1907 results about "Pyrazole" patented technology

This invention relates to a crystalline 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I),and compositions thereof. Also disclosed herein are methods of making the same and methods of using the same.

The invention belongs to the technical field of liquid chromatography-mass spectrometry detection pretreatment, and particularly relates to a pretreatment method for liquid chromatography-tandem mass spectrometry analysis of pesticide and veterinary drug residues in serum, which comprises the following steps: (S1) carrying out heating reaction on Sc (III) salt, Cu (II) salt and 1H-pyrazole-4-formic acid (H2PyC) in a polar aprotic solvent, and cooling to obtain a green crystal, namely MOF-919; the chemical formula of the MOF-919 is [Sc < 3 > (mu3-O) (OH) < 3 >] [Cu3 (mu3-O) (mu-PyC) < 3 > (H2O) < 6 >] < 2 >; (S2) mixing the serum sample with an acetonitrile solution containing formic acid, carrying out ultrasonic treatment, vortex oscillation and centrifugation, taking supernate, and diluting the supernate with an aqueous solution containing formic acid to obtain a to-be-purified solution; and (S3) adding MOF-919 into the to-be-purified liquid, mixing, performing ultrasonic treatment, performing vortex oscillation, centrifuging, and taking supernate, thereby completing the pretreatment of the to-be-purified liquid. According to the method, the MOF-919 is used for adsorbing chemical pollutant residues in serum, especially phospholipids, so that the purpose of removing the chemical pollutant residues in blood is achieved. The method is simple and convenient to operate, small in organic solvent consumption and good in purification effect, and can be widely applied to residue analysis of chemical pollutants in serum.

The invention relates to a pyrazole fused ring compound as well as a preparation method and application thereof. Specifically, the invention relates to a compound shown in a general formula (I), a preparation method of the compound, a pharmaceutical composition containing the compound and application of the compound serving as an FGFR inhibitor in tumor treatment. Wherein each group in the general formula (I) is defined in the specification. # imgabs0 #

The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-TH-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

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.

A dry film resist, a photosensitive dry film, and a copper clad laminate. The dry film resist includes an alkali-soluble resin (A), a photopolymerization monomer (B), a photoinitiator (C), and a sensitizer (D); and the sensitizer (D) includes a compound containing a pyrazoline structure.

The present invention provides a compound having the basic structure shown by Formula (I) in which the indole ring and the pyrazolopyridine structure is bound through a substituent, a salt thereof or a solvate of either the compound or a salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound, salt or solvate as an active ingredient.

The present invention relates to the technical field of pesticides, and in particular to a pyrazole amide compound and a use thereof. The compound is as shown in general formula I, wherein Q represents O or S, W represents CH or N, X represents hydrogen, halogen, alkyl, etc., Y represents halogen or alkyl, Z represents alkyl, alkenyl, alkynyl, cycloalkyl, etc., and M represents hydrogen or alkyl. The compound has good prevention and treatment activity on pests such as green peach aphids, peanut aphids, and bird cherry-oat aphids.

Methods for treating immune thrombocytopenia comprising administering at least one compound chosen from (R)-2-[3-[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 (rilzabrutinib) and pharmaceutically acceptable salts thereof are disclosed.

The present invention provides pyrazole-containing fused ring compounds, a pharmaceutical composition thereof and the use thereof. The present invention provides compounds as shown in formula I or pharmaceutically acceptable salts thereof. The compounds are small molecule compounds for non-invasive administration, have the same or similar effect as polypeptide GLP-1 agonists, and have the advantages of one or more of higher biological activity, better metabolic stability and excellent bioavailability.

The present invention relates to a ternary insecticidal composition of 3-[benzoyl(methyl)amino]-N-[2-bromo-4-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)- 6-(trifluoromethyl)phenyl]-2-fluorobenzamide (Component A), 4-chloro-5-ethyl-2-methyl-N-[[4-(4-methylphenoxy)phenyl]methyl] pyrazole-3-carboxamide (Component B) and at least one insecticide (Component C) demonstrating an effective and synergistic broad spectrum control of insects-pests and mites with one shot application by developing delay in resistance of hard to kill and resistant towards insects-pests and mites Further, the ternary insecticidal composition provides residual control and increases yield of treated plants due to protection against insect-pests and mites. The ternary insecticidal composition of present invention increases overall health and plant vigor and is environmentally safe.

The invention relates to substituted pyrazolo piperidine carboxylic acids, their salts and to processes for their preparation, and also to their use for preparing medicaments for the treatment and / or prophylaxis of diseases, in particular cardiovascular and cardiac diseases, preferably heart failure with reduced and preserved ejection fraction (HFrEF, HFmrEF and HFpEF), hypertension (HTN), peripheral arterial diseases (PAD, PAOD), cardio-renal and kidney diseases, preferably chronic and diabetic kidney disease (CKD and DKD), cardiopulmonary and lung diseases, preferable pulmonary hypertension (PH), and other diseases, preferably neurodegenerative diseases and different forms of dementias, fibrotic diseases, systemic sclerosis (SSc), sickle cell disease (SCD), wound healing disorders such as diabetic foot ulcer (DFU).

Modified release formulations, such as solid oral dosage forms comprising a core composition comprising Compound (I) and / or a pharmaceutically acceptable salt thereof; a sub-coating layer coating the core composition, said sub-coating layer comprising a polyvinyl alcohol and / or a hydroxypropyl methyl cellulose; and an enteric coating layer encapsulating the sub-coating layer and the core composition, said enteric coating layer comprising at least one polymer selected from an acrylic / methacrylic / ethacrylic acid homopolymer and copolymers thereof, a cellulose derivative, and a polyvinylpyrrolidone, and methods of administration of a Bruton's tyrosine kinase (BTK) inhibitor using said formulations.

The invention discloses a pesticide composition containing a pyrazolecarboxamide pesticide and application of the pesticide composition. The pesticide composition comprises an active component A which is the pyrazolecarboxamide pesticide and a component B which is at least one other pesticide defined in the specification, specifically, the invention relates to a pesticide composition for preventing and treating common lepidoptera, coleoptera, diptera, thysanoptera and homoptera pests of plants.

The invention relates to a compound according to general formula (I), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to said compound(s) for use as in a method of treating a skin disorder; eye disease; ear disease; mouth, throat and respiratory disease; gastrointestinal disease; liver, gallbladder and pancreatic disease; urinary tract and kidney disease; disease of male genitale organs and female genitale organs; disease of the hormone system; metabolic disease; cardiovascular disease; blood disease; lymphatic disease; disorder of the central nervous system; brain disorder; musculoskeletal system disease; allergy disorder; pain; infectious disease; inflammatory disorder; injury; immunology disorder; cancer; hereditary disease; or edema.

The invention relates to the technical field of energetic materials, in particular to a laser response type high-entropy alloy-based initiating explosive material and a preparation method thereof. The initiating explosive material is mainly formed by uniformly loading a heat-sensitive high-energy compound (such as lead stilbeneate or hexa (4-amino-3, 5-dinitropyrazole) copper) on high-entropy alloy nanoparticles containing five or more metal elements, wherein the heat-sensitive high-energy compound is such as lead stilbeneate or hexa (4-amino-3, 5-dinitropyrazole) copper. The preparation method comprises the following steps: mixing acetylacetone metal salt, a surfactant and a reducing agent in an organic solvent, and stirring and reacting at 180-220 DEG C to prepare high-entropy alloy nanoparticles; the nano particles and a high-energy compound are co-dispersed in a mixed solvent containing a dispersing agent, ultrasonic treatment is carried out to form suspension liquid, and freeze drying is carried out to obtain the nano particles. The method is characterized in that the excellent photo-thermal conversion performance of the high-entropy alloy is utilized, under low laser energy irradiation, a high-energy compound can be effectively excited, and stable detonation of secondary charge CL-20 is successfully achieved. According to the invention, the problems of high response threshold and low output energy of the existing laser initiating explosive material are solved.

The invention relates to a novel compound as well as a preparation method and application thereof, in particular to (Z / E)-1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-3-aryl-2-(1H-pyrazol-1-yl)-2-propylene-1-ketone as well as a preparation method and application thereof in preparation of an anti-tumor drug, and discloses a preparation method of (Z / E)-1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-3-aryl-2-(1H-pyrazol-1-yl)-2-propylene-1-ketone. The structural formula of the compound 1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-3-aryl-2-(1H-pyrazol-1-yl)-2-propylene-1-ketone is as shown in a formula I or a formula II: # imgabs 0 #, and the structural formula of the compound 1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-3-aryl-2-(1H-pyrazol-1-yl)-2-propylene-1-ketone is as shown in a formula II. Wherein R1 is selected from a methoxy group, an ethyoxyl group or a propoxy group; r1 is selected from methyl, methoxy, ethyoxyl, nitro, iodine, bromine, chlorine, fluorine, 2, 4-difluoro, 2, 4-dichloro, 2, 3, 4-trichloro, 2, 4-dimethoxy and 2, 3, 4-trimethoxy, and R2 is selected from methyl, methoxy, ethyoxyl, nitro, iodine, bromine, chlorine, fluorine, 2, 4-difluoro, 2, 4-dichloro, 2, 3, 4-trichloro, 2, 4-dimethoxy and 2, 3, 4-trimethoxy.

The invention relates to the technical field of synthesis of pyroxasulfone intermediates, in particular to a synthesis method and application of a pyroxasulfone intermediate. Comprising the following preparation steps: (1) adding a reaction solvent into sodium formaldehyde sulfoxylate, adding 1-methyl-3-trifluoromethyl-5-hydroxy-1H-pyrazole, heating, and completely reacting to obtain sodium hydroxypyrazole methyl sulfinate; and (2) cooling the reaction liquid, adding acetonitrile and alkali liquor, introducing monochlorodifluoromethane gas, after the reaction is completed, concentrating, removing acetonitrile and water, adding methanol, stirring, filtering, and concentrating the filtrate to obtain the pyroxasulfone intermediate difluoromethoxy pyrazole methyl sodium sulfinate. The specific reaction process is as follows. According to the method, the sodium formaldehyde sulfoxylate which is low in cost and easy to obtain is used, synthesis of a 5, 5-dimethyl-4, 5-dihydroisoxazole thioether compound is avoided when pyroxasulfone is prepared from the intermediate obtained in the invention, three wastes and production cost are reduced, industrial production is easy to realize, and the method has relatively high practical value.

Described herein are pharmaceutical formulations of a farnesoid X receptor agonist, 4-((4-(1-(tert-butyl)-1H-pyrazol-4-yl)pyridin-2-yl)((4-(4-methoxy-3-methylphenyl)bicyclo[2.2.2]octan-1-yl)methyl)carbamoyl)cyclohexyl 3-hydroxyazetidine-trans-1-carboxylate, and methods of using such pharmaceutical formulations in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Provided herein are optionally substituted pyrazolylacetamides, pharmaceutical compositions comprising a therapeutically effective amount of such compounds and a pharmaceutically acceptable excipient, and methods of treating diseases or disorders, such as, epilepsy, amyotrophic lateral sclerosis, various types of pain, hyperexcitability, a dyskinesia, dystonia, mania, tinnitus, neurodevelopmental diseases or disorders, a smooth muscle contractility disorder, Dravet syndrome, posttraumatic stress disorder (PTSD), with such compounds and pharmaceutical compositions.

Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for the treatment of retinal binding protein (RBP4) related diseases, such as obesity and the like.

Methods for treating patients with moderate-to-severe asthma comprising administering a therapeutically effective amount of at least one compound chosen from (R)-2-[3-[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 (rilzabrutinib) and pharmaceutically acceptable salts thereof are disclosed.

Provided are crystalline forms of N-methyl-N-((1s,3s)-3-methyl-3-((6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)oxy)cyclobutyl)acrylamide, pharmaceutical compositions, methods of use and methods of making thereof.

The invention belongs to the technical field of pesticide preparations, and particularly relates to kresoxim-methyl drug-loaded microspheres as well as a preparation method and application thereof. The 9% pyraclostrobin drug-loaded microspheres (Pyr (at) COzein) are prepared by modifying a Zein-pesticide emulsifier 500 # complex with n-caprylic alcohol, and the n-caprylic alcohol has a synergistic effect on pyraclostrobin, so that not only can the defect of a sustained and controlled release preparation in the aspect of fast-acting sterilization be made up, but also the use dosage of pyraclostrobin can be reduced, the risk of pesticide residue can be reduced, and the drug-loaded microspheres have a good application prospect. The ecological safety is improved.

The invention discloses a continuous flow production method of high-purity chlorantraniliprole, and belongs to the technical field of chemical synthesis. The method comprises the following steps: simultaneously pumping a mixed solution containing 3-bromo-1-(3-chloro-2-pyridyl)-1H-pyrazole-5-formic acid, a solvent, an acid-binding agent and 2-amino-5-chloro-N, 3-dimethylbenzamide and a catalyst solution into a mixing unit of a continuous flow reactor I to form a reaction mixture flow; the material flow enters a continuous flow reactor I for condensation reaction to obtain a chlorantraniliprole solution; simultaneously pumping the mixed solution and a quenching agent solution into a continuous flow reactor II, and quenching to separate out crystals; and continuously centrifugally separating the quenching liquid containing the crystals, washing and drying to obtain a chlorantraniliprole refined product. According to the present invention, the full continuous flow process is adopted, the reaction unit and the post-treatment unit are included, the material continuously flows, and when the process is stable, the material composition, the temperature and other parameters in the reactor are only related to the reaction position and do not change with time, such that the production process and the product quality stability are ensured.

The invention belongs to the technical field of organic synthesis, and particularly relates to a pyroxasulfone preparation method which specifically comprises the following steps: dissolving 3-(5-difluoromethoxy-1-methyl-3-trifluoromethyl-1H-pyrazol-4-ylmethylthio)-5, 5-dimethyl-2-isoxazoline serving as a raw material with a solvent, then adding a boron compound, finally dropwise adding hydrogen peroxide, and reacting at room temperature to obtain the pyroxasulfone. Reacting for several hours to obtain pyroxasulfone; the adopted boron compound is cheap and easy to obtain, so that the use of a transition metal catalyst is avoided, and the raw material cost is reduced; organic acid reagents with heavy odor are not used, waste water and solid waste are less, and the method has great advantages in the aspect of environmental protection; the method is simple to operate, free of complex treatment steps and suitable for industrial production, and when the boron compound is selected from sodium metaborate, sodium perborate or a mixture of borax and sodium metaborate, the yield and purity of the process are higher, and sulfoxide impurities are fewer.

The invention provides an epoxy adhesive solution composition, a preparation method of an epoxy adhesive solution and a modified cellular board. The epoxy adhesive liquid composition comprises the following components in parts by weight: 53-58 parts of epoxy resin, 2-10 parts of a silane coupling agent, 1-10 parts of a curing agent, 1-5 parts of blocked isocyanate and 60-70 parts of water, wherein a blocking group of the blocked isocyanate is selected from hydroxyl, oximido, acylamino, amino, imidazolyl, pyrazolyl or piperazinyl. By introducing the blocked isocyanate with the specific structure, the epoxy adhesive liquid can be subjected to pre-crosslinking reaction in the early drying treatment process, the modulus and high temperature resistance of a formed dry film are improved, and the phenomenon of glue overflow in the subsequent curing stage is inhibited; therefore, the structural integrity and the bonding strength of the adhesive layer in the modified cellular board under the high-temperature condition are improved.

The present disclosure relates to pyrazoloheteroaryl derivatives, their preparation methods, and their pharmaceutical applications. Specifically, the present disclosure relates to pyrazoloheteroaryl derivatives represented by general formula (I), their preparation methods, pharmaceutical compositions containing the derivatives, and their use as therapeutic agents, particularly their use as ATR kinase inhibitors and in the preparation of medicaments for treating and / or preventing hyperproliferative diseases. The definitions of each group in general formula (I) are as described in the specification. TIFF2023502458000095.tif4136

Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.

There is provided a process for preparing 5,7-dimethyl-N-((1R,4R)-4- (pentyloxy)cyclohexyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide, said process comprising at least a step of amide coupling a 5,7-Dimethylpyrazolo[1,5-a]pyrimidine-3-carboxylic acid with trans-4-(pentyloxy)cyclohexanamine using carbonyldiimidazole (CDI).