25 results about "Bephenium Compounds" patented technology

The present invention addresses the problem of providing a compound having an NLRP3 inflammasome activation inhibitory activity and being useful for the prevention and / or treatment of autoinflammatory diseases, autoimmune diseases and / or inflammatory diseases, or a pharmaceutically acceptable salt thereof. The solution of the present invention is a compound represented by general formula (1) or a pharmaceutically acceptable salt thereof, # imgabs0 # [wherein the symbols are as defined below. In the formula, A represents a carbon atom or the like, R1 represents a halogen atom or the like, R1'represents a hydrogen atom or the like, R1 ''represents a hydrogen atom or the like, R1' 'represents a hydrogen atom or the like, R2 represents a hydrogen atom or the like, R2'represents a hydrogen atom or the like, and R3 represents a C1-C3 alkyl group or the like.

The present in vention is directed to methods of treating a metabolic disorder in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a nitro-vinyl benzene compound and administering to the subject a therapeutically effective amount of a GLP-1 agonist or analog. The present invention is also directed to kits and / or pharmaceutical compositions suitable for practicing the claimed methods.

The application belongs to the technical field of aniline compound preparation, and particularly relates to a synthesis method of deuterated aniline based on transition metal catalyzed nitrobenzene compound. The method uses nitrobenzene compound as raw material, is catalyzed by a low-load transition metal catalyst, and adopts one-pot method to complete the series reaction of high-selectivity hydrogenation and hydrogen-deuterium exchange of the nitrobenzene compound, so that the deuterated aniline compound with high added value is obtained. The yield of the deuterated product and the deuterium substitution rate of the product are better than those of conventional hydrogenation and deuterium substitution, the product is stable and cannot be easily replaced by hydrogen to return to the raw material, and the operation and application are convenient.

The present invention addresses the problem of developing a rare-earth element separating agent having higher durability. The present invention provides: a compound in which diglycol amide acid is introduced into a supporting polymer via an alkyl-substituted benzene compound; and a rare-earth element separating agent and a rare-earth element recovering method which use said compound.

The invention relates to the field of drug synthesis, in particular to an amine compound for fungi drugs and a preparation method of the amine compound. Comprising the following steps: 1) adding N-bromosuccinimide (NBS) into 4-iodobenzene serving as an initial raw material in an acetonitrile solvent in the presence of benzoyl peroxide serving as a catalyst, and reacting to obtain a 1-bromomethyl-4-iodobenzene compound II; 2) adding N-methylacetamide into the compound II in a tetrahydrofuran solvent by using potassium carbonate as alkali, and reacting to obtain an N-(4-iodobenzyl)-N-methylacetamide compound III; and 3) heating the compound III in a sodium hydroxide solution for deacetylation to obtain the compound IN-methyl-1-(4-iodophenyl) methylamine. The invention aims to provide a preparation process of the N-methyl-1-(4-iodophenyl) methylamine compound I, which is simple, convenient, green, environment-friendly and suitable for industrial production.

A novel disulfide biphenol ether compound and its preparation method and application for treating inflammatory skin diseases, the structural formula of the disulfide biphenol ether compound is: biphenyl diester is first dissolved in anhydrous tetrahydrofuran solvent, lithium aluminum hydroxide is added, quenched, filtered, extracted with dichloromethane, water is added to quench the reaction, extracted with dichloromethane, the organic phases are combined, after removing residual moisture, the reduced pressure rotary evaporation and recrystallization are removed to obtain intermediate 2; intermediate 2 and potassium thioacetate are added to solvent N, N-dimethylformamide and extracted, the organic phases are combined, and the solvent is evaporated and concentrated to obtain a light intermediate 3; intermediate 3 is dissolved in anhydrous methanol, sodium methoxide is added, stirred, extracted with ethyl acetate, and the organic phases are combined to obtain. The disulfide biphenyl compound prepared by the present invention has good anti-inflammatory ability, can effectively reduce inflammatory infiltration in tissue, improve the inflammatory phenotype of animal models, and can prevent and treat inflammatory skin diseases.

The present in vention is directed to methods of treating a metabolic disorder in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a nitro-vinyl benzene compound and administering to the subject a therapeutically effective amount of a GLP-1 agonist or analog. The present invention is also directed to kits and / or pharmaceutical compositions suitable for practicing the claimed methods.

The invention relates to a diaryl thioether photoinitiator as well as a preparation method and application thereof, an aryl thioether photocompound is prepared by reacting substituted benzene with sulfur chloride, and the preparation method specifically comprises the following steps: reacting a substituted benzene compound with S2Cl2 to synthesize an intermediate diaryl thioether compound; the preparation method comprises the following steps: reacting diaryl sulfide with parachlorobenzophenone or parachlorophenyl aminoketone, and synthesizing to obtain an aryl sulfide benzophenone compound or an aryl sulfide alpha-aminoketone compound; according to the synthesis method, thiophenol with stink is not used, and the preparation process is green and environment-friendly and is easy to industrialize; the synthesized compound can be used as a photoinitiator and shows a better photocuring effect.

The present invention provides a new method for producing a 3-hydroxybiphenyl compound and a new method for producing a derivative of a 3-hydroxybiphenyl compound using the same. Specifically, the present invention provides a method for producing a compound represented by formula (3), the method comprising a step for obtaining the compound represented by formula (3) by reacting, in a solvent and under the presence of a base, a compound represented by formula (1) [in the formula, R1 and R2 may be the same or different from each other and each represent a C1-C6 chain hydrocarbon group, or may form -(CH2)a- or -(CH2)2-O-(CH2)2- through binding between R1 and R2, and a represents 4 or 5] or a salt thereof with a compound represented by formula (2) [in the formula, R3 represents a C1-C6 chain hydrocarbon group, a chlorine atom, or a hydrogen atom, and X1 represents a chlorine atom, a bromine atom, or an iodine atom].

This invention relates to the field of nanomaterials, and discloses a composite nanoparticle, its preparation method, and its application. The preparation method includes: mixing noble metal nanoparticles with an organic synthetic oil and then heating the mixture to react; wherein the organic synthetic oil contains at least one selected from biphenyl compounds, hydrogenated products of biphenyl compounds, biphenyl ether compounds, and alkyl aromatic hydrocarbons. The composite nanoparticle includes a core and a shell covering the core; the core is a noble metal nanoparticle, and the shell is carbon quantum dots; wherein the carbon quantum dots are carbonized products of the organic synthetic oil; and the organic synthetic oil contains at least one selected from biphenyl compounds, hydrogenated products of biphenyl compounds, biphenyl ether compounds, and alkyl aromatic hydrocarbons. This composite nanomaterial exhibits excellent stability and light absorption properties.

The invention provides an ON-DNA 3, 4-substituted 3, 4-dihydroquinoxaline-2 (1H)-ketone compound and a preparation method thereof, and relates to the technical field of coding compound libraries. According to the invention, by controlling the conditions of solvent, temperature, pH and the like during reaction, the ON-DNA halogenated nitrobenzene compound can be used for preparing the ON-DNA 3, 4-substituted 3, 4-dihydroquinoxaline-2 (1H)-ketone compound through a two-step method. The method can be carried out in a mixed aqueous phase of an organic solvent / aqueous phase, has the advantages of single product, simple operation and environmental friendliness, and is suitable for synthesis of a DNA coding compound library by using a porous plate.

The present invention provides: a novel method for producing a 3-phenylcyclohexenone compound having a substituent at the 6-position; and a novel method for producing, by using the same, a derivative of a 3-phenylcyclohexenone compound having a substituent at the 4-position. Provided is a method for producing a compound represented by formula (3), the method comprising a step for mixing a compound represented by formula (1) [in the formula, R1, R2, R3, R4, and R5 are the same as or different from each other, and each represent a hydrogen atom or the like, R6 represents a C1-C6 chain hydrocarbon group which may be substituted with one phenyl group, R7 represents a hydrogen atom or the like, or R6 and R7 may be taken together to form –(CH2)4- or the like] or a salt thereof, a compound represented by formula (2) [in the formula, R8 represents a C1-C12 chain hydrocarbon group, and R9 represents a hydrogen atom or the like], and an alkali metal carbonate, and reacting these components in the presence of pyrrolidone to obtain a compound represented by formula (3) [in the formula, R1, R2, R3, R4, R5, R8, and R9 have the same meanings as above].

The present invention provides a novel EZH2 inhibitor compound represented by formula (I) and a use of the inhibitor compound in preventing or treating a disease mediated by EZH2.

The present invention provides a novel EZH2 inhibitor compound represented by formula (I) and a use of the inhibitor compound in preventing or treating a disease mediated by EZH2.

The present application provides a visible light responsive thienyl azobenzene compound, which belongs to the technical field of azo compounds. 3-aminothiophene-2-carboxylic acid methyl ester and nitrosobenzene are added to glacial acetic acid as raw materials, and the reaction is stirred at a temperature of 40-60°C until the nitrosobenzene reaction is complete. Deionized water is added to the reaction system, extracted, the organic phases are combined, the organic phases are washed, dried, and separated by column chromatography to obtain the finished product visible light responsive thienyl azobenzene compound. The above-mentioned compound is based on readily available raw materials and has mild reaction conditions. By adjusting the types of substituents on the benzene ring of the thienyl azobenzene molecule, not only the yield of bidirectional visible light isomerization can be improved, but also the yield of the product can be significantly improved. Z The half-life of the isomers is achieved at the monthly level of half-life.

Antibiotic resistance leads to deadly hospital-acquired infections globally. The World Health Organization (WHO) and the Centers for Disease Control and Prevention (CDC) have identified priority bacteria, including Methicillin-resistant Staphylococcus aureus, Pseudomonas aeruginosa, Acinetobacter baumannii, and particularly those carbapenem- resistant strains, also found in Enterobacterales (CRE) such as Escherichia coli and Klebsiella, as requiring new antibiotics. The present disclosure provides a chemical class of drugs less susceptible to existing mechanisms of antibiotic resistance and targeting difficult-to-treat bacterial infections. It more particularly provides compounds of formula (I), and compositions and uses thereof.

The invention discloses a near-infrared fluorescent probe and its preparation method and application. The present invention is refluxed at 110 DEG C for 12h by prepared 1,3-dimethoxy-5-nitrosoisobenzene compound 5 and excess 48wt% hydrobromic acid aqueous solution, and the reactant is extracted, washed, dried, purified to obtain 5-nitro-1,3-benzenediol compound 6, potassium carbonate and compound 6 are added to DMF and stirred at room temperature for 0.5h, prepared compound 4 is added to the mixed system, under nitrogen light protection, refluxed at 110 DEG C for 6h, the solvent is removed under reduced pressure, and the purified mixture obtains a near-infrared fluorescent probe. The probe has the advantages of near-infrared absorption, good water solubility, high stability, etc., and can effectively detect the activity of nitroreductase.

The application belongs to the technical field of organic compound preparation, and particularly relates to a method for preparing diphenylhydrazine or 2H-indazole compound by using azobenzene compound. The method comprises the following steps: mixing azobenzene compound, biborate, water and organic solvent, and reacting to prepare 2H-indazole compound; the reaction is carried out under visible light; the reaction time is less than 2 hours; the azobenzene compound is selected from any one of the following: the application uses azobenzene compound as raw material, uses water as hydrogen source, adds biborate, and carries out the reaction under visible light irradiation without metal catalyst, and 2H-indazole compound product with a yield of not less than 70% can be prepared in a reaction time of less than 1 hour. Moreover, the method of the application shows wide functional group compatibility, so that various types of azobenzene compounds can be converted into 2H-indazole compounds.

The application provides a production device, a production device control method and a preparation method of a phenyl chlorosilane. The production device comprises a reactor, a catalyst circulation device and a catalyst. The reactor is used for accommodating a reaction raw material and is provided with an outlet and an inlet. The catalyst circulation device is in communication with the outlet and the inlet respectively and is used for driving at least part of the catalyst to circulate in and out of the reactor. The reaction raw material comprises a chlorosilane and a benzene compound, and the catalyst comprises boron trifluoride or boron trichloride. The application can realize the recycling of the catalyst in the production process of the phenyl chlorosilane, separate the catalyst from hydrogen generated in the reaction, improve the reaction efficiency of the catalyst, and thus reduce the production cost of the phenyl chlorosilane.

The application belongs to the technical field of homogeneous catalysis, and provides application of a ten-core 3d-4f supramolecular nanocage material in catalyzing a three-component aza-Darzens reaction. The application comprises the following steps: mixing an aldehyde compound, an amino benzene compound, ethyl diazoacetate, the ten-core 3d-4f supramolecular nanocage material and an organic solvent, and then performing a reaction to obtain a reaction product, namely completing the three-component aza-Darzens reaction. The ten-core 3d-4f supramolecular nanocage material is used as a catalyst to catalyze the three-component aza-Darzens reaction to realize synthesis of a drug precursor with biological activity, and the catalyst has high catalytic efficiency, the operation steps are simple, and the yield of the target product is also high.

Provided are a novel method for producing a 3-hydroxybiphenyl compound, and a novel method for producing a derivative of a 3-hydroxybiphenyl compound using the same. Specifically, the present invention provides a method for producing a compound represented by formula (3), which comprises a step for reacting a compound represented by formula (1) (in the formula, R1, R2, R3, R4 and R5 are the same or different from each other and represent a hydrogen atom or the like, and R6 represents a phenylsulfonyl group or the like) with a compound represented by formula (2) (in the formula, a combination of R8 and R9 represents a combination of R8 being CH2NR12R13 or the like, R9 is a combination of hydrogen atoms or the like, R10 and R11 are the same or different from each other and represent a hydrogen atom or the like, and a combination of R8 and R9 is a combination of hydrogen atoms or the like). A compound represented by formula (1) (in the formula, R1, R2, R3, R4, R5, R10 and R11 represent the same meanings as the preamble) is obtained by reacting a compound represented by formula (2) in the presence of 0.1-5 moles of a base per 1 mole of the compound represented by formula (1) (in the formula, R1, R2, R3, R4, R5, R10 and R11 represent the same meanings as the preamble), and a compound represented by formula (3) (in the formula, R1, R2, R3, R4, R5, R10 and R11 represent the same meanings as the preamble).

The invention belongs to the field of biological medicine, and particularly relates to application of a biphenyl compound in resisting drug-resistant bacteria and a product. The invention provides an application of 2, 4-dihydroxy-4 '-pentylbiphenyl and / or 3, 5-dihydroxy-4'-pentylbiphenyl in preparation of a product for resisting drug-resistant bacteria, and a preparation method of the 2, 4-dihydroxy-4 '-pentylbiphenyl. The result of the embodiment shows that compared with other antibiotics such as penicillin, ceftaroline fosamil, oxacillin and levofloxacin, the 2, 4-dihydroxy-4 '-pentylbiphenyl and / or the 3, 5-dihydroxy-4'-pentylbiphenyl can effectively inhibit various drug-resistant bacteria, and the effect is good. The 3, 5-dihydroxy-4 '-pentylbiphenyl can damage cell nucleuses by destroying cell membranes so as to achieve an antibacterial effect, and has a remarkable inhibition effect on MRSA (Methicillin-Resistant Staphylococcus Aureus). The 2, 4-dihydroxy-4 '-pentylbiphenyl and the 3, 5-dihydroxy-4'-pentylbiphenyl disclosed by the invention are used for resisting drug-resistant bacteria, can effectively inhibit or kill various drug-resistant bacteria, and have a good effect.

The present invention is directed to methods of treating a metabolic disorder in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a nitro-vinyl benzene compound and administering to the subject a therapeutically effective amount of a GLP-1 agonist or analog. The present invention is also directed to kits and / or pharmaceutical compositions suitable for practicing the claimed methods.

The application belongs to the technical field of organic compound preparation, and discloses a non-column chromatography method for preparing 2H-indazole compounds from azobenzene compounds. The non-column chromatography method comprises the following steps: mixing azobenzene compounds, diboate, water and an organic solvent, reacting, removing the organic solvent, extracting and recrystallizing to separate the 2H-indazole compounds. The reaction is carried out under sunlight, and the reaction time is less than 1 hour. In the method, the product separation and purification does not need to use a chromatography column. Moreover, the method has wide functional group compatibility, so that various types of azobenzene compounds can be converted into 2H-indazole compounds. From the time cost and economic cost, the method has significant advantages compared with the existing method, and does not use toxic silica gel powder.

Disclosed in the present invention are a biphenyl compound, a method of preparation thereof, and an intermediate, a pharmaceutical composition and its uses. Specifically provided is a compound as shown in formula I or a pharmaceutically acceptable salt thereof. Said compound has good activity and selectivity at a γ retinoic acid receptor agonist, has virtually no agonistic activity at α and / or β retinoic acid receptors, and is thus beneficial for reducing systemic side effects.Preferably, the compound has a rather partial agonistic activity, has low skin irritation and few adverse reactions while maintaining its efficacy, and thus has good safety and compliance, such that the problems commonly present in existing RAR compounds are effectively resolved, and the compound can be used to treat and prevent diseases related to retinoic acid receptor γ.