25 results about "Pyrazolylchalcone" patented technology

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.

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 present disclosure relates to choline salts, 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-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection including an infection caused by the HIV virus.

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.

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof, wherein - - - - -, R1, R2, R3a, R3b, R4a , R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

This pyrazole-based squarylium compound is represented by formula (1).　In formula (1), RC represents a primary alkyl group having 2-5 carbon atoms, a secondary alkyl group having 3 or more carbon atoms, or a tertiary alkyl group having 5 or more carbon atoms, and RN represents a primary alkyl group having 2 or more carbon atoms, a secondary alkyl group having 3 or more carbon atoms, or a tertiary alkyl group having 4 or more carbon atoms. When RN represents a tertiary alkyl group having 4 carbon atoms, RC represents at least one selected from a cyclopropyl group, a cyclohexyl group, and a 3-pentyl group.

This invention belongs to the field of environmental protection and discloses a method for synthesizing metal-organic frameworks (MOFs) using a one-pot aqueous phase method. The method includes the following steps: mixing an amino- or aldehyde-containing pyrazolyl derivative, an aldehyde- or amino-containing linker, a copper salt, and pyruvate; adding an acidic solution of water; and then sonicating or stirring at room temperature to obtain a highly crystalline MOF. The amount of pyruvate used may be zero or not zero. When an amino-containing pyrazolyl derivative is selected as the raw material, an aldehyde-containing linker is selected; when an aldehyde-containing pyrazolyl derivative is selected as the raw material, an amino-containing linker is selected. The one-pot aqueous phase synthesis method provided by this invention eliminates the use of organic solvents, greatly reducing environmental impact. It also allows for large-scale synthesis with good reproducibility, a simple synthesis process, and strong operability, showing broad application prospects.

To provide treatment or preventive medication for autism spectrum disorder. [Solution] The present invention provides a PDE10A inhibitor for treating or preventing autism spectrum disorder. The inhibitor is 1-[2-fluoro-4-(1H-pyrazole-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazole-5-yl)pyridazine-4(1H)-one or a salt thereof, and is a therapeutic or prophylactic agent for autism spectrum disorder selected from the group consisting of childhood disintegrative disorder, Rett syndrome, Cleefstra syndrome, Pitt-Hopkins syndrome, Angelman syndrome, Kabuki syndrome, Asperger syndrome, Heller syndrome, and pervasive developmental disorder.

The present application relates to the technical field of electrode, especially to a kind of triatomic catalyst integrated electrode and its preparation method and application.The pyrazole precursor monomer and metal salt are dissolved in solvent respectively in the present application;Then two solutions are sprayed on carbon cloth or carbon paper in turn evenly, and solidified at room temperature;Pyrazole precursor monomer is 2,4,6-tris (4- (1H-pyrazol-4-yl) phenyl) -1,3,5-triazine and / or 1,3,5-tris (1H-pyrazol-4-yl) phenyl;Metal is one or more of Co, Fe, Mn and Ni.The present application utilizes the high reactivity of pyrazole monomer, and generates triatomic catalyst under the traction of metal ion at room temperature, and is in-situ synthesized and grown on the surface of conductive substrate at room temperature, without high-temperature heat treatment, avoids using binder, improves electron conduction rate and structural stability, has good catalytic performance, and has excellent electrochemical performance when assembled into zinc-air battery.

This disclosure relates to the phosphate of 1-((3S,4R)-3-((2-(((1-ethyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-4-fluoropiperidin-1-yl)prop-2-en-1-one, its crystalline form, and a method for its preparation. The phosphate and crystalline form exhibit lower hygroscopicity and improved stability and solubility compared to the free base, thus making them suitable for pharmaceutical applications. Furthermore, the method for preparing the phosphate and crystalline form according to this disclosure has the advantages of large-scale production and improved safety of the preparation process through the use of safer materials than those used in conventional preparation methods.

The application belongs to the technical field of new materials, and particularly relates to a Fe(II) spin crossover complex, a crystal and a preparation method and application thereof. The complex has a molecular formula of [Fe(L 1 )(L 2 )]2(ClO4)4·1.5H2O; a ligand L 1 is trans-4-pentylcyclohexyl-2,6-di(1H-pyrazol-1-yl)isonicotinate; a ligand L 2 is 6,6''-2,6-dimethoxyphenyl-substituted terpyridine; the ligand L 1 of the application is a unique rigid head-flexible tail structure, which is helpful to guide a more ordered packing effect; the ligand L 2 provides a highly rigid and planar structural unit, overcomes the crystallization difficulty of a flexible ligand, and stabilizes a supramolecular structure; the obtained crystal exhibits a unique crystal packing and spatial configuration in a spin state transition process at different temperatures, and realizes optimization of a molecular structure and regulation of spin transition characteristics.

This invention relates to flake silver pigments having a dm in the range of 2.0 to 100.0 µm. 50 With an aspect ratio greater than 25, at least partially coated with an additive component, wherein the additive component is: I) A thiol represented by general formula (Ia): A1-S-A2 or a dithiol represented by general formula (Ib): A1-S-S-A2, wherein A1 and A2 represent alkyl groups having 1 to 8 carbon atoms and A1=A2, or A1 and A2 independently represent residues containing polar or polarizable functional groups selected from the group consisting of esters, carboxyl groups, amines, hydroxyl groups, benzyl groups, benzoic acid groups, furanyl groups, furfuryl groups, pyrroleyl groups, pyridyl groups, pyrazolyl groups, pyrazolyl groups, oxazolyl groups, isoxazolyl groups, ethers, and combinations thereof, wherein these polar or polarizable functional groups are separated from the sulfur or disulfide atom by a maximum of 3 non-aromatic carbon atoms, and wherein the maximum total length of the thiol or dithiol involves a chain containing a maximum of 8 non-aromatic carbon atoms, and the maximum length difference between A1 and A2 is within 2 atoms of each other, or (II) From general formula (IIa): HS-(CH(A3)) x -(R) 1 ) y -A3 represents or is derived from general formula (IIb): HS-R 4 -CO-O-R 5 The thiol represented by R 1 It is an alkylene or phenylene having 1 to 6 carbon atoms, wherein A3 is independently selected from NR. 2 2. OH, COOH, COOR 3 The group consisting of N-succinimide and 1-amino-2-carboxyethyl, wherein integers x and y are 0 or 1, and x + y = 1 or 2, and wherein R 2 Independently selected from the group consisting of H, methyl, ethyl, and propyl, and R among them. 3 Select from the group consisting of H, methyl, ethyl or propyl, butyl, pentyl, hexyl, N-succinimide and 2-aminoacetyl acid, and R among them. 4 It is methylene or ethylene, and R in it 5 The additive component is selected from the group consisting of alkyl groups having 1 to 6 C atoms and N-succinimides, wherein the maximum total length of the thiol of formula (IIa) or (IIb) involves a chain containing up to 8 non-aromatic C atoms, or (III) is an amine having ether functionality and not more than 8 non-aromatic C atoms, and wherein the additive component can be one molecule or a mixture of two or more of any molecule represented by any one of formulas (Ia), (Ib), (IIa), (IIb) and (III).

The present disclosure relates to methods of making N2-(3-(2-(2H-1, 2, 3-triazol-2-yl)propan-2-yl)-1-cyclopropyl-1H-pyrazol-5-yl)-N4-ethyl-5-(trifluoromethyl)pyrimidine-2,4-diamine and intermediates thereof.

The present disclosure relates to targeted drug conjugates comprising an ALK5 inhibitor and a targeting moiety that directs the ALK5 inhibitor to cells involved in fibrosis and cancer, such as myofibroblasts, activated fibroblasts and transitional fibroblasts, and their uses, in particular wherein the ALK5 inhibitor is N-methyl-2-(4-(4-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)phenoxy)ethan-1-amine.

This invention discloses a method for preparing a key intermediate of an androgen receptor inhibitor. The method uses (S)-4-(1-(2-aminopropyl)-1H-pyrazol-3-yl)-2-chlorobenzonitrile or its salt and 5-acetyl-1H-pyrazol-3-carboxylic acid as starting materials, and synthesizes the compound (S)-5-acetyl-N-[1-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]propyl-2-yl]-1H-pyrazol-3-carboxamide (Formula 1) under the action of a triazine condensing agent. This method has the advantages of simple and safe operation, low cost, and high yield, providing a new industrially feasible method for the synthesis of dallotamine.

This invention discloses an anionic energetic complex based on APTTz, its preparation method, and its applications. APTTz is 6-(1H-pyrazol-1-yl)-[1,2,4]triazolo[4,3-b][1,2,4,5]tetraazine-3-amine. The general structural formula of the anionic energetic complex based on APTTz is [X m (APTTz) p Y t ] n· In zH₂O, X is a metal cation, and Y is an acid radical anion; the values ​​of m range from 1 to 2, P range from 1 to 3, t range from 1 to 2, and z range from 0 to 2. The triazolotetraazine anionic energetic complex obtained in this invention exhibits a detonation response upon laser irradiation, demonstrating good safety and detonation performance. It can be used as a laser-initiated explosive or as a component of explosives and propellants, showing promising application prospects in the field of high-energy insensitive energetic materials. The APTTz-based anionic energetic complex prepared in this invention can be used as a combustion catalyst for composite propellants and modified double-base propellants, significantly improving the combustion rate of composite propellants and modified double-base propellants and reducing the platform pressure index.

This invention belongs to the field of molecular-based functional materials and molecular electronic devices, specifically disclosing a coordination compound material based on an iron-cobalt bimetallic center, its preparation method, and its application. The chemical formula of the material is {[(pzTp)Fe Ⅲ (CN)3]2Co Ⅱ (3,4-bit)}·4CH3OH·2.5H2O, where pzTp is the tetra(1-pyrazolyl)borate ligand of the iron center, and 3,4-bit is the bidentate bridging ligand 3,4-bis(1-imidazolyl)thiophene. The material uses iron and cobalt ion centers as electron transfer pairs, and cyano (CN) groups as bridging groups to construct Fe–CN–Co coordination units. The coordination field strength, steric hindrance, and crystal stacking mode of the iron and cobalt metal centers are controlled by nitrogen-containing ligands. This invention develops a novel Fe–Co molecular device material that integrates electron transfer, spin-transformation, and multi-physics signal output in a single material. This material has outstanding advantages such as structural stability, reversible signal switching, and significant multi-stable-state coupling, and has broad application prospects in molecular information storage, multifunctional switches, and intelligent response materials.

This invention discloses a micron-scale, bulk-stable trimetallic MOF oxygen evolution catalyst, its preparation method, and its application. The catalyst is prepared by reacting a pyrazolyl-Salen with a nickel salt in methanol at room temperature overnight. After the reaction, the precipitate is filtered, washed, and then slurried in methanol. Finally, it is vacuum dried to obtain Ni-pyrazolyl-Salen, with the following structural formula: The obtained Ni-pyrazolyl-Salen and Zn salt are dispersed in a reaction solvent and reacted at 100-140℃ for 60-80 h. After precipitation, washing, and drying, it undergoes an ion exchange reaction with a divalent Fe salt, thus completing the preparation. This catalyst, used in water electrolysis under strongly alkaline conditions, exhibits excellent oxygen evolution performance and electrochemical stability, superior to commercial RuO2 catalysts and most original MOF oxygen evolution catalysts.

The present invention provides compounds of Formula (I): wherein all of the variables are as defined herein. These compounds are inhibitors of calcium calmodulin dependent protein kinase 2 (CAMK2), which may be used as medicaments for the treatment of heart failure, and related diseases.

This invention relates to a europium-based metal-organic framework material constructed based on 4-((3-(pyrazin-2-yl)-1H-pyrazol-1-yl)methyl)benzoic acid ligand, its preparation method, and its applications. The invention pertains to the fields of metal-organic framework materials, luminescent functional materials, and fluorescence sensing technologies. The chemical formula of the europium-based metal-organic framework material prepared by this invention is: [Eu(ppmb)2(NO3)(H2O)2] n ; where ppmb is the ligand after deprotonation of Hppmb; the structure of Hppmb is; the europium-based metal-organic framework material belongs to the triclinic crystal system, space group P-1, and unit cell parameters are a=9.727(4) Å, b=14.197(5) Å, c=25.615(9) Å, α=77.899(1)°, β=86.231(1)°, γ=70.044(1)°, and it is used in the detection of furazolidone.