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1500 results about "Racemization" patented technology

In chemistry, Racemization is a conversion, by heat or by chemical reaction, of an optically active compound into an optically inactive form which half of the optically active substance becomes its mirror image (enantiomer) referred as racemic mixtures(i.e. contain equal amount of '+' and '-' forms) .If the racemization results in a mixture where the D and L enantiomers are present in equal quantities, the resulting sample is described as a racemic mixture or a racemate. Racemization can proceed through a number of different mechanisms, and it has particular significance in pharmacology as different enantiomers may have different pharmaceutical effects.

2-Aryl Imidazo[1,2-a]Pyridine-3-Acetamide Derivatives, Preparation Methods and Uses Thereof

Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification. Preparation methods of said compounds and use of said compounds in treating and / or preventing central nervous system disease associated with TSPO functional disorder
Owner:INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A

Ketone bodies and ketone body esters as blood lipid lowering agents

ActiveUS9211275B2Reduce serum cholesterol and/or triglyceride levelLowering of total serum cholesterol levelHydroxy compound active ingredientsMetabolism disorderChemistryNutritional composition
The subject disclosure provides compositions for reducing serum cholesterol and / or triglyceride levels in subjects. These compositions can comprise racemic β-hydroxybutyrate or D-β-hydroxybutyrate, optionally in the acid form, physiologically compatible salts of racemic β-hydroxybutyrate or D-β-hydroxybutyrate, esters of D-β-hydroxybutyrate, oligomers of D-β-hydroxybutyrate containing from 2 to 20 or more monomeric units in either linear or cyclic form, racemic 1,3 butandiol or R-1,3 butandiol alone and can be, optionally, administered in conjunction with a low fat diet to a subject. Alternatively, compositions comprising racemic β-hydroxybutyrate or D-β-hydroxybutyrate, optionally in the acid form, physiologically compatible salts of racemic β-hydroxybutyrate or D-β-hydroxybutyrate, esters of D-β-hydroxybutyrate, oligomers of D-β-hydroxybutyrate containing from 2 to 20 or more monomeric units in either linear or cyclic form, racemic 1,3 butandiol, R-1,3 butandiol or combinations thereof can be formulated as nutritional supplements (also referred to as nutritional compositions) or incorporated into therapeutic compositions containing a) anti-hypertensive agents; b) anti-inflammatory agents; c) glucose lowering agents; or d) anti-lipemic agents) which are administered to a subject, optionally in combination with a low fat diet, in order to cause a reduction or lowering of: serum cholesterol levels; triglyceride levels; serum glucose levels, serum homocysteine levels, inflammatory proteins (e.g., C reactive protein) and / or hypertension in treated subjects. Alternatively, compositions disclosed herein can be administered alone, or in combination with other therapeutic agents to prevent or reverse vascular disease.
Owner:OXFORD UNIV INNOVATION LTD +1

Stereoisomers of p-hydroxy-milnacipran, and methods of use thereof

ActiveUS7038085B2Equal potencyBiocideNervous disorderAdrenergicChemistry
The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (−)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient. Finally, the present invention relates to methods of treating mammals suffering from various afflictions, e.g., depression, chronic pain, or fibromyalgia, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of the present invention.
Owner:COLLEGIUM PHARMA INC

Method for catalyzing dynamic kinetic resolution of arylamine via racemization catalyst

The invention discloses a method for catalyzing dynamic kinetic resolution of arylamine via a racemization catalyst, comprising the following steps of: 1) adding p-chlorophenol, n-pentanoic acid, dicyclohexylcarbodiimide and 4-dimethylamino-pyridine, and carrying out mixing, filtration, drying, concentration and column chromatography to obtain a pentanoic acid p-chlorophenyl ester acyl donor; 2) carrying out coprecipitation on magnesium chloride solution and aluminum chloride solution and carrying out water-heat treatment to obtain chloridion intercalated hydrotalcite, adding the chloridion intercalated hydrotalcite in lauryl sodium sulfate aqueous solution, and carrying out backflow, cooling, centrifugation, water washing, acetone washing and drying to obtain a carrier; 3) adding palladium salt and the carrier, and carrying out heating, ascorbic acid addition, centrifugation, water washing, acetone washing and freeze-drying to obtain the racemization catalyst; and 4) adding arylamine, the acyl donor, lipase and the racemization catalyst in toluene and placing in a stainless steel reactor to add hydrogen so as to obtain amide. The method provided by the invention is used for catalyzing the dynamic kinetic resolution of arylamine, has rapid reaction rate, low temperature, high conversion rate and high product optical purity, and has great application value.
Owner:ZHEJIANG UNIV

Preparation method and application for phosphine-oxazoline ligand, and ionic metal complex, enantiomer or racemate thereof

The invention discloses a preparation method and an application for phosphine-oxazoline ligand, and ionic metal complex, enantiomer or racemate thereof. The ligand and the ionic metal complex thereof have the following structural formulas. The phosphine ligand related by the invention employs biphenyl as a skeleton, and realizes completely transmission from planar chirality to axial chirality through an asymmetric desymmerization. The synthetic method is simple and economic, omits a common and complex chiral separation process in the preparation of the chiral ligand. The obtained chiral ligand has the advantages of high reactive activity, good enantiomorphous selectivity and the like in a model reaction.
Owner:SUN YAT SEN UNIV

Preparation method and application of bencycloquidium bromide optical isomer and composition of bencycloquidium bromide optical isomer

The invention relates to the technical field of medicaments, in particular to a preparation method and application of a bencycloquidium bromide optical isomer. The isomer is obtained by a chemical resolution method, the activity of the isomer is far beyond that of other isomers and racemic forms; when the isomer is taken as a medicament to be taken, the taking dosage is reduced, and side effects caused by other isomers are simultaneously eliminated; moreover, the bencycloquidium bromide optical isomer has a romurtide cyclodextrin inclusion compound with higher pharmaceutical value and a preparation thereof. The romurtide is coated by the cyclodextrin, so that the problems of low water-solubility, unstable preparation prepared by the romurtide cyclodextrin inclusion compound and the like are solved. The romurtide cyclodextrin inclusion compound has the characteristics of high stability, good water-solubility, and low toxic and side effects, and is a quite good immunomodulator.
Owner:YINGU PHARMA

Process for controlling polyvinylbutyral physical properties by controlling stereochemistry of same

The present invention is method for controlling the stereoisomerism of PVB resin as well as a PVB resin having a meso / racemic stereoisomer ratio of from about 2.5 to about 5.0. Manipulation of the PVB stereoisomer ratio can provide an additional method of controlling the physical properties of PVB, in addition to or in lieu of changing additives or manipulating the PVB composition.
Owner:KURARAY AMERICA INC

Racemization control method for under-actuated satellite

The invention discloses a racemization control method for an under-actuated satellite. The method comprises the following steps of: (1) determining an initial self-rotating shaft position of the under-actuated satellite by the adoption of an attitude sensor, and determining a direction and an amount of racemization control according to a position of a target self-rotating shaft; (2) determining geometric relationship between an injection control moment and a racemization control direction produced by each injection control engine, and selecting the injection control engine with the largest amount of the injection control moment in the racemization control direction as a racemization control engine; and (3) in a preliminary stage of racemization, adopting an integer multiple self-rotating period fully spraying method, in a final phase of racemization, adopting a symmetrical point spraying method, using the racemization control engine to carry out racemization control, after primary racemization is finished, enabling a planet to be naturally damped for a period of time, and then carrying out the next racemization control until a self-rotating shaft of a satellite reaches a target self-rotating shaft. According to the method, the operation of a racemization control strategy is simple and convenient, and nutation produced by racemization control can be reduced at the same time.
Owner:BEIJING INST OF CONTROL ENG
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