120 results about "Propanamide" patented technology

Stable and bioavailable formulations and dosage forms comprising a dispersion (e.g., spray-dried dispersion) of solid amorphous 6-(cyclopropancamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide (Formula (I): BMS-986165) in a solid polymer matrix are provided for the treatment of auto-immune and auto-inflammatory diseases such as an inflammatory bowel disease (IBD) and psoriasis.

The present invention belongs to the technical field of petroleum fracturing production enhancement and modification, and specifically discloses a fracturing fluid pre-fluid for optimizing the size of in-situ autogenous proppant and its application, which is used to solve the problem of small particle size of proppant particles generated by hydrothermal reaction of formation minerals. The fracturing fluid pre-fluid is suitable for calcium-rich reservoirs and is composed of clean water, phosphate, pH regulator and Ca 2+ The chelating agent composition comprises 1 to 10 parts by weight of phosphate relative to 100 parts by weight of clean water, a volume molar concentration of the pH regulator is 1 to 5 mol / L, and Ca 2+ The molar concentration of the chelating agent is 0.001~1mol / L; the pH regulator is urea, ammonia, propionamide, etc. 2+ The chelating agent is EDTA, glutamic acid, etc. The present invention increases the average particle size of proppant particles generated by hydrothermal reaction of formation minerals, thereby improving the supporting effect thereof in micro-fractures of the formation.

The invention belongs to the technical field of petroleum fracturing yield increase transformation, and particularly discloses fracturing fluid prepad fluid for optimizing the size of an in-situ authigenic proppant and application of the fracturing fluid prepad fluid, which are used for solving the problem of small particle size of proppant particles generated by a formation mineral hydrothermal reaction in the prior art. The fracturing fluid prepad fluid is suitable for a calcium-rich reservoir and is composed of clear water, phosphate, a pH regulator and a Ca < 2 + > chelating agent, relative to 100 parts by weight of clear water, the content of the phosphate is 1-10 parts by weight, the volume molar concentration of the pH regulator is 1-5 mol / L, and the volume molar concentration of the Ca < 2 + > chelating agent is 0.001-1 mol / L; the pH regulator is urea, ammonia water, propanamide and the like, and the Ca < 2 + > chelating agent is EDTA (Ethylene Diamine Tetraacetic Acid), glutamic acid and the like. The average particle size of the proppant particles generated by the formation mineral hydrothermal reaction is increased, and the supporting effect of the proppant particles in formation microfractures is improved.

Disclosed herein is a compound that is (R)-(2-(3-((((2-ethylbutanoyl)oxy)methoxy)carbonyl)-2-hydroxyphenyl)-1-propionamidoethyl)boronic acid citrate coordination complex, or a pharmaceutically acceptable salt or solvate thereof. Also disclosed herein are methods of treating a bacterial with a compound that is (R)-(2-(3-((((2-ethylbutanoyl)oxy)methoxy)carbonyl)-2-hydroxyphenyl)-1-propionamidoethyl)boronic acid citrate coordination complex, or a pharmaceutically acceptable salt or solvate thereof in combination with ceftibuten.

The application belongs to the technical field of organic synthesis, and particularly relates to a preparation method of 5-chloro-2-methyl-4-isothiazoline-3-ketone. N,N'-dimethyl-3,3'-dithiodipropionamide is mixed with ethyl acetate, cooled to 8-10 DEG C, and chlorine is added in stages, and the reaction is continued after the chlorine is passed; the adding mode of the chlorine is as follows: in the first stage, 25-30% of the chlorine is passed in 0.5h while maintaining the temperature of the reaction system at 10-12 DEG C; in the second stage, 25-30% of the chlorine is passed in 1h while maintaining the temperature of the reaction system at 13-14 DEG C; and in the third stage, the remaining chlorine is passed in 1.5h while maintaining the temperature of the reaction system at 15-18 DEG C. The application controls the generation of 5-chloro-2-methyl-4-isothiazoline-3-ketone by controlling the adding amount of the chlorine and the reaction temperature, and improves the yield of 5-chloro-2-methyl-4-isothiazoline-3-ketone.

The invention discloses application of a propanamide derivative in preparation of a medicine for treating nervous system diseases, and belongs to the technical field of medicines, and the propanamide derivative is N-[(6-methoxy-1H-benzimidazole-2-yl) methyl]-3-(pyridine-3-yl) propanamide. The invention discloses the neuroprotection application of the propanamide derivative for the first time by adopting the propanamide derivative to prepare a medicine for treating nervous system diseases, and the protection efficacy of the propanamide derivative is equivalent to that of a positive medicine MK-801.

The present invention relates to a composition containing (a) a guanidine and / or an unsubstituted guanidine salt, and (b) at least one further component selected from the group consisting of 5-chloro-2-methyl-4-isothiazolin-3-one, 2-methyl-4-isothiazolin-3-one, 1, 2-benzisothiazolin-3-one, N-butyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, the cleaning agent is prepared from 2-benzisothiazolin-3-one, octyl isothiazolinone, bronopol, dibromo-nitrilopropionamide, dibromo-dicyanobutane, butyl carbamic acid iodopropynyl ester, aminomethyl propanol, aminoethyl propylene glycol, monoethanolamine, ethylhexylglycerin, hexylglycerin, 1, 2-pentanediol, 1, 2-hexanediol, 1, 2-heptanediol, 1, 2-octylene glycol, phenoxy ethanol and phenethyl alcohol. The cleaning agent is prepared from phenyl propanol, benzyl alcohol, isopropanol, ethylenediamine tetraacetic acid, (1-hydroxyethylidene) diphosphonic acid, 2-mercaptopyridine sodium oxide, 2-mercaptopyridine zinc oxide, o-phenylphenol, sorbic acid, benzoic acid, salicylic acid, lactic acid, citric acid and zinc. The invention also relates to an industrial product containing components (a) and (b), and to the use of said composition for the preservation of containers and for the preservation of industrial products. The invention also relates to the use of (a) a guanidine and / or an unsubstituted guanidine salt for improving the antimicrobial efficacy of one or more compounds selected from the group (b) described above.

The application belongs to the technical field of dental antibacterial materials, and discloses a kind of nanometer composite antibacterial coating for dental material and preparation method thereof.Method: monomer modified arginine, monomer N-isopropyl acrylamide, monomer methyl hexyl acrylate, initiator azobisdimethylamino propanamide hydrochloride, dispersing agent cetyltrimethylammonium bromide and crosslinking agent N,N-methylene bis(acrylamide) are dissolved in water, and the reaction is carried out under protective atmosphere, dialysis, to obtain nanogel dispersion;The nanogel dispersion is mixed with the nanometer zinc oxide dispersion to obtain a nanogel composite zinc oxide antibacterial coating, and a coating is formed after coating.The nanometer composite antibacterial coating for dental material has excellent retention capacity and antibacterial performance.

This invention discloses a continuous synthesis apparatus and process for chloroamines, belonging to the field of organic synthesis technology. The continuous synthesis apparatus for chloroamines includes, in series, an acetamide sodium salt reactor, an allylamide reactor, a chloroamine synthesis reactor, and an automatic phase separator. The lower liquid outlet of the automatic phase separator is connected to a solvent removal tower, and the upper liquid outlet is connected to a dealcoholization tower. A condenser and an alcohol receiving tank are connected in series at the top of the dealcoholization tower, and the bottom of the dealcoholization tower is connected to an alkalization reactor, an automatic phase separator, and a product distillation tower. This invention also discloses a continuous synthesis process for chloroamines. The equipment of this invention can accurately monitor the reaction, shorten the reaction time, significantly improve product yield and output, and ensure stable product quality.

The invention discloses a biological catalytic synthesis method of chiral 2-amino-1-methylenepropanamide and an enzyme catalyst of the chiral 2-amino-1-methylenepropanamide. According to the present invention, one or more key amino acids in the amide hydrolase derived from Rhodococcus erythropolis AJ270 are subjected to mutation to obtain the mutant, the mutant has characteristics of high or reverse enantioselectivity when the hydrolysis reaction of the racemization 2-substituted-2-amino-1-methylene propanamide substrate is catalyzed, and the chiral compound is obtained with the high ee value; and an enantiomer of a wild type amide hydrolase catalytic product can be obtained. A method for preparing chiral 2-substituted-2-amino-1-methylene propanamide by using the mutant through biological catalysis has the characteristics of simplicity and convenience in operation, high reaction efficiency, mild reaction conditions, high enantioselectivity, easiness in product separation and high product purity, and has a very good application prospect.

The invention relates to preparation and application of diarylamine compounds containing a propionamido indole structure. The compounds have a structural formula as shown in a general formula (I). The invention relates to a compound shown in a general formula (I), which has a strong effect of inhibiting L858R / T790M / C797S and Del19 / T790M / C797S drug-resistant mutant EGFR kinase, and also relates to application of the compound and pharmaceutically acceptable salt thereof in preparation of drugs for treating and / or preventing diseases caused by drug-resistant mutation of EGFR kinase, the invention particularly relates to application in preparation of medicines for treating and / or preventing cancers. The invention also provides a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the pharmaceutical composition. The compound is especially used for preparing drugs for treating and / or preventing lung cancer, and has good antitumor drug development and application prospects. (I)

The application relates to the technical field of drug synthesis, in particular to a synthesis method and application of a 2-(cyclopropylamide)thiazole-4-amide derivative. The thiazole structure is shown in formula I. The preparation method of the 2-(cyclopropylamide)thiazole-4-amide derivative is as follows: the compound shown in formula I is obtained by reacting the compound shown in formula II in the presence of HATU, DIPEA, a primary amine or a secondary amine and tetrahydrofuran. The 2-(cyclopropylamide)thiazole-4-amide derivative has the effect of relieving Alzheimer's disease, and is characterized by strong cholinesterase inhibition activity.

Disclosed herein are crystalline forms of ((2-Ethylbutanoyl)oxy)methyl(R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate. Also disclosed herein are methods of treating a bacterial with a crystalline form of ((2-Ethylbutanoyl)oxy)methyl(R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate.

The application discloses a preparation method of bacteriostatic and deodorant plastic and relates to the technical field of plastics. The self-prepared antibacterial agent is prepared by using triethoxysilane butyraldehyde, 4-chloro-1-butylamine and (R)-2-(dimethylamino) propionamide, the Schiff base structure and the quaternary ammonium structure in the molecular chain of the self-prepared antibacterial agent interact, bacterial growth is effectively inhibited, and then the antibacterial and deodorant properties of the plastic are improved; then porous calcium silicate and porous calcium carbonate are used as deodorant fillers of the plastic, the self-prepared antibacterial agent is used as a crosslinking agent, the fillers and the urea-formaldehyde resin are combined with each other, the uniform dispersion of the fillers is facilitated, meanwhile, a crosslinked network structure is formed in the plastic, and the mechanical properties of the plastic are greatly improved.

The invention discloses a treatment method of a florfenicol by-product N, N-diethyl-2, 3, 3, 3-tetrafluoropropionamide, and belongs to the technical field of chemical engineering, the treatment method comprises a hydrolysis addition reaction and a cyclization reaction; the hydrolysis addition reaction comprises the following steps: mixing N, N-diethyl-2, 3, 3, 3-tetrafluoropropionamide with diethylamine and alkali liquor, and then carrying out hydrolysis reaction and addition reaction to obtain N, N, N ', N'-tetraethyl malonamide; the cyclization reaction comprises the following steps: mixing organic solvent solutions of N, N, N ', N'-tetraethyl malonamide and sodium methoxide, adding a mixed solution of formamidine and an organic solvent, carrying out reflux heat preservation reaction, evaporating materials to dryness, acidifying and filtering. According to the method, the malonamide intermediate is generated through fewer reaction steps, then the 4, 6-dihydroxypyrimidine is prepared, most of materials can be recycled, the atom economy is high, and the pollution to the environment and the post-treatment pressure are also reduced.

The invention relates to the technical field of concrete admixtures, in particular to a micro-crosslinking type water-retaining agent for inhibiting delayed bleeding of concrete and a preparation method of the micro-crosslinking type water-retaining agent. The water-retaining agent takes dodecanoic acid containing halogen and hydroxyl as a raw material to synthesize a 13-membered ring lactone intermediate, the 13-membered ring lactone intermediate reacts with straight-chain saturated dicarboxylic acid to form a linear polyester chain intermediate with an alternating repeating unit, and then 3-aminopropanamide and linear polyethyleneimine are added to prepare the water-retaining agent. The linear polyethyleneimine and halogen atoms in 13-membered ring lactone on a linear polyester chain intermediate are subjected to nucleophilic substitution reaction, linear polyethyleneimine is used as a cross-linking agent and subjected to nucleophilic substitution with halogen atoms on different polyester chains through primary amine groups at the two ends of the linear polyethyleneimine, and finally the micro-cross-linking type water-retaining agent is formed. According to the micro-crosslinking type water-retaining agent, the problems of segregation, bleeding and pump blockage in the middle and later periods of concrete premixing are remarkably solved on the premise that the workability of concrete in the early stage of premixing is not influenced, meanwhile, the air content of the concrete is not influenced, and the negative influence on the strength of the concrete is avoided.

The invention relates to the field of food, in particular to an antioxidant and application thereof in food preparation. The invention provides application of N-[2-(3, 4-dimethoxyphenyl) ethyl]-3, 4-dimethoxycinnamic acid amide and / or 3-[(4-amino-2, 2-dioxo-1H-2, 1, 3-benzothiadiazine-5-yl) oxygen]-2, 2-dimethyl-N-propyl propionamide in any of the following items: N-[2-(3, 4-dimethoxyphenyl) ethyl]-3, 4-dimethoxycinnamic acid amide and / or 3-[(4-amino-2, 2-dioxo-1H-2, 1, 3-benzothiadiazine-5-yl) oxygen]-2, 2-dimethyl-N-propyl propionamide. Oxidation resistance; and / or preparing an antioxidant. The antioxidant composition disclosed by the invention has a remarkable protection effect on food containing fat and other photosensitive components, can prevent fat oxidation and attenuation of nutritional components, and keeps fresh sensory experience and nutritional and healthy properties of the food.

This application relates to a method for preparing (S)-2-((3-((benzo[d][1,3]dioxopenta-5-oxy)methyl)benzyl)-amino)propionamide of formula I or a pharmaceutically acceptable salt thereof, and also to an intermediate for preparing the compound. This method is low-cost, simple to operate, safe and environmentally friendly, exhibits high reaction selectivity and high yield, and is suitable for large-scale industrial production.

The application provides a preparation method of chiral alpha-hydroxy-amidoxime ether and belongs to the technical field of organic synthesis. The preparation method of the chiral alpha-hydroxy-amidoxime ether comprises the following steps: S1, protecting the hydroxyl group of chiral alpha-hydroxy propionamide by a protecting group; S2, sequentially reacting the chiral alpha-protecting group-propionamide with an oxonium salt donor and an alkoxyamine hydrochloride to prepare chiral 1-[(E)-alkoxyimino] alpha-protecting group-prop-1-amine; and S3, removing the protecting group from the chiral 1-[(E)-alkoxyimino] alpha-protecting group-prop-1-amine to prepare a product. The application aims to overcome the core defects of a low yield, a high impurity content, a big reagent safety and environmental protection risk, a high pyridine consumption and a complicated operation of an existing process, and develop a new chiral alpha-hydroxy-amidoxime ether synthesis process with high yield, high purity, low cost, high safety and suitability for industrial amplification.

The present invention encompasses a microcrystalline form of (R)-2-(N-[4-amino-5-(4-methoxybenzoyl) thiazol-2-yl]-4-fluoro-anilino) propanamide (I), and a process for the preparation thereof, as well as a pharmaceutical composition comprising the same. The present invention also encompasses a process for the preparation of (R)-2-(N-[4-amino-5-(4-methoxybenzoyl) thiazol-2-yl]-4-fluoro-anilino) propanamide.

The invention relates to the technical field of pesticide preparations, and particularly discloses a potato seed dressing agent with a disease-resistant function, which is prepared from the following raw materials in parts by weight: 8 to 12 parts of N-methoxy-N-o-tolyl-3-(furyl) propanamide, 5 to 8 parts of eugenol polyoxyethylene ether derivatives, 3 to 5 parts of salicylic acid glucoside, 6 to 10 parts of cationized modified chitosan and 2 to 4 parts of EDTA (Ethylene Diamine Tetraacetic Acid) chelated zinc. The preparation method comprises the following steps: treating raw materials; capsule preparation; mixing and granulating; and drying and screening. N-methoxy-N-tolyl-3-(furyl) propanamide is adopted to directly act on a key metabolic link of pathogenic bacteria, a plant-derived derivative plays a broad-spectrum antibacterial role, an inductive component activates a disease-resistant mechanism of potatoes, and meanwhile, cationized modified chitosan and other auxiliary components cooperate with each other, so that slow release of active components is realized, and the disease resistance of the potatoes is improved. The pathogenic bacteria are difficult to generate drug resistance, and the prevention and control effect is long-term and stable.

The invention discloses an anti-tumor application of a thiazole compound, and belongs to the technical field of medical chemistry. The thiazole compound is 3-[(4-fluorophenyl) thio]-N-[4-(pyridine-2-yl) thiazole-2-yl] propanamide, and the English name of the thiazole compound is 3-((4-fluoropheyl) thio)-N-(4-(pyridin-2-yl) thiazol-2-yl) propanamide. The structural formula of the thiazole compound is shown in the description. The invention provides the thiazole compound with broad-spectrum anti-tumor activity, the compound has relatively strong inhibitory activity on clinical refractory breast cancer, osteosarcoma, colorectal cancer, liver cancer and lung cancer, and a new candidate compound is provided for broad-spectrum anti-tumor drugs.

The present disclosure provides suspendable ophthalmic solutions with excellent redispersibility. The present disclosure provides an aqueous suspension agent comprising (E)-2-(7-trifluoromethylchroman-4-ylidene)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide or a pharmaceutically acceptable salt or solvate thereof, a cellulosic polymer, and a nonionic surfactant.

Examples of a biocide composition include an activated halogen compound selected from the group consisting of 2,2-dibromo-3-nitrlopropionamide; 2-bromo-2-nitropropane-1,3-diol; and 1,2-dibromo-2,4-dicyanobutane; benzisothiazolin-3-one; a pyridine-N-oxide selected from the group consisting of zinc pyrithione and sodium pyrithione; and a carbamate derivative selected from the group consisting of 3-iodo-2-propynyl butyl carbamate; zinc bis(dimethyldithiocarbamate); and bis(dimethyl carbamoyl) disulfide.

The invention relates to an androgen receptor antagonist with a disubstituted-N-(substituted polynary fused cyclo-2-yl) propanamide structure as well as a preparation method and application of the androgen receptor antagonist, the androgen receptor antagonist is shown in a general formula I, and the androgen receptor antagonist inhibits growth and proliferation of prostate cancer cells by inhibiting AR activity and blocking an androgen signal channel. Compared with the traditional AR antagonist, the novel compound provided by the invention has a novel action mechanism, and effectively overcomes the problem of drug resistance of the existing drug.

This disclosure provides a means for treating dry eye. This disclosure can provide: a composition for use in treating dry eye; and a use thereof. The composition includes (E)-2-(7-trifluoromethyl-chroman-4-ylidene)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalene-1-yl)acetamide, a pharmaceutically acceptable salt thereof, or a solvate thereof. This disclosure can provide: a composition for treating dry eye; and a use thereof. The composition includes a Vi / Vc zone inhibitor.

Use of an ester group-containing aromatic propanamide compound and its metabolite in the preparation of a drug for treating heart failure, wherein the ester group-containing aromatic propanamide compound is C<subgt;25< / subgt;H<subgt;17< / subgt;F<subgt;3< / subgt>N<subgt;4< / subgt>O<subgt;4< / subgt>. The ester group-containing aromatic propanamide compound can improve the reduction of ejection fraction, fractional shortening and cardiac output in rats with chronic heart failure, and increase the LVSP of heart failure rats.

The present disclosure relates to a molecular N-ethyl-3-(methylsulfonyl)-N-(2-(pyridin-3-yl) thiazol-5-yl) propanamide (S6a), or a hydrochloride salt thereof (S6a-HCl); and a process for the preparation of S6a, S6a-HCl; and N-(4-chloro-2-(pyridin-3-yl) thiazol-5-yl)-N-ethyl-3-(methylsulfonyl) propanamide (S7a) having a pesticidal effect on pests in Phyla Arthropoda, Phyla Mollusca and Phyla Nematoda.

The application discloses a 2,3-dihydrofuran derivative, and also discloses a synthesis method of the 2,3-dihydrofuran derivative, which takes an alpha-carbonyl cyclopropane amide compound as raw material, is dissolved in an organic solvent, and is subjected to intramolecular rearrangement cyclization reaction under the synergistic catalysis of an organic base and a bromide, so that the 2,3-dihydrofuran derivative is obtained at a very high yield; and the application of the 2,3-dihydrofuran derivative is also disclosed. The application has the advantages of high specificity, high conversion rate, only one product, good yield, and the like. The bioactivity test shows that the compound has moderate or excellent insecticidal activity, and has a good application prospect in the field of pesticides.