198 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 invention discloses a preparation method and application of a pyrazole compound, and relates to a compound with a novel structure and a composition of the compound, and the pyrazole compound shows better activity in vivo and does not show obvious toxicity. The compound provided by the invention can be developed into drugs for protecting multiple diseases such as nerve cells, cardiovascular diseases and the like. # imgabs0 #

Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitor compounds and compositions comprising such compounds. The compounds may have a structure according to Formula IAlso disclosed are methods of making and using the compounds and compositions. The disclosed compounds and / or compositions may be used to treat or prevent an IRAK-associated disease or condition.

The invention discloses an N-aryl pyrazole compound and a pharmaceutical composition and application thereof.The structure of the compound is shown in the formula I. The N-aryl pyrazole compound further comprises pharmaceutically acceptable salt of the N-aryl pyrazole compound, the N-aryl pyrazole compound exerts obvious inhibitory activity on COX-2 or PDE4 or the COX-2 or the PDE4 or the COX-2 or the PDE4 or the COX-2 or the PDE4 or the COX-2 or the PDE4 at the micromolar concentration level, the inhibition rate reaches 50% or above, and the N-aryl pyrazole compound has an exact structure-function relationship; as a single-target or double-target inhibitor drug, the compound has a wide application range. # imgabs0 #

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 invention belongs to the technical field of synthesis of organic compounds, and particularly relates to a method for synthesizing an N-alkyl substituted 3, 5-dimethyl pyrazole compound by a one-pot method. The method comprises the following steps of: 1, adding a cerium catalyst and an organic solvent into alkyl methanol and di-tert-butyl azodicarboxylate serving as raw materials, uniformly stirring, and reacting for a certain time under the illumination condition to obtain a precursor of N-alkyl substituted 3, 5-dimethylpyrazole; spin-drying the reaction system obtained in the first step, and adding a hydrochloric acid methanol solution for reaction; and 3, spin-drying the reaction system obtained in the step 2, and adding acetylacetone, triethylamine and methanol for reaction to obtain the N-alkyl substituted 3, 5-dimethyl pyrazole compound. According to the method, raw materials are easy to obtain, reaction conditions are mild and safe, the cerium catalyst is easy to synthesize and prepare on a large scale, and the method is suitable for green synthesis of the N-alkyl substituted 3, 5-dimethylpyrazole compound.

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 provides: a pyrazole compound having a structure represented by formula (1) or a salt thereof; and a novel fungicide, particularly an agricultural and horticultural fungicide, containing the pyrazole compound or the salt thereof as an active ingredient. In the formula, G represents G-1, G1 represents a C1-C6 haloalkyl group or the like, T represents an oxygen atom or the like, RX represents a C1-C6 alkyl group 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 a C1-C6 alkyl group or the like, m5 and n5 represent integers 0, 1, 2, 3, 4 or 5, and p represents an integer 0 or 1. [Chemical Formula 1] # imgabs0 #

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 invention relates to the preparation and use of pyrazole compounds containing 3,5-dichloropyridyloxyarylmethyl. It is obtained by the condensation of 3,5-dichloropyridyloxyarylmethylamine with substituted pyrazole acids. The pyrazole compounds containing 3,5-dichloropyridyloxyarylmethyl exhibit good insecticidal effects against harmful insects, and these compounds can be used to prepare insecticides in the fields of agriculture, horticulture, etc.

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 method for preparing a pyrazole derivative 3-bromo-5-methyl-1-H-pyrazole-N-2-chloropyridine (compound of formula I) is disclosed, wherein the method is by reacting a compound of formula II with a halogen-substituted pyridine, or by decarboxylating a pyrazole carboxylic acid of formula XI in the presence of an acid, optionally in the presence of a base and an organic solvent. In addition, a method for preparing a synthetic precursor of formula II, formula IV, formula V, formula VI, formula XI, and a method for preparing a compound of formula VII are provided, including reacting a compound of formula I with an oxidant, optionally in the presence of a catalyst. A compound of formula I as a useful synthetic precursor for preparing an o-aminobenzamide of formula VIII is also disclosed.

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 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 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.

This invention discloses a method for synthesizing polysubstituted pyrazole compounds, belonging to the field of organic synthesis. The method utilizes an alkenyl sulfonium salt represented by Formula I, a pyrazole represented by Formula II, and a halogenated succinimide (NIS, NBS, NCS) represented by Formula III as raw materials, without the need for metal catalysis, to produce the pyrazole compound represented by Formula IV. This method utilizes readily available, inexpensive raw materials, eliminates the need for metal catalysts, and is environmentally friendly and pollution-free. It also boasts a wide substrate range, high yield, simple operation, and easy product separation and purification. #imgabs0#

The present invention provides a substituted pyrazole compound and a composition comprising the compound and its use, wherein the compound is a compound represented by formula (I) or its tautomer, stereoisomer, prodrug, crystal form, pharmaceutically acceptable salt, hydrate or solvent compound. The compound of formula (I) can be used as a reversible Bruton's tyrosine kinase (BTK) inhibitor for treating diseases related to BTK, and has high selectivity and good pharmacokinetic properties.

The present invention provides a pyrazole compound represented by a formula (1) or a salt thereof, and a novel fungicide, in particular, agricultural-horticultural fungicide that contains it as an active ingredient. The formula indicates a structure in which G represents G-1, G1 represents C1-C6 haloalkyl, etc., T represents an oxygen atom, etc., RX represents C1-C6 alkyl, etc., RY represents a hydrogen atom, etc., R1 represents a hydrogen atom, etc., R2 represents a hydrogen atom, etc., R3 represents a hydrogen atom, etc., Ra represents a hydrogen atom, etc., Z represents Z-1, etc., Z1 represents C1-C6 alkyl, etc., m5 and n5 each represent an integer of 0, 1, 2, 3, 4, or 5, and p represents an integer of 0 or 1.

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.