2254 results about "Pyridyne" patented technology

The present disclosure relates generally to methods for treating or preventing central nervous system (CNS) metastases with a KRAS inhibitor, and more specifically to treating CNS metastases with a pyridopyrimidine derivative.

Provided are a crystal form of a pyridopyrimidine derivative, a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically disclosed are a crystal form of a compound of formula (I), a preparation method therefor, a pharmaceutical composition thereof and the use thereof.

The present disclosure relates generally to methods for treating cancer with a KRAS inhibitor in combination with an immune checkpoint inhibitor, and more specifically to treating cancer with a pyridopyrimidine derivative in combination with a PD-1 or PD-L1 inhibitor.

The invention provides a salt-responsive temperature-resistant salt-resistant water-based drilling fluid tackifying filtrate reducer as well as a preparation method and application thereof, and belongs to the technical field of drilling. The tackifying filtrate reducer is prepared from the following raw materials in parts by mass: 30 to 50 parts of 1-(2-carboxyethyl)-2-vinylpyridine, 20 to 40 parts of (3-(methacrylamido) propyl) dimethyl (3-thiopropyl) ammonium hydroxide inner salt, 35 to 55 parts of N, N-dimethylacrylamide, 10 to 25 parts of 4-vinylpyridine, 300 to 500 parts of water and 1 to 5 parts of an initiator. According to the filtrate reducer, cations and anions are concentrated on one monomer molecule, so that the synthesized product contains the cations and the anions with the same charge number, has good adsorption capacity and salt response characteristics, is compatible with salt essentially, can effectively resist high temperature and high salt, and can be recycled. And the viscosity-increasing and filtrate-reducing agent has good viscosity-increasing and filtrate-reducing effects on the drilling fluid.

The present disclosure relates generally to polymorphic forms of a KRAS inhibitor, and more specifically to polymorphic forms of a pyridopyrimidine derivative, and uses thereof.

The invention discloses a preparation method and application of a conjugated microporous polymer microsphere filler with a hollow structure, silicon dioxide nanospheres are placed in an organic solvent, after uniform ultrasonic dispersion, 1, 3, 5-triacetylene benzene and 2, 6-dibromo-3-aminopyridine are added, after a catalyst is added, a stirring reaction is carried out in a nitrogen atmosphere to obtain yellow powder, and the yellow powder is dried to obtain the conjugated microporous polymer microsphere filler with the hollow structure. Etching with hydrofluoric acid, cleaning the treated product until the filtrate is transparent and colorless, and drying in vacuum to obtain the conjugated microporous polymer microsphere filler with the hollow structure. Nanoscale holes are formed in the hollow-structure conjugated microporous polymer microsphere filler, so that the hollow-structure conjugated microporous polymer microsphere filler has good heat insulation performance and good heat stability at high temperature, and can be used as a heat-resistant performance enhancing filler.

The present disclosure relates generally to polymorphic forms of a KRAS inhibitor, and more specifically to polymorphic forms of a pyridopyrimidine derivative, and uses thereof.

The invention discloses a method for synthesizing 2, 3-dichloropyridine through electrochemical dechlorination, which comprises the following steps of: adopting a diaphragm electrolytic tank, taking a noble metal element modified material as a cathode, taking a chemical inert material as an anode, taking a solution containing 2, 3, 6-trichloropyridine as a catholyte, taking an aqueous solution of sulfuric acid or hydrochloric acid as an anolyte, and enabling current to pass through the solution containing 2, 3, 6-trichloropyridine from the anode to the cathode, the method comprises the following steps: preparing a solution containing 2, 3, 6-trichloropyridine, performing electrolytic reduction and dechlorination on the 2, 3, 6-trichloropyridine in the solution to obtain 2, 3-dichloropyridine, and recovering the 2, 3-dichloropyridine after electrolysis is finished. According to the method, the reaction temperature is reduced from 140 DEG C to room temperature or the reaction pressure is reduced from 3MPa to normal pressure; the use of hydrogen is avoided; and the yield of the target product is increased by 5-10%.

Compounds of formula (II) and formula (I) which are inhibitors of QPCTL and QPCT: (II) and (I) are provided herein. Also provided are pharmaceutical compositions containing this compound, as well as compounds for use in methods of treating cancer, neurodegenerative, inflammatory or autoimmune diseases. Exemplary compounds are, for example, 3-(6-fluoropyridin-3-yl)-2-[4-(4-methyl-4H-1,2,4-triazol-3-yl)piperidin-1-yl]benzonitrile (Example 1): (1), and pharmacological data are provided. TIFF2025524039000368.tif70128

Provided herein is a process comprising heating a composition comprising (P)-compound A or a salt thereof and a solvent to a temperature of 250° C. to 350° C. to form racemized compound A. Also provided is a process for isolating (P)-compound A from a composition comprising (P)-compound A and a tartrate, as described herein. Further provided herein, is a process for isolating a free acid of a tartrate or a hydrate thereof from a composition comprising a tartrate, (P)-compound A, and an organic solvent.

The invention belongs to the technical field of catalyst preparation, focuses on a high-entropy alloy nanowire catalyst, and mainly relates to a preparation method and application of an AuCuAgPtNi catalyst. A one-pot wet chemical method is innovatively adopted, a 4-aminopyridine solvent and metal precursors of gold, copper, silver, platinum and nickel are fully and evenly mixed and placed in an oil bath pot at the temperature of 90 DEG C, then a reducing agent ascorbic acid is rapidly added, after specific reaction time, washing, drying and other operations are sequentially carried out, and the high-entropy alloy nanowire AuCuAgPtNi catalyst can be successfully prepared. The preparation method disclosed by the invention has the remarkable advantages of simple process, simple steps, convenience in operation and the like. In an alkaline environment, the prepared nanowire-shaped high-entropy alloy AuCuAgPtNi catalyst shows extremely excellent catalytic activity and selectivity for catalytic degradation of waste plastic polylactic acid, the waste plastic can be efficiently upgraded and converted into pyruvic acid, a new way is opened up for resource utilization of the waste plastic, and the application prospect is wide. The method has a wide application prospect in the fields of environmental protection and resource recovery.

This application relates to the field of biosynthesis technology, and specifically discloses a pyridone compound, its biosynthesis method and application. Based on synthetic biology-related technologies, this application modifies non-ribosomal peptide synthetase, heterologously expresses non-ribosomal peptide synthetase mutants in a variety of hosts, and for the first time discovers and obtains a pyridone compound, and determines its chemical formula as C5H4N2O3, named 5-amino-pyridine-2,3,6-trione or 5-hydroxy-3-imino-pyridine-2,6-dione. This novel pyridone compound can be used as a raw material or intermediate in the development and preparation of novel antibiotics, drugs and dyes.

Provided herein is a process for preparing compound A comprising (a) admixing 2-isopropyl-4-methylpyridin-3-amine (Compound B), or a salt thereof, a first base, and a reactive compound comprising phosgene or a phosgene equivalent in an organic solvent to form 3-isocyanato-2-isopropyl-4-methylpyridine (Compound C); (b) admixing Compound C and 2,6-dichloro-5-fluoronicotinamide (Compound D) to form 2,6-dichloro-5-fluoro-N-((2-isopropyl-4-methylpyridin-3-yl)carbamoyl)nicotinamide (Compound E); and (c) admixing Compound E and a second base to form a product mixture comprising Compound A and the second base. Also provided herein is a process for synthesizing AMG 510 comprising using Compound A prepared according to the disclosed processes

The invention belongs to the technical field of organic synthesis, and particularly discloses an ammonia aromatic alkene modified near-infrared BODIPY fluorescent probe as well as a preparation method and application thereof.The near-infrared BODIPY fluorescent probe is obtained by adopting 6-(dimethylamino) nicotinic aldehyde to directionally modify the alpha position of BODIPY and constructing an expanded conjugated system through Knoevenagel condensation. Wherein dimethylamino provides a strong electron donating effect, a molecular structure is twisted into a non-planar configuration due to steric hindrance of a pyridine ring, pi-pi accumulation is reduced, and an ACQ effect is inhibited. According to the structural modification strategy, significant red shift of absorption / emission wavelength is realized by expanding a molecular pi-conjugated skeleton, and meanwhile, the stability of the BODIPY core and the quantum yield are effectively enhanced. The probe molecule can specifically recognize the diphenylalanine dipeptide structural unit by utilizing the synergistic coordination effect of the 2-aminopyridine derivative and the BODIPY mother nucleus, so that the selective detection of the Alzheimer's disease biomarker Abeta42 is realized, and a novel optical detection tool is provided for the early molecular diagnosis and targeted therapy of AD (Alzheimer's disease).

The invention relates to a heat dissipation coating composition, a preparation method thereof and application of the heat dissipation coating composition in a battery protection plate, and belongs to the technical field of new energy heat dissipation coatings. According to the preparation method, methyl methacrylate, 2-vinylpyridine, methacrylamide, dipropylene glycol diacrylate, azodiisobutyronitrile and tetradecane are taken as raw materials, a coating dispersion liquid is prepared firstly, then hydroxylated graphene is subjected to polymerization coating by utilizing the coating dispersion liquid based on an in-situ polymerization method, a coating layer with amino and pyridine rings is constructed, and the coating layer with amino and pyridine rings is prepared. The preparation method comprises the following steps: coating a coating particle with amino boron nitride to obtain a coated particle, compounding the amino boron nitride onto the coated particle through addition of amino and epoxy groups by taking ethylene glycol diglycidyl ether containing double-terminal epoxy groups as a bridging agent to prepare a modified composite particle, and blending the modified composite particle with water-borne epoxy resin and other components to obtain the heat-dissipating coating composition. The coating has excellent heat dissipation performance, can still keep a good heat dissipation effect even after being heated and cooled for multiple times, and is suitable for being applied to the battery protection plate.

To provide a compound which is a novel proline derivative, and to provide a pharmaceutical composition comprising the compound for the treatment of diseases, for example, systemic lupus erythematosus.SOLUTION: A pharmaceutical composition comprises, as a cGAS inhibitor, a compound which is a novel proline derivative of formula (I) (where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are as defined in claim 1), or a prodrug, a pharmaceutically acceptable salt, or a stereoisomer of the compound.SELECTED DRAWING: None

The invention relates to the technical field of marine antifouling materials, in particular to a modified polyurethane marine antifouling coating based on a metal pyridine structure and a preparation method. According to the modified polyurethane marine antifouling paint based on the metal pyridine structure, polyhydric alcohols and diisocyanate monomers with different molecular weights are subjected to condensation polymerization to obtain a polyurethane prepolymer; then reacting a diaminopyridine monomer or a dihydroxypyridine monomer with a metal ion compound to obtain a chain extender with a metal pyridine structure; finally, the marine antifouling paint is prepared through the reaction between the terminal amino or hydroxyl of the metal pyridine structure chain extender and the terminal isocyanate group of the polyurethane prepolymer, the metal pyridine structure is introduced into polyurethane, the mechanical performance of the marine antifouling paint is enhanced, the marine antifouling paint is endowed with the antibacterial effect through metal ion release, and the service life of the marine antifouling paint is prolonged. Adhesion and growth of marine fouling organisms can be effectively inhibited, and an efficient and durable solution is provided for development of a polyurethane marine antifouling coating.

The invention discloses a yellow reduction dyeing agent, a dyeing solution and a preparation method and application thereof, and relates to the technical field of dyeing and finishing. According to the yellow reduction dyeing agent provided by the invention, the 5-hydroxy-3-aminopyridine-2, 6-(1H, 3H)-diketone is adopted as a reduction dye, and the sodium sulfite is independently used as a reducing agent for reduction dyeing, so that the obtained dye leuco body is proper in dyeing capacity, and a dyed fabric can show excellent light brittle damage resistance. The fabric dyed by the dyeing agent has similar breaking strength before and after dyeing and even is slightly improved after dyeing and illumination, meanwhile, the color depth K / S of the fabric dyed by the dyeing agent reaches 3.2 or above, the dry and wet rubbing color fastness can reach level 4 or above, and the color fastness to illumination reaches level 6 or above.

The invention discloses a preparation method of pyridinetriazolone, and belongs to the technical field of organic synthesis, and the preparation method comprises the following steps: taking hydrazine hydrate as a starting raw material, adding urea in batches at the temperature of 80-85 DEG C, carrying out heat preservation reaction to obtain semicarbazide, dropwise adding hydrochloric acid to form salt, and drying under reduced pressure to obtain semicarbazide hydrochloride; adding the semicarbazide hydrochloride obtained in the previous step and 2-chloropyridine into an ethylene glycol monomethyl ether system, heating to 130-135 DEG C, refluxing, adding a catalytic amount of concentrated sulfuric acid, and carrying out heat preservation reaction to obtain pyridine triazolone; and drying the post-treated mother liquor under reduced pressure, weighing, adding quantitative urea, heating to 130-135 DEG C, and reacting to obtain the pyridinium triazolone. The initial raw materials are hydrazine hydrate and urea, are common industrial raw materials, are easy to obtain and low in price, and are beneficial to industrial production; the by-product 2-hydrazinopyridine is recovered and reacts with urea to prepare the pyridintriazolone, so that the raw material utilization rate and the product yield are greatly improved, the total yield reaches more than 80%, and the purity of the pyridintriazolone is more than or equal to 99.0%.

The invention discloses an antibacterial material rich in a bismuth metal organic framework and a preparation method thereof, the method comprises the following steps: adding an indole monomer and an alcohol monomer into a solvent, and then adding nitrosalicylaldehyde into the solvent to obtain a spiropyran compound; the preparation method comprises the following steps: adding humic acid into a binary solvent consisting of dioxane and butanol to obtain a mixed solution; the ratio of the mass of the humic acid to the volume of the binary solvent is (2-3): (20-40) g / ml; sequentially adding a bismuth source, 2-bromo-5-(trifluoromethyl) pyridine and 4-(trifluoromethyl) phenylboronic acid into the mixed solution to obtain a bismuth metal organic framework; and adding the spiropyran compound into the bismuth metal organic framework to obtain the antibacterial material rich in the bismuth metal organic framework. The antibacterial capability of the antibacterial material is improved.

The invention discloses a pyranopyridine compound as well as a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound as shown in a formula (I), a pharmaceutically acceptable salt or a stereoisomer thereof, and the compound has a relatively strong inhibition effect on aldosterone synthetase, almost has no influence on cortisol synthetase, has high selectivity and relatively high safety, and can be used for preventing and / or treating various diseases related to aldosterone. # imgabs0 #

The invention relates to a preparation method of 2-(2-amino-5-bromo-benzoyl) pyridine, which comprises the following steps: by taking 1, 2-diphenyl-1H-benzimidazole (I) as a starting material, oxidizing under the action of chromium trioxide and acetic acid to obtain N-[2-(2-pyridinecarbonyl) phenyl] benzamide (II), hydrolyzing the N-[2-(2-pyridinecarbonyl) phenyl] benzamide (II) under the action of sulfuric acid to obtain 2-(2-aminobenzoyl) pyridine (III), and reacting the 2-(2-amino-5-bromo-benzoyl) pyridine (III) with the 2-(2-amino-5-bromo-benzoyl) pyridine (III) to obtain the 2-(2-amino-5-bromo-benzoyl) pyridine. And (III) performing substitution reaction with NBS in DCM to obtain the target product 2-(2-amino-5-bromo-benzoyl) pyridine. The method has the advantages of mild reaction conditions, higher product purity, high yield, simplicity and convenience in operation, low cost and easiness in industrialization.

The invention relates to a green preparation method of fluopyram intermediate 3-chloro-5-(trifluoromethyl)-2-ethylaminopyridine, which comprises the following steps: step 1, Ullmann reaction: coupling 3-chloro-2-methyl-5-trifluoromethylpyridine (C1) and N-bromomethyl phthalimide (C2) in the presence of a copper catalyst and potassium tert-butoxide to generate an intermediate (C3); and step 2, hydrolysis reaction: hydrolyzing the intermediate (C3) in the presence of hydrazine sulfate and an alkaline condition to generate the fluopyram intermediate 3-chloro-5-(trifluoromethyl)-2-ethylamino pyridine. The method has the advantages of short synthesis steps, easily available raw materials, no use of high-toxicity cyanogen compounds, low catalyst cost, difficult poisoning, recycling, simple post-treatment process, and less waste liquid generation, greatly reduces the production cost, improves the production safety, reduces the waste liquid discharge amount, and accords with the idea of green synthesis.

The present application relates to a crystal form of 4-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenethyl]pyridine-2(1H)-one, a preparation method therefor, a composition containing the crystal form and the use thereof in the treatment of phosphodiesterase-related diseases.

Disclosed is a series of pyrazolopyridine compounds, and application thereof in the preparation of RET kinase inhibitors for treatment. Specifically disclosed is the compound represented by formula (I), or a pharmaceutically acceptable salt thereof.

The invention relates to a preparation method of 3-[(1S, 2S)-1-[5-[(4S)-2, 2-dimethyl oxacyclohexane-4-yl]-2-[(4S)-2-(4-fluoro-3, 5-dimethyl phenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6, 7-dihydro-4H-pyrazolo [4, 3-c] pyridine-5-carbonyl] indol-1-yl]-2-methylcyclopropyl]-4H-1, 2, 3-triazolo [4, 3-c] pyridine-5-carbonyl] indol-1-yl]-2-methylcyclopropyl]-1, 2, 4-triazolo [4, 3-c] pyridine-5- The invention relates to synthesis of 1, 2, 4-oxadiazole-5-one or a salt thereof, and related synthesis intermediate compounds.

Disclosed in the present application are a pyridopyrimidinone compound, and a preparation method therefor and the use thereof, wherein the pyridopyrimidinone compound, or a racemate, R-isomer, S-isomer, pharmaceutically acceptable salt thereof or a mixture thereof has a structure as shown in formula (I). The pyridopyrimidinone compound provided by the present application has an agonistic effect on an HsClpP protease, and can be used for treating diseases related to HsClpP receptor activation.

The invention belongs to the technical field of medicinal chemistry, and discloses a preparation method and application of a benzofuran [2, 3-b] pyridine derivative of a targeted nuclear receptor co-activator 4 (NCOA4). The derivative has a structural general formula as shown in the following formula (I), wherein R1, R2 and R3 substituent groups can be combined at will. The compounds are combined with NCOA4 to interfere the cell iron autophagy process and effectively inhibit the ferroptosis of various cells induced by RSL3 or Erastin. Particularly, the binding affinity of the compound 4k and NCOA4 is optimal (Kd is equal to 0.78 mu M), and the compound 4k has remarkable ferroptosis inhibition activity and can be used for research and development of medicines for ferroptosis-related diseases. # imgabs0 #

Methods for treating patients with chronic spontaneous urticaria (CSU) comprising administering at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxyphenyl) pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof are disclosed.

The invention discloses a fluopyram preparation method, which comprises: S1, carrying out a heating reaction on 2-vinyl-3-chloro-5-trifluoromethylpyridine, ammonia water, a catalyst and a solvent, carrying out reduced pressure distillation after the heating reaction to recover the solvent so as to obtain a residue, and adding dichloromethane and triethylamine to the residue so as to obtain a reaction liquid; and S2, dropwise adding o-trifluoromethyl benzoyl chloride into the reaction liquid in an ice bath, then removing the ice bath, stirring at the room temperature, adding water into the reaction liquid obtained in the step S1, extracting an organic layer, drying with anhydrous magnesium sulfate, recovering the solvent under reduced pressure, and performing vacuum drying to obtain the fluopyram. The method has the advantages of high reaction yield, high product purity, recyclable and reusable solvent, simple and mild production process, and suitableness for mass production.