Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention relates to a method of preparing a 2-alkylcysteine comprising condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, esterifying the 2-arylthiazoline-4-carboxylic acid using a substituted or unsubstituted alcohol group comprising one or more chiral carbons, and alkylating at the 4-position of the thiazoline ring to form a 2-aryl-4-alkyl-thiazoline-4-carboxylic acid ester. The chiral templates present in the thiazoline carboxylic acid ester can provide face selectivity, and consequently desired stereochemistry, during the delivery of an alkyl group to the 4-position of the thiazoline ring. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring.

Abstract: A process for preparing N,N-Dimethyl Glycine Hydrochloride, comprises treating a chloroacetic acid with aqueous dimethylamine, and then dropping by hydrochloric acid to obtain N,N-dimethyl glycine as well as its hydrochloride salt, wherein decompression process is utilized to assure the product purity and active carbon is employed for cost saving aspect.

Abstract: Dipeptide derived inhibitors of the ?-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A? peptide in a mammal. The compounds of the invention provide useful methods of treatment by administration of these inhibitors to reduce A? peptide formation and in pharmaceutical compositions.

Abstract: A process for producing 4-bromo-2-oxyimino butyric acid, predominantly as the (Z)-isomer of formula (I), wherein R is hydrogen; a linear or branched C1-4 alkyl group; a linear or branched C1-4 alkyl group substituted by a carboxylic acid or an aryl group; a substituted or unsubstituted cyclic alkyl group of 3-6 carbon atoms or a substituted or unsubstituted aryl group. The product is produced by reacting bromine with a 2-(oxyimino)-3-oxo butyric acid derivative of formula (II) wherein R is as defined above and R1 is a tert-butyl group in presence of an organic solvent and in presence of a C1-4 alcohol and acetyl bromide at a temperature ranging from about ?15° C. to about +15° C. Bromine is used in a proportion of about 0.90 to about 1.35 moles per mole of compound (II), preferably 0.90 to 1.10 moles. The acetyl bromide is used in molar proportions of 0.9 to 2 moles per mole of compound (II), preferably 0.9 to 1.5 moles.

Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.

Abstract: The present invention pertains to specific peptides obtainable from cocoa beans and giving rise to a particular and distinct savor when subjected to a Maillard reaction with reducing sugars. In particular, the present invention pertains to the use of one or more of these specific peptides for the preparation of a chocolate flavor, specifically a cocoa and a caramel flavor, a floral or specifically, a bonbon flavor, a bready flavor, a roasted flavor or a meat flavor.

Abstract: A production method of an optically active &bgr;-amino acid represented by the formula (I) 1

Abstract: The present invention is directed to a S-nitrosothiol derivative of penicillamine or glutathione, of formula I: or its pharmaceutically acceptable salt thereof, in which: A and B are independently phenyl groups or together form the group —CH2—Q—CH2—constituting a six membered ring in which Q represents oxygen, sulfur, or a group N—R3, in which R3 is hydrogen or a C1-C4 alkyl group; R1 is an acyl group, which may be an aliphatic C1-C5 acyl group or an acyl group of glutamic acid bonded via its gamma carboxyl group; R2 is a hydroxyl group or a glycine group bonded via a peptide bond; with the proviso that if R1 is an aliphatic acyl group, then R2 is a hydroxyl group, and if R1 is a glutamic acid, then R2 is a glycine group. The compounds have vasodilating activity and inhibit the aggregation of the platelets which make them useful for the treatment of dysfunctions of the circulating system, especially at the cardiovascular level.

Abstract: Fluorinated alkyl compounds may be used as reaction intermediates or reaction products in polymerizing amino acid structures into peptides. Fluorinated methyl groups have been found to be particularly useful. A compound having a fluorinated methyl group such as that set forth below: wherein R is selected from the group consisting of: alkyls, hydrogen, aryls, aromatic compounds, amines, sulfur-containing alkyl groups, sulfur-containing aryl groups, and heterocyclic compounds may be utilized alone, or reacted in combination with other amino acids, to form a dipeptide, or polypeptide.

Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: Compounds of formula I are disclosed 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 tumor cells.

Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds having the following structure: wherein A, B, R, R1, R1′ p and q are as defined herein. The invention is also directed to pharmaceutical compositions containing one or more of these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmnune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: This invention relates to a process for the synthesis and method of use of an effective amount of a 3-hydroxy-3-methylbutyrate (HMB) amino acid salt for the regulation athletic function in humans.

Abstract: A method for preparing a compound of formula I or a salt thereof is disclosed.

Abstract: Process for the preparation of 3-aminoalkanoic acid esters of the general formula: in which R is C1-6-alkyl and R1 is hydrogen, C1-6-alkyl or phenyl, or their salts, by catalytic hydrogenation of the corresponding 3-amino-2-alkenoic acid esters of the general formula: in which R and R1 have the above mentioned meanings. The hydrogenation is carried out in the presence of a strong acid and the salt of the 3-aminoalkanoic acid ester (I) and the strong acid formed is optionally converted into the free 3-aminoalkanoic acid ester (I) or into another salt in a manner known per se.

Abstract: The present invention relates to a method for introducing an amino group into an organic acid or an organic ester by reacting an organic salt or an organic ester and ammonia under high-temperature and high-pressure water conditions, a method for synthesizing an amino acid or an amino ester by the above method, and a method for manufacturing an amino acid compound by synthesizing an amino acid or an amino ester by the above method and separating and refining it with an ion exchange resin.

Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.

Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluorleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbonfluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.

Abstract: Compounds having the formula: are disclosed. M1 and M2 are the same or different and are transition metal atoms or ions; Z2 and Z3, independently, are the atoms necessary to complete a 3-12 membered heterocyclic ring; Z1 is an alkylene or arylene group; Q1 and Q2 are the same or different and are electron withdrawing groups; L1 and L3, taken together, represent —O—CR13—O—; L2 and L4, taken together, represent —O—CR14—O—; and R13 and R14 are the same or different and are selected from the group consisting of alkyl groups and aryl groups or R13 and R14 represent alkylene or arylene groups that are directly or indirectly bonded to one another. Methods for making such compounds are also disclosed, as are intermediates which can be used in their preparation. Also disclosed are methods for carrying out C—H insertion reactions using bis-transition metal catalysts, such as the above compounds.

Abstract: The invention concerns compounds of formula (I) wherein in particular G presents the —N(CH3)2—, —N(C2H5)2-group or N-pyrrolidine: n is an integer equal to 1 or 2: R1, R2 and R3 independently of one another, represent a hydrogen atom or a methyl group, the successive unsaturated units capable of being moreover identical or different, provided that at least one of the substituents R1, R2 and R3 is different from H: and Y1 and Y2 represent each a —COOCH3 group or a —COOC2H5 group.

Abstract: A compound of formula: comprising the Dmt-Tic pharmacophore and related compositions and methods of use in the inhibition of the binding of an opioid receptor-binding compound with a P-glycoprotein, specifically hMDR-1, are provided.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: A process for synthesizing L and D-5,5,5,5′,5′,5′-hexafluoroleucine and protected analogs is disclosed. These compounds have utility in the preparation of fluorous peptides and proteins, which display interesting and unusual properties including strong self-association and an affinity for lipid bilayers.

Abstract: The present invention relates to a method of manufacturing compoundable carboxylic acid and amino acid or amino acid condensate reactants by an extremely simple method that does not use substances toxic to human beings, as well as to carboxylic acid and amino acid or amino acid condensate reactants manufactured according to the method. In the present invention, carboxylic acid and amino acid or amino acid condensate reactants are manufactured by mixing carboxylic acids and amino acids or amino-acid condensates under an aqueous system and heating to 100° C. or more, less than 180° C. without vaporizing the water away.

Abstract: There are described 4-aminobut-2-ynecarboxylic acid derivatives of formula wherein R1 and R2 are each independently of the other hydrogen, C1-C20alkyl; C3-C12cycloalkyl; unsubstituted or C1-C5alkyl-, C3-C12cycloalkyl-, C1-C5alkoxy-, C3-C12cycloalkoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C12cycloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl, phenyl-C1-C5alkyl, naphthyl and naphthyl-C1-C5alkyl; and R3 is C1-C20alkyl; C3-C12cycloalkyl. The compounds exhibit a pronounced activity against gram-positive and gram-negative bacteria, and also against yeasts and moulds.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: An inner salt of L-carnitine is prepared by reduction, with a suitable reducing agent, of a compound of formula (I): 1

Abstract: Ionic compounds with a freezing point of up to 100° C. are formed by the reaction of an one amine salt of formula (I) R1R2R3R4N+X−, such as choline chloride with an organic compound (II) capable of forming a hydrogen bond with X; such as urea, wherein the molar ration of I to II is from 1:1.5 to 1:2.5. R1, R2, R3 and R4 may be H, optionally substituted C1 to C5 alkyl, optionally substituted C6 to C10 cycloalkyl, optionally substituted C6 to C12 aryl, optionally substituted C7 to C12 alkaryl, or R1 and R2 taken together may represent a C4 to C10 optionally substituted alkylene group, thereby forming with the N atom of formula I a 5 to 11-membered heterocyclic ring and all of R1, R2, R3 and R4 are not identical, X− may be NO3−, F, Cl−, Br−, I−, BF4−, ClO4−, CN−, SO3CF3−, or COOCF3−. The ionic compounds are useful as solvents, and electrolytes for example in electroplating, electrowinning, and electropolishing, and as catalysts.

Abstract: Compounds are disclosed with the general formula A-B, which in the vicinity of tumor cells result in a positively charged moiety B and an uncharged or negatively charged moiety A. Moiety B is able to induce blood clotting by interacting with negatively charged heparin-like substances lining vascular endothelia and the positive charge is reversibly masked by the uncharged or negatively charged moiety A in order to prevent unspecific disseminated blood coagulation and toxicity. Moiety B is either a covalent assembly of positively charged chemical groups or a positively charged molecule, which in aqueous solutions forms non-covalent polycations due to its propensity to form intermolecular aggregates. Pharmaceutical compositions including the compound and a pharmaceutically acceptable adjuvant or excipient are also disclosed. The disclosed compounds are useful in medicine, in particular for the manufacture of a medicament and its use for the treatment of a subject.

Abstract: The present invention relates to a method for introducing an amino group into an organic acid by reacting the organic acid and ammonia under high-temperature and high-pressure water conditions, a method for synthesizing an amino acid by reacting an organic acid and ammonia under high-temperature and high-pressure water conditions, and thereby introducing amino group into the organic acid to synthesize an amino acid, and a method for manufacturing an amino acid by reacting an organic acid and ammonia under high-temperature and high-pressure water conditions, thereby introducing an amino group into the organic acid to synthesize an amino acid, and then separating and refining it with an ion exchange resin.

Abstract: The present invention features improved methods for producing pantothenate compositions. In particular, the invention features methods of culturing microorganisms such that spray-dryable compositions of pantothenate are produced. Also featured are pantothenate compositions produced by the processes herein-described.

Abstract: The invention relates to a novel acylate which is the reaction product of (a) a substance which is selected from the group consisting of naturally occuring alpha-aminocarboxylic acids, neurotransmitters other than such acids, and central or peripheral nervous system pharmacologically active compounds, and containing a functional group including an acylatable hydrogen atom, or a reactive derivative thereof; and (b) an essential fatty acid or a reactive derivative thereof; and including the pharmaceutically acceptable salts of such acylates possessing a basic and (or) acidic function; and to their functional derivatives. The acylates and their functional derivatives may be used for treatment of a disease or condition related to a neurotransmitter defector deficiency, or to another central or peripheral nervous system defect or deficiency, and in particular Parkinson's disease.

Abstract: Novel chemical species capable of simultaneously alkylating double-stranded DNA and cleaving the same; methods for alkylating and cleaving DNA by using these species; and anticancer agents with the use of these compounds. Compounds represented by the following general formula (I) which are capable of simultaneously alkylating double-stranded DNA and cleaving the same; a method for alkylating DNA and a method for cleaving double stranded DNA by using these compounds; and medicinal compositions with the use of these compounds: B—L—A(I) wherein B represents a chemical structure capable of recognizing the base sequence of DNA, for example, optionally substituted pyrrole-imidazole polyamide; A represents a chemical structure capable of binding to one base of DNA, for example, the alkylation moiety of duocarmycin A; and L represents a linker capable of binding the chemical structures A and B, for example, vinyl.

Abstract: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ═O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(═O)R′, P(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH,

Abstract: Water-soluble metal ion affinity compounds and methods for using the same are provided. The subject compounds include an aspartate based metal chelating ligand bonded to a water-soluble polymeric substrate, where the ligand is complexed with a metal ion. In certain embodiments, the subject compounds further include a member of a signal producing system, e.g., a directly or an indirectly detectable label moiety. Also provided are water-insoluble supports having the subject compounds present on, e.g., immobilized on, at least one surface thereof. The subject compounds find use in a variety of different applications, including analyte detection and analyte purification applications.

Abstract: A process for the preparation of &agr;-amino acids by hydrolysis of hydantoins in the presence of water and at least one metallic oxide under conditions such that all the starting materials are completely dissolved in the water as a result of high pressure and high temperature and only one further phase is present in the reactor in addition to the metallic oxide phase.

Abstract: The present invention provides a method for enantioselectively reducing a prochiral carbon centered radical having one or more electron donator groups attached directly to the central prochiral carbon atom of the radical, and/or attached to a carbon atom within 1 to 4 atoms of the central prochiral carbon atom, comprising treating said radical with a chiral non-racemic organotin hydride in the presence of a Lewis acid.

Abstract: An improved process is described for the industrial preparation of L-carnitine or alkanoyl L-carnitine mucate, which allows operations in a homogeneous phase in conditions of greater dilution, in a normal chemical reactor with stirring, in a batch process.

Abstract: Described herein are both non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with taurine chloride (2-aminoethane-sulphonic chloride) and non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with glycine chloride which lend themselves favourably to the preparation of solid compositions suitable for oral administration. Also described are solid compositions containing said salts.

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

Abstract: New optically active bis[1-phospha-2,3-diphenyl-4,5-dimethylnorbornadiene] diphosphines and new optically active transition metal complexes with said phosphines are described. The complexes are useful as catalysts to promote hydrogenation of substrates.

Abstract: The present invention relates to a process for the resolution of DL-racemic mixtures of compounds which crystalize in the form of a conglumerate. Both, the D and L-enantiomers are obtained according to the invention in a industrially feasable process by adding chiral enantioselective polymers to the supersaturated solution of the racemat to inhibit crystalization of one enantiomer. Next a DL-racemic mixture of said compound is suspended in about twice the amount of the crystallized enantiomer. Consequently, the opposite enantiomer could be recovered by said suspension by physical separation.

Abstract: P-chiral bisphospholane ligands and methods for their preparation are described. Use of metal/P-chiral bisphospholane complexes to catalyze asymmetric transformation reactions to provide high enantiomeric excesses of formed compounds is also described.

Abstract: The invention relates to a process for preparing highly functionalized &ggr;-butyrolactams and &ggr;-amino acids by reductive amination of mucohalic acid or its derivatives, and discloses a process for preparing pregabalin, a GABA analog with desirable medicinal activity.

Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).

Abstract: The invention relates to amino acids, a method for the production thereof, medicaments containing said amino acids and the use of amino acids in the production of medicaments for treating pain.

Abstract: the present invention provides novel compounds represented by formula I: 1

Abstract: The invention relates to a process for preparing highly functionalized &ggr;-butyrolactams and &ggr;-amino acids by reductive amination of mucohalic acid or its derivatives, and discloses a process for preparing pregabalin, a GABA analog with desirable medicinal activity.

Abstract: A process for producing an optically active 3-azide-carboxylic acid ester by reacting an optically active 3-hydroxycarboxylic acid ester and a thionyl halide in the presence of a basic substance in an organic solvent to produce an optically active 3-halogenocarboxylic acid ester which is then reacted with an azide salt represented by the formula: MN3 (wherein M is an alkaline metal) in water or a mixture of water and a water soluble organic solvent.

Abstract: A compound of the formula 1