403 results about "Oxadiazole" patented technology

The invention belongs to the technical field of medicines, and discloses a substituted oxadiazole-aniline compound, a preparation method thereof, a pharmaceutical composition taking the compound as an active component, and application of the substituted oxadiazole-aniline compound and the pharmaceutical composition in treatment and / or prevention of infectious diseases caused by coronavirus. Specifically, the invention relates to a compound shown as a formula (I) and an isomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound disclosed by the invention, and R1, R2, R3, R4 and n are described in the specification. The invention aims to prepare a new compound with anti-coronavirus activity, and the new compound can be used as a potential new drug for treatment or prophylactic treatment of infectious diseases caused by viruses, especially pneumonia diseases caused by coronaviruses. # imgabs0 #

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.

Disclosed herein is a solid Form A of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)piperidin-4-amine hydrochloride exhibiting at least X-ray lines (in degrees 2θ ± 0.2) at 4.30, 8.59, 12.88, 18.82 and 21.34 in a powder diffraction pattern when measured using Cu Kα radiation. The solid Form A is an antagonist of the kappa-opioid receptor (KOR) and is useful for treating conditions that benefit from the same. Compositions comprising the solid Form A, as well as related methods of use are also disclosed.

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 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 discloses an aromatic poly-1, 3, 4-oxadiazole membrane material and a preparation method thereof, relates to the technical field of high polymer materials, and solves the problem of poor membrane flexibility caused by brittle fracture in the existing POD material graphitization process. Synthesizing functional terephthalic acid from amino-substituted phthalic acid and substituted succinic anhydride through dehydration; carrying out condensation polymerization on the obtained functionalized terephthalic acid, terephthalic acid and hydrazinium salt under the action of fuming sulfuric acid to prepare a POD solution; the POD solution is extruded to a solidification roller through a forming die head after being subjected to vacuum defoaming and filtering, a wet film layer is obtained after the POD solution is solidified through a multi-stage solidification bath, the obtained wet film is fully washed and then dried, and the aromatic poly-1, 3, 4-oxadiazole film material is obtained. The method has wide application prospects in the field of high-thermal-conductivity materials, and can be particularly applied to novel products such as folding screen mobile phones and square batteries.

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.

The invention provides an application of a compound based on a 3-phenyl-1, 2, 4-oxadiazole-5-formamide skeleton in preparation of a medicine for treating tumor diseases, and belongs to the technical field of biological medicines. The compound based on the 3-phenyl-1, 2, 4-oxadiazole-5-formamide skeleton provided by the invention regulates and controls the palmitoylation modification level of Cofilin1 by inhibiting the activity of PPT2, and finally achieves the effect of inhibiting cancer.

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 provides an application of a compound based on a 3-phenyl-1, 2, 4-oxadiazole-5-formamide skeleton in preparation of a medicine for treating pathological retinal neovascular diseases, and belongs to the technical field of biological medicines. The compound based on the 3-phenyl-1, 2, 4-oxadiazole-5-formamide skeleton developed by the invention can be used as an inhibitor of PPT1, and the palmitoylation modification level of a substrate is improved by inhibiting the enzyme activity of the PPT1. According to the compound, the palmitoylation modification of Gpx1 is improved by inhibiting PPT1, so that the generation of pathological retinal neovascularization is inhibited.

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 present invention relates to an oral capsule composition comprising 3-[(1S, 2S)-1-[5-[(4S)-2, 2-dimethyloxane-4-yl]-2-[(4S)-2-(4-fluoro-3, 5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6, 7-dihydro-4H-pyrazolo [4, 5-a] pyrimidine-2-yl]-3-(4-fluoro-1-methylindazol-5-yl)-4-methyl-6, 7-dihydro-4H-pyrazolo [4, 5-a] pyrimidine-2-yl]-3-(4-fluoro-1-methylindazol-5-yl)-4, 4 '- The invention relates to a pharmaceutical composition, in particular to a pharmaceutical composition containing 4-(2, 3-c) pyridine-5-carbonyl] indole-1-yl]-2-methylcyclopropyl]-4H-1, 2, 4-oxadiazole-5-ketone or a pharmaceutically acceptable salt thereof. And a pH adjusting agent.

In production of crops of agriculture and horticulture or the like, damage caused by diseases is still large, and, due to factors such as occurrence of resistant diseases to existing drugs, development of new agrohorticultural fungicides is desired. The present invention provides an agrohorticultural fungicide and a method of use thereof, an active ingredient thereof being a compound represented by the general formula (I) or salts thereof:{wherein R1 denotes a hydrogen atom or (C1-C6)alkyl group or the like. R2 denotes a hydrogen atom or the like. R3 denotes a hydrogen atom or (C1-C6)alkyl group or the like. R4 denotes a (C1-C6)alkyl group, (C3-C6)cycloalkyl group or aryl group or the like. X1 and X2 denote a hydrogen atom or halogen atom or the like. Y denotes an oxygen atom.}.

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.