Abstract: The present disclosure provides a process for the preparation of compounds of formula (III), compounds of formula (V), and corresponding salts of formula (IV). The compounds made by the methods and processes of the invention are particularly useful for administration in humans and animals.

Abstract: A process for synthesizing 4-amino-2,4-dioxobutanoic acid involves reacting diethyl oxalate with an alkoxide in ethanol to form a reaction mixture, and afterward adding ethyl cyanoacetate to the reaction mixture and allowing a reaction to proceed under conditions suitable to form a first reaction product of the formula diethyl 2-cyano-3-hydroxy-butenedioate, and then isolating the diethyl 2-cyano-3-hydroxy-butenedioate, and afterward reacting the diethyl-2-cyano-3-hydroxy-butenedioate with an aqueous hydroxide under conditions suitable to form 4-amino-2,4-dioxobutanoic acid.

Abstract: A first process for synthesizing 4-amino-2,4-dioxobutanoate involves reacting a dialkyl oxalate with an alkoxide in ethanol to form a reaction mixture, and afterward adding an alkyl cyanoacetate to the reaction mixture and allowing a reaction to proceed under conditions suitable to form a first reaction product of the formula diethyl 2-cyano-3-hydroxy-butenedioate, and then isolating the diethyl 2-cyano-3-hydroxy-butenedioate, and afterward reacting the diethyl-2-cyano-3-hydroxy-butenedioate with an aqueous hydroxide under conditions suitable to form 4-amino-2,4-dioxobutanoate.

Abstract: This disclosure teaches the novel use of trifluoroacetamide for N-terminal protection. The disclosure also teaches novel compositions and chemical structures associated therewith. These methods and compositions are useful for site-specific methylation of peptide backbone amides, performed, for example, to modulate the pharmacokinetic properties of peptide drugs.

Abstract: A salt of an acidic chelating agent including an amine functionality, the salt comprising at least 0.25 mole of an alkaline earth metal per mole of acidic protons provided by the chelating agent; wherein the acidic chelating agent is not ethylene diamine disuccinic acid.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: The invention provides formulations that contain an immunogenic or immunostimulatory cargo, delivery moiety and/or lipid, and a lipid that functions to reduce or prevent induction in a subject of an immune response which would otherwise occur when the immunogenic or immunostimulatory cargo, delivery moiety and/or lipid is administered to a subject as a component of an appropriate control formulation lacking the immune response reducing lipid. Specific immune response reducing lipids and uses thereof are further provided.

Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

Abstract: Provided are novel symmetrical and asymmetrical bifunctional photodecomposable bases (PDBs) with dicarboxylate anion groups that show increased imaging performance. Also provided are photoresist compositions prepared with the bifunctional dicarboxylated PDBs and lithography methods that use the photoresist compositions of the present invention.

Abstract: Provided are a polyphenol compound absorption promoter which is widely applicable to foods and drinks over a wide range, and a method for producing a food, drink or food material containing a polyphenol compound. The polyphenol compound absorption promoter comprises, as the active ingredient, at least one member selected from the group consisting of serine, aspartic acid, malic acid, capric acid, lauric acid, grapefruit juice and Camellia sinensis (L.) O. Kuntze extract. The method for producing a food, drink or food material containing a polyphenol compound comprises: adding at least one member selected from the group consisting of serine, aspartic acid, malic acid, capric acid, lauric acid, grapefruit juice and Camellia sinensis (L.) O.

Abstract: Compounds having the formulas below. The values n and x are independently selected positive integers.

Abstract: A new method for preparing salts of metal cations and organic acids, especially divalent salts of alkaline earth metal ions from group II of the periodic system and carboxylic acids. The method comprising the use of a high temperature (about 90° or more) and, optionally. high pressure, in order to obtain a higher yield, purity and faster reaction speed than obtained with known synthesis methods. In particular, the present invention relates to the production of strontium salts of carboxylic acids. Novel strontium salts are also provided by the present method.

Abstract: A salt of an acidic chelating agent including an amine functionality, the salt comprising at least 0.25 mole of an alkaline earth metal per mole of acidic protons provided by the chelating agent; wherein the acidic chelating agent is not ethylene diamine disuccinic acid.

Abstract: The present invention relates to a process for preparing ether carboxylates.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: A compound having the formula below. The values n and m are independently selected positive integers.

Abstract: An acylamino acid compound is described which can be used in food preparations to generate a savory tingling sensation without burning effect.

Abstract: A method is provided for the parallel identification of one or more metabolite species within a biological sample. The method comprises analyzing the sample to produce a spectrum containing individual spectral peaks representative of the one or more metabolite species contained within the sample; subjecting each of the individual spectral peaks to a statistical pattern recognition analysis to identify the one or more metabolite species contained within the sample; and identifying the one or more metabolite species contained within the sample by analyzing the individual spectral peaks of the spectra.

Abstract: The compounds and the synthesis of [F-18]-labeled L-glutamic acid, [F-18]-labeled L-glutamate, their derivatives as set forth in formula (I) and their uses are described.

Abstract: The invention provides a fluoroethercarboxylic acid which is represented by the general formula (I): Rf1OCHFCF2ORf2COOM??(I) wherein Rf1 represents a partially or fully fluorinated alkyl group, which may optionally be interrupted with one or more oxygen atoms, Rf2 represents a partially or fully fluorinated alkylene group, which may optionally be interrupted with one or more oxygen atoms, and M represents a monovalent alkali metal, NH4 or H. The fluoroethercarboxylic acid can be suitably used as a surfactant and is low in bioaccumulation. The invention is also a method of fluoropolymer production and an aqueous fluoropolymer dispersion, using the fluoroethercarboxylic acid as a surfactant.

Abstract: Methods of production for Tricreatine Hydroxycitrate are disclosed. Tricreatine hydroxycitrate can be used as supplemental dietary ingredient for the purposes of reducing adiposity, suppression of appetite, improvement of muscle and exercise performance and recovery. The salts are useful in the dietetic, food supplement and food industries.

Abstract: The present invention relates to new butylammonium modulators of fatty acid transport, and/or removal of toxic acyl-CoA compounds, pharmaceutical compositions thereof, and methods of use thereof

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: The present invention relates to aminoalkyl substituted fumarates and there use as malodor neutralizers.

Abstract: The present invention relates to photosensitive derivatives of optically active L-threo-?-benzyloxyaspartate or its benzene ring-substituted analogs, represented by the following formula (1) or (2): (1) (2) wherein R1 represents hydrogen atom, amino group, straight or branched lower aliphatic acylamino group optionally substituted at the acyl group portion, alicyclic acylamino group or aromatic acylamino group optionally having a substituent on the aromatic ring, R2 represents hydrogen atom or one or more straight or branched optionally substituted lower aliphatic alkyloxy groups on the benzene ring, R3 represents hydrogen atom, methyl group or carboxyl group, and R4 and R5 each represent hydrogen atom, hydroxyl group, straight or branched lower alkyloxy group optionally substituted at the alkyl portion, amino group, straight or branched lower alkyl-substituted amino group, or a halogen atom, which upon photoirradiation can produce compounds exhibiting a function of suppressing the glutamate uptake activity o

Abstract: A new method for preparing salts of metal cations and organic acids, especially divalent salts of alkaline earth metal ions from group II of the periodic system and carboxylic acids. The method comprising the use of a high temperature (about 90° or more) and, optionally. high pressure, in order to obtain a higher yield, purity and faster reaction speed than obtained with known synthesis methods. In particular, the present invention relates to the production of strontium salts of carboxylic acids. Novel strontium salts are also provided by the present method.

Abstract: The present invention is a method for calorimetrically determining a metal in a sample using a chelating coloring agent, characterized by coexistence of a masking agent for iron, copper or nickel. Also, the present invention is a reagent for calorimetrically determining a metal in a sample using a chelating coloring agent, characterized by inclusion of a masking agent for iron, copper and/or nickel. Further, the present invention is a masking agent for iron, copper and/or nickel and a method for reducing positive errors due to iron, copper or nickel contained in a sample.

Abstract: The present invention provides a method of using a physiologically-based pharmacokinetic model to select a prodrug molecule (NO—X) comprising a therapeutic agent X (e.g. nonsteroidal anti-inflammatory drug, (NSAID)) and an appropriate nitric oxide donor NO. The NSAID can be a non-selective or selective cyclooxygenase inhibitor or other biocompatible compound comprising a carboxyl group. The pharmacokinetic model uses in vitro and/or in silico data to estimate an optimal set of parameters that can predict whether a particular NO—X candidate is capable of producing desirable therapeutic effects, e.g. enhanced anti-inflammatory activity, reduced intestinal, cardiac and renal toxicity. Accordingly, the present invention can greatly enhance proper selection of an appropriate candidate for drug development, thereby minimizing development time and conserving costs.

Abstract: L-threo-?-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): wherein R is hydrogen, a linear or branched lower aliphatic acyl group with the acyl portion optionally substituted, an alicyclic acyl group, an aromatic acyl group with a substituent on the aromatic ring, an amino acid-derived group or a biotin derivative-derived group, having an amino substituent on the benzene ring, and salts thereof, which can easily bind to affinity column chromatography carriers as ligands of glutamate transporter proteins.

Abstract: Alcohol and water solvates of 6-(5-carboxy-5-methyl-hexyloxy)-2,2-dimethylhexanoic acid monocalcium salt are crystalline and have the formula wherein R1 is H or lower alkyl, and x is a number from 0 to 10, and are useful for treating dyslipidemia.

Abstract: An inner salt of L-carnitine is prepared by reduction, with a suitable reducing agent, of a compound of formula (I): where X1 and X2, which may be the same or different, are hydroxy, C1–C4 alkoxy, phenoxy, halogen, or X1 and X2, when taken together are an oxygen atom and the resulting compound is a derivative of succinic anhydride; Y is halogen, a mesyloxy or a tosyloxy group, and subsequent treatment with water, then with a base and then with trimethylamine.

Abstract: Alcohol and water solvates of 6-(5-carboxy-5-methyl-hexyloxy)-2,2-dimethylhexanoic acid monocalcium salt are crystalline and have the formula (I), wherein R1 is H or lower alkyl, and x is a number from 0 to 10, and are useful for treating dyslipidemia.

Abstract: ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV): wherein the variables are as described in the specification. Pharmaceutical compositions containing the compounds are also discussed. The pharmaceutical compositions may contain an effective amount of a compound of the invention to treat ACE-2 associated disorders such as a blood pressure related disease or disorder, cell proliferation disorder, kidney disorder, kinetensin associated disorder, inflammation associated disorder, or an allergic disorder.

Abstract: Compounds represented by the formula wherein R and R1 independently represent H, —CH2CN or —CH2CO2X, with the proviso that R and R1 can not be both H or —CH2CO2X; and X represents hydrogen, an alkali metal or alkaline earth metal are disclosed. These compounds are useful as intermediate compounds in the preparation of N-[2-(carboxymethoxy)ethyl]-N-(carboxy-methyl)glycine. These intermediates can be formed by contacting 3-morpholinone with glycolonitrile under alkaline conditions to form an aminonitrile which can be hydrolyzed and contacted with additional glycolonitrile to form the nitrile intermediate which can be converted to N-[2-(carboxymethoxy)ethyl]-N-(carboxymethyl)glycine via hydrolysis.

Abstract: The instant invention is improved gamma amino butyric acid analogs, processes for their preparation, and methods of using them as agents for treating epilepsy and other neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal damage, and inflammation.

Abstract: Methods for the preparation of an N-alkyl-N-bis-(2-( 1,2-dicarboxy-ethoxy)-ethyl)-amine derivative are described, products of the methods as well as uses of the products. The derivative is prepared by reacting an alkali or earth alkali metal salt of maleic acid with an N-substituted diethanolamine, the reaction taking place with the two ethanol groups of the diamine while the substituent group bound to the N atom remains unaffected, or alternatively by first reacting diethanolamine with an alkali or earth alkali metal salt of maleic acid to yield N-bis-(2-(1,2-dicarboxy-ethoxy)-ethyl)-amine, which is then reacted with a substitution reagent to obtain the final product. The derivative is useful as chelating agents, e.g., in the bleaching of chemical or mechanical pulp or in textile bleaches containing hydrogen peroxide or a peracid, or as a calcium binder in detergents and cleaning agents.

Abstract: This invention is directed to a process for making an iminodiacetic acid compound from a monoethanolamine substrate having the formula: wherein R1 is hydrogen, hydrocarbyl, or substituted hydrocarbyl. The process includes a series of reactions comprising a cyanomethylation, a hydrolysis and a dehydrogenation with the hydrolysis and dehydrogenation steps being carried out either sequentially or concurrently. In a particular embodiment, the iminodiacetic acid produced is disodium iminodiacetic acid and the monoethanolamine substrate used is 2-aminoethanol.

Abstract: An amino acid derivative composition which comprises two or more kinds of amino acid derivatives represented by the general formula (1): wherein R's are the same or different and each represents a hydrogen atom or an alkyl group containing 1 to 18 carbon atoms; L1 represents —M1—X or —CHX—M2—X; L2 represents —CH2—M3—X or —CHX—M4—X; M1, M2, M3 and M4 are the same or different and each represents a straight or branched alkylene group containing 1 to 6 carbon atoms; X represents COOM; M's are the same or different and each represents a hydrogen atom, an alkali metal atom, an alkaline earth metal atom or an ammonium group; m represents an integer of 1 or 2 and n represents an integer of 0 or 1 on the condition that m+n is equal to 2 is provided.

Abstract: Compounds represented by the formula wherein R and R1 independently represent H, —CH2CN or —CH2CO2X, with the proviso that R and R1 can not be both H or —CH2CO2X; and X represents hydrogen, an alkali metal or alkaline earth metal are disclosed. These compounds are useful as intermediate compounds in the preparation of N-[2-(carboxymethoxy)ethyl]-N-(carboxy-methyl)glycine. These intermediates can be formed by contacting 3-morpholinone with glycolonitrile under alkaline conditions to form an aminonitrile which can be hydrolyzed and contacted with additional glycolonitrile to form the nitrile intermediate which can be converted to N-[2-(carboxymethoxy)ethyl]-N-(carboxymethyl)glycine via hydrolysis.

Abstract: The present invention deals with novel compounds their applications and a process their preparation. The compounds are novel amphoteric surfactants that contain a hydroxyl group and two carboxylic groups per hydroxyl group. The compounds have a unique structure, having multiple carboxyl groups on each amino group. The utility for these novel polymers is as softening, anti-tangle, and conditioning agents for use in personal care, textile and related applications.

Abstract: Compounds represented by the formula 1

Abstract: The present invention provides a triaminepentaacetic acid compound which can be used as a ligand to coordinate to a metal ion to form a paramagnetic metal complex. The paramagnetic metal complex of the present invention can be used as a contrast agent for magnetic resonance imaging (MRI).

Abstract: A process for the preparation of 3,4-dihydroxybutanoic acid (I) and 3-hydroxy-&ggr;-butyrolactone (V) thereof from a 3-leaving group substituted pentose source is described. In particular, the process relates to the synthesis of (R)-3,4-dihydroxybutanoic acid and (R)-3-hydroxy-&ggr;-butyrolactone from a 3-leaving group substituted L-pentose sugars. The process uses a base and a peroxide to convert the pentose source to the chiral 3,4-dihydroxybutanoic acid compound. The chiral 3,4-dihydroxybutanoic acid can be further converted to 3-hydroxy-&ggr;-butyrolactone by acidification. The chiral compound is useful as a chemical intermediate to the synthesis of various drugs and other products.

Abstract: Compounds represented by the formula wherein R and R1 independently represent H, —CH2CN or —CH2CO2X, with the proviso that R and R1 can not be both H or —CH2CO2X; and X represents hydrogen, an alkali metal or alkaline earth metal are disclosed. These compounds are useful as intermediate compounds in the preparation of N-[2-(carboxymethoxy)ethyl]-N-(carboxy-methyl)glycine. These intermediates can be formed by contacting 3-morpholinone with glycolonitrile under alkaline conditions to form an aminonitrile which can be hydrolyzed and contacted with additional glycolonitrile to form the nitrile intermediate which can be converted to N-[2-(carboxymethoxy)ethyl]-N-(carboxymethyl)glycine via hydrolysis.

Abstract: The present invention provides blockers for glutamate transporters. During a series of syntheses searching for glutamate uptake inhibition in Xenopus oocytes injected with bovine glutamate transporter genes (BGLAST), we obtained .beta.-hydroxyaspartic acid derivatives of the following chemical formula (1): ##STR1## wherein R represents an aromatic acyl group which may be substituted on the ring, a straight or branched lower aliphatic acyl group, an aryl group which may be substituted on the ring, an aralkyl group which may be substituted on the ring, or a straight or branched lower alkyl group; and salts thereof. These compounds are blockers of glutamate transporters, which are useful for the understanding of the function of glutamate transporters and show promise for the treatment of various neurodegenerative diseases.

Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel .alpha.,.alpha.-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.

Abstract: The invention relates to N-bis- or N-tris-[(1,2-dicarboxy-ethoxy)-ethyl]-amine derivatives having the formula (I) ##STR1## and R.sub.2 is hydrogen, an alkali metal or an earth-alkali metal. The invention also relates to a method for preparing the same and their use as chelating agents.

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: An aqueous iminocarboxylic acid salt solution composition the iminocarboxylic acid salt of which has a structure of the formula (II): ##STR1## wherein R is a hydrogen atom or a hydroxyl group and Y is a sodium atom, a potassium atom, or an ammonium group, contains an aspartic acid backbone moiety whose molar ratio of the isomers, i.e. D form/L form, is in the range of 1/0 to 0.7/0.3 or D form/L form, in the range of 0/1 to 0.3/0.7, and accounts for a concentration in the range of 40 to 70% by weight and a method for handling the composition while keeping the pH value thereof kept in the range of 7 to 12.

Abstract: The use of triacids of the formula I ##STR1## where X.sup.1 to X.sup.3 are, independently of one another, carboxylic acid groups of the formula COOM, sulfonic acid groups of the formula SO.sub.3 M or phosphonic acid groups of the formula PO.sub.3 M.sub.2, whereM is hydrogen, alkali metal, ammonium or substituted ammonium,A.sup.1 to A.sup.3 are, independently of one another, 1,2-alkylene with 2 to 18 carbon atoms,R.sup.1 to R.sup.3 are, independently of one another, C.sub.1 -C.sub.8 -alkylene, andx, y and z are, independently of one another, a number from 0 to 10, where the total of x+y+z must be greater than or equal to 1,as complexing agents for complexing heavy metals or for preparing heavy metal complexes for changing the redox potential, and as builders in detergents and cleaners.