3154 results about "Pyridyne" patented technology

Provided herein are compounds of Formula (I) and Formula (II) and compositions thereof that capable of disrupting, interrupting, and / or preventing an interaction between a small GTPase protein and a PI3K protein (e.g., PI3Kα). The present disclosure also provides methods of treating cancers and other indications with such compounds or compositions thereof. (I) (II)

The invention provides a pyridopyrimidine derivative as a small GTP enzyme KRAS mutation inhibitor, and particularly provides a pyridopyrimidine derivative with a structural formula as shown in a general formula (A) and pharmaceutically acceptable salts thereof, and the pyridopyrimidine derivative has inhibitory activity on mutants such as KRAS G12D and the like. The invention also provides a preparation method of the derivative, a pharmaceutical composition and a salifying compound of the derivative, and medical application of the derivative as a small GTP enzyme KRAS mutation inhibitor in treatment of different types of tumors.

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.

Disclosed herein are novel methods for preparing 2-[(3R)-2-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4[4-(oxetan-3-yl)piperazin-1-yl]-pent-2-enenitrile, including various solvate forms and intermediates thereof. Also disclosed herein are novel solvate forms and intermediates of 2-[(3R)-2-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4[4-(oxetan-3-yl)piperazin-1-yl]-pent-2-enenitrile.

The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein.

Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-α.

The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein.

The invention discloses a pyridyl anti-aging agent as well as a synthesis method and application thereof, the anti-aging agent is obtained by taking 5-nitro-N-phenylpyridine-2-amine synthesized by 2-chloro-5-nitropyridine and aniline and iodide synthesized by alcohol and iodine as raw materials, and reacting in the presence of a hydrogen source and a catalyst. The anti-aging agent provided by the invention can effectively slow down the emigration speed of the anti-aging agent in rubber and greatly improve the phenomenon that the appearance of a tire becomes red, has one more N heteroatom than other anti-aging agents in the structure, has good oxidation resistance and flex cracking resistance, and is high in anti-ozone activity, environment-friendly and small in pollution.

The invention relates to the technical field of electronic elements, in particular to a ternary compound for a memristor array and a preparation method of the ternary compound. The ternary complex comprises A, B and C, A is a guest molecule of a pyridine derivative with an amino terminal, B is a bridging molecule, and C is a host molecule with a cucurbituril structure. A, B and C are self-assembled in an aqueous solution through Van der Waals force and hydrophobic interaction among molecules to form a ternary complex; the host molecule C has a barrel-shaped cavity structure, and the guest molecule A and the bridging molecule B are included in the barrel-shaped cavity structure. The ternary complex forms a supramolecular chain junction at the end part of the graphene electrode, so that the graphene electrode with different gaps can be adapted, and the molecular connection success rate of the array is greatly improved. The preparation method of the ternary complex is simple, convenient, easy to operate and suitable for large-scale production.

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 high-performance unsaturated polyester resin, and relates to the field of polyester resin. When the high-performance unsaturated polyester resin is prepared, diatomite and a silver nitrate solution are uniformly mixed to obtain silver-loaded diatomite; then, the silver-loaded diatomite is subjected to a reaction with 3-aminopropyltrimethoxysilane and 3-allyl salicylaldehyde in sequence, and modified diatomite is obtained; the preparation method comprises the following steps: reacting tris (dimethylaminopropyl) amine with 3-chloropropene to obtain a cross-linking monomer; 2-formyl pyridine and 3-aminopropane phosphoric acid are subjected to a reaction, and a flame-retardant monomer is obtained; reacting terephthalic acid, fumaric acid, 1, 3-propylene glycol and a flame-retardant monomer to obtain modified unsaturated polyester resin; and uniformly mixing the modified unsaturated polyester resin, the modified diatomite and a crosslinking monomer to obtain the high-performance unsaturated polyester resin. The prepared high-performance unsaturated polyester resin has excellent flame retardance, antibacterial property, antistatic property, anti-aging property and self-repairing property.

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%.

Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-α.

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 present application discloses an acetylated glucomannan electrospun membrane, and a preparation method therefor and a use thereof. The preparation method for an electrospun membrane of the present application comprises: first adding glucomannan into a mixed solution of pyridine and acid anhydride, carrying out solid-liquid separation after the reaction, collecting a solid phase, adding ethanol for precipitation, and collecting the precipitate to obtain acetylated glucomannan; then dissolving the acetylated glucomannan in a mixed solution of chloroform and N,N-dimethylformamide, and carrying out ultrasonic treatment to obtain an electrospinning solution; and finally, using the electrospinning solution as a raw material, and carrying out electrospinning to obtain an acetylated glucomannan electrospun membrane.

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.

The invention provides a modified porous chitosan gel bead, a preparation method thereof and application of the modified porous chitosan gel bead in cobalt-nickel separation, and belongs to the technical field of chitosan preparation. The preparation method comprises the following steps: firstly, modifying chitosan by using polyethylene glycol and glutaraldehyde to obtain a porous chitosan gel bead with a cross-linked structure, and then grafting by using epichlorohydrin, ethylenediamine and 2-chloromethylpyridine hydrochloride to obtain the modified porous chitosan gel bead containing an aminomethylpyridine functional group. The modified porous chitosan gel bead has excellent selective adsorption on nickel ions in a cobalt-nickel solution with the pH value range of 2-5, and nickel-cobalt separation can be achieved. In addition, the modified porous chitosan gel bead also has a good nickel-cobalt separation effect in a salt-containing system. The preparation method of the modified porous chitosan gel bead provided by the invention is simple in process, and the raw material chitosan is wide in source, non-toxic and environment-friendly.

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 relates to the technical field of oil and gas field development, in particular to a double-network CO2 response type gel particle and application thereof.The first-layer network is formed by covalent bonds between acrylamide, zwitterions and CO2 response monomers (composed of vinylpyridine and DMAEMA) in the gel particle and a cross-linking agent, and the first-layer network is formed by covalent bonds between Ca < 2 + > in mineralized water, pyridine, SO3 <-> in the zwitterionic monomers and coordinated water; coordination bonds exist among Mg < 2 + >, pyridine, carboxyl (acylamino is partially hydrolyzed) and coordinated water, a second-layer network is formed under the synergistic effect of pi-pi bonds among aromatic rings, and the strength of the gel is enhanced through the toughness of the double-network structure. Due to the introduction of an aromatic ring sulphobetaine monomer and water molecules carried by coordinate bonds, the strength of the gel particles in mineralization water is increased, and meanwhile, the gel particles show higher water-retaining property. Due to the introduction of CO2 response monomers with different pKa values, the particles have good CO2 responsiveness, and still have the dual-network structure in mineralized water after response.

The invention relates to the field of medicine synthesis, and particularly discloses a preparation method of abesilib and an intermediate thereof. The invention relates to an abesiril intermediate, which is 4-chloro-5-fluoro-2-(methylsulfonyl) pyrimidine (IV) and 4-fluoro-6-(5-fluoro-2-(methylsulfonyl) pyrimidine-4-yl)-1-isopropyl-2-methyl-1H-benzo [d] imidazole (V). The invention further provides a preparation method of the abesiril intermediate. And carrying out nucleophilic substitution reaction on the abesilib intermediate V and 5-[(4-ethyl piperazine-1-yl) methyl] pyridine-2-amine to prepare the abesilib. According to the preparation method, the raw materials are cheap and easy to obtain, the reaction selectivity of functional groups is high, ectopic impurities generated by a halogen atom competition reaction are effectively avoided, meanwhile, introduction of heavy metal palladium can be reduced, and therefore the cost is reduced. The synthetic route is simple, the atom economy is high, the controllability in production is high, and the method is suitable for industrial production.

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.