262 results about "Pyrazole" patented technology

The disclosure provides the development of enantiomer-specific 7V-arylpyrazole dipeptides as novel N0D2 agonists which are effective at promoting immune checkpoint inhibitor therapy requiring N0D2 for activity. Given the significant functions of N0D2 in innate and adaptive immunity, these novel agonists afford new therapeutic compounds for a variety of NOD2-responsive diseases.

The present application provides novel compounds that inhibit MYLK4 activity and their medical use. A compound of Formula (I) or a pharmaceutically acceptable derivative thereof is provided: (in the formula, R 1 to R 5 each independently is hydrogen or a C 1‑3 linear aliphatic hydrocarbon; R 6 a 5- to 10-membered aromatic hydrocarbon optionally substituted, a 5- to 10-membered heterocycle optionally substituted having 1 to 5 heteroatoms independently selected from nitrogen, oxygen, and sulfur as ring constituent atoms, or a condensation ring of any of the foregoing with a 4- to 10-membered heterocyclic group optionally substituted having 1 to 3 heteroatoms independently selected from nitrogen, oxygen, and sulfur as ring constituent atoms), and the like as medicines.

This invention discloses the preparation and gas adsorption separation application of pyrazole-3,4,5-tricarboxylic acid ligand heteronuclear metal-organic framework materials, comprising the following steps: 1) Weighing CuCl2·2H2O, Ba(NO3)2, and 1H-pyrazole-3,4,5-tricarboxylic acid as raw materials; 2) Placing the raw materials in a polytetrafluoroethylene-lined reactor, adding distilled water, and adjusting the pH to 2-4 with malonic acid; 3) Sealing the reactor and heating the reaction, raising the temperature from room temperature to 80-120℃ over 0-12 hours, holding the temperature for 70-75 hours, and then lowering it to room temperature over another 0-12 hours; 4) Collecting the product, washing, and vacuum drying to obtain the chemical formula [Cu2Ba(HL)2(H2O)3]. n The crystal is a pyrazole-3,4,5-tricarboxylic acid. By combining the multi-site coordination advantages, heterometallic node construction advantages, and pore functionalization control advantages of pyrazole-3,4,5-tricarboxylic acid, a stable framework structure can be constructed while simultaneously adjusting pore size, optimizing pore wall polarity, and constructing local adsorption sites, thereby enhancing the material's application potential in SF6 capture and separation, and C2 gas adsorption and storage.

The application discloses a preparation method of baricitinib, and belongs to the technical field of drug synthesis. The method comprises the following steps: firstly, 2-[1-(ethylsulfonyl)-3-azetidinyl]acetonitrile and 4-pyrazole boron pinacol ester are subjected to a Michael addition reaction to obtain 1-(ethylsulfonyl)-3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]-3-azetidine acetonitrile as an intermediate I; secondly, a protection group is introduced on the amino group of 4-chloropyrrolopyrimidine to obtain an intermediate II; finally, the intermediate I and the intermediate II are subjected to a Suzuki coupling process by adopting a method of combining a nickel pre-catalyst with a supporting ligand to obtain the baricitinib. The preparation method creatively realizes cross coupling of the baricitinib by adopting the cheap metal nickel as a catalyst, avoids the use of a heavy metal palladium catalyst, and has the advantages of low cost, low toxicity, small pollution, green environmental protection and the like.

The present application relates to the technical field of pesticide chemistry and medicinal chemistry, and particularly relates to a substituted pyrazole-containing ortho-hydroxy aryl formamide derivative, a preparation method and application thereof. The substituted pyrazole-containing ortho-hydroxy aryl formamide derivative is prepared from a 5-amino pyrazole intermediate (I) and a different substituted ortho-hydroxy aryl formic acid (II) as raw materials through an amide condensation reaction. The substituted pyrazole-containing ortho-hydroxy aryl formamide derivative prepared by the present application has a broad-spectrum inhibitory activity on plant pathogenic fungi, and particularly has excellent inhibitory activity on Valsa mali, Sclerotinia sclerotiorum and Botrytis cinerea, and is expected to be developed into a new type of green fungicide with high efficiency, safety, economy and environmental friendliness.

This invention relates to the solid form of propionic acid (1R,3S)-3-[3-({[3-(methoxymethyl)-1-methyl-1H-pyrazol-5-yl]carbonyl}amino)-1H-pyrazol-5-yl]cyclopentyl ester, pharmaceutical compositions comprising such solid forms, and the use of such solid forms and pharmaceutical compositions for the treatment of cancer.

The invention belongs to the technical field of pesticides, and relates to 11 bactericide compositions for mainly preventing and treating crop diseases caused by pyricularia oryzae and colletotrichum gloeosporioides. The compound YJY-22 provided by the invention is novel in structure and unique in action mode, and has no cross resistance with isoprothiolane, fenoxanil, pyraclostrobin, tricyclazole, azoxystrobin, mancozeb, captan, difenoconazole, prochloraz, chlorothalonil and tebuconazole. As the action mechanism of the compound YJY-22 is different from that of the medicament, and the compound YJY-22 and the medicament have no cross resistance, the compound YJY-22 and the medicament are compounded, so that the sterilization range can be expanded, the sterilization effect can be enhanced, the drug resistance of phytopathogen can be delayed, the safety to crops is good, the prevention and control spectrum is expanded, and the requirements of pesticide reduction and synergism are met.

This invention provides a chemical mechanical polishing (CMP) slurry and its application. The CMP slurry comprises: a catalyst, a stabilizer, an oxidant, a pH adjuster, abrasive particles, a corrosion inhibitor, and water. The corrosion inhibitor is a nitrogen-containing heterocyclic carboxylic acid compound, wherein the nitrogen-containing heterocyclic carboxylic acid compound includes at least one selected from nicotinic acid, isonicotinic acid, pyridinecarboxylic acid, imidazocarboxylic acid, pyrazolecarboxylic acid, 3-pyridineacetic acid, 3-pyridinepropionic acid, 3-methyl-2-pyridinecarboxylic acid, and L-piperidine acid. The CMP slurry provided by this invention can simultaneously polish tungsten and silicon oxide, and can also control the polishing rate of silicon oxide while inhibiting tungsten corrosion, thus making it suitable for different application scenarios. In addition, the CMP slurry has good stability and can maintain its performance even after long-term standing.

The invention discloses a pyrazolo [5, 1-a] isoindole derivative as well as a synthesis method and application thereof, and belongs to the technical field of organic chemical synthesis. The invention solves the problems of harsh reaction conditions, limited substrate range and the like of continuous multi-step synthesis of a precursor in the existing pyrazolo [5, 1-a] isoindole compound synthesis process. According to the invention, a polarity reversal strategy is adopted, a cyano group is introduced into 1, 5-enyne to change the electronic characteristics of 1, 5-enyne, diazo, olefin and ethynyl benzene are reacted under mild conditions, two rings and three new chemical bonds are constructed through a series of intermolecular [3 + 2] cycloaddition, intramolecular cycloaddition and elimination reactions, and pyrazolo [5, 5-a]-1, 5-a-phenanthrene is efficiently synthesized. According to the present invention, the 1, 1-a] isoindole derivative has characteristics of good synthesis yield, simple operation of the synthesis method, easily available raw materials, good substrate universality and step economy, and provides the effective strategy for the drug design synthesis.

This invention discloses a method for preparing ethyl 4-pyrazolamide. A dichloromethane solution of ethyl 3-(N,N-dimethylamino)acrylate is added dropwise to a dichloromethane solution containing a chlorine-containing reagent and N,N-dimethylformamide. After addition, the mixture is stirred until the reaction is complete, yielding a reaction solution. The reaction solution is then directly added dropwise to an alcoholic solution of hydrazine hydrate, and the resulting reaction yields ethyl 4-pyrazolamide. This method uses readily available raw materials, has mild reaction conditions, high yield, and is easily industrialized.

A low-density, high-temperature, creep-resistant benzoxazine hybrid epoxy paste and its preparation method are disclosed, relating to the field of adhesive technology. The aim is to address the insufficient long-term high-temperature creep resistance of existing lightweight epoxy adhesives. The paste is prepared from the following raw materials: Raw materials are weighed, and amide-containing trifunctional benzoxazine resin, amide-containing difunctional benzoxazine resin, amide-containing monofunctional benzoxazine resin, multifunctional epoxy resin, bisphenol A type epoxy resin, and toughening agent are added to a reaction vessel. The mixture is heated and stirred to obtain a homogeneous resin premix. The mixture is then cooled, and hollow glass microspheres, a coupling agent, and 2-methyl-pyrazolo[1,5-A]pyrimidine-6-carboxylic acid are added, and the mixture is stirred to obtain an intermediate product. Finally, a curing agent is added and stirred to obtain the low-density, high-temperature, creep-resistant benzoxazine hybrid epoxy paste. This invention is applicable to structural bonding applications in aerospace, rail transportation, and electronic packaging where lightweighting and long-term high-temperature reliability are critical.

A method for treating pruritus in patients with atopic dermatitis (AD) and / or nodular prurigo (PN) is disclosed, comprising administering a therapeutically effective amount of at least one compound selected from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-carbonyl]-4-methyl-4-[4-(oxecyclobutane-3-yl)piperazin-1-yl]pent-2-enonitrile (rezabrutinib) and pharmaceutically acceptable salts thereof.

The present application relates to a pyrazole ring post-processing method, through simple operation, residual moisture, tar and by-products in the reaction system can be efficiently removed, which is beneficial to improve the yield of reaction and product quality, improve the yield, reduce the cost, and further help to realize large-scale industrial production.

This invention relates to the crystalline form (form 7) of the free base of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-5-oxo-10,15,16,17-tetrahydro-2H-8,4-(methiminated bridged)pyrazolo[4,3-h][2,5,11]benzoxazadiazetatetracycline-3-carboxynitrile (lorlatinib). The invention also relates to pharmaceutical compositions comprising form 7 and to methods of treating abnormal cell growth in mammals, such as cancer, using form 7 and such compositions.

The present invention relates to combinations of a compound of formula (A-1) with a compound selected from the group consisting of dimpropyridaz, emamectin and isocycloseram, bentioflumin, pioxaniliprole, isoflualanam, cybenzoxasulfyl, vinylfluthrin, cyclobunofen, flupymezotiaz, fentiazoluron, 1-(1,2-dimethylpropyl)-5-methyl-N-prop-2-ynyl-N-(3-pyridyl)pyrazole-4-carboxamide, 1 -[4- [5-ethylsulfonyl-1-methyl-4-[3-methyl-6-(trifluoromethyl)imidazo[4,5-b]pyridin-2-yl]imidazol-2- yl]phenyl]cyclopropanecarbonitrile, [(Z)-[[3-ethylsulfonyl-5-[4-(trifluoromethoxy)phenyl]-2-pyridyl]-[[5- (trifluoromethyl)-2-pyridyl]amino]methylene]amino] acetate, 3-[3-ethylsulfonyl-5-[4- (trifluoromethoxy)phenyl]-2-pyridyl]-4-[5-(trifluoromethyl)-2-pyridyl]-1,2,4-oxadiazol-5-one, 1-(4- chlorophenyl)-2-fluoro-4-methyl-5-(2,2,2-trifluoroethylsulfanyl)benzene, and emamectin benzoate; and to methods of controlling or preventing damage to plants using such combinations; and to formulations, concentrates and seed treatments comprising such combinations.

This application relates to a series of novel compounds that are selective inhibitors of phosphodiesterase type 9 ("PDE9") for the treatment of chronic heart failure. More particularly, the application relates to pyrazolo[3,4-d]pyrimidinone compounds for use in the treatment and prevention of chronic heart failure.

The invention relates to a novel process for the production of 3-difluoromethyl-1-methyl1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methanonaphthalen-5-yl)-amide of formula Ithat makes it possible to prepare said compound in high yields and good quality' in an economically advantageous way, which process comprises a) reacting a compound of formula II (11), wherein X is chloro or bromo, with an organometallic species in an inert atmosphere to a halobenzyne of formula Xreacting the halobenzyne of formula X so formed with cyclopentadiene to III b) reacting III in the presence of an inert solvent with an oxidant to IVc) reacting IV in the presence of a Lewis acid and a hydride source to Vd) reacting V in the presence of an oxidizing agent, a base and an inert solvent to VI e) converting VI in the presence of a triphenyl phosphane and CCI4 or CHCI3 to VII, andf2) reacting the compound of formula VIIin the presence of a solvent, a base, a copper catalyst and at least one ligand with the compound of formula IXato the compound of formula I.

This invention discloses an environmentally adaptive high-energy-absorbing smart anti-corrosion coating and its preparation method, comprising: synthesizing a dipyrazole diamine chain extender, formulating a long-chain polymer backbone A and a catechol-terminated short-chain polymer B, and preparing a high-energy-absorbing smart anti-corrosion coating; the coating utilizes the interaction between dipyrazole and Zn in the long chain. 2+ Multiple coordination reduces the entropy increase effect of bond breaking and enhances energy dissipation; gradient hierarchical hydrogen bonds between long and short chains, in coordination with metal coordination bonds, act as sacrificial bonds to dissipate energy through stepwise breakage under external force; the slightly alkaline nature of seawater triggers deprotonation of catechols and reconstructs the coordination network, increasing crosslinking density and enhancing shielding; and the Fe released at the breakage site... 3+ By strongly coordinating with catechins to form a passivation layer in situ, and using its photothermal effect to drive the self-repair of the substrate, this invention solves the problem of the difficulty in simultaneously achieving high energy absorption, fatigue resistance, environmental response, efficient self-repair and intelligent corrosion prevention in offshore wind turbine tower coatings, which helps to extend the service life of wind turbine towers and ensure the reliability of the units.

To address the shortcomings of existing antitumor chemotherapy drugs, this invention provides a class of pyrazolopyridone derivatives and their preparation method. The compounds are structurally designed and modified using pyrazolopyridone as the parent core, resulting in a class of pyrazolopyridone derivatives (I) with good stability and significant antitumor effects: wherein: R 1 The compound is 4-methoxyphenyl,N-phenylbenzamide. This invention relates to the field of tumor treatment, specifically to a class of novel pyrazolopyridone derivatives with advantages such as structural stability and ease of preparation. These compounds can be used to treat diseases such as tumors and condyloma acuminata.

The invention relates to a solid water-dispersible pharmaceutical composition for use in the treatment of a disease, said treatment comprising dispersing said pharmaceutical composition into an aqueous liquid to produce an enteraliy administrable liquid containing at least 0.5 gram of said pharmaceutical composition and at least 0.3 g / 1 of edaravone, followed by enteral administration of said enteraliy administrable liquid to a human patient in an amount to provide a dose of 30-300 mg of edaravone, said pharmaceutical composition comprising: 2-50 weight % of 3-methyl-l-phenyl-2-pyrazolin-5-one (edaravone); and 3-50 weight % of a water-soluble alkalizing agent. This solid composition containing edaravone can be easily dispersed in an aqueous liquid to prepare an aqueous solution of edaravone that can be ingested by a patient. The solid composition of the invention provides the advantage that when the composition is introduced into water the edaravone dissolves very rapidly and the enteraliy administrable liquid thus obtained has a high oral bioavailability.

11 fungicide compositions mainly used for controlling crop diseases caused by Pyricularia oryzae and Colletotrichum spp.. Compound YJY-22 has a novel structure and a unique mode of action, and exhibits no cross-resistance with isoprothiolane, fenoxanil, pyraclostrobin, tricyclazole, azoxystrobin, mancozeb, captan, difenoconazole, prochloraz, chlorothalonil, or tebuconazole. Because compound YJY-22 and the described agents have different mechanisms of action and have no cross-resistance, combining compound YJY-22 and the described agents not only can broaden the antifungal spectrum and enhance antifungal efficacy, but also can delay fungicide resistance of plant pathogens, ensure high crop safety, expand the control spectrum, and meet the requirement of pesticide reduction with increased efficiency.

The application discloses a pyrazolyl porous organic polymer loaded ruthenium nanocluster material and a preparation method and application thereof, relates to the field of nanometer material synthesis and the field of energy electrocatalysis technology. The pyrazolyl porous organic polymer (Pz-POP) material is prepared through a polycondensation reaction of 2,4,6-triformylphloroglucinol and 1H-pyrazole-3,5-diamine. Subsequently, the Pz-POP material loaded with ruthenium (Ru) nanoclusters (Ru@Pz-POP) is prepared by using a liquid phase sodium borohydride reduction method. The Pz-POP material synthesized by the application presents a nanowire morphology, the particle size of the Ru nanoclusters is about 2.5 nm, the preparation method is simple and the condition is mild, and the obtained Ru@Pz-POP material exhibits excellent electrocatalytic hydrogen evolution reaction performance and has a potential application prospect.

This invention provides a high-purity pyrazole trace metal ion ultrafiltration-impurity trapping synergistic impurity removal system and method, relating to the field of deep purification technology for electronic chemicals. The method first constructs a supramolecular trapping model based on steric hindrance, utilizing the coordination specificity of functionalized ionic liquids to induce trace metal ions to assemble into nanoscale micelle clusters under isopotential conditions, solving the problems of solute damage and ion back-migration contamination in traditional purification processes. Then, a two-stage synergistic mechanism of chemical complexation and physical sieving is employed, utilizing a surface-modified submicroporous composite membrane to achieve efficient retention of impurity clusters in the organic phase system through size exclusion effect. Finally, dynamic differential pressure compensation and quality self-judgment are performed based on feedforward-feedback dual closed-loop control logic, outputting a purified solution with high purity assurance and intervention strategies. This invention effectively improves the selectivity and stability of the impurity removal process, achieving the ultrapure preparation of electronic-grade pyrazole.