304 results about "Oxadiazole" patented technology

The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as V-domain immunoglobulin suppressor of T-cell activation (VISTA) inhibitors or as dual inhibitors of VISTA and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by VISTA and its ligands, PD-1, PD-L1, and / or PD-L2.

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 present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as T-cell immunoglobulin and mucin-domain containing-3 (TIM-3) inhibitors or as dual inhibitors of TIM-3 and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by TIM-3, PD-1, PD-L1, and / or PD-L2.

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 #

The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.

The present invention relates to a pyrido[1,2-a]pyrimidine mesoionic derivative containing a 1,2,4-oxadiazole structure and a preparation method and use thereof. The compound has a structure of formula (I), has excellent insecticidal activity against bean aphids, white-backed plant hoppers, diamondback moths, fall armyworms, striped stem borers, armyworms, etc., and can be used to prepare drugs or medicaments for preventing and controlling pests such as aphids, rice plant hoppers, diamondback moths, fall armyworms, striped stem borers, armyworms, etc. The compound has a simple structure and preparation process, and has low production cost.

The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, including an anhydrous crystalline form, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.

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 present invention relates to the technical field of heat-conducting graphite materials, and particularly relates to a POD precursor film, a POD-based graphite film and a preparation method. The preparation method is as follows: terephthalic acid, isophthalic acid, hydrazine salt and boron arene compounds are added into a fuming sulfuric acid system, and a polycondensation copolymerization reaction is carried out under heating conditions, and benzoic acid is added as a capping agent. After the reaction is completed, an antioxidant-modified polyarylene oxadiazole polymer solution is obtained; the antioxidant-modified polyarylene oxadiazole polymer solution is coated and scraped into a film, and then solidified and formed in a multi-stage coagulation bath, and finally neutralized, washed and dried to obtain a POD precursor film; the coagulation bath is an aqueous solution of sulfuric acid, boron compounds and sulfuric acid aqueous solution. The POD-based graphite film is obtained after the POD precursor film is subjected to carbonization treatment and graphitization treatment. The present invention realizes the significant improvement of the antioxidant performance of the graphite film while maintaining high thermal conductivity by synergistically introducing boron elements inside and outside the POD precursor film.

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 invention belongs to the technical field of preparation of oxadiazole derivatives. The invention provides a method for preparing a 2-amino-1, 3, 4-oxadiazole derivative through electro-catalysis, which comprises the following steps: adding 0.2 mmol of benzoyl hydrazine compound, 0.4 mmol of tetrabutylammonium iodide, 0.4 mmol of 1, 4-diazabicyclo [2.2. 2] octane, 0.4 mmol of sodium bicarbonate and 6 mL of acetonitrile into an electrolytic tank; then, 0.3 mmol of a phenyl isothiocyanate compound is added dropwise; the reaction is carried out under a direct-current constant current between the electrode anode and the electrode cathode. According to the method, benzoyl hydrazine and phenyl isothiocyanate are taken as reaction substrates through electro-catalysis, reagents such as acetonitrile which is low in price and low in toxicity are taken as solvents, an oxidizing agent in a conventional reaction is replaced by a mode of introducing current, and the oxadiazole compound is synthesized under mild and green conditions.