101 results about "Pyrazole Compound" patented technology

To provide a novel pest control agent composition, particularly a bactericidal composition.SOLUTION: A bactericidal or bacteriostatic composition comprising an active ingredient A selected from pyrazole compounds or salts thereof represented by formula (I): [G represents G-1; G1 represents C1-C6 haloalkyl or the like; T represents an oxygen atom or the like; RX represents C1-C6 alkyl or the like; RY represents a hydrogen atom or the like; R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom or the like; R3 represents a hydrogen atom or the like; Ra represents a hydrogen atom or the like; Z represents Z-1 or the like; Z1 represents C1-C6 alkyl or the like; m5 and n5 each represent an integer of 0, 1, 2, 3, 4, or 5; and p represents an integer of 0 or 1] and an active ingredient B selected from known bactericidal or bacteriostatic compounds.SELECTED DRAWING: None

The present invention belongs to the technical field of pesticides and specifically relates to a substituted pyrazole compound containing pyrimidine and a use thereof. The compound is represented by general formula I: where Q represents an aryl group or a heterocyclic group; Y1 and Y2 each independently represent hydrogen, alkyl, or the like; R1 and R2 each independently represent hydrogen, halogen, nitro, or the like; R3 represents hydrogen, alkyl, or the like; R4, R5, R6, and R7 each independently represent hydrogen, alkyl, or halogenated alkyl; and R8 and R9 each independently represent hydrogen, halogen, cyano, alkyl, or the like. The described compound exhibits good control activity against fungi, etc.

Disclosed herein are embodiments of a pyrazole compound according to formula I.Compositions comprising the compound, and a method for making the composition also are disclosed. The composition may comprise a carrier, such as a polymer and / or the composition may be a spray-dried formulation. Also disclosed is a method for using the compound and / or composition. The compound and / or composition may be useful to inhibit an IRAK protein and / or to ameliorate, treat and / or prevent an IRAK-associated disease or condition in a subject.

The present invention describes novel boron containing pyrazole compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as Janus kinase (JAK) inhibitors and are useful in the in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described are methods of treating inflammation, auto-immune diseases, cancer, and other conditions that are susceptible to the inhibition of a Janus kinase by administering a compound herein described.

The present application relates to a kind of preparation method of trifluoromethyl pyrazole compound, belong to the technical field of organic synthesis.The specific method is: (1) trifluoroacetyl ethyl acetate is first with hydrazine hydrate cyclization reaction and generates compound of formula III;(2) under the catalysis of base, compound of formula III is reacted with difluoromethylation reagent and generates compound of formula II;(3) compound of formula II is reacted with methylating agent and obtains compound of formula I;The difluoromethylation reagent is difluoro-monochloromethane or sodium difluoro-monochloroacetate;The methylating agent is chloromethane, bromomethane, iodomethane, dimethyl sulfate or dimethyl carbonate.The present application is prepared by changing reaction route, and the higher-priced raw material methylhydrazine is replaced, and isomer impurity is no longer generated in the product prepared.Not only raw material cost is reduced, but also the purity of product is improved.

The present application belongs to the field of agricultural fungicides, and particularly relates to a fungicidal composition and application thereof.The composition comprises two active components A and B, the weight ratio of the active component A to the active component B is 1:99-99:1; the active component A is one or more of substituted pyrazole compounds containing pyrimidine or salts thereof, and the active component B is selected from one fungicide.The fungicidal composition is particularly suitable for preventing and treating various plant pathogenic fungi and bacterial diseases.

Disclosed herein are embodiments of a method for treating a disease or condition in a subject, comprising administering to the subject, a pyrazole compound according to formula I.The compound may be administered as a composition, such as a spray-dried formulation. The disease or condition may be hidradenitis suppurativa, or a lymphoid neoplasm, and may be chronic myeloid leukemia or chronic myelomonocytic leukemia.

The application discloses a kind of thieno [2, 3-c] pyrazole compounds in preparation antitumor drug purposes, belong to pharmaceutical chemistry technical field.The application provides a kind of small molecule skeleton thieno [2, 3-c] pyrazole compound I and II, compound I is 2-oxo benzo [d] [1, 3] oxathiole-6-yl 1-(3-fluorophenyl)-3-methyl-1H-thieno [2, 3-c] pyrazole-5-carboxylate.Compound II is 1-(4-chlorophenyl)-N-[4-((4-ethylpiperazine-1-yl)methyl)phenyl]-3-methyl-1H-thieno [2, 3-c] pyrazole-5-formyl.Both have strong antitumor activity.Compound II has strong inhibition to a variety of human tumor cells, such as bone sarcoma MG63, breast cancer HCC1806, liver cancer LM3, lung cancer A549, colorectal cancer HCT-8 and the like, provides new candidate compounds for broad-spectrum antitumor drugs.

The present invention relates to the use of novel nitrification inhibitors of formula I, which are N-functionalized alkoxy pyrazole compounds. Moreover, the invention relates to the use of compounds of formula I as nitrification inhibitors, i.e. for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors of formula I.

This invention discloses a method for preparing 4-(trifluoromethylsulfinyl)pyrazole compounds, comprising: dissolving terminal alkyne in n-hexane under nitrogen atmosphere, adding anhydrous zinc chloride, and reacting trifluoromethylsulfinyl chloride to obtain α-trifluoromethylalkynyl sulfoxide; adding benzoyl chloride dropwise to a CH2Cl2 solution of phenylhydrazine and triethylamine under nitrogen atmosphere to obtain acylhydrazine; adding carbon tetrachloride to a suspension of acylhydrazine and triphenylphosphine in acetonitrile to obtain hydrazone chloride; and reacting α-trifluoromethylalkynyl sulfoxide, hydrazone chloride, potassium carbonate, and anhydrous ethanol at room temperature to obtain 4-(trifluoromethylsulfinyl)pyrazole compounds. This invention uses inexpensive and readily available raw materials, the entire reaction route is mild and simple to operate, does not require stringent reaction conditions, and most of the reaction process is carried out at room temperature. The product yield is high, and the prepared trifluoromethylalkynyl sulfoxide pyrazole structure has multiple derivatization sites, showing good application prospects.

The present application belongs to the field of agricultural fungicides, and particularly relates to a fungicidal composition and application thereof.The composition comprises two active components A and B, the weight ratio of the active component A to the active component B is 1:99-99:1; the active component A is one or more of substituted pyrazole compounds containing pyrimidine or salts thereof, and the active component B is selected from one fungicide.The fungicidal composition is particularly suitable for preventing and treating various plant pathogenic fungi and bacterial diseases.

A fluorine-containing pyrazole compound is represented by the following general formula (1):wherein in formula (1) above, R represents a hydrocarbon group having 1 to 12 carbon atoms, and a ring Z represents an aromatic heterocyclic ring containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom.

The present invention relates to a preparation method and use of a pyrazole compound containing a fluorinated phenyloxybipyridine unit. The compound is obtained by condensing a fluorinated phenyloxypyridylamine with a substituted pyrazole carboxylic acid. The pyrazole compound containing a fluorinated phenyloxybipyridine unit has excellent insecticidal activity against harmful insects and can be used to prepare insecticides for use in agriculture, horticulture, and other fields.

The application discloses a preparation method of an amido pyrazole compound and a method for preparing sildenafil by using the same. The amido pyrazole compound is shown as formula I. The compound of formula I is prepared by using 2-pentanone as an industrial chemical, and can be used for synthesizing sildenafil which is a selective inhibitor of type 5 phosphodiesterase (PDE5). The method has the advantages of easy availability of raw materials, simple operation, avoidance of nitration reaction, avoidance of safety hidden dangers caused by the nitration reaction from a technical source, and avoidance of environmental protection pressure caused by a large amount of nitration waste liquid, and is suitable for development into a green and sustainable production process of sildenafil bulk drug.

The invention discloses a pyrazole STING inhibitor and medical application thereof, the structure of the pyrazole compound is shown as a formula I. The compound shown as the formula I is a potent STING inhibitor and has good pharmacokinetic properties, and the compound shown as the formula I or pharmaceutically acceptable salt thereof can be used for preparing drugs for preventing or treating STING-mediated diseases.

The application discloses a kind of benzofuran pyrazole compounds or its pharmaceutically acceptable salt or deuteride and preparation method and application thereof.A variety of biological experiments confirm that the compound prepared in the application has MYC inhibitory activity, and has significant antitumor activity and can enhance the response of tumor to immunotherapy, and can be used as MYC inhibitor for the treatment of tumor and other MYC related diseases, and has good application prospect.

The application belongs to the technical field of organic synthesis, and particularly relates to a 1,3,5-trisubstituted pyrazole compound and a preparation method thereof. The preparation method of the 1,3,5-trisubstituted pyrazole compound provided by the application comprises the following steps: mixing a hydrazine compound, an alpha-bromoketone compound, a photocatalyst, an alkaline compound, an additive and a polar organic solvent, and performing an addition cyclization reaction under light irradiation to obtain the 1,3,5-trisubstituted pyrazole compound. The preparation method has the advantages of mild conditions, easy control, high reaction efficiency, economical steps, cheap and easily available raw materials, no use of oxidants, good functional group tolerance and the like, and the prepared 1,3,5-trisubstituted pyrazole compound has high purity, the purity is 98.5-99.9%, and has great market promotion value.

Compounds represented by Formula I in which A0-A2, R0-R6, L, Z and Q are defined herein. The compounds of Formula I are CHK 1 inhibitors. Therefore, the compounds can be used to treat diseases, disorders and conditions associated with continuous activation of CHK1 or with high internal DNA damage or injury during DNA replication, such as cancers.

The invention discloses application of a thieno [2, 3-c] pyrazole compound in preparation of antitumor drugs, and belongs to the technical field of medical chemistry. The invention provides a small molecular skeleton thieno [2, 3-c] pyrazole compound I and a small molecular skeleton thieno [2, 3-c] pyrazole compound II, and the compound I is 2-oxobenzo [d] [1, 3] oxathiacyclopentane-6-yl 1-(3-fluorophenyl)-3-methyl-1H-thieno [2, 3-c] pyrazole-5-formate. And the compound II is 1-(4-chlorphenyl)-N-[4-((4-ethyl piperazine-1-yl) methyl) phenyl]-3-methyl-1H-thieno [2, 3-c] pyrazole-5-formyl. The two compounds have relatively strong anti-tumor activity. Wherein the compound II has a relatively strong inhibition effect on various human tumor cells such as osteosarcoma MG63, breast cancer HCC1806, liver cancer LM3, lung cancer A549, colorectal cancer HCT-8 and the like, and a new candidate compound is provided for broad-spectrum antitumor drugs.

The application belongs to the technical field of chemical drugs, and particularly relates to a pyrazole compound and a preparation method and application thereof. The application provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, which not only has good myeloperoxidase (MPO) inhibitory activity, but also can be used for treating and / or preventing cardiovascular diseases. (I)

The utility model belongs to the technical field of 5-hydroxy-1-methyl-3-trifluoromethyl-1H-pyrazole preparation, and particularly relates to a pyrazole compound suction filtration device which comprises a Buchner funnel, a suction filtration box, a liquid collection box and a vacuum assembly, the Buchner funnel is connected to the suction filtration box, the vacuum assembly comprises a first guide pipe and a second guide pipe, and the first guide pipe is connected with the liquid collection box. One end of the first guide pipe is connected with the top of the suction filtration box, and the other end of the first guide pipe is connected with the top of the liquid collection box; a third guide pipe is further arranged at the position, close to the top, of the liquid collecting box and connected with a power device. Compared with the prior art, the device disclosed by the utility model can be used for amplifying production and realizing continuous suction filtration, and meanwhile, the stability of the device in an operation process is improved.

Disclosed herein are pyrazole compounds, formulations thereof, and methods of using the compounds and / or formulations. Disclosed herein are embodiments of pyrazole compounds according to Formula (I). Also disclosed are compositions comprising the compounds, and methods of making the compositions. The composition may comprise a carrier, such as a polymer, and / or the composition may be a spray-dried formulation. Methods of using the compounds and / or compositions are also disclosed. The compounds and / or compositions may be used to inhibit IRAK proteins and / or to ameliorate, treat and / or prevent IRAK related diseases or conditions in a subject. (I)

The present application belongs to the field of agricultural fungicides, and particularly relates to a fungicidal composition and application thereof.The composition comprises two active components A and B, the weight ratio of the active component A to the active component B is 1:99-99:1; the active component A is one or more of substituted pyrazole compounds containing pyrimidine or salts thereof, and the active component B is selected from one fungicide.The fungicidal composition is particularly suitable for preventing and treating various plant pathogenic fungi and bacterial diseases.

The invention belongs to the technical field of pesticides, and particularly relates to a substituted pyrazole compound, a preparation method thereof, a weeding composition and application. The compound is shown as a general formula I, in the general formula I, M1 and M2 independently represent N or CR9, and at least one of M1 and M2 is N; m3 represents N or CR5; x represents hydrogen, halogen,-OX1,-(CO) OX2,-(CO) SX2 or-(CO) N (X2) 2; x1 represents hydrogen, an alkyl group, an alkenyl group, an alkynyl group, or the like; each X2 independently represents hydrogen, an alkyl group, an alkenyl group, an alkynyl group, or the like; z represents halogen, cyano, nitro and the like; y, R1, R2, R3, R4, R5, R6, R7, R8, and R9 each independently represent hydrogen, halogen, cyano, or the like. The compound has excellent herbicidal activity and crop safety.

Provided is a radioactive triphenylpyrazole compound that is useful as an active ingredient of a pharmaceutical composition, particularly an imaging agent, and is stable in vivo. 4-(4-[18F]fluoro-2-(1-phenyl-5-(2-(trifluoromethyl)phenyl)-1H-pyrazole-3-yl)phenoxy)butanoic acid or a salt thereof can be used as a radioactive triphenylpyrazole compound according to the present invention.

The present application relates to the technical field of organic synthesis, in particular to a synthesis method of polysubstituted pyrazole compounds, which comprises adding aryl diazonium salt 0.6 mmol, enone 0.9 mmol, 0.5 ml of acid and 0.3 mmol of electrolyte into a 10 ml three-necked bottle, and then adding 6 ml of solvent to dissolve; using a carbon rod as an anode and a platinum plate as a cathode, stirring the reaction, monitoring the reaction process by using thin layer chromatography, after the reaction is completed, extracting the mixture with ethyl acetate; drying the organic layer of the mixture with anhydrous sodium sulfate, rotary evaporating the solvent under reduced pressure, purifying the residue by column chromatography, and obtaining the target product; the method uses aryl diazonium salt as a double synthetic substrate under mild electrochemical conditions, continuously generates two free radicals by electrochemical reduction of aryl diazonium salt, directly synthesizes a series of polysubstituted pyrazole compounds, directly and orderly constructs polysubstituted pyrazole compounds without transition metal or external redox agent, is environment-friendly, efficient and high in atom economy.

The invention belongs to the technical field of pesticides, and particularly relates to a pyrimidine-containing substituted pyrazole compound and application thereof. The compound is shown as a general formula I, wherein Q represents aryl or heterocyclic radical; y1 and Y2 each independently represent hydrogen, an alkyl group, or the like; r1 and R2 respectively and independently represent hydrogen, halogen, nitro and the like; r3 represents hydrogen, alkyl or the like; r4, R5, R6, and R7 each independently represent hydrogen, an alkyl group, a haloalkyl group, or the like; r8 and R9 independently represent hydrogen, halogen, cyano, alkyl or the like. The compound has good control activity on fungi and the like.

The application belongs to the technical field of organic compounds and agricultural fungicides, and particularly relates to the antifungal application of a novel pyrazole compound. The application provides a novel pyrazole compound, which has a structure shown in formula (a). The pyrazole derivative has good antibacterial activity on various fungi and can be used for preparing an agricultural fungicide. Moreover, the pyrazole compound in the application has the advantages of simple synthesis and high yield, and overcomes the problems of complex synthesis and low yield of current pyrazole fungicides. The application has important significance for promoting the application of pyrazole fungicides in the disease control of crops, fruits and vegetables. The application not only provides a new control drug for crop fungi and fungal diseases caused by the fungi, but also enriches the resource library of pyrazole fungicides, and provides more choices for the application of pyrazole derivatives in the fields of medicine and agricultural research.