 600.degree. C. for 2 to 4 hours and finally reduced at 200 to 250.degree. C. in a hydrogen stream for 2 to 4 hours.