C07C229/24

WATER SOLUBLE SALTS OF ALDOSE REDUCTASE INHIBITORS FOR TREATMENT OF DIABETIC COMPLICATIONS
20170362237 · 2017-12-21 ·

The present invention relates to pharmaceutically acceptable water soluble salts of aldose reductase inhibitors, 2-(8-oxo-7-((5-trifluromethyl)-1H-benzo[d]imidazol-2-yl)methyl)7,8-dihydropyrazin[2,3-d]pyridazin-5-yl)acetic acid and [4-oxo-(5-trifluoromethyl-benzothaiazol-2-yl)methyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid (also known as zopolrestat), pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to mammals these salt and compositions.

WATER SOLUBLE SALTS OF ALDOSE REDUCTASE INHIBITORS FOR TREATMENT OF DIABETIC COMPLICATIONS
20170362237 · 2017-12-21 ·

The present invention relates to pharmaceutically acceptable water soluble salts of aldose reductase inhibitors, 2-(8-oxo-7-((5-trifluromethyl)-1H-benzo[d]imidazol-2-yl)methyl)7,8-dihydropyrazin[2,3-d]pyridazin-5-yl)acetic acid and [4-oxo-(5-trifluoromethyl-benzothaiazol-2-yl)methyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid (also known as zopolrestat), pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to mammals these salt and compositions.

Method of obtaining complex acidic salts of divalent metals and dicarboxylic acids

A method of obtaining a complex acidic salt of a divalent metal and a dicarboxylic acid includes heating water in a reactor; adding a dicarboxylic acid to the heated water; stirring the water to dissolve the dicarboxylic acid in the heated water to produce a solution or a suspension of the dicarboxylic acid in the heated water; adding MeO to the solution or the suspension, where Me is a divalent metal; continuing the stirring of the solution or suspension until formation of the complex acidic salt Me(AcH).sub.2.nH.sub.2O begins, where Ac is an anion of the dicarboxylic acid, and n=0-8; cooling the complex acidic salt to below a temperature of crystallization; sedimenting the complex acidic salt; filtering the complex acidic salt to remove water from the complex acidic salt; and drying the complex acidic salt.

Method of obtaining complex acidic salts of divalent metals and dicarboxylic acids

A method of obtaining a complex acidic salt of a divalent metal and a dicarboxylic acid includes heating water in a reactor; adding a dicarboxylic acid to the heated water; stirring the water to dissolve the dicarboxylic acid in the heated water to produce a solution or a suspension of the dicarboxylic acid in the heated water; adding MeO to the solution or the suspension, where Me is a divalent metal; continuing the stirring of the solution or suspension until formation of the complex acidic salt Me(AcH).sub.2.nH.sub.2O begins, where Ac is an anion of the dicarboxylic acid, and n=0-8; cooling the complex acidic salt to below a temperature of crystallization; sedimenting the complex acidic salt; filtering the complex acidic salt to remove water from the complex acidic salt; and drying the complex acidic salt.

Amino acid compositions

Improved methods of causing vasodilation in a human subject are disclosed. In one implementation, the human subject is administered a dose of a nitrate salt of arginine, norvaline, or ornithine, wherein the dose of the nitrate salt of the amino acid in moles of the amino acid is less than a molar amount of the amino acid needed to cause vasodilation in the human subject. In another implementation, the human subject is administered a composition comprising a dose of a nitrate salt and an amount of an amino acid, wherein the dose of the nitrate salt in the composition in moles of the nitrate salt is less than a molar amount of the nitrate salt that needs be administered alone in order to induce vasodilation in the human subject. The amino acid in the composition is selected from the group consisting of: arginine, citrulline, creatine, glutamine, leucine, norvaline, and ornithine.

FORMULATIONS FOR THE DELIVERY OF ACTIVE AGENTS TO INSECTS, PLANTS, AND PLANT PATHOGENS

The present disclosure is directed to formulations comprising (1) at least one formulation transport agent, (2) at least one complexing agent, and (3) at least one active agent that modulates one or more traits of a target insect, plant, or plant pathogen. The present disclosure is also directed to methods of delivering such formulations to the target organism, as well as to formulation transport agents used to prepare such formulations.

Mixtures of MGDA enantiomers, and process for making such mixtures

Mixture of L- and D-enantiomers of methyl glycine diacetic acid (MGDA) or its respective mono-, di or trialkali metal or mono-, di- or triammonium salts, said mixture containing predominantly the respective L-isomer with an enantiomeric excess (ee) in the range of from 10 to 75%.

Mixtures of MGDA enantiomers, and process for making such mixtures

Mixture of L- and D-enantiomers of methyl glycine diacetic acid (MGDA) or its respective mono-, di or trialkali metal or mono-, di- or triammonium salts, said mixture containing predominantly the respective L-isomer with an enantiomeric excess (ee) in the range of from 10 to 75%.

Method for stepwise separating amino acid active ingredients of Camellia nitidissima Chi

The present invention relates to the technical field of Camellia nitidissima Chi processing and application, and provides a method for stepwise separating amino acid active ingredients of Camellia nitidissima Chi. The method comprises the following steps: taking a graphene nano material as a selective extraction, adsorption and separation carrier material; carrying out stepwise separation through stepwise controlling the pH value of Camellia nitidissima Chi concentrated solution and adjusting the isoelectric points of the amino acid active ingredients, wherein the amino acid active ingredients comprise aspartic acid, threonine, serine, glutamic acid, proline and glycine, and the pH values of the aspartic acid, the threonine, the serine, the glutamic acid, the proline and the glycine corresponding to the stepwise separated isoelectric points are less than 2.77, 5.98-6.15, 3.23-5.67, 2.78-3.21, 6.17-6.29 and 5.69-5.96. The method for stepwise separating amino acid active ingredients of Camellia nitidissima Chi has the characteristics of superior selectivity, superior separation speed, good product purity and low cost.

Method for stepwise separating amino acid active ingredients of Camellia nitidissima Chi

The present invention relates to the technical field of Camellia nitidissima Chi processing and application, and provides a method for stepwise separating amino acid active ingredients of Camellia nitidissima Chi. The method comprises the following steps: taking a graphene nano material as a selective extraction, adsorption and separation carrier material; carrying out stepwise separation through stepwise controlling the pH value of Camellia nitidissima Chi concentrated solution and adjusting the isoelectric points of the amino acid active ingredients, wherein the amino acid active ingredients comprise aspartic acid, threonine, serine, glutamic acid, proline and glycine, and the pH values of the aspartic acid, the threonine, the serine, the glutamic acid, the proline and the glycine corresponding to the stepwise separated isoelectric points are less than 2.77, 5.98-6.15, 3.23-5.67, 2.78-3.21, 6.17-6.29 and 5.69-5.96. The method for stepwise separating amino acid active ingredients of Camellia nitidissima Chi has the characteristics of superior selectivity, superior separation speed, good product purity and low cost.