Abstract: The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.

Abstract: Pregabalin besylate and pregabalin tosylate are pharmaceutically acceptable acid addition salts of pregabalin that are isolatable in solid state, particularly crystalline state, sufficiently soluble in water, and stable both in the solid state and in the solution.

Abstract: Suspensions having additives for controlled dispersion including a solvent, an ion source, a particle source selected from a partially dissolving colloid or a non-dissolving colloid, and an additive where the additive is added to the solvent prior to the ion source and the particle source when the particle source is the partially dissolving colloid.

Abstract: Derivative compounds of 11-nonyloxy-undec-8(Z)-eonic acid that mimic epoxide metabolites are provided. Also provided are compositions comprising a therapeutically effective amount of the derivative compounds. The present invention further provides methods for the use of such compositions for the treatment of renal or cardiovascular disease and/or related conditions.

Abstract: Synthetic amino acids containing one or more non-fouling groups or moieties are described herein. In one embodiment, the amino acid has the following chemical formula: where L is a linker group and Z is a non-fouling group including, but not limited to, polyethylene glycol (PEG); oligoethylene glycol (OEG); zwitterionic group, such as phosphorycholine, carboxybetaine, and sulfobetaine; groups that are hydrogen bond acceptors but not hydrogen bond donors. The non-fouling amino acids can be incorporated into a bioactive peptide as single amino acid residues, multiples amino acid residues, or as blocks of amino acids. The non-fouling amino acids, or peptides containing one or more non-fouling amino acids, can be applied to surfaces in order to improve biocompatibility, reduce thrombogenesis, and/or reduce fouling by proteins or bacteria present in solution.

Abstract: Integrated processes of preparing industrial chemicals starting from seed oil feedstock compositions containing one or more unsaturated fatty acids or unsaturated fatty acid esters, which are essentially free of metathesis catalyst poisons, particularly hydroperoxides; metathesis of the feedstock composition with a lower olefin, such as ethylene, to form a reduced chain olefin, preferably, a reduced chain ?-olefin, and a reduced chain unsaturated acid or ester, preferably, a reduced chain ?,?-unsaturated acid or ester. The reduced chain unsaturated acid or ester may be (trans)esterified to form a polyester polyolefin, which may be epoxidized to form a polyester polyepoxide. The reduced chain unsaturated acid or ester may be hydroformylated with reduction to produce an ?,?-hydroxy acid or ?,?-hydroxy ester, which may be (trans)esterified with a polyol to form an ?,?polyester polyol.

Abstract: A process for the preparation of a compound of formula (I), comprising: a) the reaction of a compound of formula (II) with hydrazine to obtain a compound of formula (III), b) the conversion of a compound of formula (III) by rearrangement via formation of nitrene/isocyanate, in a solvent of formula R1—OH, wherein R1 is as herein defined, to obtain a compound of formula (IV); c) the enantiomeric enrichment of a compound of formula (IV) to obtain the enantiomer (S) of a compound of formula (V) d) the hydrolysis of a compound of formula (V).

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The present invention provides 3-(aminomethyl)-5-methylhex-4-enoic acid (Pregabalin-4-eliminate or PRG-4E) and 3-(aminomethyl)-5-methylhex-5-enoic acid (Pregabalin-5-eliminate or PRG-5E), and their uses as reference markers and standards for determining the purity of Pregabalin. The invention also provides a method to produce Pregabalin containing low levels of these impurities.

Abstract: The invention relates to biochemical synthesis of 6-amino caproic acid from 6-aminohex-2-enoic acid compound or from 6-amino-2-hydroxyhexanoic acid, by treatment with an enzyme having ?,?-enoate reductase activity towards molecules containing an ?,?-enoate group and a primary amino group. The invention also relates to processes for obtaining suitable genetically engineered cells for being used in such biotransformation process, and to precursor fermentation of 6-amino caproic acid from intermediates leading to 6-amino caproic acid. Finally, the invention relates to certain novel biochemically produced compounds, namely 6-aminohex-2-enoic acid, 6-aminohexanoic acid, as well as to caprolactam produced therefrom and to nylon-6 and other derivatives produced from such biochemically produced compounds or caprolactam.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The present invention relates to a novel biomarker which can be used to determine the extent of interference of a substance with the farnesyl pathway.

Abstract: The invention relates to compounds of formula (I) that provide a kokumi flavour to consumables and flavour compositions, and to consumables and flavour compositions comprising such compounds. Enzymatic methods to prepare the compounds are provided.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: Materials and Methods for preparing (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid and structurally related compounds via enantioselective hydrogenation of prochiral olefins are disclosed. The methods employ novel chiral catalysts, which include C1-symmetric bisphosphine ligands bound to transition metals.

Abstract: The subject invention provides dipeptides useful in promoting healthy muscle tissues as well as effective immune responses. The dipeptides of the subject invention are particularly advantageous because they are stable, bioavailable, and can be formulated in an aqueous solution.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

Abstract: Materials and Methods for preparing (S)-(+)-3-aminomethyl-5-methyl-hexanoic acid and structurally related compounds via enzymatic kinetic resolution are disclosed.

Abstract: The use of R(+)-2-amino-3-hydroxypropanoic acid derivatives, nitrogen substituted by a (C1-C6)alkyl, (C3-C6)alkenyl, 3-oxo(C5-C6)alkyl, 3-oxo(C4-C6)alken-2-yl, phenyl(C1-C6)alkyl, phenyl(C2-C6)alkenyl, gem-diphenyl(C1-C6)alkyl, gem-diphenyl(C2-C6)alkenyl, (C1-C6)alcanoyl, optionally N-substituted alanyl, optionally N,N?-disubstituted lysinoyl, phenyl(C1-C6)alkylydene or gem-diphenyl(C1-C6)alkylidene group, and of the pharmaceutically acceptable salts thereof, for preparation of medicaments intended for the treatment of CNS diseases due to reduced glycinergic transmission, particularly for the treatment of autism, schizophrenia and Alzheimer's disease, is described.

Abstract: The present invention provides a process for the preparation of a nonracemic a-amino acid derivative from an optically active N-acyl lactam using an organometallic reagent to effect the opening of the ring followed by reduction of the ketone carbonyl to an alcohol or a methylene, or by a reductive amination to an amine, or by a ketalization reaction.

Abstract: The invention encompasses the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, via the intermediate, (3R)-5-methyl-3-(2-oxo-2{[(1R)-1-phenylethyl]amino}ethyl)hexanoic acid.

Abstract: A process for the preparation of (S)(+)-3-(aminomethyl)-5-methylhexanoic acid (pregabalin) of formula (I) or a salt thereof, comprising the reaction of a compound of formula (II) with an alcohol ROH, in the presence or absence of enzyme, to give a compound of formula (III) as herein defined the transformation of a compound of formula (III) into a compound of formula (VI) or (VIII) as herein defined, and the subsequent hydrolysis of a compound of formula (VI) or (VIII), to give pregabalin.

Abstract: The invention encompasses the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, via the intermediate, (3R)-5-methyl-3-(2-oxo-2{[(1R)-1-phenylethyl]amino}ethyl)hexanoic acid.

Abstract: Provided are syntheses of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin via a chiral intermediate of the following formula 4 wherein Ar is a C6-10 aromatic group, R is a straight or branched C1-4 alkyl, ester, or carboxylic acid, and R1 is a straight or branched C1-5 alkyl, aralkyl, or substituted aralkyl.

Abstract: Provided are processes for the synthesis of R-(+)-3-(carbamoylmethyl)-5-methylhexanoic acid and salts thereof, intermediates in the synthesis of S-pregabalin.

Abstract: A Pregabalin having a low level of 3-isobutylglutaric acid is provided.

Abstract: The present invention is directed compounds for reversibly modification of biologically active molecules. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery conjugates. The use of reversible modification provides for physiologically responsive activity modulation.

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: Disclosed herein are a composition for peritoneal dialysis comprising an ?-keto amino acid, and a method for peritoneal dialysis using the same. The composition allows peritoneal dialysis to be effected without the problems accompanying conventional compositions, including tissue toxicity and uremia.

Abstract: To provide a method for producing an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid, a basic amino acid salt thereof or an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid ester with high yield and high optical purity by simple operation. An optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid is obtained by precipitating a basic amino acid salt of optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid from a solvent solution containing an optical isomer mixture of (4E)-5-chloro-2-isopropyl-4-pentenoic acid and an optically active basic amino acid or a salt thereof, and then the basic amino acid salt of optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid is subjected to a desalting reaction. Further, an esterification reaction is carried out to obtain an optically active (4E)-5-chloro-2-isopropyl-4-pentenoic acid ester.

Abstract: Corrosion and gas hydrate inhibitors having improved water solubility and increased biodegradability The invention thus provides the use of compounds of the formula (1) where R1, R2 are each independently C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R3 is C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, —CHR5—COO? or —O?, R4 is M, hydrogen or an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, B is an optionally substituted C1- to C10-alkylene group, D is an ethylene group substituted by an organic radical having from 1 to 600 carbon atoms, X, Y are each independently O or NR6, R5, R6 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and M is a cation as corrosion and gas hydrate inhibitors, and also the compounds of formula 1.

Abstract: The invention relates to a process for preparing ?-aminopropionic acid derivatives by reacting a primary or secondary amine with an acrylic acid derivative, wherein comprises (i) a first primary or secondary amine is provided as an amine of value and reacted with the acrylic acid derivative, to obtain a reaction mixture comprising a first ?-aminopropionic acid derivative as a product of value and additionally unconverted acrylic acid derivative, (ii) the unconverted acrylic acid derivative present in the reaction mixture is reacted with a second secondary amine as a scavenger amine virtually fully to give a second ?-aminopropionic acid derivative to obtain a reaction mixture comprising the first ?-aminopropionic acid derivative as a product of value, the second ?-aminopropionic acid derivative and unconverted secondary amine.

Abstract: This invention relates to a stereoselective preparation of fluoroleucine alkyl esters.

Abstract: This invention relates to methods of synthesis of amino acid analogs contained within peptide sequences that is adapted for preparation of peptides containing analogs of basic amino acids lysine and arginine.

Abstract: The present invention relates to methods for preparing an L-carnitine valproate salt and administering this compound to a subject in need of treatment with valproate. Pharmaceutical compositions are also provided that are useful therapies for the treatment of neurological, immunological, and viral-mediated disorders in warm-blooded mammals.

Abstract: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: A continuous process for decarboxylating carboxylic acids proceeds by I.) initially charging a carbonyl compound as a catalyst in a solvent at reaction temperature, to obtain a catalyst solution; II.) metering a carboxylic acid into the catalyst solution as an aqueous solution, aqueous suspension or as a water-comprising solid, to obtain a reaction mixture; and III.) continuously removing a mixture of CO2, solvent, water and a reaction product or mixture of reaction products from the reaction mixture as a vapor.

Abstract: Use of a preparation comprising an isolated peptide selected from the group consisting of: Leu-Val (LV) (SEQ ID NO: 1) and lie-Val (IV) (SEQ ID NO: 2) for the preparation of a composition having angiotensin-converting enzyme (ACE) inhibitor effect. The peptides may e.g. be used to make a functional food with anti-hypertensive properties.

Abstract: Crystalline form of Pregabalin characterized by X-ray powder diffraction peaks at about 5.8, 18.4, 19.2, 20.7, and 23.7° 2?±0.2° 2?, methods for its preparation, its pharmaceutical compositions thereof, and methods for the preparation of crystalline form of Pregabalin characterized by X-ray powder diffraction peaks at about 5.7, 15.4, 17.2, 18.2, and 23.0° 2?±0.2° 2?, are provided.

Abstract: This invention relates to a process for purifying a polypeptide, a capture tag useful for purifying a polypeptide and a periodate-cleavable amino acid derivative useful for purifying a polypeptide.

Abstract: Disclosed are materials and methods for preparing optically active ?-amino acids, which bind to the alpha-2-delta subunit of a calcium channel and are useful for treating pain, fibromyalgia, and a variety of psychiatric and sleep disorders. The method includes reacting a chiral allyl amine with a 2-alkynoate in the presence of a Lewis acid and a base to give a chiral tertiary enamine, which after reaction with ammonia, is hydrogenated to give optically active ?-amino acids.

Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.

Abstract: Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.

Abstract: The present invention provides a Dpp4 inhibitor which comprises a leucine derivative of the following formula (1) or a methionine derivative of the following formula (2): wherein each R1 and R3 represents a hydrogen atom (H) and an L-amino acid residue; R2 represents a hydroxyl group (OH), alkoxy group having 1 to 6 carbon atoms, amino group (NH2), alkylamino group having 1 to 6 carbon atoms, glycine residue, ?-alanine residue, L-amino acid (except for proline, alanine and phenylalanine) residue or L-amino-acid amide (except for proline amide, alanine amide and phenylalanine amide) residue; and R4 represents a hydroxyl group (OH), alkoxy group having 1 to 6 carbon atoms, amino group (NH2), alkylamino group having 1 to 6 carbon atoms, glycine residue, ?-alanine residue, L-amino acid (except for proline and alanine) residue or L-amino-acid amide (except for proline amide and alanine amide) residue. These derivatives also act as autophagy regulators.

Abstract: The present invention provides a pharmaceutical agent and the like that decreases the level of oxidized albumin. Specifically, the present invention provides an agent for decreasing oxidized albumin, which contains at least one kind of branched-chain amino acid selected from isoleucine, leucine and valine.