360 results about "Acid derivative" patented technology

The invention discloses an oil-controlling and acne-removing synergistic composition which comprises the following components in percentage by weight: 0.8 to 2.0 percent of succinic acid, 0.3 to 1.0 percent of salicylic acid derivative and 0.5 to 1.5 percent of PCA (Principal Component Analysis) zinc. The invention also provides a sustained-release body. The sustained-release body is prepared from the following components in percentage by weight: 0.8 to 2.0 percent of succinic acid, 0.3 to 1.0 percent of salicylic acid derivative, 0.5 to 1.5 percent of PCA zinc, 1.0 to 2.5 percent of lactobionic acid, 1.0 to 3.0 percent of lactobacillus fermentation product, 2.0 to 4.0 percent of aminated modified diatomite and 0.1 to 0.3 percent of citric acid. The invention also provides a preparation method and application of the sustained release body. The acne-removing shampoo has low irritation, and can be used for controlling oil and removing acnes for a long time and efficiently dredging hair follicles.

Provided are: a liquid crystal aligning agent which contains two or more polyamic acids and in which deterioration in liquid crystal aligning properties when stored at room temperature is suppressed; a liquid crystal alignment film obtained from the liquid crystal aligning agent; and a liquid crystal display element. The liquid crystal aligning agent is characterized by containing the following polymer (A) and polymer (B). Polymer (A): a polyamic acid (A) having a structural unit derived from a tetracarboxylic acid derivative and a structural unit derived from a diamine, the polyamic acid containing, as the structural unit derived from the tetracarboxylic acid derivative, a structural unit (a-1Ta) represented by formula (1Ta), and containing, as the structural unit derived from the diamine, a structural unit (a-1Da) represented by formula (1Da), at least a part of the terminal of the polyamic acid (A) contains a non-amino group, the non-amino group is a functional group represented by structural formula (E), and the presence rate of the terminal amino group in the polyamic acid (A) is 60% or less based on the total terminal of the polyamic acid (A). Polymer (B): a polyamic acid (B) having a structural unit derived from a tetracarboxylic acid derivative and a structural unit derived from a diamine, the polyamic acid including a structural unit (b-1Tb) represented by formula (1Tb) as the structural unit derived from the tetracarboxylic acid derivative, and including a structural unit (b-1Db) represented by formula (1Db) as the structural unit derived from the diamine. (Definition of each symbol is as defined in the specification) (Definition of each symbol is as defined in the specification) (Definition of each symbol is as defined in the specification) (Definition of each symbol is as defined in the specification)

The invention discloses a preserving fluid for stably preserving sample DNA at normal temperature and a preparation method thereof, and belongs to the technical field of biological sample preservation. The preserving fluid comprises a lysis system, a nucleic acid protection system and a buffering and stabilizing system, the cracking system comprises a composite surfactant and an enzymolysis auxiliary agent; the composite surface active agent is prepared from polyether polyol fatty acid ester and cocamidopropyl hydroxy sulfobetaine; the enzymolysis auxiliary agent comprises lysozyme Lyso-V and protease K; the nucleic acid protection system comprises a nitrogen heterocyclic polyamine-carboxylic acid derivative and dextran sulfate; the nitrogen heterocyclic polyamine-carboxylic acid derivative comprises 1, 4, 7, 10-tetraazacyclododecane-N, N ', N' ', N ''tetraacetic acid, 1, 4, 7-triazacyclononane-N, N', N''-triacetic acid, disodium ethylene diamine tetraacetate-nitrogen heterocyclic derivative, and diethylenetriamine pentaacetic acid-piperazine derivative, and the nitrogen heterocyclic polyamine-carboxylic acid derivative comprises 1, 4, 7, 10-tetraazacyclododecane-N, N ', N '', N'' tetraacetic acid, 1, 4, 7-triazacyclononane-N, N', N ''-triacetic acid. The buffering and stabilizing system comprises an amphoteric buffering agent and a polymer stabilizer; the amphoteric buffering agent comprises 2-(N-morpholino) ethanesulfonic acid and N-tri (hydroxymethyl) methylglycine.

The application provides a starch-indole acid derivative and a preparation method and application thereof, and relates to the technical field of modified starches. The starch-indole acid derivative refers to esterified starch generated by esterification reaction of starch, a condensing agent and alkali and indole acid. The starch-indole acid derivative has high resistance and can resist degradation of the stomach and small intestine. After reaching the colon site, the starch-indole acid derivative can be fermented by intestinal flora to release indole acid beneficial to intestinal health. Compared with traditional drug delivery modes such as intragastric administration and intraperitoneal injection, the starch-indole acid derivative has obvious advantages and can significantly increase the content of indole acid in the colon and hepatic portal vein blood. In addition, indole acid can activate an aromatic hydrocarbon receptor to play an immunoregulatory role. The immunoregulatory role of indole acid is superimposed on the regulation role of short-chain fatty acids released by starch fermentation by intestinal flora, so that a product playing an immunoregulatory role through multiple immune system signal pathways is provided.

The invention relates to preparation and application of a desoxyribonucleic acid and desoxyribonucleic acid derivative transdermal delivery system, and belongs to the technical field of biological medicine and skin care products. Desoxyribonucleic acid and derivatives thereof have the effects of resisting aging, repairing and the like, but are difficult to penetrate through a skin barrier due to large molecular weight and strong polarity. According to the invention, hydroxyethyl chitosan, desoxyribonucleic acid and derivatives thereof are combined through electrostatic interaction to form the nano-composite. The compound is small in particle size and can promote transdermal absorption through hair follicle or cuticle gaps. The preparation method is simple, does not need an auxiliary reagent, and comprises the step of mixing a hydroxyethyl chitosan solution and a deoxyribonucleic acid derivative solution. Experiments show that the compound significantly enhances the transdermal efficiency, and has the effects of promoting cell repair and proliferation and resisting inflammation. The composition can be used for skin care products, and is high in safety and wide in application prospect.

Provided are: a liquid crystal aligning agent which contains two or more types of polyamic acids and which suppresses variations in the pretilt angle of a liquid crystal aligning film when stored at room temperature; a liquid crystal aligning film obtained from the liquid crystal aligning agent; and a liquid crystal display element. The liquid crystal aligning agent is characterized in that the liquid crystal aligning agent can form a liquid crystal alignment film with a pretilt angle of more than 0 degree and less than 3 degrees, and the liquid crystal aligning agent contains the following polymer (A) and polymer (B) or the following polymer (B) and polymer (B '). (Here, polymer (A) does not include polymer (B)) Polymer (A): a polyamic acid (A) having a structural unit derived from a tetracarboxylic acid derivative and a structural unit derived from a diamine, the polyamic acid containing, as the structural unit derived from the tetracarboxylic acid derivative, a structural unit (a-1Ta) represented by formula (1Ta) and containing, as the structural unit derived from the diamine, a structural unit (a-1Da) represented by formula (1Da). Polymer (B): a polyamic acid (B) having a structural unit derived from a tetracarboxylic acid derivative and a structural unit derived from a diamine, the polyamic acid containing, as the structural unit derived from the tetracarboxylic acid derivative, a structural unit (b-1Tb) represented by formula (1Tb), and containing, as the structural unit derived from the diamine, a structural unit (b-1Db) represented by formula (1Db). At least a part of the terminal of the polyamic acid (B) contains a non-amino group, the non-amino group is a functional group represented by structural formula (E), and the presence rate of the terminal amino group in the polyamic acid (B) is 60% or less based on the total terminal of the polyamic acid (B). Polymer (B '): a polyamic acid (B') having a structural unit derived from a tetracarboxylic acid derivative and a structural unit derived from a diamine, the polyamic acid containing a structural unit (b-1Tb) represented by formula (1Tb) as the structural unit derived from the tetracarboxylic acid derivative and not containing a structural unit (a-1Da) represented by formula (1Ta), and the polyamic acid containing a structural unit (b-1Da) represented by formula (1Ta) as the structural unit derived from the diamine as the structural unit derived from the diamine. The polyamic acid (B) contains a structural unit (b-1Db) represented by formula (1Db) or a structural unit (b-1Db ') represented by formula (1Db'), and the content of terminal amino groups in the polyamic acid (B ') is greater than 60% based on the total terminals of the polyamic acid (B). (Definition of each symbol is as defined in the specification) (Definition of each symbol is as defined in the specification) (Definition of each symbol is as defined in the specification) (Definition of each symbol is as defined in the specification) .

The present disclosure relates to analytical LC-MS / MS methods for second tier testing in Newborn Screening Program (2ndtier test or 2TT) for the simultaneous measuring of organic acids, acylcarnitines, aminoacids derivatives and acylglicines in dried blood spot samples.

The invention relates to a sustained-release pharmaceutical preparation of a fused tricyclic gamma-amino acid derivative and a preparation method of the sustained-release pharmaceutical preparation. The fused tricyclic gamma-amino acid derivative is a compound as shown in a formula (I) or a stereoisomer, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a co-crystal thereof.

The invention relates to an amino acid derivative carrier as well as a preparation method and application thereof, and belongs to the technical field of biology, and the preparation method of the amino acid derivative carrier comprises the following steps: providing a cationic amino acid monomer and a neutral-polyanion block polymer template; a cationic amino acid monomer, a neutral-polyanion block polymer template, a cross-linking agent and a photoinitiator are mixed and react under the irradiation of ultraviolet light to obtain an amino acid derivative carrier, and the amino acid derivative carrier is cationic nanogel. The amino acid derivative carrier prepared by the preparation method disclosed by the invention can be used as a nucleic acid drug delivery carrier, and has the advantages of strong nucleic acid loading capacity, high transfection efficiency, safety and the like.

The invention relates to a non-gadolinium magnetic resonance contrast agent and a preparation method thereof, and belongs to the field of contrast agents. The invention aims to provide a non-gadolinium contrast agent with high biological safety aiming at the risks of renal fibrosis and cerebral deposition existing in a gadolinium-based magnetic resonance contrast agent. The invention provides a phosphate group modified non-gadolinium magnetic resonance contrast agent. The phosphate group modified non-gadolinium magnetic resonance contrast agent consists of a ligand of a phosphate group substituted trans-cyclohexanediamine tetraacetic acid derivative (tmPCDTA or tqPCDTA) and metal ions Fe < 3 + > or Mn < 2 + >, the contrast agent disclosed by the invention is high in biological safety: endogenous Fe < 3 + > / Mn < 2 + > is used for replacing gadolinium, and cell experiments prove that the survival rate of 4T1 cells is not influenced at the concentration of 500 mu M; clinical applicability is high, kidney excretion is rapid, bladder signals are enhanced 3-5 minutes after mouse intravenous injection, and liver retention is avoided.

The application belongs to the technical field of organic synthesis, and particularly relates to a synthesis method of chiral N-alkyl amino acid derivatives. The synthesis method is improved on the basis of the synthesis method of chiral N-alkyl amino acid derivatives in the prior art, has mild reaction conditions, high yield, is beneficial to industrial large-scale production, and solves the amplification effect of the synthesis method in the prior art.

The present invention provides a liquid crystal aligning agent that can form a liquid crystal alignment film having excellent mechanical properties, and can provide a liquid crystal element that exhibits good liquid crystal alignment properties, a high voltage holding ratio, and excellent reliability. [Solution] A liquid crystal aligning agent contains polymer (A), which is at least one selected from the group consisting of polyamic acid, polyamic acid ester, and polyimide, and is obtained using two or more tetracarboxylic acid derivatives including a compound represented by formula (1), and satisfies at least one of requirements 1 and 2. Requirement 1: Further, polymer (B) different from polymer (A) is contained. Requirement 2: Two or more types of polymer (A) are contained. In formula (1), Y 1 and Y 2 are each independently a tetravalent organic group. 1 is a divalent organic group. TIFF0007758236000037.tif24168

Described is a compound for substituting amino acids of proteins or peptides, wherein the compound has the formula (1)wherein the stereocenter C1* represents CH that either results in the D- or L-form of the compound of formula (1); A− is a negatively charged ion compensating the positive charge; X1 is H or an amine protecting group; X2 is OH, an ester residue or an amide residue or an activated carboxylic acid derivate to be used for the formation of an amide bond; Y1, Y2 and Y3 are independently from each other a C1-C6 alkyl, and Z1 and Z2 are independently from each other a nucleobase, a C1 to C16 alkyl group, an aromatic residue or a heteroaromatic residue, wherein the aromatic residue or the heteroaromatic residue contains one 5, 6, or 7-membered ring or two condensed 5, 6, or 7-membered rings sharing two carbon atoms, wherein the aromatic residue or the heteroaromatic residue can be substituted by a linear or branched C1 to C16 alkyl group and / or a further aromatic group. Furthermore, a method for preparing this compound and proteins and peptides containing this compound are disclosed.

The present invention relates to a novel synthesis of 2-fluoromethyl acrylate (MFA), which is a key precursor for the production of Veltassa® (Patiromer). The process according to the invention obtains MFA (III) by reacting an alpha-substituted beta-hydroxy propionic acid derivative (I) via one or more intermediate steps involving one or more alpha-, beta-substituted propionic acid derivatives (II).

The invention provides a method for synergistically removing impurities through pH regulation and complexing of ionic rare earth ore leachate, the ionic rare earth ore leachate is stirred and mixed uniformly, a plant polyphenol sulfonic acid derivative complexing agent is added, the complexing agent is prepared through sulfonation, neutralization, concentration and drying by taking gallic acid as a raw material, and the complexing agent can automatically regulate the pH value of the solution and stabilize the pH value at 5.1-5.3; under the condition, phenolic hydroxyl groups, carboxyl groups and sulfonic functional groups in complexing agent molecules preferentially form stable precipitates with impurity ions such as Al < 3 + > and Fe < 3 + > in the leachate, and the complexing effect with rare earth ions (RE < 3 + >) is weak; and after the reaction is completed, carrying out solid-liquid separation to obtain the purified leachate and impurity-containing precipitation slag. The method solves the problem of ammonia nitrogen pollution caused by use of ammonium bicarbonate, ammonia water and other ammonium salts in the traditional process, is a novel method with high impurity removal rate, simple process flow and environmental friendliness, and is suitable for industrial application.

The invention relates to the technical field of organic chemical synthesis, and discloses a method for preparing a chlorogenic acid derivative by condensing chlorogenic acid and a bifunctional amino acid derivative, which comprises the following step: in the presence of EDCI and HOBt, reacting chlorogenic acid with the bifunctional amino acid derivative in a DMF solvent to obtain the chlorogenic acid derivative. The method does not need to protect hydroxyl, the synthesis steps are simple, and the reaction is green, environment-friendly and pollution-free.

This invention discloses a 1,6-diamino-dibenzo[a,o]perylene-7,16-dione-2,5-disulfonic acid derivative, its preparation method, and its application. Using a vat dye derivative PR177 as the parent material, a 4,4'-diamino-1,1'-dianthraquinone-3,3'-disulfonic acid derivative is formed by the Ullmann condensation of a 1-amino-4-bromoanthraquinone-2-sulfonic acid derivative. This derivative is then cyclically closed via the McMurray reaction to form the 1,6-diamino-dibenzo[a,o]perylene-7,16-dione-2,5-disulfonic acid derivative. This allows for direct dyeing without the use of sodium hydrosulfite. Compared to soluble vat dyes, it is stable when exposed to air. Furthermore, due to its good planarity, it exhibits excellent dyeing performance as an acid dye. It combines the advantages of good directness of vat dyes and good water solubility of acid dyes, especially showing excellent color fastness and exhaustion rate in wool dyeing.

The present invention relates to pharmaceutical preparations containing as active ingredients 3-N-formylhydroxylaminopropylphosphonic acid derivatives or 3-N-acetylhydroxylaminopropylphosphonic acid derivatives in combination with clindamycin and artesunate for the treatment of malaria, in particular for the acute therapy of cerebral malaria, and to an associated dosage, in particular for the patient group of children.

The invention relates to a liquid crystal aligning agent, a liquid crystal alignment film, a manufacturing method of the liquid crystal alignment film, a liquid crystal element and a compound. A liquid crystal aligning agent which contains a polymer (A) that is at least one selected from the group consisting of polyamic acids, polyamic acid esters and polyimides and is obtained using two or more tetracarboxylic acid derivatives containing compounds represented by formula (1), and which satisfies at least one of requirements 1 and 2. Condition 1: In addition, a polymer (B) different from the polymer (A) is contained. Requirement 2: Two or more polymers (A) are contained. In formula (1), Y1 and Y2 independently represent a tetravalent organic group. And X1 represents a divalent organic group.

This application relates to the fields of chemistry and biomedicine, specifically to a tofenamic acid lipid composition, its preparation method, and its application. A tofenamic acid derivative is obtained by reacting a morpholine solution with tofenamic acid, ethyldimethylaminopropylcarbodiimide, and 4-dimethylaminopyridine, followed by purification. The morpholine in the morpholine solution is an N-alkylmorpholine compound. The tofenamic acid derivative is used to prepare tofenamic acid prodrug liposomes via ethanol injection, which are then used in combination with a STING agonist. The synergistic effect of the combined treatment stems from the dual regulation of the tumor immune microenvironment (TME), overcoming the immune escape induced by STING monotherapy. After STING agonist treatment, the intratumoral COX-2 / PGE2 axis is activated, leading to immunosuppression. The combination of tofenamic acid liposomes and a STING agonist inhibits COX-2, thus relieving this negative feedback loop.

Use of a composition containing a 5-oxo-pyrrolidine-2-carboxylic acid derivative with formula IIa for the fixation and optional preservation of biological organs and / or tissues and / or whole body specimens and / or corpses.

The application belongs to the technical field of chiral catalysis and medicine, and particularly relates to a dendritic chiral phase transfer catalyst, a structural formula of which is shown as formula (I) or formula (II). A series of chiral phase transfer catalysts based on soluble dendritic macromolecules are synthesized by changing the number of repeated carbon chains on the core molecular structure, and it is found through catalyzing asymmetric alkylation of amino acid derivatives that the dendritic chiral phase transfer catalysts provided by the application have excellent yield and enantioselectivity in catalyzing preparation of chiral amino acid derivatives.

An environmental cracking inhibitor includes a base corrosion inhibitor and a sulfur compound modifier. The base corrosion inhibitor can be an imidazoline, an amine, a quaternary amine, a fatty acid derivative, a phosphate ester, or combinations thereof. The sulfur compound modifier can have the general formula HS—X, where X is a heteroatom substituted alkyl, cycloalkyl, aryl, and / or alkylaryl group. Suitable heteroatoms are sulfur, oxygen, phosphorus, nitrogen, and combinations thereof. The sulfur compound modifier can be 2 mercaptoethanol, cysteamine, or a cysteamine salt.

The invention belongs to the field of biological medicine and beauty makeup health care, and provides a preparation method and application of a soothing oat alkali-amino acid derivative co-assembly, the preparation method comprises the following steps: S1, adding an amino acid derivative into an alcohol-water mixed solution, heating, slowly adding oat alkali, keeping the temperature, adding cyclodextrin, and fully mixing; and S2, cooling the mixture obtained in the S1 to room temperature, centrifuging, taking supernate, carrying out suction filtration, collecting filtrate, carrying out rotary evaporation until the filtrate is pasty, carrying out vacuum drying, grinding, and carrying out sealed storage, so as to obtain the soothing oat alkali-amino acid derivative co-assembly. Compared with similar products sold in the market, the oat alkali, the amino acid derivative and the cyclodextrin are organically combined, the solubility of the oat alkali is improved by more than 1000 times through the synergistic effect of the hydration shell of the amino acid derivative and the inclusion effect of the cyclodextrin, and meanwhile, the solubility of the oat alkali is improved based on the synergistic effect of the oat alkali and the amino acid derivative. The co-assembly can resist inflammation, relieve allergy, resist aging and repair for a long time, and comprehensively meet the product requirements of mitochondria energy skin care.

The invention discloses an alpha-aminophosphoryl derivative as well as a preparation method and application thereof. The method comprises the following steps: by taking a quinoline derivative as a raw material and tetrahydrofuran (THF) as a solvent, adding boron trifluoride diethyl etherate in a nitrogen system at the reaction temperature of 0 DEG C, stirring for 15 minutes, reducing the temperature of the reaction system to T1 (-60 DEG C to-30 DEG C), adding a Grignard reagent into the reaction system, and reacting for 30 minutes to obtain a solution A; dissolving a phosphorus reagent in the organic solvent at room temperature in a nitrogen atmosphere to obtain a solution B; and adding the solution A into the solution B, reacting for 6-15 hours at the reaction temperature T2 (0-50 DEG C), and after the reaction is finished, extracting, concentrating and carrying out column chromatography to obtain the target product alpha-aminophosphoryl derivative. The invention provides a novel synthetic route for preparing the alpha-aminophosphonyl derivative, and various phosphorus reagents such as diaryl phosphorus oxide and phosphite ester can be compatible with the reaction. The alpha-aminophosphoryl derivative synthesized by the invention has a good antibacterial effect on gram-positive bacteria, especially staphylococcus aureus.

The invention discloses a ferulic acid derivative and a preparation method and application thereof.The ferulic acid derivative is a compound shown in the formula (I) or pharmaceutically acceptable salt of the compound, and the compound is a natural compound extracted from rubus corchorifolius stems, has anti-inflammatory activity and anti-tumor activity and has the potential of being developed into anti-inflammatory or anti-tumor drugs. Or as a lead compound.

New derivatives of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl) phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo [3,4c] pyridine-3-carboxamide (Apixaban) able to increase its water solubility. These derivatives are cocrystals derivatives ofApixaban of different acids, from which the most outstanding are the following: Apixaban Malonic Acid derivative, Apixaban-a-Ketoglutaric Acid derivative, Apixaban-Gallic Acid derivative, Apixaban-Maleic Acid derivative, Apixaban-L-Tartaric Acid derivative, and Apixaban Citric Acid derivative.

The present disclosure relates to a method for synthesizing a substituted phenylpropionic acid derivative. Specifically, the present disclosure relates to a method for preparing a compound as represented by formula I or a pharmaceutically acceptable salt thereof, which method exhibits a good yield.

The purpose of the present invention is to provide a plant activator which is low in soil contamination and toxicity and excellent in plant growth promoting effect. A plant activator characterized by containing, as an active ingredient, a hydroxide fatty acid derivative having a structural formula (I) and / or (II), or a salt or ester thereof. (In the formula, R1 is a linear or branched hydrocarbon group having 4-12 carbon atoms, may include one or more double bonds and / or OH groups, and if a double bond is included, the position of the double bond is not limited; r2 is a linear or branched hydrocarbon group having 2 to 8 carbon atoms, may contain one or more double bonds and / or OH groups, and if a double bond is contained, the position of the double bond is not limited. HOOC-(R1)-CH (OH)-CH = CH-CH (OH)-R2 (I) HOOC-(R1)-CH (OH)-CH = CH-CH (OH)-R2 (II)

The present invention relates to a 6-Aryl imidazo[2,1-b]thi / oxazole-2-carboxilic acid derivative, and the compound according to the present invention is useful as a JNK3 inhibitor capable of acting specifically against JNK3. The inhibitory activity of the compound according to the present invention against JNK3 is relatively higher than that against JNK1 and JNK2, and thus it can be used as an Alzheimer's disease therapeutic agent with a low risk of side effects.