259 results about "Oxadiazole" patented technology

Provided herein are compounds that selectively inhibit HDAC6, a protein whose activity is associated with a variety of diseases (e.g., cancer, neurological disorders). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating HDAC6-related diseases and disorders (e.g., Alzheimer's disease, cancer) with the compounds in a subject, by administering the compounds and / or compositions described herein.

The invention provides a coumarin derivative containing oxadiazole (thiadiazole) thioether and a preparation method and application thereof, the structural general formula of the coumarin derivative containing oxadiazole (thiadiazole) thioether is shown as I, and the structural general formula of the coumarin derivative containing thiadiazole thioether is shown as II, the synthesis route of the coumarin derivative containing oxadiazole (thiadiazole) thioether is simple and practical, the preparation raw materials are easy to obtain, the cost is low, and the prepared compound has a good control effect on plant viruses including tobacco mosaic virus, cucumber mosaic virus, potato Y virus, southern rice black-streaked dwarf virus or rice stripe virus. According to the invention, a favorable lead compound is provided for the creation of a natural bionic antiviral agent; # imgabs0 #

Provided herein are solid forms and methods of prepapation relating to (R) -3- (tert-butyl) -N-(1- (4- (6- (6- (4- ( (1- (4- (2, 4-dioxotetrahydropyrimidin-1 (2H) -yl) phenyl) piperidin-4-yl) methyl) piperazin-1-yl) pyridin-3-yl) -7H-pyrrolo [2, 3-d] pyrimidin-4-yl) -2-methylphenyl) ethyl) -1,2,4-oxadiazole-5-carboxamide.

The invention relates to a high-thermal-conductivity polyaryloxadiazole polymer, a film, a preparation method and application, and belongs to the technical field of high polymer materials. The preparation method comprises the following steps: mixing fuming sulfuric acid and phosphoric acid to obtain a composite acid solvent; adding a POD monomer and a heat-conducting filler into the composite acid solvent under the condition of inert gas; carrying out gradient heating polymerization reaction to obtain a polymerization solution containing the polyaryloxadiazole polymer; the surface of the heat-conducting filler is modified with amino, hydroxyl or carboxyl functional groups; the polymerization reaction temperature is less than or equal to 80 DEG C. According to the preparation method of the high-thermal-conductivity polyaryloxadiazole polymer, the polyaryloxadiazole polymer with relatively excellent thermal conductivity, mechanical property and high-temperature stability can be obtained in a low-temperature polymerization manner. The material is suitable for heat dissipation application in the fields of 5G high-frequency circuits, flexible electronic devices and the like, and has the advantages of simple process, excellent performance, moderate cost and the like.

The application discloses a continuous synthesis method of an amicarbazone intermediate 5-isopropyl-1,3,4-oxadiazole-2(3H)-ketone. The method comprises two continuous processes of hydrazinolysis and phosgenation: continuously feeding a mixture of isobutyric acid and a solvent, a mixture of hydrazine hydrate and a catalyst into a hydrazinolysis continuous reactor respectively, carrying out a warming reflux dehydration reaction, and obtaining an isobutyryl hydrazine solution shown in formula I; continuously feeding the isobutyryl hydrazine solution and phosgene into a phosgenation continuous reactor, carrying out a phosgenation reaction, and after distillation and desolventizing treatment of a reaction solution, obtaining 5-isopropyl-1,3,4-oxadiazole-2(3H)-ketone shown in formula II. The application has the advantages of simple reaction flow, high product yield, and significant production efficiency improvement, and is suitable for industrial large-scale production.

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I)In the formula Q is O, R1 is the side chain of Ser, R2 is —CO-Thr, R3 is the side chain of Asn or Glu, and R4, R5 and R6 are each H.

The invention discloses an aryl oxadiazole compound with a chemical structural formula as shown in the specification or pharmaceutically acceptable salt thereof. In-vitro experiment results show that the compound has a remarkable inhibition effect on DENV, the therapeutic index (TI) of the compound is far higher than that of a clinical reference substance ribavirin, the TI value of a preferred compound such as I-29 exceeds 1131.86, and the TI value of the preferred compound is far higher than that of the clinical reference substance ribavirin. The characteristics of high efficiency and low toxicity are highlighted. In addition, the preparation method is simple in process, high in yield, mild in reaction condition and suitable for large-scale production and clinical popularization.

The application discloses a blue fluorescent molecule, which has a D-pi-A structure, contains an oxadiazole as an acceptor group and a phenyl carbazole as a donor group, and connects the acceptor group and the donor group with an aromatic ring having a thermal excitation energy level arrangement characteristic as a pi bridge. The application also provides a preparation method and application of the blue fluorescent molecule. The application uses the aromatic ring having the thermal excitation energy level arrangement characteristic as the pi bridge, reasonably regulates a high-energy excited state of the acceptor by introducing the donor, activates a thermal excitation channel of the molecule, breaks through a limitation of 25% of an excitation utilization rate of a fluorescent material, and thus improves the excitation utilization rate.

This invention relates to the field of thermally conductive graphite materials technology, specifically disclosing a high thermal conductivity, high carbon residue aromatic heterocyclic polymer-based graphite film and its preparation method. The invention provides a high thermal conductivity, high carbon residue aromatic heterocyclic polymer-based graphite film, wherein the graphite film is prepared by first obtaining a dry base film using polyarylene oxadiazole as a polymer-based precursor, and then obtaining it through carbonization and graphitization treatments. The polyarylene oxadiazole is prepared by a segmented multi-step polymerization reaction using naphthalenedicarboxylic acid, hydrazine salt, terephthalic acid, and isophthalic acid as raw materials. The resulting graphite film exhibits significantly improved carbon residue and thermal conductivity compared to general organic precursors.

This invention relates to a compound containing trifluoromethyloxadiazole and a spirocyclic structure, or a pesticide-acceptable salt, hydrate, or solvate thereof, characterized in that the structure of the compound containing trifluoromethyloxadiazole and a spirocyclic structure is shown in general formula I. Compared with the prior art, the compound provided by this invention can be used to prepare histone deacetylase inhibitors, effectively inhibiting the growth and reproduction of various rust fungal spores, with effects comparable to fluopyram.

The invention discloses an indole styryl oxadiazole bridging compound with toxoplasma gondii resisting activity, which is formed by bridging three pharmacophores of 3-indoleacetonitrile, oxadiazole and cinnamic acid. The invention relates to the technical field of antiparasite, and has the beneficial effects that the compound provides a new chemical entity for development of toxoplasma gondii resistant drugs, opens up a new direction for design of the antiparasite drugs, has a wide application prospect, and is suitable for industrial production. Particularly, the gene has an important transformation value in the aspects of immunodeficiency patient treatment and toxoplasma gondii prevention and control in the livestock breeding industry.

A 2-amino-5-substituted-1,3,4-oxadiazole is used to identify Cr(VI). A test solution is prepared using the 2-amino-5-substituted-1,3,4-oxadiazole. An anionic solution is added to the test solution, and Cr(VI) is identified by naked-eye observation and UV-visible absorption spectroscopy. The method demonstrates excellent selectivity for Cr(VI) identification, with no interference from other ions, enabling better detection of Cr(VI) in the environment.

The present application relates to a kind of aromatic oxadiazole polymer modified membrane and its preparation method.The preparation method of the modified membrane includes the following steps: step (1) with terephthalic dihydrazide as raw material, with polyphosphoric acid as solvent and dehydrating agent, polymerization is carried out to obtain prepolymer solution, wherein ternary acid and polyol are added during polymerization reaction;Step (2) the prepolymer solution obtained in step (1) is made into film, dried, to obtain modified membrane.The present application constructs the new network structure of aromatic oxadiazole polymer, and the modified membrane prepared has good film-forming property, is soft and transparent, has good mechanical property, has high thermal stability and chemical stability.

The invention discloses a 1, 2, 4-oxadiazole compound and a preparation method and application thereof.The preparation method comprises the steps that 1, 2, 4-oxadiazole serves as a parent nucleus structure and reacts with aromatic amine intermediates containing different substituent groups, structures such as alkyl, halogen, alkoxy and trifluoromethyl are introduced, oxalyl chloride serves as an acylating agent, a condensation reaction is conducted in THF and other solvents, and the 1, 2, 4-oxadiazole compound is obtained; a series of target compounds are synthesized. The structure of the obtained compound is confirmed by NMR, the compound has clear and controllable hydrogen spectrum and fluorine spectrum signals, the synthesis process is simple, the raw materials are easy to obtain, the reaction condition is mild, the yield is good (most yield is more than 65%), and the developed 1, 2, 4-oxadiazole compound not only has clear structure and stable physicochemical properties, but also has wide application prospects. Good sterilization performance and structure regulation and control space are also shown, and high further research and development value is achieved.

The application provides a palladium ion extractant material and a preparation method thereof, and the pyridine-oxadiazole ligand is used as the extractant, most Pd 2+ in the aqueous phase can be extracted into the organic phase in a short time, and has a very high extraction rate; selective extraction separation of Pd 2+ under acidic conditions can be realized, the applicable range of acidity is wide, and excellent extraction capacity is achieved in the range of 0.2-4M nitric acid concentration; the extractant has excellent selectivity to Pd 2+ in the aqueous phase containing various metal ions; the pyridine-oxadiazole extractant has a good application prospect in the separation and recovery of Pd 2+ in high-level radioactive waste; the m-nitro-trifluorotoluene is used as a diluent of the extraction system, has good solubility to the organic ligand and the extractant, and the 2-bromohexanoic acid can increase the lipophilicity of the extractant.

The embodiment of the invention provides an oxadiazole-steroid compound, a pharmaceutical composition and application. The oxadiazole-steroid compound is a compound with a structure as shown in a formula I or pharmaceutically acceptable salt of the compound or a mixture of the compound and the pharmaceutically acceptable salt. The oxadiazole-steroid compound provided by the embodiment of the invention can effectively activate a metabolic regulation target FXR, and has excellent potential for preventing or treating MAFLD and related complications thereof. Meanwhile, the compound has no excitation effect on an MRGPRX4 receptor possibly causing pruritus while maintaining the FXR excitation activity, and a safer choice is provided for treatment of related diseases. Therefore, the oxadiazole-steroid compound has a more remarkable application prospect in preparation of the medicine for treating the metabolism-related fatty liver disease.

N-[(S)-[3-[1-(2,2-difluoropropylcarbamoyl)-3-hydroxy-3-methyl- cyclobutyl]imidazo[1,2-b][1,2,4]triazin-6-yl]-[4-(trifluoromethyl)cyclohexyl]methyl]-4-5 methyl-1,2,5-oxadiazole-3-carboxamide, or a pharmaceutically acceptable salt and / or solvate thereof, being a potent modulator of human IL-17 activity, is accordingly of benefit in the treatment and / or prevention of various human ailments, including inflammatory and autoimmune disorders.

Embodiments of the present disclosure are directed towards spray-dried compositions including a Zr phenol-oxadiazole complex and methods utilizing these spray-dried compositions.

The application belongs to the field of fungicides, and discloses a 1,3,4-oxa / thia-diazole pyrogallol derivative, a preparation method and application, and the structure of the compound is as shown in the formula I: in the formula I, X is an oxygen atom or a sulfur atom; R is a hydrogen atom, a halogen atom or a methoxy group; the halogen is one of F, Cl and Br. The compound has the effect of inhibiting plant pathogenic fungi and preventing and treating plant fungal diseases, and can be applied to plant protection as a fungicide.

The present application relates to a kind of 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative purposes, 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative structure as shown in formula I, this 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative has the potential to be developed as anti-radiation drug and antitumor drug.

This invention discloses a high-fire-resistant concrete, characterized by being composed of the following components in parts by weight: 20-25 parts cement, 30-35 parts crushed stone, 10-25 parts river sand, 10-12 parts volcanic ash, 10-20 parts water, 1-3 parts epoxy-propionic acid modified octa-tetramethylcyclotetrasilazane, 0.3-0.6 parts guanidine carbonate, 1-3 parts calcium borate, 0.5-1 part waste polyarylene diazole fiber, and 0.1-0.3 parts 3-chloro-2-hydroxypropanesulfonic acid modified 2,5-bis(diethylamino)phenyl-1,3,4-diazole. This invention also discloses a method for preparing the aforementioned high-fire-resistant concrete. The high-fire-resistant concrete disclosed in this invention exhibits high fire resistance, good workability, excellent comprehensive performance, impermeability and crack resistance, durability, and high compressive strength.

The present invention discloses a class of acyl imine derivatives containing trifluoromethyl oxadiazole as shown in the following general formula (I): for each substituent, see the specification. The present invention also discloses a preparation method and uses of the acyl imine derivatives containing trifluoromethyl oxadiazole. The acyl imine derivatives containing trifluoromethyl oxadiazole are particularly suitable for preventing and controlling soybean rust, wheat rust, corn rust, crop anthracnose, etc.

The application discloses a preparation method and product of a myrtenyl-1,3,4-oxadiazole formylhydrazine compound and application of the compound, and synthesizes myrtenic acid by oxidizing myrtenal; myrtenyl hydrazine is generated by reacting the myrtenic acid with hydrazine hydrate; myrtenyl-1,3,4-oxadiazole methyl ester is generated by reacting the myrtenyl hydrazine with oxalyl chloride methyl ester; the myrtenyl-1,3,4-oxadiazole formylhydrazine compound is generated by reacting the myrtenyl-1,3,4-oxadiazole methyl ester with each substituted phenylhydrazine; the compound has a general formula I: wherein R is H, 4-F, 4-Cl, 4-Br, 4-I, 4-CH3, 2-CH3, 2-F, 3-F, 2-Cl, 3-Cl, 2-Br, 3-Br or 4-OCH3; the compound has good prevention effects on sclerotinia sclerotiorum, botryosphaeria dothidea and fusarium graminearum under an in-vitro condition, and can be used for preventing and treating fungal diseases of agricultural or forestry plants. The preparation method of the compound is simple, the yield is high, and the product is stable in property.

The invention discloses a preparation method and application of an indole C2-position derivative containing a 1, 3, 4-oxadiazole and thioether structure. The compound can be used for effectively preventing and treating bacterial diseases such as kiwi fruit canker pathogen, citrus canker pathogen and rice bacterial blight pathogen. Wherein the EC50 value of the compound 2-((2-fluorophenyl) sulfo)-5-(1H-indol-2-yl)-1, 3, 4-oxadiazole on pathogenic bacteria of the kiwifruit canker is 27.35 mu g / mL, and the prevention and treatment effect is the best; the EC50 values of the compound 2-(1H-indole-2-yl)-5-((4-trifluoromethoxy-phenyl) sulfo)-1, 3, 4-oxadiazole on pathogenic bacteria of citrus canker and pathogenic bacteria of rice bacterial blight are 32.94 mu g / mL and 49.52 mu g / mL respectively, and the control effect is the most ideal. The pesticide composition is obviously superior to control pesticides such as bismerthiazol and thiediazole copper. The indole C2-site derivative containing the 1, 3, 4-oxadiazole and thioether structure can be applied to prevention and treatment of bacterial diseases of crops, and is simple in structure, convenient in preparation process, low in production cost and wide in application prospect.

The present invention provides a benzoxazine-tioxazafen derivative and its preparation method and application, belonging to the technical field of pesticide compound preparation. The benzoxazine-tioxazafen derivative described in the present invention is a derivative of 3-(5-(thiophene-2-yl)-1,2,4-oxadiazole-3-yl)-2H-benzo[b][1,4]oxazine. The present invention uses tioxazafen as the parent structure and splices active substructures with differently substituted benzoxazine derivatives to synthesize a series of new compounds with novel chemical structures. The compounds can be used to control plant parasitic nematodes such as root-knot nematodes and pine wood nematodes. Bioassay results show that the activity of the benzoxazine-tioxazafen derivative against pine wood nematodes is significantly better than that of the commercial agent tioxazafen and is comparable to that of thiazophos, indicating high commercialization prospects.

The disclosure provide compounds of Formula I and the pharmaceutically acceptable salts thereof. The variables, R1, R2, R3, X1, X2, and Z are defined herein. Certain compounds of Formula I act as selective mitochondrial protonophore uncouplers that do not affect the plasma membrane potential. Compounds and salts of Formula I are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, compounds of Formula I are useful for increasing lifespan. Compounds and salts of Formula I are also useful for regulating glucose homeostasis or insulin action in a patient.

The present invention provides the use of a compound based on a 3-phenyl-1,2,4-oxadiazole-5-carboxamide skeleton in the preparation of a drug for treating tumor diseases, belonging to the field of biomedicine technology. The compound based on a 3-phenyl-1,2,4-oxadiazole-5-carboxamide skeleton provided by the present invention inhibits the activity of PPT2 and regulates the palmitoylation level of cofilin1, ultimately achieving a tumor-suppressing effect.

The present invention belongs to the technical field of preparation of oxadiazole derivatives. The present invention provides a method for preparing 2-amino-1,3,4-oxadiazole derivatives by electrocatalysis, comprising the following steps: adding 0.2mmol of benzoylhydrazide compounds, 0.4mmol of tetrabutylammonium iodide, 0.4mmol of 1,4-diazabicyclo[2.2.2]octane, 0.4mmol of sodium bicarbonate, and 6mL of acetonitrile to an electrolytic cell; then adding 0.3mmol of phenyl isothiocyanate compounds dropwise; reacting under a DC constant current between an electrode anode and an electrode cathode. The present invention adopts electrocatalysis with benzoylhydrazide and phenyl isothiocyanate as reaction substrates, acetonitrile and other cheap and less toxic reagents as solvents, and passing current to replace the oxidant in conventional reactions, thereby synthesizing oxadiazole compounds under mild and green conditions.

The present disclosure describes compositions and methods for treating at least one symptom of an anxiety disorder in a human subject. The compositions and methods employ a therapeutically effective amount of a compound of formula I (Compound I) or formula II (Compound II, or a pharmaceutically acceptable salt, hydrate or solvate of Compound I or II.