Abstract: Provided are inhibitors of pathogenic, bacterial metabolite production and conjugates of the inhibitors. Also provided are pharmaceutical compositions containing the inhibitors or conjugates and methods of using the same.

Abstract: The invention provides pharmaceutical compositions having improved effects and synergistic efficacy against pain, and provides methods for their use to treat pain, wherein the composition comprises: a sulfur-containing amino acid; a carnitine compound; and at least one compound that is a L-citrulline compound or a beta-alanine compound.

Abstract: The present invention is directed towards a process for manufacturing a complexing agent, said process comprising the steps of (a) Providing a nitrile according to general formula (I a) or (I b) With M being selected from alkali metal and hydrogen and combinations thereof, (b) Saponification with a total alkali amount of 2.5 to 2.9 mol of alkali metal hydroxide per mole of nitrile according to general formula (I a) or (I b), respectively, and a pH value in the range of from 9.5 to 11.5 at the end of step (b), (c) Adding an amount of alkali metal hydroxide so that the total alkali content is 2.9 to 3.15 moles per mole nitrile according to general formula (I a) or (I b), respectively, and (d) Allowing further conversion.

Abstract: The present invention relates to alanine N-acetic acid precursors of formula (i) COOM-CH(CH3)—NH—(CH2CN), wherein M is hydrogen (alanine N-monoacetonitrile), or (ii) COOM-CH(CH3)—N—(CH2CN)2, wherein 0 to 50% of all M is sodium or potassium and 50 to 100% of all M is hydrogen (alanine N,N-diacetonitrile and its partial sodium or potassium salts) comprising L-alanine to D-alanine in a range of from 75:25 to 50:50 (L:D), or (iii) COOM-CH(CH3)—N—(CH2CONH2)2, wherein M is hydrogen (alanine N,N-diacetamide), in the form of crystals, and relates to a process to prepare these precursors and their use, especially to give MGMA or MGDA.

Abstract: The present invention relates to a process for preparing a crystalline solid from glycine-N,N-diacetic acid derivatives (e.g., MGDA) of sufficiently low hygroscopicity, which is characterized in that at least one crystalline compound of the formula I is introduced as seed, and a spray granulation is carried out with at least one compound of the formula I, preferably followed by a heat treatment.

Abstract: The present invention relates to a process comprising the reaction of a cyanide with an amino acid and an aldehyde, characterized in that the cyanide is a cyanide salt, the amino acid is aspartic acid and/or glutamic acid in the acidic form, and the process is performed under acidic pH by the addition of between 0 and 1 equivalent of an acid based on the amount of aspartic or glutamic acid.

Abstract: A process is proposed for the preparation of a crystalline L-MGDA trialkali metal salt by crystallization from an aqueous solution thereof which has been obtained by Strecker synthesis, starting from L-?-alanine, by reaction with formaldehyde and hydrocyanic acid to give L-?-alanine-N,N-diacetonitrile and subsequent alkaline saponification of the L-?-alanine-N,N-diacetonitrile to give the L-MGDA trialkali metal salt, wherein a temperature of 150° C. is not exceeded during the alkaline saponification.

Abstract: N-alkyl, N-alkenyl, N-cycloalkyl, N-aryl amino or imino propionic acids with an alkyl chain ranging from 6 to 18 carbons, or alkenyl chain from 8 to 30 carbons, are obtained from a reaction process in the absence of solvent at a temperature range from 30 to 180° C. and a time of 1 to 10 hours at atmospheric pressure. Formulations composed of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl amino or imino propionic acids, polyethers derived from propylene oxide or ethylene oxide or copolymer thereof and a solvent consisting of aromatic compounds such as toluene or xylene, diesel or gasoline or alcohols such as isopropanol and ethanol, or mixtures thereof, are obtained inhibit ferrous metal corrosion of pipelines and storage tanks and transport crude oil and liquid fuels. A method inhibiting corrosion of ferrous metals adds an effective amount of the corrosion inhibitor to a petroleum based material such as crude oil and liquid fuels such as gasoline, diesel fuel, and aviation fuel.

Abstract: N-alkyl, N-alkenyl, N-cycloalkyl, N-aryl amino or imino propionic acids with an alkyl chain ranging from 6 to 18 carbons, or alkenyl chain from 8 to 30 carbons, are obtained from a reaction process in the absence of solvent at a temperature range from 30 to 180° C. and a time of 1 to 10 hours at atmospheric pressure. Formulations composed of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl amino or imino propionic acids, polyethers derived from propylene oxide or ethylene oxide or copolymer thereof and a solvent consisting of aromatic compounds such as toluene or xylene, diesel or gasoline or alcohols such as isopropanol and ethanol, or mixtures thereof, are obtained inhibit ferrous metal corrosion of pipelines and storage tanks and transport crude oil and liquid fuels. A method inhibiting corrosion of ferrous metals adds an effective amount of the corrosion inhibitor to a petroleum based material such as crude oil and liquid fuels such as gasoline, diesel fuel, and aviation fuel.

Abstract: The present invention relates to pulverulent compositions of a complex between an acid and a metal and the method of preparation thereof.

Abstract: Provided herein are tri-salt compounds comprising a compound having two acidic functional groups and one basic functional groups (e.g., aspartate or glutamate), metformin, and polyunsaturated fatty acids, such as eicosapentaenoate or docosahexaenoate. The salts can be used in the treatment of diabetes, diabetes with concomitant dyslipidemia (e.g., high triglycerides) and diabetes exacerbated cardiovascular complications, such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke. The compounds of this invention are also useful in treating obesity.

Abstract: A method of inhibiting the deposition of asphaltene in a mixture comprising hydrocarbons, the method comprising contacting the mixture with a composition which comprises at least one poly(hydroxycarboxylic acid) amide salt derivative.

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: Compounds according to the formula (I) or their physiologically acceptable salts X is selected from —CH2—, and —CH2CH2— are useful to impart, enhance or modify umami- and/or salt taste in a comestible product.

Abstract: Provided herein are tri-salt compounds comprising a compound having two acidic functional groups and one basic functional groups (e.g., aspartate or glutamate), metformin, and polyunsaturated fatty acids, such as eicosapentaenoate or docosahexaenoate. The salts can be used in the treatment of diabetes, diabetes with concomitant dyslipidemia (e.g., high triglycerides) and diabetes exacerbated cardiovascular complications, such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke. The compounds of this invention are also useful in treating obesity.

Abstract: The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2. The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.

Abstract: The present invention relates to fluorinated glutamic acid (glutamate) and glutamine derivatives wherein the fluorine atom is 19F. The glutamic acid (glutamate) and glutamine derivatives are compound(s) of general Formula I, which encompasses all possible diastereoisomers and/or enantiomere derivatives or mixtures thereof.

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: A process for preparing an aqueous solution of a methylglycine-N,N-diacetic acid trialkali metal salt at a high yield and purity by Strecker synthesis, the process including: reacting an aqueous solution containing ?-alanine with formaldehyde and hydrocyanic acid, to obtain ?-alanine-N,N-diacetonitrile in one reaction unit; and saponification of the ?-alanine-N,N-diacetonitrile with a base, to obtain the methylglycine-N,N-diacetic acid trialkali metal salt, wherein the ?-alanine is partially neutralized and the addition of formaldehyde and hydrocyanic acid are controlled such that a concentration of free hydrocyanic acid in the liquid reaction mixture at any time is limited such that secondary reactions that produce formaldehyde cyanohydrin, consecutive reactions of formaldehyde cyanohydrin, and the polymerization of hydrocyanic acid, only occur insofar as the specification requirements, such as nitrilotriacetic acid content and color, for methylglycine-N,N-diacetic acid trialkali metal salts are observed.

Abstract: The present invention relates to a process for preparing aminopolycarboxylates proceeding from an amino acid which, in a first process step is reacted with ethylene oxide to give an intermediate mixture comprising the corresponding dialkanolamine, and then the intermediate mixture, in a second process step is converted catalytically using a base to the corresponding aminopolycarboxylate, wherein the amino acid, before the reaction with ethylene oxide in the first process step, is supplied to a partial neutralization with 0.70 to 0.99 equivalent of base per acid group, or, in the first process step, an amino acid which has already been partly neutralized with 0.70 to 0.99 equivalent of base per acid group is used.

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: Acidic viscoelastic cleaning compositions are disclosed which use non polymer thickening agents. According to the invention, cleaning compositions have been developed using viscoelastic surfactants in acidic cleaning formulations. These provide the dual benefit of thickening as well as an additional cleaning, thereby improving performance. Applicants have also identified several pseudo linking agents which when, used with viscoelastic surfactants provide enhanced viscoelasticity and cleaning.

Abstract: An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.

Abstract: A marker can determine whether or not a patient has a therapeutic response to an anti-cancer agent. A novel cancer therapy employs the marker. The marker can be N-acetylglucosamine, an amino-acid-metabolism-related substance, a nucleic-acid-metabolism-related substance, a substance in the pentose phosphate pathway, a substance in the glycolytic pathway, a substance in the TCA cycle, a polyamine-metabolism-related substance, lauric acid, 6-phosphogluconic acid, butyric acid, 4-methylpyrazole, isobutylamine, glycolic acid, NADH, NAD+, or a substance involved in the metabolism of any of these substances.

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: Administering a therapeutically effective dose of lithium ions mitigates the side effects of a psychoactive substance such as a cannabinoid. The therapeutically effective dose of lithium ions includes greater than 4 milligrams of lithium and less than 170 milligrams of lithium, or includes between 8 and 32 milligrams of lithium ions per milligram of the psychoactive substance. The therapeutically effective dose of lithium ions is administered using lithium carbonate, lithium citrate, lithium chloride, lithium orotate, lithium aspartate, or analogs thereof using a delivery vehicle selected from pills, tablets, capsules, gelcaps, liquids, syrups, injectable liquids, powders, or foods and administered prior to, with, or after administration of the psychoactive substance. The psychoactive substance includes one or more of anandamide, 2-arachidonoyl glycerol, 2-arachidonoyl glycerol ether, tetrahydrocannabinol, cannabinol, cannabidiol, or analogs thereof and may be administered using the delivery vehicle.

Abstract: Chelating monomers and fluoride-releasing compositions are disclosed that may be incorporated into dental composite restorative materials, dental bonding agents or other dental materials, to produce materials with high fluoride release rates, and high fluoride recharge capability. Such dental restorative materials may help reduce the level of dental caries in patients, particularly the level of caries occurring on the margins of the restorative materials.

Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

Abstract: Salts of kukoamine B, their preparation method and their pharmaceutical use in preparation of drugs for preventing and treating sepsis. Experiments indicate that salts of kukoamine B have a good effect on antagonizing the key factors inducing sepsis, and can be used in the preparation of drugs for preventing and treating sepsis. Under the current circumstances of the lack of effective measures for the treatment of sepsis in clinical practice, the medicinal formulations, which comprise the salts of kukoamine B, pharmaceutically acceptable carrier and/or diluent, provide a new approach for the prevention and treatment of sepsis.

Abstract: The present invention relates to a process for treating a subterranean formation wherein a fluid containing an ammonium salt of glutamic acid N, N-diacetic acid (GLDA) or methylglycine N, N-diacetic acid (MGDA) is introduced into the formation.

Abstract: A new method for producing antifolate agents having glutamic acid part in their structure is developed by protecting carboxyl groups of glutamic acid or its N-subsituted derivatives as cyanomethyl ester to give compounds of formula (II) which are hydrolyzed under very mild conditions to afford antifolate agents in high yield with high analytical and optical purity.

Abstract: An automatic dishwashing composition offering good performance especially in the removal of stubborn stains, such as tea stains, comprises a chelating agent selected from hydroxyethyliminodiacetic acid, glucoheptonic acid, hydroxyethylethylenediaminetriacetic acid, poly(acrylic acid-co-hypophosphite), and salts, complexes and mixtures thereof; wherein the composition is substantially free of phosphate containing builders and substantially free of bleaching compounds.

Abstract: A method of synthesizing carboxylated amines is disclosed. The method comprises reacting a mixture of a potassium salt of either a primary or secondary amine with a potassium salt of a halogenated carboxylic acid wherein the halogenated carboxylic acid is selected from the group consisting of brominated, chlorinated, or iodinated carboxylic acid in the presence of potassium hydroxide, and optionally in heating the reacting mixture; precipitating the potassium salt by optionally chilling the mixture and discarding the precipitate; purifying the carboxylate amine potassium salt from the liquid phase using water soluble alcohol and optionally adding formic acid to obtain the free aminocarboxylic acid and potassium formate. In a preferred embodiment, the halogenated carboxylic acid is chloroacetic acid.

Abstract: The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Abstract: The present invention relates to novel particles comprising polyelectrolyte polymers which are transporters of active principle (AP), in particular protein and peptide active principle, and to novel modified-release pharmaceutical formulations comprising said AP microparticles. These novel particles loaded with AP release the AP over a prolonged period of time of several days, or even several weeks.

Abstract: Process for the preparation of racemic ?-amino acids or of glycine, wherein the corresponding ?-hydroxycarboxylic acid, selected from hydroxyacetic acid, lactic acid, malic acid, ?-hydroxyglutamic acid, isocitric acid, tartronic acid and tartaric acid, or at least one salt of the corresponding ?-hydroxycarboxylic acid is reacted in the presence of at least one heterogeneous catalyst which comprises at least one transition metal, in the presence of hydrogen with at least one nitrogen compound (c), where the nitrogen compound (c) is selected from primary and secondary amines and ammonia.

Abstract: This invention relates to methods, which provide access to F-18 labeled glutamic acid derivatives.

Abstract: Provided is a method for the production of aminodicarboxylic acid N,N-diacetic acids of formula (I), wherein X is independently hydrogen or an alkali metal and n is 1 or 2. Aminodicarboxylic acid-N,N-diacetic acids of high purity can be yielded. The method involves: a) reacting an aminodicarboxylic acid, with 0.8 to 1.2 mole equivalents of formaldehyde and with 0.8 to 1.2 mole equivalents of hydrocyanic acid; b) reacting the reaction products of a) with 0.8 to 1.2 mole equivalents of hydrocyanic acid and with 0.8 to 1.2 mole equivalents of formaldehyde; c) hydrolyzing in the reaction product obtained in b).

Abstract: This invention is directed a process for preparation of a carboxylic acid salt by dehydrogenation of a primary alcohol. The invention is also directed to a catalyst for dehydrogenating primary alcohols. In one embodiment, for example, the catalyst comprises a metal support (preferably a metal sponge support) having a copper-containing coating at the surface thereof. In another embodiment, the catalyst comprises a metal selected from the group consisting of zinc, cobalt, iron, tin and combinations thereof having a copper-containing coating at the surface thereof.

Abstract: A method of stabilizing a hem protein which is effective against the denaturation and degradation of a hem protein typified by hemoglobin and a storage solution therefor. A method of stabilizing a hem protein and a storage solution therefor characterized in that an iminocarboxylic acid or its salt is made to coexist in a sample containing the hem protein, wherein the above-described iminocarboxylic acid is a compound represented by the following general formula (1) wherein R represents a hydrogen atom or a hydroxyl group; and X's represent each a hydrogen atom, an alkali metal or an ammonium group.

Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using D-amino acids are described.

Abstract: This invention relates to homoglutamic acid derivatives suitable for labeling or already labeled with 18F or 19F, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.

Abstract: The present invention relates to an alkalimetal salt of glutamic acid-N,N-diacetic acid (GLDA) of the formula NaxKyHzGLDA, wherein x is equal to or more than 2 and lower than 4 and y is more than 0 and equal to or lower than 2, x+y is 3.5-4, and x+y+z=4, to processes to prepare such salt and the use thereof.

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: A method of stabilizing a hem protein which is effective against the denaturation and degradation of a hem protein typified by hemoglobin and a storage solution therefor. A method of stabilizing a hem protein and a storage solution therefor characterized in that an iminocarboxylic acid or its salt is made to coexist in a sample containing the hem protein, wherein the above-described iminocarboxylic acid is a compound represented by the following general formula (1) wherein R represents a hydrogen atom or a hydroxyl group; and X's represent each a hydrogen atom, an alkali metal or an ammonium group.

Abstract: Disclosed herein are substituted fluoromethanes; pharmaceutical compositions comprising a therapeutically effective amount of the same; processes for preparing these fluoromethanes; and methods of using the same in alleviating infection and parasitism. Also disclosed are methods for identifying substituted fluoromethanes for modulating the activity of receptors and enzymes that bind and/or modify phosphate containing ligands and substrates.

Abstract: A process is proposed for the preparation of a crystalline L-MGDA trialkali metal salt by crystallization from an aqueous solution thereof which has been obtained by Strecker synthesis, starting from L-?-alanine, by reaction with formaldehyde and hydrocyanic acid to give L-?-alanine-N,N-diacetonitrile and subsequent alkaline saponification of the L-?-alanine-N,N-diacetonitrile to give the L-MGDA trialkali metal salt, wherein a temperature of 150° C. is not exceeded during the alkaline saponification.

Abstract: D-aspartic acid is prepared as its hydrochloride salt or as the hydrochloride salt of its diethyl ester, thereby providing soluble forms of D-aspartic acid that are readily taken up by a human body via its digestive tract. The D-aspartic acid is administered as pills, capsules, powdered drink mixes, beverages, confectionaries, syrups, chewable tablets, nasal sprays, or injectable formulations.

Abstract: The present invention relates to a process for preparing aminopolycarboxylates proceeding from an amino acid which, in a first process step is reacted with ethylene oxide to give an intermediate mixture comprising the corresponding dialkanolamine, and then the intermediate mixture, in a second process step is converted catalytically using a base to the corresponding aminopolycarboxylate, wherein the amino acid, before the reaction with ethylene oxide in the first process step, is supplied to a partial neutralization with 0.70 to 0.99 equivalent of base per acid group, or, in the first process step, an amino acid which has already been partly neutralized with 0.70 to 0.99 equivalent of base per acid group is used.

Abstract: The invention provides novel compounds and methods to carry out organocatalytic Michael additions of aldehydes to nitroethylene catalyzed by a proline derivative to provide ?-substituted-?-nitroaldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96-99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to protected ?2-amino acids, which are essential for systematic conformational studies of ?-peptide foldamers.